CO6390058A2 - Piperidina espiro pirrolidinona y piperidinona sustituidas usadas como moduladores de h3 - Google Patents
Piperidina espiro pirrolidinona y piperidinona sustituidas usadas como moduladores de h3Info
- Publication number
- CO6390058A2 CO6390058A2 CO11068488A CO11068488A CO6390058A2 CO 6390058 A2 CO6390058 A2 CO 6390058A2 CO 11068488 A CO11068488 A CO 11068488A CO 11068488 A CO11068488 A CO 11068488A CO 6390058 A2 CO6390058 A2 CO 6390058A2
- Authority
- CO
- Colombia
- Prior art keywords
- modulators
- pirrolidinona
- piperidinona
- espiro
- piperidine
- Prior art date
Links
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 2
- 102000004384 Histamine H3 receptors Human genes 0.000 abstract 2
- 108090000981 Histamine H3 receptors Proteins 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- KFIOZBMCNUODPK-UHFFFAOYSA-N n-phenyl-1-pyrrolidin-1-ylpyrrolidine-2-carboxamide Chemical class C1CCN(N2CCCC2)C1C(=O)NC1=CC=CC=C1 KFIOZBMCNUODPK-UHFFFAOYSA-N 0.000 abstract 2
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 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
Classifications
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
La presente invención describe y reivindica una serie de carboxamidas N-fenil-bipirrolidina sustituidas de fórmula (I).Donde R1, R2, R3, m, n y p son como se describen en el presente documento. Más específicamente, los compuestos de esta invención 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, la presente invención también describe métodos para la preparación de carboxamidas N-fenil-bipirrolidina sustituidas e intermedios para ello.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12008808P | 2008-12-05 | 2008-12-05 | |
| FR0955431 | 2009-07-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6390058A2 true CO6390058A2 (es) | 2012-02-29 |
Family
ID=41647030
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO11068488A CO6390058A2 (es) | 2008-12-05 | 2011-06-02 | Piperidina espiro pirrolidinona y piperidinona sustituidas usadas como moduladores de h3 |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US8227481B2 (es) |
| EP (1) | EP2373652B1 (es) |
| JP (1) | JP5538421B2 (es) |
| KR (1) | KR101687216B1 (es) |
| CN (1) | CN102239168B (es) |
| AR (1) | AR074466A1 (es) |
| AU (1) | AU2009322248B2 (es) |
| CA (1) | CA2745721C (es) |
| CO (1) | CO6390058A2 (es) |
| CR (1) | CR20110294A (es) |
| DK (1) | DK2373652T3 (es) |
| EC (1) | ECSP11011108A (es) |
| ES (1) | ES2441221T3 (es) |
| IL (1) | IL213290A (es) |
| MA (1) | MA32943B1 (es) |
| MX (1) | MX2011004939A (es) |
| NZ (1) | NZ593151A (es) |
| PE (1) | PE20120261A1 (es) |
| PT (1) | PT2373652E (es) |
| RU (1) | RU2011127401A (es) |
| TN (1) | TN2011000233A1 (es) |
| TW (1) | TWI481609B (es) |
| WO (1) | WO2010065803A1 (es) |
| ZA (1) | ZA201103448B (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| AR081908A1 (es) * | 2010-05-11 | 2012-10-31 | Sanofi Aventis | N-heteroaril-espirolactama-bipirrolidinas sustituidas, preparacion y usos terapeuticos de las mismas |
| EP2569294B1 (en) | 2010-05-11 | 2015-03-11 | Sanofi | Substituted n-heteroaryl bipyrrolidine carboxamides, preparation and therapeutic use thereof |
| JP2013529198A (ja) | 2010-05-11 | 2013-07-18 | サノフイ | 置換されたｎ−ヘテロシクロアルキルビピロリジニルフェニルアミド誘導体、その製造及び治療上の使用 |
| TW201206898A (en) * | 2010-05-11 | 2012-02-16 | Sanofi Aventis | Substituted N-phenyl spirolactam bipyrrolidines, preparation and therapeutic use thereof |
| WO2011143155A1 (en) | 2010-05-11 | 2011-11-17 | Sanofi | Substituted n-heteroaryl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof |
| AR083718A1 (es) | 2010-05-11 | 2013-03-20 | Sanofi Aventis | Fenil cicloalquil pirrolidina (piperidina) espirolactamas y amidas sustituidas, preparacion y uso terapeutico de las mismas |
| AR081498A1 (es) | 2010-05-11 | 2012-09-19 | Sanofi Aventis | Derivados de n-alquil -y n-acil-tetrahidroisoquinolina sustituidos, preparacion y su uso terapeutico de los mismos |
| BR112015007818A2 (pt) * | 2012-10-11 | 2017-11-28 | Merck Sharp & Dohme | composto, composição farmacêutica, e, uso de um composto e de uma composição farmacêutica |
| US9197285B2 (en) * | 2012-12-20 | 2015-11-24 | Deere & Company | Methods and apparatus for ameliorating signal reception |
| KR102716960B1 (ko) * | 2017-11-03 | 2024-10-11 | 브리스톨-마이어스 스큅 컴퍼니 | 디아자스피로 rock 억제제 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3256276A (en) | 1961-02-17 | 1966-06-14 | Geschickter Fund Med Res | Substituted spiroimides |
| FR2816940A1 (fr) | 2000-11-23 | 2002-05-24 | Lipha | Derives de 4-(biphenylcarbonylamino)-piperidine, compositions les contenant et leur utilisation |
| AU2003256755A1 (en) * | 2002-07-24 | 2004-02-09 | Ptc Therapeutics, Inc. | Ureido substituted benzoic acid compounds, their use for nonsense suppression and the treatment of diseases caused by such mutations |
| JP2006505590A (ja) * | 2002-10-23 | 2006-02-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒスタミンｈ３受容体調節物質としてのフェニルピペリジンおよびフェニルピロリジン |
| 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 |
| DE10306250A1 (de) * | 2003-02-14 | 2004-09-09 | Aventis Pharma Deutschland Gmbh | Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| JP4524550B2 (ja) | 2003-08-19 | 2010-08-18 | オイレス工業株式会社 | 摺動部材用樹脂組成物および摺動部材 |
| CN1902177A (zh) | 2003-09-22 | 2007-01-24 | 万有制药株式会社 | 新哌啶衍生物 |
| AU2006232871B9 (en) * | 2005-04-01 | 2011-11-24 | Eli Lilly And Company | Histamine H3 receptor agents, preparation and therapeutic uses |
| NZ568446A (en) | 2005-12-05 | 2011-12-22 | Incyte Corp | Lactam compounds and methods of using the same as modulators of 11-beta hydroxyl steroid dehydrogenase 1 |
| BRPI0619985A2 (pt) * | 2005-12-16 | 2011-10-25 | Hoffmann La Roche | compostos, processo para a sua manufatura, composições farmacêuticas, métodos para o tratamento e/ou prevenção de enfermidades que estão associadas com a modulação de receptores de h3, de obesidade e de diabetes do tipo ii em um ser humano ou animal e usos dos compostos |
| WO2007093364A1 (en) * | 2006-02-15 | 2007-08-23 | Sanofi-Aventis | 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 |
| US7479493B2 (en) | 2006-06-29 | 2009-01-20 | Janssen Pharmaceutica N.V. | Substituted benzyl amine compounds |
| US20080306102A1 (en) * | 2007-05-18 | 2008-12-11 | Kowa Co., Ltd. | Novel spirooxyindole compounds and drugs containing same |
| CL2008001839A1 (es) | 2007-06-21 | 2009-01-16 | Incyte Holdings Corp | Compuestos derivados de 2,7-diazaespirociclos, inhibidores de 11-beta hidroxil esteroide deshidrogenasa tipo 1; composicion farmaceutica que comprende a dichos compuestos; utiles para tratar la obesidad, diabetes, intolerancia a la glucosa, diabetes tipo ii, entre otras enfermedades. |
| WO2009039431A2 (en) * | 2007-09-21 | 2009-03-26 | Neurogen Corporation | Substituted aryl-fused spirocyclic amines |
| EP2205558B1 (en) * | 2007-10-17 | 2012-07-25 | Sanofi | Substituted n-phenyl-pyrrolidinylmethylpyrrolidine amides and therapeutic use thereof as histamine h3 receptor modulators |
| CA2702467C (en) | 2007-10-17 | 2012-11-27 | Sanofi-Aventis | Substituted n-phenyl-bipyrrolidine carboxamides and therapeutic use thereof |
| EP2212282B1 (en) * | 2007-10-17 | 2011-09-21 | Sanofi | Substituted n-phenyl-bipyrrolidine carboxamides and therapeutic use thereof |
| AU2009318855A1 (en) | 2008-11-23 | 2010-05-27 | Pfizer Inc. | Lactams as beta secretase inhibitors |
| 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. |
-
2009
- 2009-12-03 AR ARP090104666A patent/AR074466A1/es not_active Application Discontinuation
- 2009-12-04 KR KR1020117015340A patent/KR101687216B1/ko not_active Expired - Fee Related
- 2009-12-04 NZ NZ593151A patent/NZ593151A/xx not_active IP Right Cessation
- 2009-12-04 EP EP09793649.6A patent/EP2373652B1/en active Active
- 2009-12-04 ES ES09793649.6T patent/ES2441221T3/es active Active
- 2009-12-04 TW TW098141445A patent/TWI481609B/zh not_active IP Right Cessation
- 2009-12-04 PT PT97936496T patent/PT2373652E/pt unknown
- 2009-12-04 MX MX2011004939A patent/MX2011004939A/es active IP Right Grant
- 2009-12-04 PE PE2011001148A patent/PE20120261A1/es not_active Application Discontinuation
- 2009-12-04 JP JP2011539716A patent/JP5538421B2/ja not_active Expired - Fee Related
- 2009-12-04 RU RU2011127401/04A patent/RU2011127401A/ru not_active Application Discontinuation
- 2009-12-04 CA CA2745721A patent/CA2745721C/en not_active Expired - Fee Related
- 2009-12-04 MA MA33987A patent/MA32943B1/fr unknown
- 2009-12-04 AU AU2009322248A patent/AU2009322248B2/en not_active Ceased
- 2009-12-04 CN CN200980148493.0A patent/CN102239168B/zh not_active Expired - Fee Related
- 2009-12-04 WO PCT/US2009/066673 patent/WO2010065803A1/en active Application Filing
- 2009-12-04 DK DK09793649.6T patent/DK2373652T3/da active
-
2011
- 2011-05-11 TN TN2011000233A patent/TN2011000233A1/fr unknown
- 2011-05-11 ZA ZA2011/03448A patent/ZA201103448B/en unknown
- 2011-05-31 IL IL213290A patent/IL213290A/en not_active IP Right Cessation
- 2011-06-01 CR CR20110294A patent/CR20110294A/es unknown
- 2011-06-02 CO CO11068488A patent/CO6390058A2/es not_active Application Discontinuation
- 2011-06-02 US US13/151,946 patent/US8227481B2/en active Active
- 2011-06-03 EC EC2011011108A patent/ECSP11011108A/es unknown
-
2012
- 2012-06-19 US US13/527,147 patent/US8604046B2/en active Active
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Application refused |