AR067808A1 - Pirrolidina -aril-eteres como antagonistas de receptor de nk3 - Google Patents
Pirrolidina -aril-eteres como antagonistas de receptor de nk3Info
- Publication number
- AR067808A1 AR067808A1 ARP080103406A ARP080103406A AR067808A1 AR 067808 A1 AR067808 A1 AR 067808A1 AR P080103406 A ARP080103406 A AR P080103406A AR P080103406 A ARP080103406 A AR P080103406A AR 067808 A1 AR067808 A1 AR 067808A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- halogen
- cyano
- amino
- hydrogen
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 150000002431 hydrogen Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 abstract 1
- 208000020401 Depressive disease Diseases 0.000 abstract 1
- 102000002003 Neurokinin-3 Receptors Human genes 0.000 abstract 1
- 108010040716 Neurokinin-3 Receptors Proteins 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000028017 Psychotic disease Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- -1 cyano, amino Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
Classifications
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/22—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
- 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
- C07D401/02—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 two hetero rings
- C07D401/08—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 two hetero rings linked by a carbon chain containing alicyclic rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
La invencion se refiere a un compuesto de la formula general 1 en la que Ar1 es arilo o un heteroarilo de cinco o seis eslabones; Ar2 es arilo o un heteroarilo de cinco o seis eslabones: R1 es hidrogeno, halogeno, alquilo inferior, alcoxi inferior, alquilo inferior sustituido por halogeno, alcoxi inferior sustituido por halogeno, S-alquilo inferior, -S(O)2-alquilo inferior, -S(O)2-di (alquilo inferior)- amino, (CH2)qR, ciano, amino, mono- o di-(alquilo inferior)-amino, NHC(O)-alquilo inferior, cicloalquilo o es un heteroarilo de cinco eslabones, opcionalmente sustituido por alquilo inferior; en el que R es ciano, di (alquilo inferior) -amino o pirrolidin-1-ilo; R2 es hidrogeno, halogeno, alquilo inferior, alquilo inferior sustituido por halogeno o ciano; R3 es hidrogeno o alquilo inferior o CH2OH; R4 es hidrogeno, halogeno, alquilo inferior, alquilo inferior sustituido por halogeno o ciano; n es el. numero 1, 2 o 3; en caso de que n sea el numero 2 o 3, R1 puede ser igual o diferente; o es el numero 1, 2 o 3; en caso de que o sea el numero 2 o 3, R2 puede ser igual o diferente; p es el numero 1, 2 o 3; en caso de que p sea el numero 2 o 3, R4 puede ser igual o diferente; q es el numero 1 o 2; o a una sal farmacéuticamente activa del mismo; incluidas todas las formas estereoisoméricas, todos los diastereoisomeros y enantiomeros individuales del compuesto de la formula (1) así como las mezclas racémicas y no racémicas de los mismos. Se ha encontrado que los compuestos presentes son antagonistas potencialmente fuertes del receptor de la NK-3 para el tratamiento de la depresion, el dolor, la psicosis, la enfermedad de Parkinson, la esquizofrenia, la ansiedad y el trastorno de hiperactividad con déficit de atencion (ADHD).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07113942 | 2007-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR067808A1 true AR067808A1 (es) | 2009-10-21 |
Family
ID=39865446
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080103406A AR067808A1 (es) | 2007-08-07 | 2008-08-05 | Pirrolidina -aril-eteres como antagonistas de receptor de nk3 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8012998B2 (es) |
| EP (1) | EP2185540B1 (es) |
| JP (1) | JP2010535733A (es) |
| KR (1) | KR101167774B1 (es) |
| CN (1) | CN101778837A (es) |
| AR (1) | AR067808A1 (es) |
| AT (1) | ATE517100T1 (es) |
| AU (1) | AU2008285718A1 (es) |
| BR (1) | BRPI0815658A2 (es) |
| CA (1) | CA2695211A1 (es) |
| CL (1) | CL2008002293A1 (es) |
| ES (1) | ES2367464T3 (es) |
| IL (1) | IL203363A (es) |
| MX (1) | MX2010001080A (es) |
| PE (1) | PE20090898A1 (es) |
| RU (1) | RU2010106974A (es) |
| TW (1) | TW200916456A (es) |
| WO (1) | WO2009019163A1 (es) |
| ZA (1) | ZA201000676B (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2697325A1 (en) * | 2007-08-22 | 2009-02-26 | F. Hoffmann-La Roche Ag | Pyrrolidine aryl-ether as nk3 receptor antagonists |
| KR101372743B1 (ko) | 2009-01-30 | 2014-03-14 | 에프. 호프만-라 로슈 아게 | Ｎｋ3 수용체 길항제로서 피페리딘 유도체 |
| US8318759B2 (en) * | 2009-02-18 | 2012-11-27 | Hoffmann-La Roche Inc. | Pyrrolidine derivatives as NK3 receptor antagonists |
| US8394834B2 (en) * | 2009-08-25 | 2013-03-12 | Hoffman-La Roche Inc. | Pyrrolidines as NK3 receptor antagonists |
| JP2013508350A (ja) * | 2009-10-20 | 2013-03-07 | ファイザー・インク | ガンマ−セクレターゼモジュレーターとしての新規なヘテロアリールイミダゾールおよびヘテロアリールトリアゾール |
| US8507535B2 (en) | 2010-07-07 | 2013-08-13 | Hoffmann-La Roche Inc. | Methyl-pyrrolidine ether derivatives |
| EP3183248B1 (en) | 2014-08-21 | 2020-11-11 | Bristol-Myers Squibb Company | Tied-back benzamide derivatives as potent rock inhibitors |
| CA3015702A1 (en) | 2015-09-02 | 2017-03-09 | Trevena, Inc. | 6-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
| WO2017072629A1 (en) | 2015-10-29 | 2017-05-04 | Cadila Healthcare Limited | Pharmaceutical combination of nk3 receptor antagonist and biguanides |
| CN105399661A (zh) * | 2015-12-14 | 2016-03-16 | 华东师范大学 | 2,6-二溴甲基吡啶的制备方法 |
| US11178872B2 (en) | 2016-05-09 | 2021-11-23 | Nippon Soda Co., Ltd. | Cyclic amine compound and pest control agent |
| KR20190129867A (ko) | 2017-02-17 | 2019-11-20 | 트레베나, 인코포레이티드. | 5-원 아자-헤테로고리 함유 델타-오피오이드 수용체 조절 화합물, 및 그의 사용 및 제조 방법 |
| EP3582783B1 (en) | 2017-02-17 | 2023-06-07 | Trevena, Inc. | 7-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
| WO2021030335A1 (en) * | 2019-08-12 | 2021-02-18 | Millendo Therapeutics, Inc. | A stereoisomerically pure nk-3 receptor antagonist and crystalline forms thereof |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU506399B2 (en) | 1975-12-30 | 1980-01-03 | Showa Denko Kabushiki Kaisha | 3-(2-aryl-2-propyl) ureas |
| IN148482B (es) | 1977-06-03 | 1981-03-07 | Pfizer | |
| GB9321557D0 (en) | 1992-11-03 | 1993-12-08 | Zeneca Ltd | Carboxamide derivatives |
| IL111960A (en) | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| CN1067683C (zh) | 1993-12-29 | 2001-06-27 | 默克·夏普-道姆公司 | 取代的吗啉衍生物及其作为治疗剂的用途 |
| TW385308B (en) | 1994-03-04 | 2000-03-21 | Merck & Co Inc | Prodrugs of morpholine tachykinin receptor antagonists |
| GB9714129D0 (en) * | 1997-07-04 | 1997-09-10 | Pfizer Ltd | Azetidines |
| US5972938A (en) | 1997-12-01 | 1999-10-26 | Merck & Co., Inc. | Method for treating or preventing psychoimmunological disorders |
| EP1192952A3 (en) | 2000-09-28 | 2003-03-26 | Pfizer Products Inc. | Combination, for treating depression and anxiety, containing an NK-3 receptor antagonist and a CNS penetrant NK-1 receptor antagonist |
| US6531597B2 (en) | 2001-02-13 | 2003-03-11 | Hoffmann-La Roche Inc. | Process for preparation of 2-phenyl acetic acid derivatives |
| BR0311425A (pt) * | 2002-05-31 | 2005-03-15 | Takeda Pharmaceutical | Composto, pró-droga, método para preparar o composto, álcool oticamente ativo, e amina oticamemte ativa, e para prevenir e/ou tratar anormalidades ou doenças, medicamento, e, uso do composto ou de uma pró-droga deste |
| WO2005002577A1 (en) | 2003-07-03 | 2005-01-13 | F. Hoffmann-La Roche Ag | Dual nk1/nk3 antagonists for treating schizophrenia |
| US7468437B2 (en) * | 2003-09-30 | 2008-12-23 | Merck & Co., Inc. | Phenyl pyrrolidine ether tachykinin receptor antagonists |
| CA2552965A1 (en) * | 2004-01-14 | 2005-07-28 | Takeda Pharmaceutical Company Limited | Carboxamide derivative and use thereof |
| US7138423B2 (en) * | 2004-07-20 | 2006-11-21 | Bristol-Myers Squibb Company | Arylpyrrolidine derivatives as NK-1 /SSRI antagonists |
| KR100939347B1 (ko) | 2005-07-20 | 2010-01-29 | (주)카이로드 | 광학적으로 순수한 (ｓ)-3-히드록시 피롤리딘의 제조방법 |
-
2008
- 2008-07-29 MX MX2010001080A patent/MX2010001080A/es active IP Right Grant
- 2008-07-29 RU RU2010106974/04A patent/RU2010106974A/ru unknown
- 2008-07-29 ES ES08786547T patent/ES2367464T3/es active Active
- 2008-07-29 BR BRPI0815658-1A2A patent/BRPI0815658A2/pt not_active IP Right Cessation
- 2008-07-29 CA CA2695211A patent/CA2695211A1/en not_active Abandoned
- 2008-07-29 CN CN200880102376A patent/CN101778837A/zh active Pending
- 2008-07-29 KR KR1020107004881A patent/KR101167774B1/ko not_active Expired - Fee Related
- 2008-07-29 JP JP2010519428A patent/JP2010535733A/ja active Pending
- 2008-07-29 EP EP08786547A patent/EP2185540B1/en not_active Not-in-force
- 2008-07-29 AU AU2008285718A patent/AU2008285718A1/en not_active Abandoned
- 2008-07-29 WO PCT/EP2008/059908 patent/WO2009019163A1/en not_active Ceased
- 2008-07-29 AT AT08786547T patent/ATE517100T1/de active
- 2008-08-04 US US12/185,157 patent/US8012998B2/en not_active Expired - Fee Related
- 2008-08-04 CL CL2008002293A patent/CL2008002293A1/es unknown
- 2008-08-05 PE PE2008001308A patent/PE20090898A1/es not_active Application Discontinuation
- 2008-08-05 AR ARP080103406A patent/AR067808A1/es unknown
- 2008-08-06 TW TW097129930A patent/TW200916456A/zh unknown
-
2010
- 2010-01-18 IL IL203363A patent/IL203363A/en not_active IP Right Cessation
- 2010-01-28 ZA ZA201000676A patent/ZA201000676B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009019163A1 (en) | 2009-02-12 |
| IL203363A (en) | 2013-03-24 |
| CL2008002293A1 (es) | 2009-05-29 |
| AU2008285718A1 (en) | 2009-02-12 |
| CA2695211A1 (en) | 2009-02-12 |
| ATE517100T1 (de) | 2011-08-15 |
| BRPI0815658A2 (pt) | 2015-02-18 |
| ZA201000676B (en) | 2010-10-27 |
| RU2010106974A (ru) | 2011-09-20 |
| US8012998B2 (en) | 2011-09-06 |
| KR20100045502A (ko) | 2010-05-03 |
| EP2185540A1 (en) | 2010-05-19 |
| TW200916456A (en) | 2009-04-16 |
| EP2185540B1 (en) | 2011-07-20 |
| KR101167774B1 (ko) | 2012-07-24 |
| JP2010535733A (ja) | 2010-11-25 |
| PE20090898A1 (es) | 2009-07-13 |
| MX2010001080A (es) | 2010-03-01 |
| US20090042896A1 (en) | 2009-02-12 |
| ES2367464T3 (es) | 2011-11-03 |
| CN101778837A (zh) | 2010-07-14 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |