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1022 Exhibit: Ex 1021 US 6794388

Document IPR2021-01132, No. 1022-22 Exhibit - Ex 1021 US 6794388 (P.T.A.B. Jun. 17, 2021)
Another embodiment of the invention relates to a phar maceutical composition comprising the succinate salt of 11.04 5,8,14-triazatetracyclo[l0.3.l .02 9 ]-hexadeca-2(11 ),3, • • 5,7,9-pentaene and a pharmaceutically acceptable carrier or excipient, particularly, one for use in the treatment of inflammatory bowel disease (including but not limited to ulcerative colitis, pyoderma gangrenosum and Crohn's disease), irritable bowel syndrome, spastic dystonia, chronic pain, acute pain, celiac sprue, pouchitis, vasoconstriction, anxiety, panic disorder, depression, bipolar disorder, autism, sleep disorders, jet lag, amyotrophic lateral sclerosis (ALS), cognitive dysfunction, hypertension, bulimia, anorexia, obesity, cardiac arrythmias, gastric acid hypersecretion, ulcers, pheochromocytoma, progressive supramuscular palsy, chemical dependencies and addictions (eq., depen dencies on, or addictions to nicotine (and/or tobacco 55 products), alcohol, benzodiazepines, barbiturates, opioids or cocaine), headache, migraine, stroke, traumatic brain injury (TEI), obsessive-compulsive disorder (OCD), psychosis, Huntington's chorea, tardive dyskinesia, hyperkinesia, dyslexia, schizophrenia, multi-infarct dementia, age-related 60 cognitive decline, epilepsy, including petit mal absence epilepsy, senile dementia of the Alzheimer's type (AD), Parkinson's disease (PD), attention deficit hyperactivity disorder (ADHD) and Tourette's Syndrome.
The present invention further relates to a the method of treating inflammatory bowel disease (including but not limited to ulcerative colitis, pyoderma gangrenosum and Crohn's disease), irritable bowel syndrome, spastic dystonia, chronic pain, acute pain, celiac sprue, pouchitis, vasoconstriction, anxiety, panic disorder, depression, bipolar disorder, autism, sleep disorders, jet lag, amyotrophic lateral sclerosis (ALS), cognitive dysfunction, hypertension, bulimia, anorexia, obesity, cardiac arrythmias, gastric acid hypersecretion, ulcers, pheochromocytoma, progressive supramuscular palsy, chemical dependencies and addictions (e.q., dependencies on, or addictions to nicotine (and/or tobacco products), alcohol, benzodiazepines, barbiturates, opioids or cocaine), headache, migraine, stroke, traumatic brain injury (TEI), obsessive-compulsive disorder (OCD), psychosis, Huntington's chorea, tardive dyskinesia, hyperkinesia, dyslexia, schizophrenia, multi-infarct dementia, age-related cognitive decline, epilepsy, including petit mal absence epilepsy, senile dementia of the Alzhe imer's type (AD), Parkinson's disease (PD), attention deficit hyperactivity disorder (ADHD) and Tourette's Syndrome comprises administering to a subject in need of treatment a therapeutically effective amount of the succinate salt of 11 .04 5,8,14-triazatetracyclo[l0.3.
Another more preferred embodiment of the invention relates to a method of treatment for nicotine dependency, addiction and withdrawal, in particular for use in smoking cessation therapy activity, comprising the administration of the succinate salt of 5,8,14-triazatetracyclo 11 .04 [10.3.1.02 9 ]-hexadeca-2(11),3,5,7,9-pentaene to a sub- 30 • • ject in need thereof.
Variations 40 may nevertheless occur depending upon the weight and condition of the persons being treated and their individual responses to said medicament, as well as on the type of pharmaceutical formulation chosen and the time period and interval during which such administration is carried out.
Solid compositions of a similar type may also be employed as fillers in gelatin capsules; preferred materials in this connection also include lactose or milk sugar, as well as 10 high molecular weight polyethylene glycols.
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1016 Exhibit: Ex 1015 Bastin

Document IPR2021-01132, No. 1016-16 Exhibit - Ex 1015 Bastin (P.T.A.B. Jun. 17, 2021)
These studies can help identify problems with low melting points, determined by hot-stage microscopy, and hygroscopicity, if processed on a suitable apparatus (e.g., Dynamic Vapour Sorption Analyser, model DVS-l, Surface Measurement Systems Ltd.).
In parallel with these studies, a preliminary high perfor mance liquid chromatographic (HPLC) method is quickly developed to give an estimate of the purity of the sample, whilst infrared and other spectroscopic techniques may be Vol.
Table 2. a Preformulation studies that are normally considered for comparison of salt forms and parent compound for oral dosage forms test suitable techniques comments dissociation constant and basic physico-chemical properties melting point aqueous solubility pH of solution cosolvent solubility common ion effect on solubility hygroscopicity potentiometry, solubility, UV spectroscopy capillary m.pt., hot stage microscopy, differential scanning calorimetry overnight equilibration at 25 DC; analysis by UV spectroscopy or HPLC overnight equilibration at 25 DC, analysis by UV spectroscopy or HPLC overnight equilibration at 25 DC in suitable media and analysis by UV spectroscopy or HPLC use DVS apparatus or expose to various RH values and measure weight gain after 1 week intrinsic dissolution rate use Wood's apparatus 14 crystal shape and appearance SEM or optical microscopy particle size polymorphismJpseudopolymorphism powder properties stability SEM and laser diffraction recrystallizations, HSM, DSC, TGA bulk density measurement various determine pKa for parent drug perform on each salt and compare to parent Perform on each salt and compare to parent Examine pH of saturated solution if quantities permit.
If 20-50% of the weight of the drug substance is due to inactive counterion, the addition of suitable excipients for encapsulation or tableting may result in a powder volume that is too great, even after granulation, to fit successfully into even the largest acceptable capsule shell.
12 The aim of both the Preformulation and Process Chemistry teams is to finalise the definition of all of the characteristics of the drug substance in readiness for the initiation of Phase IIa clinical trials Acknowledgment We thank our colleagues for their scientific contributions made during these studies and for the stimulating discussions held.
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1009 Exhibit: Ex 1008 CA 2467490

Document IPR2021-01132, No. 1009-9 Exhibit - Ex 1008 CA 2467490 (P.T.A.B. Jun. 17, 2021)

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1021 Exhibit: Ex 1020 US 2870198

Document IPR2021-01132, No. 1021-21 Exhibit - Ex 1020 US 2870198 (P.T.A.B. Jun. 17, 2021)

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1010 Exhibit: Ex 1009 Berge

Document IPR2021-01132, No. 1010-10 Exhibit - Ex 1009 Berge (P.T.A.B. Jun. 17, 2021)

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1019 Exhibit: Ex 1018 US 5834495

Document IPR2021-01132, No. 1019-19 Exhibit - Ex 1018 US 5834495 (P.T.A.B. Jun. 17, 2021)

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1017 Exhibit: Ex 1016 Nyqvist

Document IPR2021-01132, No. 1017-17 Exhibit - Ex 1016 Nyqvist (P.T.A.B. Jun. 17, 2021)

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1020 Exhibit: Ex 1019 US 5073376

Document IPR2021-01132, No. 1020-20 Exhibit - Ex 1019 US 5073376 (P.T.A.B. Jun. 17, 2021)

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