SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`1. Pharmaceutical compositions based on rapamycin for treatment of cancerous tumors
`
`By: Sehgal, Surendra Nath; Vezina, Claude
`Assignee: Ayerst, McKenna and Harrison Ltd., Can.
`Patent Information: Jan 14, 1980, BE 877700, A1
`Application: Jul 13, 1979, BE 1979-196300
`Priority: Nov 03, 1978, US 1978-957626, Mar 03, 1980, US 1980-126276, Mar 22, 1984, US 1984-592193, Aug 09, 1989, US 1989-391334, Apr 09, 1991,
`US 1991-682813
`Source: Belg., 12 pp., Patent, 1980, CODEN: BEXXAL
`Accession Number: 1980:488940, CAN 93:88940, CAPLUS
`Language: French
`
`Abstract
`Rapamycin (I) [ 53123-88-9 ] significantly prolonged the life span of lab. animals bearing tumors and decreased the size of the
`tumors. The ratio of the av. survival in days of mice bearing lymphatic leukemia P-388 and treated with I (9 daily i.p. 12.5-400
`mg/kg injections) to that of nontreated leukemic mice was 1.28-1.46. In rats with mammary tumors, the ratio of the av. wt. of
`tumors at the beginning of treatment to that of tumors in nontreated animals was .10-.29. I may also be combined with presently
`used antineoplastic agents such as alkylating agents, antimetabolites, estrogens, etc.
`
`Application No.
`BE 1979-196300
`ZA 1979-5449
`JP 1979-142725
`US 1984-592193
`US 1991-784274
`
`Date
`Jul 13, 1979
`Oct 11, 1979
`Nov 02, 1979
`Mar 22, 1984
`Oct 29, 1991
`
`Patent Information
`Patent No.
`BE 877700
`ZA 7905449
`JP 55073616
`US 4885171
`US 5206018
`
`Priority Application
`US 1978-957626
`US 1980-126276
`US 1984-592193
`US 1989-391334
`US 1991-682813
`
`Kind
`A1
`A
`A
`A
`A
`
`A
`A1
`A3
`B2
`A2
`
`Date
`Jan 14, 1980
`Nov 26, 1980
`Jun 03, 1980
`Dec 05, 1989
`Apr 27, 1993
`
`Nov 03, 1978
`Mar 03, 1980
`Mar 22, 1984
`Aug 09, 1989
`Apr 09, 1991
`
`Indexing
`Pharmacodynamics (Section 1-5)
`
`Supplementary Terms
`neoplasm inhibitor rapamycin
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`1
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`2. Anticancer pharmaceuticals containing rapamycin and picibanil
`
`No Inventor data available
`Assignee: Ayerst, McKenna and Harrison Inc., Japan
`Patent Information: Oct 01, 1982, JP 57159716, A
`Application: Mar 05, 1982, JP 1982-35697
`Priority: Mar 09, 1981, US 1981-241867
`Source: Jpn. Kokai Tokkyo Koho, 4 pp., Patent, 1982, CODEN: JKXXAF
`Accession Number: 1983:22284, CAN 98:22284, CAPLUS
`Language: Japanese
`
`Abstract
`Pharmaceuticals contg. rapamycin (I) [ 53123-88-9 ] and picibanil (II) [39325-01-4] are neoplasm inhibitors for treatment of
`lymphocytic leukemia, colon neoplasm, mammary cancer, melanoma, etc. Thus, an injection was prepd. contg. I, II, butylated
`hydroxyanisole, anhyd. EtOH, Cremophor EL and H2O. Combinations of I and II were more effective than I or II alone in
`inhibiting the growth of lymphatic leukemia cells in mice.
`
`Patent Information
`Patent No.
`JP 57159716
`JP 03049893
`US 4401653
`CA 1171783
`
`Priority Application
`US 1981-241867
`
`Kind
`A
`B
`A
`A1
`
`Date
`Oct 01, 1982
`Jul 31, 1991
`Aug 30, 1983
`Jul 31, 1984
`
`Application No.
`JP 1982-35697
`
`US 1981-241867
`CA 1982-397428
`
`Date
`Mar 05, 1982
`
`Mar 09, 1981
`Mar 02, 1982
`
`A
`
`Mar 09, 1981
`
`Indexing
`Pharmaceuticals (Section 63-6)
`
`Supplementary Terms
`anticancer pharmaceutical picibanil rapamycin; neoplasm inhibitor picibanil rapamycin
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`3. Human brain tumor xenografts in nude mice as a chemotherapy model
`
`By: Houchens, David P.; Ovejera, Artemio A.; Riblet, Sylva M.; Slagel, Donald E.
`Source: European Journal of Cancer & Clinical Oncology, Volume: 19, Issue: 6, Pages: 799-805, Journal, 1983, CODEN: EJCODS, ISSN: 0277-5379, DOI:
`10.1016/0277-5379(83)90012-3
`Company/Organization: Battelle Mem. Inst., Columbus, OH, USA, 43201
`Accession Number: 1983:463770, CAN 99:63770, CAPLUS
`Language: English
`
`2
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`
`Abstract
`Two human brain tumors which were previously established in nude mice were used to det. antitumor efficacy of various
`therapeutic agents. These tumors were a medulloblastoma (TE-671) and a glioma (U-251) with mass-doubling times of 3.5 and
`5.5 days, resp., as s.c. implants in nude mice. Intracranial tumor challenge was accomplished by inoculating tissue culture-grown
`cells of either tumor into the right cerebral hemisphere to a depth of 3 mm. Groups of mice which had been inoculated with
`tumor were treated with various doses and schedules of antineoplastic compds. by the i.p. route. A new drug (rapamycin [
`53123-88-9 ]) was very effective against the U-251 tumor. This model system should prove valuable in assessing the effects of
`various chemotherapeutic modalities against brain tumors.
`
`Indexing
`Pharmacology (Section 1-1)
`
`
`Supplementary Terms
`brain tumor xenograft chemotherapy model
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`4. Demethoxyrapamycin (AY-24,668), a new antifungal antibiotic
`
`By: Sehgal S N; Baker H; Eng C P; Singh K; Vezina C
`Source: The Journal of antibiotics, Volume: 36, Issue: 4, Pages: 351-4, Journal; Article; (JOURNAL ARTICLE), 1983, ISSN: 0021-8820, Journal Code:
`0151115, Japan
`Accession Number: 1983212914, PubMed ID: 6343327, MEDLINE
`Language: English
`
`
`Abstract
`Demethoxyrapamycin is a new antifungal antibiotic which is co-produced with rapamycin by Streptomyces hygroscopicus. It
`was isolated as a minor component during recovery of rapamycin. Its antifungal and antitumor activity is compared with that of
`rapamycin.
`
`
`
`Copyright © 2018 U.S. National Library of Medicine.
`
`
`
`5. Current NCI preclinical antitumor screening in vivo: results of tumor panel screening, 1976-1982, and future
`directions
`
`By: Venditti, John M.; Wesley, Robert A.; Plowman, Jacqueline
`Source: Advances in Pharmacology and Chemotherapy, Volume: 20, Pages: 1-20, Journal, 1984, CODEN: AVPCAQ, ISSN: 0065-3144
`Company/Organization: Div. Cancer Treat., Natl. Cancer Inst., Bethesda, MD, USA, 20205
`3
`
`
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`Accession Number: 1984:603757, CAN 101:203757, CAPLUS
`Language: English
`
`Abstract
`Experiences in preclin. antitumor agent screening by the Division of Cancer Treatment of the NCI are summarized. Efficacies of
`various tumor models in uncovering agents not selected by L1210 are demonstrated.
`
`Indexing
`Pharmacology (Section 1-1)
`
`
`Supplementary Terms
`neoplasm inhibitor screening
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`6. Activity of rapamycin (AY-22,989) against transplanted tumors
`
`By: Eng, C. P.; Sehgal, S. N.; Vezina, Claude
`Source: Journal of Antibiotics, Volume: 37, Issue: 10, Pages: 1231-7, Journal, 1984, CODEN: JANTAJ, ISSN: 0021-8820, DOI: 10.7164/antibiotics.37.1231
`Company/Organization: Dep. Microbiol., Ayerst Res. Lab., Montreal, QC, Can., H3C 3J1
`Accession Number: 1984:622224, CAN 101:222224, CAPLUS
`Language: English
`
`Abstract
`Rapamycin [ 53123-88-9 ] exhibits activity against several ascites and solid transplantable tumors; it is slightly active to inactive
`against leukemias. On a wt. basis, rapamycin was less active than 5-fluorouracil, cyclophosphamide and adriamycin, but
`rapamycin's maximal activity against Colon 38 tumor was similar to that of 5-fluorouracil [51-21-8] and cyclophosphamide
`[50-18-0]. Its activity was such that it significantly inhibited tumor growth at any stage of development. In the active dose
`range, rapamycin appeared less toxic than the other drugs. In the Colon 38 tumor model, rapamycin at a given dose exhibited the
`same activity when administered i.p., i.v., i.m. and s.c., upon oral administration, its activity was reduced but not abolished.
`Rapamycin was compatible with 5-fluorouracil and cyclophosphamide. The sequential treatment 5-fluorouracil-rapamycin-
`cyclophosphamide was superior to the sequence 5-fluorouracil-adriamycin [23214-92-8]-cyclophosphamide in protecting Colon
`38 tumor-bearing mice. 29-Demethoxyrapamycin [83482-58-0] exerted only marginal activity against P388 lymphocytic
`leukemia; it was inactive against B16 melanocarcinoma and Colon 38 solid tumor.
`
`Indexing
`Pharmacology (Section 1-6)
`
`
`Supplementary Terms
`rapamycin antitumor
`
`
`
`
`
`
`4
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`7. Water-soluble rapamycin prodrugs
`
`By: Stella, Valentino J.; Kennedy, Paul E.
`Assignee: University of Kansas, USA
`Patent Information: Mar 17, 1987, US 4650803, A
`Application: Dec 06, 1985, US 1985-806152
`Priority: Dec 06, 1985, US 1985-806152, Dec 04, 1986, EP 1986-309449, Dec 03, 1986, CA 1986-524469
`Source: U.S., 6 pp., Patent, 1987, CODEN: USXXAM
`Classifications: Main IPC: A61K031-395, Secondary IPC: C07D491-06; , US 514291000
`Accession Number: 1987:464867, CAN 107:64867, CAPLUS
`Language: English
`
`Abstract
`The title prodrugs are rapamycin derivs. monosubstituted at position 28 and disubstituted at position 28 and 43 with the
`substituents CO(CH2)nNR1R2 (n = 1-3; R1,R2 = H, C1-3 alkyl; NR1R2 = heterocyclyl). The prodrugs release rapamycin in the
`presence of human plasma and animal tissue homogenates. Rapamycin was esterified with 4-pyrrolidinobutyric acid-HCl, in
`presence of dicyclohexylcarbodiimide and 4-N,N-dimethylaminopyridine to give rapamycin mono-(28)-4'-(N-pyrrolidino)butyrate
`
`ester-HCl. The soly. of the product was ∼15 mg/mL.
`
`
`
`
`
`5
`
`
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`
`Date
`Mar 17, 1987
`Sep 11, 1990
`Jun 10, 1987
`Oct 18, 1989
`Jun 11, 1987
`Apr 27, 1989
`Jul 01, 1987
`Oct 12, 1988
`Mar 25, 1992
`Sep 22, 1987
`Sep 07, 1994
`Jul 27, 1988
`May 29, 1991
`Dec 27, 1991
`Apr 15, 1992
`Mar 01, 1993
`Jun 07, 1987
`Oct 24, 1994
`May 30, 1988
`Jul 28, 1989
`Dec 29, 1992
`Mar 25, 1993
`Jan 08, 1996
`Sep 20, 1994
`May 24, 1995
`
`Dec 06, 1985
`Dec 04, 1986
`Dec 03, 1986
`
`Application No.
`US 1985-806152
`CA 1986-524469
`GB 1986-28994
`
`AU 1986-66080
`
`EP 1986-309449
`
`
`JP 1986-289750
`
`ZA 1986-9181
`EP 1991-200118
`
`AT 1986-309449
`ES 1986-309449
`DK 1986-5848
`
`HU 1986-5042
`
`CA 1990-615850
`DK 1993-347
`
`JP 1993-303867
`
`
`
`
`
`
`Date
`Dec 06, 1985
`Dec 03, 1986
`Dec 04, 1986
`
`Dec 04, 1986
`
`Dec 04, 1986
`
`
`Dec 04, 1986
`
`Dec 04, 1986
`Dec 04, 1986
`
`Dec 04, 1986
`Dec 04, 1986
`Dec 05, 1986
`
`Dec 05, 1986
`
`Aug 24, 1990
`Mar 25, 1993
`
`Dec 03, 1993
`
`
`
`
`
`
`Kind
`A
`A1
`A
`B
`A
`B2
`A2
`A3
`B1
`A
`B
`A
`A2
`A3
`T
`T3
`A
`B1
`A2
`B
`C2
`A
`B1
`A
`B
`
`Patent Information
`Patent No.
`US 4650803
`CA 1273920
`GB 2183647
`GB 2183647
`AU 8666080
`AU 583439
`EP 227355
`EP 227355
`EP 227355
`JP 62215592
`JP 06070066
`ZA 8609181
`EP 429436
`EP 429436
`AT 74134
`ES 2032750
`DK 8605848
`DK 169409
`HU 45018
`HU 198054
`CA 1312076
`DK 9300347
`DK 170750
`JP 06263765
`JP 07047593
`
`Priority Application
`US 1985-806152
`EP 1986-309449
`CA 1986-524469
`
`Indexing
`Pharmaceuticals (Section 63-6)
`
`
`Supplementary Terms
`rapamycin prodrug antitumor
`
`Citations
`1)Anon; EP 0041795 A2
`2)Anon; US 4316885 A
`3)Anon; BE 877700 A1
`
`
`A
`A
`A3
`
`
`
`6
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`8. Maleic anhydride copolymers as antidotes for the cytotoxicity of neoplasm inhibitors
`
`By: Bach, Ardalan; Shanahan, William R., Jr.
`Assignee: G.D. Searle and Co., USA
`Patent Information: Oct 24, 1990, EP 393575, A1
`Application: Apr 17, 1990, EP 1990-107246
`Priority: Apr 17, 1989, US 1989-339503, Apr 17, 1990, EP 1990-107246
`Source: Eur. Pat. Appl., 27 pp., Patent, 1990, CODEN: EPXXDW
`Classifications: Main IPC: A61K045-06, Secondary IPC: A61K031-785;
`Accession Number: 1992:99301, CAN 116:99301, CAPLUS
`Language: English
`
`Abstract
`Half-amide:half-imide copolymers comprising ethylene and maleic anhydride moieties (structure given), specifically carbetimer
`(I; a/b = 1:2-5), decrease the cytotoxic side effects of neoplasm inhibitors. Mice treated i.v. with 21 mg adriamycin/kg died
`within 5 days. When 1700 mg I/kg was administered concomitantly, no lethality was shown for >30 days.
`
`Kind
`A1
`B1
`A1
`A
`T
`T3
`
`A
`A
`
`Patent Information
`Patent No.
`EP 393575
`EP 393575
`CA 2014732
`JP 02292227
`AT 102838
`ES 2062155
`
`Priority Application
`US 1989-339503
`EP 1990-107246
`
`Indexing
`Pharmacology (Section 1-6)
`Section cross-reference(s):4
`
`
`
`
`
`
`
`Date
`Oct 24, 1990
`Mar 16, 1994
`Oct 17, 1990
`Dec 03, 1990
`Apr 15, 1994
`Dec 16, 1994
`
`Application No.
`EP 1990-107246
`
`CA 1990-2014732
`JP 1990-101530
`AT 1990-107246
`ES 1990-107246
`
`Apr 17, 1989
`Apr 17, 1990
`
`
`
`
`
`
`Date
`Apr 17, 1990
`
`Apr 17, 1990
`Apr 17, 1990
`Apr 17, 1990
`Apr 17, 1990
`
`
`
`
`7
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`
`Supplementary Terms
`anticancer antidote maleic anhydride copolymer; neoplasm inhibitor antidote
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`9. In vitro and in vivo evaluation of US-NCI compounds in human tumor xenografts
`
`By: Fiebig H H; Berger D P; Winterhalter B R; Plowman J
`Source: Cancer treatment reviews, Volume: 17, Issue: 2-3, Pages: 109-17, Journal; Article; (JOURNAL ARTICLE), 1990, ISSN: 0305-7372, Journal Code:
`7502030, Netherlands
`Company/Organization: Department of Internal Medicine, University of Freiburg, F.R.G
`Accession Number: 1991105753, PubMed ID: 2272027, MEDLINE
`Language: English
`
`
`
`
`Copyright © 2018 U.S. National Library of Medicine.
`
`
`
`10. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A
`
`By: Flanagan W M; Corthesy B; Bram R J; Crabtree G R
`Comment in: Nature. 1991 Aug 29;352(6338):754-5. MEDLINE 1991351275
`Source: Nature, Volume: 352, Issue: 6338, Pages: 803-7, Journal; Article; (JOURNAL ARTICLE); (RESEARCH SUPPORT, NON-U.S. GOV'T), 1991,
`ISSN: 0028-0836, Journal Code: 0410462, England: United Kingdom
`Company/Organization: Beckman Center for Molecular and Genetic Medicine, Howard Hughes Medical Institute, Stanford University Medical School, California
`94305
`Accession Number: 1991351285, PubMed ID: 1715516, MEDLINE
`Language: English
`
`
`Abstract
`Cyclosporin A and FK506 inhibit T- and B-cell activation and other processes essential to an effective immune response. In T
`lymphocytes these drugs disrupt an unknown step in the transmission of signals from the T-cell antigen receptor to cytokine genes
`that coordinate the immune response. The putative intracellular receptors for FK506 and cyclosporin are cis-trans prolyl
`isomerases. Binding of the drug inhibits isomerase activity, but studies with other prolyl isomerase inhibitors and analysis of
`cyclosporin-resistant mutants in yeast suggest that the effects of the drug result from the formation of an inhibitory complex
`between the drug and isomerase, and not from inhibition of isomerase activity. A transcription factor, NF-AT, which is essential
`for early T-cell gene activation, seems to be a specific target of cyclosporin A and FK506 action because transcription directed by
`this protein is blocked in T cells treated with these drugs, with little or no effect on other transcription factors such as AP-1 and
`NF-kappa B. Here we demonstrate that NF-AT is formed when a signal from the antigen receptor induces a pre-existing
`
`
`
`8
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`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`cytoplasmic subunit to translocate to the nucleus and combine with a newly synthesized nuclear subunit of NF-AT. FK506 and
`cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit.
`
`
`
`Copyright © 2018 U.S. National Library of Medicine.
`
`
`
`11. Inhibition of lymphoproliferative responses by SK&F 105685, a novel anti-arthritic agent
`
`By: Kaplan J M; Badger A M; Ruggieri E V; Olivera D L; Newman-Tarr T; Bugelski P J
`Source: Journal of clinical & laboratory immunology, Volume: 36, Issue: 4, Pages: 49-58, Journal; Article; (JOURNAL ARTICLE), 1991, ISSN: 0141-2760,
`Journal Code: 7808987, Scotland: United Kingdom
`Company/Organization: Department of Toxicology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939
`Accession Number: 1993148307, PubMed ID: 1668843, MEDLINE
`Language: English
`
`
`Abstract
`SK&F 105685 (N,N-Dimethyl-8,8-dipropyl-2-azaspiro[4.5]decane-2-propanamine+ ++ dihydrochloride) is a novel azaspirane
`with beneficial activity in animal models of autoimmune diseases such as adjuvant-induced arthritis and experimental
`autoimmune encephalomyelitis in the Lewis rat and lupus-like disease in the MRL mouse. The effect of SK&F 105685 on the
`proliferation of rat lymphoid cells was examined in vitro. The compound inhibited the proliferative response of spleen, thymus
`and lymph node cells to the mitogen concanavalin A (Con A) in a dose-dependent manner but had little or no effect on the
`mitogenic response of peripheral blood lymphocytes. Although less potent than cyclosporin A, SK&F 105685 was able to inhibit
`the proliferation of spleen cells stimulated with PMA and ionomycin or the mitogens phytohemagglutinin (PHA), Con A and
`pokeweed mitogen (PWM). Relatively early event(s) in cell proliferation were affected by SK&F 105685 since delaying addition
`of the drug by 24 to 48 hours after Con A stimulation of rat spleen cells resulted in reduced levels of suppression. The mode of
`action of SK&F 105685 appeared to differ from that of cyclosporin A or rapamycin. Unlike cyclosporin A, SK&F 105685 did
`not affect IL-2 production by Con A-stimulated spleen cells or the IL-2-producing Jurkat cell line, but, like rapamycin, the
`compound significantly reduced the IL-2-induced proliferation of rat ConA blasts. These results suggest that inhibition of
`lymphocyte proliferation by SK&F 105685 may require the activity of an intermediate effector cell(s) present in susceptible
`populations such as cells from the spleen, thymus, lymph nodes and Con A blast preparations but absent or present in low
`numbers in resistant populations such as peripheral blood cells. Indomethacin and NG-monomethyl-L-arginine (NGMMA), a
`competitive inhibitor of nitric oxide synthase, were both unable to relieve SK&F 105685-induced suppression of splenic Con A
`responses thereby ruling out a role for the production of prostaglandins or nitric oxide by macrophages as an intermediate in drug-
`mediated suppression. In summary, SK&F 105685 was unable to inhibit lymphoproliferative responses by a mechanism distinct
`from that of cyclosporin A or rapamycin and which appears to involve regulation of cellular interactions rather than a direct effect
`on responding lymphocytes.
`
`
`
`Copyright © 2018 U.S. National Library of Medicine.
`
`
`
`12. Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase
`9
`
`
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`
`By: Price, Daniel J.; Grove, J. Russell; Calvo, Victor; Avruch, Joseph; Bierer, Barbara E.
`Source: Science (Washington, DC, United States), Volume: 257, Issue: 5072, Pages: 973-7, Journal, 1992, CODEN: SCIEAS, ISSN: 0036-8075, DOI:
`10.1126/science.1380182
`Company/Organization: Diabetes Unit, Massachusetts Gen. Hosp., Boston, MA, USA, 02115
`Accession Number: 1992:563531, CAN 117:163531, CAPLUS
`Language: English
`
`Abstract
`The immunosuppressant rapamycin inhibited proliferation of the H4IIEC hepatoma cell line. Rapamycin, but not its structural
`analog FK506, also inhibited the basal and insulin-stimulated activity of the p70 ribosomal protein S6 kinase. By contrast,
`insulin stimulation of the p85 Rsk S6 kinase and mitogen-activated protein (MAP) kinase activity were unaffected by drug.
`Rapamycin treatment of COS cells transfected with recombinant p70 S6 kinase completely inhibited the appearance of the
`hyperphosphorylated form of p70 S6 kinase concomitant with the inhibition of enzyme activity toward 40 S subunits. Thus,
`rapamycin inhibits a signal transduction element that is necessary for the activation of p70 S6 kinase and mitogenesis but
`unnecessary for activation of p85 Rsk S6 kinase or MAP kinase.
`
`Indexing
`Pharmacology (Section 1-7)
`
`
`Supplementary Terms
`rapamycin immunosuppressant p70 S6 kinase inhibition; mitogenesis inhibition rapamycin p85RskS6 MAP kinase
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`13. Preparation of rapamycin silyl ethers as drugs
`
`By: Failli, Amedeo A.; Steffan, Robert J.
`Assignee: American Home Products Corp., USA
`Patent Information: Jun 09, 1992, US 5120842, A
`Application: Apr 01, 1991, US 1991-678380
`Priority: Apr 01, 1991, US 1991-678380
`Source: U.S., 5 pp., Patent, 1992, CODEN: USXXAM
`Classifications: Main IPC: A61K031-395, Secondary IPC: C07D491-06; , US 540452000
`Accession Number: 1992:571085, CAN 117:171085, CAPLUS
`Language: English
`
`Abstract
`Title compds. [I; R1 = SiR3R4R5; R2 = H, SiR3R4R5; R3-R5 = (phenyl)alkyl, alkenyl, Ph, CPh3] were prepd. Thus, rapamycin was
`converted to I (R1 = SiMe2CMe3, R2 = H) which had IC50 of 45.8 nM against lymphocyte proliferation in vitro.
`
`
`
`10
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`
`
`
`
`
`Kind
`A
`A1
`A
`A
`A2
`A
`A
`A1
`B1
`
`Date
`Jun 09, 1992
`Oct 02, 1992
`Mar 30, 1993
`Oct 02, 1992
`Apr 28, 1993
`Oct 08, 1992
`Sep 30, 1993
`Oct 07, 1992
`Jul 06, 1993
`
`Application No.
`US 1991-678380
`CA 1992-2063962
`JP 1992-67035
`NO 1992-1217
`HU 1992-1031
`AU 1992-13893
`ZA 1992-2308
`EP 1992-302843
`US 1992-90002871
`
`Date
`Apr 01, 1991
`Mar 25, 1992
`Mar 25, 1992
`Mar 27, 1992
`Mar 27, 1992
`Mar 30, 1992
`Mar 30, 1992
`Mar 31, 1992
`Oct 20, 1992
`
`Patent Information
`Patent No.
`US 5120842
`CA 2063962
`JP 05078377
`NO 9201217
`HU 62299
`AU 9213893
`ZA 9202308
`EP 507556
`US 5120842
`
`Priority Application
`US 1991-678380
`
`Indexing
`Biomolecules and Their Synthetic Analogs (Section 26-6)
`Section cross-reference(s):1
`
`
`Supplementary Terms
`rapamycin silyl ether prepn drug; immunosuppressive rapamycin silyl ether prepn; antifungal rapamycin silyl ether prepn;
`antitumor rapamycin silyl ether prepn
`
`Citations
`1)Anon; US 3929992 A
`2)Anon; US 3993749 A
`
`A
`
`Apr 01, 1991
`
`
`
`
`
`
`
`11
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`3)Anon; US 4316885 A
`4)Anon; US 4401653 A
`5)Anon; US 4650803 A
`6)Anon; US 4885171 A
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`14. Preparation of rapamycin metabolites as drugs
`
`By: Christians, Uwe; Sewing, Karl Friedrich; Sattler, Martin
`Assignee: American Home Products Corp., USA
`Patent Information: Nov 19, 1992, EP 514144, A2
`Application: May 13, 1992, EP 1992-304293
`Priority: May 14, 1991, US 1991-699505
`Source: Eur. Pat. Appl., 6 pp., Patent, 1992, CODEN: EPXXDW
`Classifications: Main IPC: C07D498-18, Secondary IPC: C12P017-18; A61K031-445;
`Accession Number: 1993:167605, CAN 118:167605, CAPLUS
`Language: English
`
`Abstract
`41-O-desmethylrapamycin (I) and a hydroxylated rapamycin metabolite (characterized by mass spectral data) were prepd. by
`incubation of rapamycin with a human liver microsome prepn. I had IC50 of 1.0 nmol/L against lymphocyte proliferation in vitro.
`
`Patent Information
`Patent No.
`EP 514144
`EP 514144
`EP 514144
`US 5776943
`CA 2068349
`CA 2068349
`AU 9216154
`AU 659452
`JP 05130884
`JP 3183554
`AT 174918
`ES 2126586
`HK 1010369
`
`Priority Application
`US 1991-699505
`
`Indexing
`
`A
`
`May 14, 1991
`
`
`
`
`
`
`
`12
`
`Kind
`A2
`A3
`B1
`A
`A1
`C
`A
`B2
`A
`B2
`T
`T3
`A1
`
`Date
`Nov 19, 1992
`Mar 03, 1993
`Dec 23, 1998
`Jul 07, 1998
`Nov 15, 1992
`Apr 09, 2002
`Nov 19, 1992
`May 18, 1995
`May 28, 1993
`Jul 09, 2001
`Jan 15, 1999
`Apr 01, 1999
`Apr 20, 2000
`
`Application No.
`EP 1992-304293
`
`
`US 1991-699505
`CA 1992-2068349
`
`AU 1992-16154
`
`JP 1992-118811
`
`AT 1992-304293
`ES 1992-304293
`HK 1998-110983
`
`Date
`May 13, 1992
`
`
`May 14, 1991
`May 11, 1992
`
`May 11, 1992
`
`May 12, 1992
`
`May 13, 1992
`May 13, 1992
`Sep 25, 1998
`
`

`

`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`Fermentation and Bioindustrial Chemistry (Section 16-2)
`Section cross-reference(s):1, 26
`
`
`Supplementary Terms
`rapamycin metabolite prepn drug; immunosuppressant rapamycin metabolite prepn; antiinflammatory rapamycin metabolite
`prepn; antifungal rapamycin metabolite prepn; antitumor rapamycin metabolite prepn
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`15. Pharmaceutical preparations containing immunosuppressants
`
`By: Badger, Alison Mary
`Assignee: SmithKline Beecham Corp., USA
`Patent Information: Feb 20, 1992, WO 9202229, A1
`Application: Aug 07, 1991, WO 1991-US5619
`Priority: Aug 10, 1990, US 1990-565826, Dec 05, 1990, US 1990-622452, Aug 07, 1991, WO 1991-US5619, Jan 10, 1994, US 1994-179462, Apr 03, 1995,
`US 1995-415875, Jan 10, 1994, US 1994-179456, Apr 03, 1995, US 1995-415876
`Source: PCT Int. Appl., 31 pp., Patent, 1992, CODEN: PIXXD2
`Classifications: Main IPC: A61K031-70, Secondary IPC: A61K031-44; A61K031-40;
`Accession Number: 1992:241940, CAN 116:241940, CAPLUS
`Language: English
`
`Abstract
`The title prepn. contains a nonspecific (NS) suppressor cell-inducing compd. such as N,N-dimethyl-8,8-dipropyl-2-
`azaspiro[4,5]decane-2-propanamine (I) and a non-NS suppressor cell-inducing immunosuppressant such as cyclosporin A (II). A
`capsule contained I 10, II 100, Mg stearate 2, lactose 30, and starch 10mg.
`
`Patent Information
`Patent No.
`WO 9202229
`AU 9184120
`AU 658577
`EP 542860
`EP 542860
`JP 06500321
`AT 166228
`ES 2118087
`ZA 9106320
`US 6051596
`US 20010014676
`
`Priority Application
`US 1990-565826
`
`Application No.
`WO 1991-US5619
`AU 1991-84120
`
`EP 1991-915005
`
`JP 1991-514153
`AT 1991-915005
`ES 1991-915005
`ZA 1991-6320
`US 1997-904932
`US 2001-772389
`
`Kind
`A1
`A
`B2
`A1
`B1
`T
`T
`T3
`A
`A
`A1
`
`Date
`Feb 20, 1992
`Mar 02, 1992
`Apr 27, 1995
`May 26, 1993
`May 20, 1998
`Jan 13, 1994
`Jun 15, 1998
`Sep 16, 1998
`Sep 30, 1992
`Apr 18, 2000
`Aug 16, 2001
`
`Date
`Aug 07, 1991
`Aug 07, 1991
`
`Aug 07, 1991
`
`Aug 07, 1991
`Aug 07, 1991
`Aug 07, 1991
`Aug 09, 1991
`Aug 01, 1997
`Jan 29, 2001
`
`
`
`A
`
`Aug 10, 1990
`
`
`
`13
`
`
`
`

`

`US 1990-622452
`WO 1991-US5619
`US 1994-179462
`US 1995-415875
`US 1994-179456
`US 1995-415876
`
`Indexing
`Pharmaceuticals (Section 63-6)
`Section cross-reference(s):1
`
`
`Supplementary Terms
`immunosuppressant cyclosporin azaspirododecanepropanamine capsule
`
`Citations
`1)Anon; US 4963557 A
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`16. Method using rapamycin for treating adult T-cell leukemia/lymphoma
`
`By: Miller, Glenn A.; Rabin, Mark B.; Harrington, William J., Jr.
`Assignee: American Home Products Corp., USA
`Patent Information: Dec 19, 1992, CA 2071456, A1
`Application: Jun 17, 1992, CA 1992-2071456
`Priority: Jun 18, 1991, US 1991-717773
`Source: Can. Pat. Appl., 9 pp., Patent, 1992, CODEN: CPXXEB
`Classifications: Main IPC: A61K031-445
`Accession Number: 1993:183404, CAN 118:183404, CAPLUS
`Language: English
`
`Abstract
`An antiproliferative amt. of rapamycin (I) is used to treat adult T-cell leukemia/lymphoma (ATL). The effect of I on ATL was
`established in an in vitro std. pharmacol. test using 10 HTLV-1 virus-transformed human T-cell lines cultured from ATL patients.
`I inhibited proliferation of 8/10 of the ATL cell lines at concns. ≥100 nM, with a 50% redn. in proliferation in 4 of the cell lines at
`a concn. of 1 nM.
`
`Patent Information
`Patent No.
`CA 2071456
`EP 525960
`IL 102185
`ZA 9204369
`
`Application No.
`CA 1992-2071456
`EP 1992-305287
`IL 1992-102185
`ZA 1992-4369
`
`Date
`Jun 17, 1992
`Jun 09, 1992
`Jun 12, 1992
`Jun 15, 1992
`
`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`
`
`Dec 05, 1990
`A
`
`
`Aug 07, 1991
`A
`
`
`Jan 10, 1994
`B2
`
`
`Apr 03, 1995
`B1
`
`
`Jan 10, 1994
`B2
`
`
`Apr 03, 1995
`B1
`
`Kind
`A1
`A1
`A
`A
`
`Date
`Dec 19, 1992
`Feb 03, 1993
`Sep 30, 1997
`Dec 15, 1993
`
`
`
`14
`
`

`

`A
`
`Jun 18, 1991
`
`
`
`
`
`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`Dec 24, 1992
`Jun 16, 1992
`A
`AU 1992-18255
`
`Jul 28, 1994
`B2
`
`Jan 28, 1993
`Jun 17, 1992
`A2
`HU 1992-2023
`
`Mar 02, 1998
`B
`
`Feb 09, 1993
`Jun 17, 1992
`A
`BR 1992-2287
`Jul 09, 1993
`Jun 17, 1992
`A
`JP 1992-157854
`
`Dec 11, 1996
`B2
`
`
`AU 9218255
`AU 651698
`HU 61480
`HU 214326
`BR 9102287
`JP 05170771
`JP 2562548
`
`Priority Application
`US 1991-717773
`
`Indexing
`Pharmacology (Section 1-6)
`
`
`Supplementary Terms
`adult T cell leukemia lymphoma rapamycin
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`17. Immunosuppressants for treatment of lung diseases
`
`By: Kay, Anthony Barry; Barnes, Neil Christopher; Cole, Peter John
`Assignee: National Heart and Lung Institute, UK
`Patent Information: May 29, 1992, WO 9208474, A2
`Application: Nov 20, 1991, WO 1991-GB2049
`Priority: Nov 20, 1990, GB 1990-25154, Dec 07, 1990, GB 1990-26620, Nov 20, 1991, WO 1991-GB2049
`Source: PCT Int. Appl., 70 pp., Patent, 1992, CODEN: PIXXD2
`Classifications: Main IPC: A61K037-02
`Accession Number: 1992:463005, CAN 117:63005, CAPLUS
`Language: English
`
`Abstract
`Specific pharmacol. targeting of T-lymphocytes provides a new approach to the treatment of chronic asthma (both in patients
`relatively sensitive and resistant to the effects of corticosteroids) and to the treatment of other lung diseases (e.g. bronchiectasis
`and cystic fibrosis), as well as sinusitis. Cyclosporin A (I) and other immunosuppressants (e.g. FK 506, rapamycin, humanized
`anti-CD4 antibodies) with the same or similar mode or site of action are provided for the treatment of diseases characterized by
`airflow obstruction and/or of chronic sinusitis. Also provided is an in vitro test for prediction of clin. response to corticosteroids
`and immunosuppressants. Corticosteroid resistance can be identified by the in vitro test, and corticosteroid-resistant patients thus
`identified can be treated with I or other suitable immunosuppressant. When patients with long-standing corticosteroid-dependent
`asthma were treated with I, there were significant increases above placebo in both morning and evening peak expiratory flow both
`pre- and post-bronchodilator. Patients on I suffered significantly fewer exacerbations requiring rescue prednisolone compared to
`placebo.
`
`
`
`
`15
`
`

`

`Application No.
`WO 1991-GB2049
`
`AU 1991-89108
`
`Date
`Nov 20, 1991
`
`Nov 20, 1991
`
`
`
`
`
`
`
`
`
`SciFinder® Search Results for Rapamycin References limited to Tumor or Cancer (1980-2002)
`Patent Information
`Patent No.
`WO 9208474
`WO 9208474
`AU 9189108
`
`Priority Application
`GB 1990-25154
`GB 1990-26620
`WO 1991-GB2049
`
`Indexing
`Pharmacology (Section 1-9)
`
`
`Supplementary Terms
`immunosuppressant lung disease treatment; cyclosporin A lung disease treatment; asthma treatment immunosuppressant; sinusitis
`treatment immunosuppressant; antiasthmatic immunosuppressant
`
`
`
`Copyright © 2018 American Chemical Society (ACS). All Rights Reserved.
`
`
`
`18. carbamoylrapamycin derivatives, a method for their preparation and their use as immunosuppressants
`
`By: Kao, Wenling; Vogel, Robert L.; Musser, John H.
`Assignee: American Home Products Corp., USA
`Patent Information: Jun 02, 1992, US 5118678, A
`Application: Apr 17, 1991, US 1991-686728
`Priority: Apr 17, 1991, US 1991-686728, Feb 18, 1992, US 1992-837048
`Source: U.S., 7 pp., Patent, 1992, CODEN: USXXAM
`Classifications: Main IPC: A61K031-395, Secondary IPC: C07D491-06; , US 514183000
`Accession Number: 1992:511387, CAN 117:111387, CAPLUS
`Language: English
`
`Abstract
`Certain derivs. of rapamycin, i.e., carbamoylrapamycin derivs., are claimed. Pharmaceuticals contg. said compds. as
`immunosuppressive agents are claimed. Rapamycin derivs. are also potential neoplasm inhibitors and antifungal agents.
`Treatment of rapamycin with 4-fluor