AR081908A1 - N-heteroaril-espirolactama-bipirrolidinas sustituidas, preparacion y usos terapeuticos de las mismas - Google Patents
N-heteroaril-espirolactama-bipirrolidinas sustituidas, preparacion y usos terapeuticos de las mismasInfo
- Publication number
- AR081908A1 AR081908A1 ARP110101610A ARP110101610A AR081908A1 AR 081908 A1 AR081908 A1 AR 081908A1 AR P110101610 A ARP110101610 A AR P110101610A AR P110101610 A ARP110101610 A AR P110101610A AR 081908 A1 AR081908 A1 AR 081908A1
- Authority
- AR
- Argentina
- Prior art keywords
- hydrogen
- preparation
- espirolactama
- bipirrolidinas
- heteroaril
- Prior art date
Links
- 230000001225 therapeutic effect Effects 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 102000004384 Histamine H3 receptors Human genes 0.000 abstract 2
- 108090000981 Histamine H3 receptors Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008177 pharmaceutical agent Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (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)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Más específicamente, los compuestos son moduladores de los receptores H3 y, por lo tanto, son útiles como agentes farmacéuticos, especialmente en el tratamiento y/o prevención de una variedad de enfermedades moduladas por los receptores H3, incluyendo enfermedades asociadas con el sistema nervioso central. Además, también describe métodos de preparación de N-heteroaril-espirolactama-bipirrolidinas de fórmula (1) y compuestos intermedios para los mismos.Reivindicación 1: Un compuesto de fórmula (1) en la que m, p = 1 ó 2; n, s = 1 ó 2; X es O, NR3 o CR4R5; Q1 a Q4 son independientemente CH o N, con la condición de que al menos uno de Q1 a Q4 sea N; R1 es hidrógeno, alquilo C1-4, CF3 o alcoxi C1-4; R2 es hidrógeno, halógeno, alquilo C1-4, alcoxi C1-4 o CF3; R3 es hidrógeno o alquiloxi C1-6-carbonilo; R4 es hidrógeno; y R5 es hidrógeno u OH; o una sal del mismo o un enantiómero o un diastereoisómero del mismo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33339310P | 2010-05-11 | 2010-05-11 | |
| FR1061074 | 2010-12-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR081908A1 true AR081908A1 (es) | 2012-10-31 |
Family
ID=44305055
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101610A AR081908A1 (es) | 2010-05-11 | 2011-05-10 | N-heteroaril-espirolactama-bipirrolidinas sustituidas, preparacion y usos terapeuticos de las mismas |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US8796278B2 (es) |
| EP (1) | EP2569304A1 (es) |
| JP (1) | JP5833105B2 (es) |
| AR (1) | AR081908A1 (es) |
| TW (1) | TW201202251A (es) |
| WO (1) | WO2011143148A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201202251A (en) | 2010-05-11 | 2012-01-16 | Sanofi Aventis | Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof |
| IL311645B2 (en) | 2016-07-12 | 2025-11-01 | Revolution Medicines Inc | 2,5- disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines asallosteric shp2 inhibitors |
| KR20190110588A (ko) | 2017-01-23 | 2019-09-30 | 레볼루션 메디슨즈, 인크. | 알로스테릭 shp2 억제제로서의 피리딘 화합물 |
| SG11201906209SA (en) | 2017-01-23 | 2019-08-27 | Revolution Medicines Inc | Bicyclic compounds as allosteric shp2 inhibitors |
| CA3078565A1 (en) * | 2017-10-12 | 2019-04-18 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| EP3704121B1 (en) | 2017-11-03 | 2022-12-21 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
| KR20200099530A (ko) | 2017-12-15 | 2020-08-24 | 레볼루션 메디슨즈, 인크. | 알로스테릭 shp2 억제제로서의 다환식 화합물 |
| KR102581268B1 (ko) | 2019-09-03 | 2023-09-22 | 주식회사 엘지화학 | 에어로겔 블랭킷 제조방법 |
| EP4251148A1 (en) | 2020-11-27 | 2023-10-04 | Richter Gedeon Nyrt. | Histamine h3 receptor antagonists/inverse agonists for the treatment of autism spectrum disorder |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3960961A (en) | 1970-08-31 | 1976-06-01 | The Upjohn Company | 4'-Fluoro-4-{[4-(phenyl)cyclohexyl]amino}butyrophenones and the salts thereof |
| US20030073836A1 (en) | 2001-07-05 | 2003-04-17 | Boehringer Ingelheim Pharma Kg | Heteroarylcarboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions |
| CA2504272A1 (en) * | 2002-10-23 | 2004-05-06 | Janssen Pharmaceutica, N.V. | Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators |
| DE10306250A1 (de) * | 2003-02-14 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US7223788B2 (en) | 2003-02-14 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Substituted N-aryl heterocycles, process for their preparation and their use as medicaments |
| AU2004274309B2 (en) | 2003-09-22 | 2010-04-08 | Msd K.K. | Novel piperidine derivative |
| GB0405628D0 (en) | 2004-03-12 | 2004-04-21 | Glaxo Group Ltd | Novel compounds |
| BRPI0511778A (pt) | 2004-06-02 | 2008-01-15 | Hoffmann La Roche | derivados da naftalina úteis como ligantes do receptor 3 da histamina |
| US7517991B2 (en) * | 2004-10-12 | 2009-04-14 | Bristol-Myers Squibb Company | N-sulfonylpiperidine cannabinoid receptor 1 antagonists |
| RU2391338C2 (ru) * | 2004-10-19 | 2010-06-10 | Ф.Хоффманн-Ля Рош Аг | Производные хинолина |
| ZA200703950B (en) | 2004-10-21 | 2008-07-30 | Vertex Pharma | Triazoles useful as inhibitors of protein kinases |
| WO2006103045A1 (en) * | 2005-03-31 | 2006-10-05 | Ucb Pharma S.A. | Compounds comprising an oxazole or thiazole moiety, processes for making them, and their uses |
| WO2006132914A2 (en) | 2005-06-03 | 2006-12-14 | Abbott Laboratories | Cyclobutyl amine derivatives |
| EP1790646A1 (fr) * | 2005-11-24 | 2007-05-30 | Sanofi-Aventis | Derives de Isoquinoline et Benzo[h]Isoquinoline, leur preparation et leur utilisation en thérapeutique en tant qu'antagonistes du recepteur de l'histamine H3. |
| TW200800908A (en) * | 2006-02-15 | 2008-01-01 | Sanofi Aventis | Novel azacyclyl-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments |
| US20080247964A1 (en) * | 2006-05-08 | 2008-10-09 | Yuelian Xu | Substituted azaspiro derivatives |
| TW200918062A (en) | 2007-09-12 | 2009-05-01 | Wyeth Corp | Azacyclylisoquinolinone and-isoindolinone derivatives as histamine-3 antagonists |
| WO2009039431A2 (en) | 2007-09-21 | 2009-03-26 | Neurogen Corporation | Substituted aryl-fused spirocyclic amines |
| KR20100092443A (ko) | 2007-10-17 | 2010-08-20 | 사노피-아벤티스 | 치환된 ｎ-페닐-피롤리디닐메틸피롤리딘 아미드 및 히스타민 ｈ3 수용체 조절제로서의 이의 치료적 용도 |
| NZ584692A (en) | 2007-10-17 | 2011-12-22 | Sanofi Aventis | Substituted n-phenyl-bipyrrolidine ureas and therapeutic use thereof |
| CN101903340B (zh) | 2007-10-17 | 2013-03-27 | 赛诺菲-安万特 | 取代的n-苯基联吡咯烷羧酰胺及其治疗用途 |
| PT2212282E (pt) * | 2007-10-17 | 2012-01-09 | Sanofi Sa | Carboxamidas de n-fenil-bipirrolidina substituídas e sua utilização terapêutica |
| GEP20125590B (en) | 2008-07-18 | 2012-07-25 | Takeda Pharmaceutical | Benzazepine derivatives and usage thereof as histamine h3 antagonists |
| CN102272135A (zh) * | 2008-10-08 | 2011-12-07 | 百时美施贵宝公司 | 唑并吡咯酮黑色素浓集激素受体-1拮抗剂 |
| AR074466A1 (es) | 2008-12-05 | 2011-01-19 | Sanofi Aventis | Piperidina espiro pirrolidinona y piperidinona sustituidas y su uso terapeutico en enfermedades mediadas por la modulacion de los receptores h3. |
| AR074467A1 (es) * | 2008-12-05 | 2011-01-19 | Sanofi Aventis | Tetrahidropiran espiro pirrolidinonas y piperidinonas sustituidas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento y/o prevencion de enfermedades del snc ,tales como alzheimer y parkinson, entre otras. |
| TW201202251A (en) | 2010-05-11 | 2012-01-16 | Sanofi Aventis | Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof |
-
2011
- 2011-05-10 TW TW100116248A patent/TW201202251A/zh unknown
- 2011-05-10 JP JP2013510220A patent/JP5833105B2/ja not_active Expired - Fee Related
- 2011-05-10 EP EP11731172A patent/EP2569304A1/en not_active Withdrawn
- 2011-05-10 WO PCT/US2011/035824 patent/WO2011143148A1/en not_active Ceased
- 2011-05-10 AR ARP110101610A patent/AR081908A1/es unknown
-
2012
- 2012-11-06 US US13/670,067 patent/US8796278B2/en not_active Expired - Fee Related
-
2014
- 2014-06-27 US US14/318,272 patent/US9533995B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011143148A1 (en) | 2011-11-17 |
| US20140315923A1 (en) | 2014-10-23 |
| TW201202251A (en) | 2012-01-16 |
| US20130059863A1 (en) | 2013-03-07 |
| JP5833105B2 (ja) | 2015-12-16 |
| EP2569304A1 (en) | 2013-03-20 |
| US9533995B2 (en) | 2017-01-03 |
| US8796278B2 (en) | 2014-08-05 |
| JP2013526526A (ja) | 2013-06-24 |
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