OA11742A - 5HT1 antagonists for antidepressant therapy. - Google Patents
5HT1 antagonists for antidepressant therapy. Download PDFInfo
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- OA11742A OA11742A OA1200100172A OA1200100172A OA11742A OA 11742 A OA11742 A OA 11742A OA 1200100172 A OA1200100172 A OA 1200100172A OA 1200100172 A OA1200100172 A OA 1200100172A OA 11742 A OA11742 A OA 11742A
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Claims (20)
1. 10 15 20 -31- CLAIMS
11742 (l) wherein R1, R2, R3 and R4 are selected, independently, from hydrogen, (C,-C4) alkyloptionally substituted with from one to three fluorine atoms, (C,-C4)alkoxy optionallysubstituted with from one to three fluorine atoms, and (C1-C4)alkoxy-(C1-C4)alkyl wherein eachof the alkyl moieties may optionally be substituted with from one to three fluorine atoms; and X is CH or N; or a pharmaceutically acceptable sait thereof.
2. A compound according to claim 1, wherein having an absolute sterochemistryof (7R, 9aS)-trans or (7S, 9aS)-cis.
3. A compound according to claim 1 that is selected from: (7R,9aS)-trans-f2-(5-Fluoro-benzo[d1isoxazol-3-yl)-octahydro-pvridoff ,2-alpyrazin-7- ylmethyl]-(5-fluoro-pyrirnidin-2-yl)-amine; (7R,9aS)-trans-f2-(5-Fluoro-benzo[d1isoxazol-3-yl)-octahydro-pyridof1,2-a]pyrazin-7-ylmethy!]-pyrimidin-2-yl)-amine; (7S,9aS)-çis-[2-(5-Fluoro-benzo[d]isoxazol-3-yI-ocîahydro-pyrido[1,2-a]pyrazin-7- ylmethyi-(5-fluoro-pyridin-2-yl)-amine; (7S,9aS)-cis-(2-Benzo[d]isoxazol-3-yi)-octahydro-pyrido[1,2-a]pyrazin-7-ylmethyl)- pyrimidin-2-yl-amine; (7S,9aS)-cis-(2-Benzo[d]isoxazo!-3-yl-octahydro-pyrido[1,2-a]pyrazin-7-ylmethyl)-(5- fluoro-pyrimidin-2-yl)-amine; (7R,9aS)-trans-(2-Benzofdlisoxazol-3-yl-octahydro-pyridof1.2-alpvrazin-7-vlmethvl)- (5-methyl-pyrimÎdin-2-yl)-amine; (7S,9aS)-cis-(2-Benzo[d]isoxazol-3-yi-octahydro-pyrido[1,2-a]pyrazin-7-ylmethyl)-(5- methyl-pyrimidin-2-yl)-amine; 117 4 2 -32- (7R,9aS)-trans-(2-Benzo[d1isoxazol-3-yl-octahydre-pyridof1,2-ajpyrazin-7-ylmethyl)-(5-chloro-pyrimidin-2-yl)-amine; (7S,9aS)-cis-(2-Benzo[d]isoxazol-3-yl-octahydro-pyrido[1,2-a]pyrazin-7-ylmethyl)-(5-chloro-pyrimidin-2-yl)-amine; 5 (7R,9aS)-trans-(5-C.hloro-pyrimidin-2-yl)-[2-(5-fluoro-benzo[d]isoxazol-3-yl)- octahydro-pyrido[1,2-a]pyrazin-7-ylmethyl]-amine; (7S,9aS)-cis-(5-Chloro-pyrimidin-2-yi)-[2-(5-fiuoro-benzo[d]isoxazol-3-yl)-octahydro-pyrido[1,2-a]pyrazin-7-ylmethylJ-amine; (7R,9aS)-trans-[2-(5-Fluoro-benzo[d]isoxazol-3-yl)-octahydro-pyrido[1,2-alpyrazin-7-10 ylmethyl]-(5-methyl-pyrimÎdin-2-yl)-amÎne; (7S,9aS)-cis-[2-(5-Fluoro-benzo{d]isoxazol-3-yl)-octahydro-pyrido[1,2-a]pyrazin-7- ylrnethyl]-(5-methyl-pyrirnidin-2-yl)-amine; (7R,9aS)-trans-(2-Benzo[djisoxazoi-3-yl-octahydro-pyrido[1,2-a]pyrazin-7-ylmethyl)-(5-fiuoro-pyridin-2-yl)-amine; 15 (7S,9aS)-cis-(2-Benzo[d]isoxazol-3-yi-octahydro-pyrido[1,2-a]pyrazin-7-ylmethyl)-(5- fluoro-pyridin-2-yl)-amine; (7R,9aS)-trans-[2-(5-Fluoro-benzo[d1isoxazol-3-yl)-octahydro-pyridot1,2-a1pyrazin-7- ylmethyl]-{5-fiuoro-pyndin-2-yl)-amine; (7S,9aS)-cis-I2-(5-Fluoro-benzo[dlisoxazol-3-yl)-octahydro-pyridof1.2-a]pvrazin-7-20 ylmethyl]-(5-fluoro-pyridin-2-yl)-amine; (7R,9aS)-trans-(2-Benzofd]isoxazol-3-yl-octahydro-pyridof1,2-a]pyrazin-7-ylmethyl)-(5-fluoro-3-methyl-pyridin-2-yl)-amine; (7S,9aS)-cis-(2-Benzo[d1isoxazol-3-yl-octahydro-pyrido[1,2-a1pyrazin-7-ylmethyl)-(5- fiuoro-3-methyi-pyridin-2-yl)-amine; 25 (7R,9aS)-trans-[2-(5-Fluoro-benzojdlisoxazol-3-yl)-octahydro-pyridof1,2-a1pyrazin-7- ylmethyl]-pyridin-2-yl)-amine; (7R,93S)-trans-[2-(5-Fluoro-benzofd1isoxazoi-3-vl)-octahydro-pvridoi1.2-a1pyrazin-7- ylmethyl]-(5-fiuoro-3-methyl-pyridin-2-yl)-amine; (7S,9aS)-cis-[2-(5-Fluoro-benzo[d3isoxazoi-3-yl)-octahydro-pyridof1,2-a]pyrazin-7-30 ylmethyi)-(5-fluoro-3-methyI-pyridin-2-yl)-amine; and (7R,9aS)-trans-(2-Benzo[d]isoxazo1-3yl-octahydro-pyrido[1,2-a3pyrazin-7-yl- methyl)-(5-fluoro-pyrimidin-2-yl)-amine.
4. A pharmaceutical composition for treating a disorder or condition seiectedfrom hypertension, dépréssion, generalized anxiety disorder, phobias, posttraumatic stress 35 syndrome, avoidant personality disorder, prématuré éjaculation, eating disorders, obesity,Chemical dependencies, cluster headache, migraine, pain, Alzheimer’s disease, obsessive- 117 4 2 -33- compulsive disorder, panic disorder, memory disorders, Parkinson's diseases, endocrinedisorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, négative symptomsof schizophrénie, premenstrual syndrome, fibromyalgia syndrome, stress incontinence,Tourette’s syndrome, trichotillomania, kleptomania, male impotence, cancer, chronic 5 paroxysmal hemicrania and headache in a mammal, comprising an amount of a compoundaccording to claim 1 that is effective in treating such disorder or condition and apharmaceütically acceptable carrier.
5. A pharmaceutical composition for treating a disorder or condition that can betreated by moduiati.ng serotonergic neurotransmission in a mammal, comprising an amount of 10 a compound according to claim 1 that is effective in treating such disorder or condition and apharmaceütically acceptable carrier.
6. Use of a compound according to claim 1 in the manufacture of a médicament' for the treatment of a disorder or condition selected from hypertension, dépréssion,generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant 15 personality disorder, prématuré éjaculation, eating disorders, obesity, Chemical dependencies,cluster headache, migraine, pain, Alzheimer’s disease, obsessive-compulsive disorder, panicdisorder, memory disorders, Parkinson's diseases, endocrine disorders, vasospasm,cerebellar ataxia, gastrointestinal tract disorders, négative symptoms of schizophrénie,premenstrual syndrome, fibromyalgia syndrome, stress incontinence, Tourette’s syndrome, 20 trichotillomania, kleptomania, male impotence, cancer, chronic paroxysmal hemicrania andheadache in a mammal
7. Use of a compound according to claim 1 in the manufacture of a médicamentfor the treatment of a disorder or condition that can be treated or prevented by modulatingserotonergic neurotransmission in a mammal. 25
8. A pharmaceutical composition for treating a disorder or condition selected from hypertension, dépréssion, generalized anxiety disorder, phobias, posttraumatic stresssyndrome, avoidant personality disorder, prématuré éjaculation, eating disorders, obesity,Chemical dependencies, cluster headache, migraine, pain, Alzheimer's disease, obsessive-compulsive disorder, panic disorder, memory disorders, Parkinson's diseases, endocrine 30 disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, négative symptomsof schizophrenia, premenstrual syndrome, fibromyalgia syndrome, stress incontinence,Tourette’s syndrome, trichotillomania, kleptomania, male impotence, cancer, chronicparoxysmal hemicrania and headache in a mammal, comprising a serotonin receptor 11742 -34- antagonizing or agonizing effective amount of a compound according to claim 1 and apharmaceutically acceptable carrier.
9. A pharmaceutical composition for treating a disorder or condition that can betreated by modulating serotonergic neurotransmission in a mammal, comprising a serotonin 5 receptor antagonizing or agonizing effective amount of a compound of according to claim 1and a pharmaceutically acceptable carrier.
10. Use according to Claim 6 wherein the compound is used in a serotonin IAreceptor antagonizing or agonizing effective amount, or a serotonin 1D receptor antagonizingeffective amount, _ 1®
11· Use according to Claim 7 wherein the compound is used in a serotonin IA receptor antagonizing or agonizing effective amount, or a serotonin 1D receptor antagonizingeffective amount. 20
12. A pharmaceutical composition for treating disorder or condition that can betreated or prevented by modulating serotonergic neurotransmission in a mammal, comprising: a) a pharmaceutically acceptable carrier, b) a compound of according to ciaim 1 ; and c) a 5-HT re-uptake inhibitor or a pharmaceutically acceptable sait thereof;wherein the amount of the active compounds are such that the combination is effective in treating such disorder or condition.
13. Use of (a) a compound according to claim 1 ; and (b) a 5-HT re-uptake inhibitor or a pharmaceutically acceptable sait thereof, in the manufacture of a médicament for the treatment of a disorder or a condition that can betreated by modulating serotonergic neurotransmission in a mammal. 25
14. A pharmaceutical composition according to ciaim 12, wherein the 5-KT re- uptake inhibitor is sertraline or a pharmaceutically acceptable sait thereof. 117 4 2 -35-
15. Use according to claim 13, wherein the 5-HT re-uptake inhibitor is sertralineor a pharmaceutically acceptable sait thereof.
16. Use of (a) a compound according to claim 1; and 5 (b) a 5-HT re-uptake inhibitor or a pharmaceutically acceptable sait thereof in the manufacture of a médicament for the treatment of a disorder or condition selected fromhypertension, dépréssion, generalized anxïety disorder, phobias, posttraumatic stresssyndrome, avoidant personality disorder, sexual dysfunction, eating disorders, obesity, Chemical dependencies, cluster headache, migraine, pain, Alzheimer’s disease, obsessive- Wcompulsive disorder, panic~disorder, memory disorders, Parkinson's diseases, endocrinedisorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, négative symptomsof schizophrénie, premenstrual syndrome, fibromyalgia syndrome, stress incontinence,Tourette’s syndrome,’ trichotillomania, kleptomanie, male impotence, cancer, chronicparoxysmal hemicrania and· headache in a mammai *5
17. Use of (a) a 5-HT IA antagonist or agonist or a pharmaceutically acceptable saitthereof; and (b) a 5-HT 1D antagonizing compound according to claim 1; for the manufacture of a médicament for the treatment of a disorder or condition that 2Q:an be treated or prevented by modulating serotonergic neurotransmission in a mammai.
18. Use of (a) a 5-HT1A agonist or antagonist or a pharmaceutically acceptable sait thereof;and (b) a 5-HT 1D antagonizing compound according to claim 1; 25for the manufacture of a médicament for the treatment of a disorder or condition selectedfrom: hypertension dépréssion, generalized anxiety disorder, phobias, posttraumatic stresssyndrome, avoidant personality disorder, sexual dysfunction, eating disorders, obesity, Chemical dependencies, cluster headache, migraine, pain, Alzheimer’s disease, obsessive-·compuisive disorder, partie disorder, memory disorders, Parkinson’s diseases, endocrine 3° disorders, vasospasm, cerebellar ataxia, gastrointestinal tr3ct disorders, négative 11742 -36- symptoms of schizophrenia, premenstruai syndrome, fibromyalgia syndrome,stress incontinence,· Tourette’s syndrome, trichotiiiomania, kleptomania, maleimpotence, cancer, chronic paroxysmal hemicransa and headache in a mammal
19. A pharmaceutica! composition for treating a disorder or condition that can betreated by modulating serotonergic neurotransmission in a mammai, comprising: a) a 5-HT1A agonist or antagonist or a pharmaceutically acceptable sait thereof;and b) a 5-HT1D antagonizing compound according to claim 1; wherein the amounts of the active compounds are such that the combination iseffective in treating such disorder or condition.
20. A pharmaceutical composition for treating a disorder or condition selectedfrom hypertension, dépréssion, generalized anxiety disorder, phobias, posttraumatic stresssyndrome, avoidant personaiity disorder, sexuai dysfunction, eating disorders, obesity,Chemical dependencies, cluster headache, migraine, pain, Alzheimer's disease, obsessive-compulsive disorder, panic disorder, memory disorders, Parkinson's diseases, endocrinedisorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, négative symptomsof schizophrenia, premenstruai syndrome, fibromyalgia syndrome, stress incontinence,Tourette’s syndrome, trichotiiiomania, kieptomania, male impotence, cancer, chronicparoxysmal hemicrania and headache in a mammal, comprising: a) a 5-HT1A agonist or antagonist or a pharmaceutically acceptable sait thereof;and b) a 5-HT1D antagonizing compound according to claim 1 ; wherein the amounts of the active compounds are such that the combination iseffective in treating such disorderor condition.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11395798P | 1998-12-28 | 1998-12-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| OA11742A true OA11742A (en) | 2005-05-13 |
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ID=22352526
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| OA1200100172A OA11742A (en) | 1998-12-28 | 1999-11-03 | 5HT1 antagonists for antidepressant therapy. |
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Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60229123D1 (de) * | 2001-02-20 | 2008-11-13 | Dinan Timothy Gerard | Behandlung von fibromyalgie mit pindolol |
| GB0203778D0 (en) * | 2002-02-18 | 2002-04-03 | Glaxo Group Ltd | Compounds |
| BRPI0408248A (pt) | 2003-03-12 | 2006-03-01 | Pfizer Prod Inc | derivados azabicìclicos de piridiloximetila e de benzisoxazol |
| GB0316915D0 (en) * | 2003-07-18 | 2003-08-20 | Glaxo Group Ltd | Compounds |
| JP2007519705A (ja) * | 2004-01-29 | 2007-07-19 | ファイザー・プロダクツ・インク | Ｃｎｓ障害を治療するための非定型抗精神病薬とアミノメチルピリジルオキシメチル／ベンゾイソオキサゾールアザビシクロ誘導体の組合せ |
| AR048112A1 (es) * | 2004-03-25 | 2006-03-29 | Solvay Pharm Bv | Derivados de 1-(2h-1-benzopiran-2-on-8-il)-piperazina para el tratamiento de dolor |
| AR049478A1 (es) | 2004-03-25 | 2006-08-09 | Solvay Pharm Bv | Un procedimiento para la preparacion de 3-amino-8-(1-piperazinil)-2h-1-benzopiran-2-ona. sales e hidratos y composiciones farmaceuticas. |
| BRPI0515143A (pt) * | 2004-09-10 | 2008-07-08 | Pfizer Prod Inc | usos de derivados azabicìclicos de piridiloximetila e benzisoxazol para a preparação de uma composição farmacêutica para o tratamento dos distúrbios de humor |
| EP1791540A2 (fr) * | 2004-09-10 | 2007-06-06 | Pfizer Products Incorporated | Methodes destinees a traiter des troubles cognitifs au moyen de derives azabicycliques de pyridyloxymethyle et de benzisoxazole |
| DE102005026194A1 (de) * | 2005-06-06 | 2006-12-07 | Grünenthal GmbH | Substituierte N-Benzo[d]isoxazol-3-yl-amin-Derivate und deren Verwendung zur Herstellung von Arzneimitteln |
| WO2008019431A1 (fr) * | 2006-08-14 | 2008-02-21 | Brc Operations Pty Limited | Procédé et compositions pour réguler simultanément la mémoire et l'humeur |
| CA2891122C (fr) | 2012-11-14 | 2021-07-20 | The Johns Hopkins University | Methodes et compositions pour le traitement de la schizophrenie |
| WO2020183011A1 (fr) | 2019-03-14 | 2020-09-17 | Institut Curie | Inhibiteurs de htr1d et leurs utilisations dans le traitement du cancer |
| US20230057844A1 (en) * | 2019-12-20 | 2023-02-23 | The Jackson Laboratory | Molecular targets for addiction |
Family Cites Families (6)
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| US5157034A (en) * | 1991-02-27 | 1992-10-20 | Pfizer Inc. | Neuroleptic perhydro-1H-pyrido[1,2-a]pyrazines |
| GB9410512D0 (en) * | 1994-05-25 | 1994-07-13 | Smithkline Beecham Plc | Novel treatment |
| AU2565595A (en) * | 1994-05-28 | 1995-12-21 | Smithkline Beecham Plc | Amide derivatives having 5ht1d-antagonist activity |
| BR9809092A (pt) * | 1997-04-18 | 2002-01-22 | Smithkline Beecham Plc | Derivados de indol tendo atividade combinada de antagonista de receptor de 5ht1a, 5ht1b e 5ht1d |
| IT1293807B1 (it) * | 1997-08-01 | 1999-03-10 | Recordati Chem Pharm | Derivati 1- (n-fenilaminoalchil) piperazinici sostituiti alla posizione 2 dell'anello fenilico |
| PA8469101A1 (es) * | 1998-04-09 | 2000-09-29 | Pfizer Prod Inc | Ligandos azabiciclicos de receptores 5ht1 |
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