BR9911280A - Aryl piperazines, piperidines and tetrahydro pyridines substituted with an alkyl cycle as serotonergic agents - Google Patents
Aryl piperazines, piperidines and tetrahydro pyridines substituted with an alkyl cycle as serotonergic agentsInfo
- Publication number
- BR9911280A BR9911280A BR9911280-9A BR9911280A BR9911280A BR 9911280 A BR9911280 A BR 9911280A BR 9911280 A BR9911280 A BR 9911280A BR 9911280 A BR9911280 A BR 9911280A
- Authority
- BR
- Brazil
- Prior art keywords
- piperidines
- group
- aryl
- alkyl
- serotonergic agents
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 title abstract 2
- 150000003053 piperidines Chemical group 0.000 title abstract 2
- 239000003762 serotonin receptor affecting agent Substances 0.000 title abstract 2
- -1 Aryl piperazines Chemical class 0.000 title 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- RQMWVVBHJMUJNZ-UHFFFAOYSA-N 4-chloropyridin-2-amine Chemical compound NC1=CC(Cl)=CC=N1 RQMWVVBHJMUJNZ-UHFFFAOYSA-N 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 230000007278 cognition impairment Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 150000004885 piperazines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
- C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
- C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Indole Compounds (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
Abstract
Patente de Invenção: <B>"ARIL PIPERAZINAS, PIPERIDINAS E TETRAIDRO PIRIDINAS SUBSTITUìDAS COM CICLO ALQUILA COMO AGENTES SEROTONéRGICOS"<D>. Esta invenção refere-se a compostos que têm atividade como agonistas e antagonista 5-HT~ 1A~ que podem ser úteis para o tratamento de ansiedade, depressão, déficits cognitivos, e câncer de próstata. Compostos úteis são aqueles de fórmula (I) onde: X é selecionado do grupo consistindo em (1), (2), (3); n é selecionado dos inteiros 1 até 5; R^ 1^ é opcionalmente C~ 6-10~ arila substituído ou hetero arila substituído ou hetero arila mono ou bicíclico, com a condição de que hetero arila não é tiadiazol; R^ 2^ é selecionado do grupo consistindo em H e C~ 1-6~ alquila; R^ 3^ é selecionado do grupo consistindo em H, COR^ 5^, COOR^ 5^, e CONR^ 5^R^ 6^, R^ 4^, R^ 5^ e R^ 6^ são como definidos anteriormente; ou um isómero ótico, ou um seu sal farmaceuticamente aceitável.Invention Patent: <B> "ARIL PIPERAZINES, PIPERIDINES AND PYRIDINES TETRAIDRO REPLACED WITH ALKYL CYCLE AS SEROTONERGIC AGENTS" <D>. This invention relates to compounds that have activity as 5-HT ~ 1A ~ agonists and antagonists that may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer. Useful compounds are those of formula (I) where: X is selected from the group consisting of (1), (2), (3); n is selected from integers 1 through 5; R ^ 1 é C is optionally substituted C ~ 6-10 ~ aryl or hetero aryl or mono or bicyclic hetero aryl, with the proviso that hetero aryl is not thiadiazole; R ^ 2 ^ is selected from the group consisting of H and C ~ 1-6 ~ alkyl; R ^ 3 ^ is selected from the group consisting of H, COR ^ 5 ^, COOR ^ 5 ^, and CONR ^ 5 ^ R ^ 6 ^, R ^ 4 ^, R ^ 5 ^ and R ^ 6 ^ are as previously defined ; or an optical isomer, or a pharmaceutically acceptable salt thereof.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9746398A | 1998-06-15 | 1998-06-15 | |
| PCT/US1999/013397 WO1999065887A1 (en) | 1998-06-15 | 1999-06-14 | Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9911280A true BR9911280A (en) | 2001-03-13 |
Family
ID=22263490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9911280-9A BR9911280A (en) | 1998-06-15 | 1999-06-14 | Aryl piperazines, piperidines and tetrahydro pyridines substituted with an alkyl cycle as serotonergic agents |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1087954A1 (en) |
| JP (1) | JP2002518382A (en) |
| CN (1) | CN1312802A (en) |
| AU (1) | AU4566399A (en) |
| BR (1) | BR9911280A (en) |
| CA (1) | CA2334254A1 (en) |
| WO (1) | WO1999065887A1 (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6376494B1 (en) * | 1998-06-15 | 2002-04-23 | American Home Products Corporation | Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents |
| US6696450B2 (en) | 2001-04-04 | 2004-02-24 | Wyeth | Serotonergic agents with long-acting in vivo effects |
| JP5080716B2 (en) | 2001-07-20 | 2012-11-21 | サイコジェニックス・インコーポレーテッド | Treatment of attention deficit / hyperactivity disorder |
| US7067518B2 (en) | 2002-09-05 | 2006-06-27 | Wyeth | Pyridinyl-methyl-ethyl cyclohexanecarboxamides as serotonergic agents |
| EP2338873A1 (en) | 2009-12-22 | 2011-06-29 | Gmeiner, Peter | New aminotetraline derivatives |
| JP2016079168A (en) * | 2014-10-17 | 2016-05-16 | 塩野義製薬株式会社 | 9 membered condensed-ring derivative |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2140374T3 (en) * | 1989-04-22 | 2000-03-01 | American Home Prod | DERIVATIVES OF PIPERAZINE FUNCTIONALIZED WITH TERTIARY RENTALS. |
| FR2655988B1 (en) * | 1989-12-20 | 1994-05-20 | Adir Cie | NOVEL DERIVATIVES OF NAPHT-1-YL PIPERAZINE, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. |
| US5159081A (en) * | 1991-03-29 | 1992-10-27 | Eli Lilly And Company | Intermediates of peripherally selective n-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists |
| MX9201991A (en) * | 1991-05-02 | 1992-11-01 | Jonh Wyeth & Brother Limited | DERIVATIVES OF PIPERAZINE AND PROCEDURE FOR ITS PREPARATION. |
| IT1251144B (en) * | 1991-07-30 | 1995-05-04 | Boehringer Ingelheim Italia | BENZIMIDAZOLONE DERIVATIVES |
| GB9125900D0 (en) * | 1991-12-05 | 1992-02-05 | Wyeth John & Brother Ltd | Piperazine derivatives |
| GB9306103D0 (en) * | 1993-03-24 | 1993-05-12 | Wyeth John & Brother Ltd | Piperazine derivatives |
| GB9411099D0 (en) * | 1994-06-03 | 1994-07-27 | Wyeth John & Brother Ltd | Piperazine derivatives |
| ZA954688B (en) * | 1994-06-08 | 1996-01-29 | Lundbeck & Co As H | Serotonin 5-HT1A and dopamin D2 receptor ligands |
| GB9413772D0 (en) * | 1994-07-08 | 1994-08-24 | Wyeth John & Brother Ltd | 5-HT1A ligands |
| FR2727682A1 (en) * | 1994-12-02 | 1996-06-07 | Pf Medicament | NOVEL DERIVATIVES OF 3,5-DIOXO- (2H, 4H) -1,2,4-TRIAZINES, THEIR PREPARATION AND THEIR USE AS A MEDICINAL PRODUCT |
| US5486518A (en) * | 1995-04-10 | 1996-01-23 | American Home Products Corporation | 4-indolylpiperazinyl derivatives |
| DE19615232A1 (en) * | 1996-04-18 | 1997-10-23 | Merck Patent Gmbh | New carbamoyl derivatives and their use as 5-HT ¶1¶¶A¶ antagonists |
-
1999
- 1999-06-14 CA CA002334254A patent/CA2334254A1/en not_active Abandoned
- 1999-06-14 AU AU45663/99A patent/AU4566399A/en not_active Abandoned
- 1999-06-14 CN CN99809567A patent/CN1312802A/en active Pending
- 1999-06-14 JP JP2000554713A patent/JP2002518382A/en active Pending
- 1999-06-14 EP EP99928648A patent/EP1087954A1/en not_active Withdrawn
- 1999-06-14 WO PCT/US1999/013397 patent/WO1999065887A1/en not_active Ceased
- 1999-06-14 BR BR9911280-9A patent/BR9911280A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CN1312802A (en) | 2001-09-12 |
| EP1087954A1 (en) | 2001-04-04 |
| AU4566399A (en) | 2000-01-05 |
| CA2334254A1 (en) | 1999-12-23 |
| JP2002518382A (en) | 2002-06-25 |
| WO1999065887A1 (en) | 1999-12-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25D | Requested change of name of applicant approved | ||
| B08F | Application fees: dismissal - article 86 of industrial property law | ||
| B08K | Lapse as no evidence of payment of the annual fee has been furnished to inpi (acc. art. 87) |
Free format text: REFERENTE AO DESPACHO PUBLICADO NA RPI 1937 DE 19/02/2008 |