`United States Patent No. 9,815,827
`
`U.S. PATENT NO. 9,815,827 CLAIM LISTING
`Limitation
`
`1. A method
`
`
`
`No.
`1P
`
`1.1
`
`for treating schizophrenia in a patient
`
`1.2 without a clinically significant weight gain, comprising:
`
`1.3
`
`1.4
`
`1.5
`
`1.6
`
`2P
`
`administering orally to the patient
`
`(1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide or a pharmaceutically
`acceptable salt thereof
`
`at a dose of from 20 to 120 mg/day such that
`
`the patient does not experience a clinically significant weight gain.
`
`2. The method of claim 1,
`
`2.1 wherein (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-
`yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride is administered.
`
`3P
`
`3.1
`
`3. The method of claim 2, wherein the administering is conducted
`such that
`
`the patient does not experience a clinically significant weight gain
`after six weeks of administration.
`
`4P
`
`4. The method of claim 3,
`
`4.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`5P
`
`5.1
`
`6P
`
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`5. The method of claim 2, further comprising:
`
`detecting a weight gain after six weeks of administration.
`
`6. The method of claim 1,
`
`
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`6.1 wherein said patient has a BPRS score of at least 42 and wherein
`
`6.2
`
`the patient's BPRS score is significantly reduced from a baseline
`measurement prior to the administering.
`
`7P
`
`7. The method of claim 3,
`
`7.1 wherein the dose is from 40 to 120 mg once daily.
`
`8P
`
`8.1
`
`8. A method
`
`for treating manic depressive psychosis in a patient
`
`8.2 without a clinically significant weight gain, comprising:
`
`8.3
`
`8.4
`
`8.5
`
`8.6
`
`9P
`
`administering orally to the patient
`
`(1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide or a pharmaceutically
`acceptable salt thereof
`
`at a dose of from 20 to 120 mg/day such that
`
`the patient does not experience a clinically significant weight gain.
`
`9. The method of claim 8,
`
`9.1 wherein (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-
`yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride is administered.
`
`10P 10. The method of claim 9,
`
`10.1 wherein the administering is conducted such that the patient does
`not experience a clinically significant weight gain after six weeks
`of administration.
`
`11P 11. The method of claim 9, further comprising:
`
`11.1 detecting a weight gain after six weeks of administration.
`
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`12P 12. The method of claim 10,
`
`12.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`13P 13. The method of claim 10,
`
`13.1 wherein the dose is 20 mg once daily.
`
`14P 14. The method of claim 10,
`
`14.1 wherein the dose is 40 mg once daily.
`
`15P 15. The method of claim 10,
`
`15.1 wherein the dose is 60 mg once daily.
`
`16P 16. The method of claim 10,
`
`16.1 wherein the dose is 80 mg once daily.
`
`17P 17. The method of claim 10,
`
`17.1 wherein the dose is 120 mg once daily.
`
`18P 18. The method of claim 9,
`
`18.1 wherein the dose is 20 mg, 40 mg, 60 mg, 80 mg or 120 mg once
`daily.
`
`19P 19. The method of claim 3,
`
`19.1 wherein the dose is 20 mg once daily.
`
`20P 20. The method of claim 3,
`
`20.1 wherein the dose is 40 mg once daily.
`
`21P 21. The method of claim 3,
`
`21.1 wherein the dose is 60 mg once daily.
`
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`22P 22. The method of claim 3,
`
`22.1 wherein the dose is 80 mg once daily.
`
`23P 23. The method of claim 3,
`
`23.1 wherein the dose is 120 mg once daily.
`
`24P 24. The method of claim 2,
`
`24.1 wherein the dose is 20 mg, 40 mg, 60 mg, 80 mg or 120 mg once
`daily.
`
`25P 25. A method
`
`25.1 of treating a patient with an antipsychotic
`
`25.2 without a clinically significant weight gain in the patient,
`comprising:
`
`25.3 orally administering the antipsychotic to the patient
`
`25.4 once daily at a dose of from 20 to 120 mg such that
`
`25.5 the patient does not experience a clinically significant weight gain,
`
`25.6 wherein the antipsychotic is (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-
`benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-
`2,3-bicyclo[2.2.1]heptanedicarboximide or a pharmaceutically
`acceptable salt thereof.
`
`26P 26. The method of claim 25,
`
`26.1 wherein the antipsychotic is (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-
`benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-
`2,3-bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`27P 27. The method of claim 26,
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`27.1 wherein the administering is conducted such that the patient does
`not experience a clinically significant weight gain after six weeks
`of administration.
`
`28P 28. The method of claim 26, further comprising:
`
`28.1 detecting a weight gain after six weeks of administration.
`
`29P 29. The method of claim 27,
`
`29.1 wherein the method treats schizophrenia in the patient.
`
`30P 30. The method of claim 27,
`
`30.1 wherein the method treats manic depressive psychosis in the
`patient.
`
`31P 31. The method of claim 25,
`
`31.1 wherein the method treats the patient without the patient
`experiencing a weight gain.
`
`32P 32. The method of claim 29,
`
`32.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`33P 33. The method of claim 30,
`
`33.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`34P 34. The method of claim 27,
`
`34.1 wherein the dose is 20 mg.
`
`35P 35. The method of claim 27,
`
`35.1 wherein the dose is 40 mg.
`
`36P 36. The method of claim 27,
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`36.1 wherein the dose is 60 mg.
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`Inter Partes Review
`United States Patent No. 9,815,827
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`Limitation
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`37P 37. The method of claim 27,
`
`37.1 wherein the dose is 80 mg.
`
`38P 38. The method of claim 27,
`
`38.1 wherein the dose is 120 mg.
`
`39P 39. The method of claim 26,
`
`39.1 wherein the dose is 20 mg, 40 mg, 60 mg, 80 mg or 120 mg.
`
`40P 40. A method
`
`40.1 of treating a patient with an antipsychotic
`
`40.2 without a clinically significant weight gain, comprising:
`
`40.3 orally administering
`
`40.4 once daily to the patient
`
`40.5 a pharmaceutical composition comprising 20 to 120 mg of
`
`40.6 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide or a pharmaceutically
`acceptable salt thereof
`
`40.7 as a sole active ingredient such that
`
`40.8 the patient does not experience a clinically significant weight gain.
`
`41P 41. The method of claim 40,
`
`41.1 wherein the sole active ingredient is (1R,2S,3R,4S)-N-[(1R,2R)-2-
`[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-
`cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide
`hydrochloride.
`
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`42P 42. The method of claim 41,
`
`42.1 wherein the pharmaceutical composition is a tablet.
`
`43P 43. The method of claim 41,
`
`43.1 wherein the administering is conducted such that the patient does
`not experience a clinically significant weight gain after six weeks
`of administration.
`
`44P 44. The method of claim 41, further comprising:
`
`44.1 detecting a weight gain after six weeks of administration.
`
`45P 45. The method of claim 43,
`
`45.1 wherein the method treats schizophrenia in the patient.
`
`46P 46. The method of claim 43,
`
`46.1 wherein the method treats manic depressive psychosis in the
`patient.
`
`47P 47. The method of claim 45,
`
`47.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`48P 48. The method of claim 46,
`
`48.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`49P 49. The method of claim 41,
`
`49.1 wherein the pharmaceutical composition includes 40 to 120 mg of
`
`49.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
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`50P 50. The method of claim 41,
`
`50.1 wherein the pharmaceutical composition includes 20 mg, 40 mg,
`60 mg, 80 mg or 120 mg of
`
`50.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`51P 51. The method of claim 41,
`
`51.1 wherein the pharmaceutical composition includes 20 mg of
`
`51.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`52P 52. The method of claim 41,
`
`52.1 wherein the pharmaceutical composition includes 40 mg of
`
`52.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`53P 53. The method of claim 41,
`
`53.1 wherein the pharmaceutical composition includes 60 mg of
`
`53.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`54P 54. The method of claim 41,
`
`54.1 wherein the pharmaceutical composition includes 80 mg of
`
`54.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
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`55P 55. The method of claim 41,
`
`55.1 wherein the pharmaceutical composition includes 120 mg of
`
`55.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`56P 56. A method
`
`56.1 of treating a patient with an antipsychotic
`
`56.2 without a weight gain, comprising:
`
`56.3 orally administering
`
`56.4 once daily to the patient
`
`56.5 a pharmaceutical composition comprising 20 to 120 mg of
`
`56.6 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide or a pharmaceutically
`acceptable salt thereof
`
`56.7 as a sole active ingredient such that
`
`56.8 the patient does not experience a weight gain.
`
`57P 57. The method of claim 56,
`
`57.1 wherein the sole active ingredient is (1R,2S,3R,4S)-N-[(1R,2R)-2-
`[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-
`cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide
`hydrochloride.
`
`58P 58. The method of claim 57,
`
`58.1 wherein the pharmaceutical composition is a tablet.
`
`59P 59. The method of claim 57,
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`59.1 wherein the administering is conducted such that the patient does
`not experience a weight gain after six weeks of administration.
`
`60P 60. The method of claim 57, further comprising:
`
`60.1 detecting a weight gain after six weeks of administration.
`
`61P 61. The method of claim 57,
`
`61.1 wherein the method treats schizophrenia in the patient.
`
`62P 62. The method of claim 57,
`
`62.1 wherein the method treats manic depressive psychosis in the
`patient.
`
`63P 63. The method of claim 61,
`
`63.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`64P 64. The method of claim 62,
`
`64.1 wherein the administering is conducted without concurrently
`administering another antipsychotic medication.
`
`65P 65. The method of claim 61,
`
`65.1 wherein the pharmaceutical composition includes 40 to 120 mg of
`(1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`66P 66. The method of claim 57,
`
`66.1 wherein the pharmaceutical composition includes 20 mg, 40 mg,
`60 mg, 80 mg or 120 mg of
`
`66.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
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`67P 67. The method of claim 62,
`
`67.1 wherein the pharmaceutical composition includes 20 mg of
`
`67.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`68P 68. The method of claim 61,
`
`68.1 wherein the pharmaceutical composition includes 40 mg of
`
`68.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`69P 69. The method of claim 62,
`
`69.1 wherein the pharmaceutical composition includes 40 mg of
`
`69.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`70P 70. The method of claim 61
`
`70.1 wherein the pharmaceutical composition includes 60 mg of
`
`70.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`71P 71. The method of claim 62
`
`71.1 wherein the pharmaceutical composition includes 60 mg of
`
`71.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`72P 72. The method of claim 61,
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`72.1 wherein the pharmaceutical composition includes 80 mg of
`
`72.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`73P 73. The method of claim 62,
`
`73.1 wherein the pharmaceutical composition includes 80 mg of
`
`73.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`74P 74. The method of claim 61,
`
`74.1 wherein the pharmaceutical composition includes 120 mg of
`
`74.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
`
`75P 75. The method of claim 62,
`
`75.1 wherein the pharmaceutical composition includes 120 mg of
`
`75.2 (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1 -
`piperazinylmethyl]-1-cyclohexylmethyl]-2,3-
`bicyclo[2.2.1]heptanedicarboximide hydrochloride.
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