MX347239B - Derivados de pirazol. - Google Patents
Derivados de pirazol.Info
- Publication number
- MX347239B MX347239B MX2013013853A MX2013013853A MX347239B MX 347239 B MX347239 B MX 347239B MX 2013013853 A MX2013013853 A MX 2013013853A MX 2013013853 A MX2013013853 A MX 2013013853A MX 347239 B MX347239 B MX 347239B
- Authority
- MX
- Mexico
- Prior art keywords
- halogen
- disorders
- sup
- lower alkyl
- substituted
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
-
- 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
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- 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
- A61P3/06—Antihyperlipidemics
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la fórmula (Ver Formula) en donde: R1 es hidrógeno o fenilo opcionalmente sustituido por halógeno, CN o alcoxi inferior o alcoxi inferior sustituido por halógeno R2 es hidrógeno o alquilo inferior; R3 es hidrógeno o alquilo inferior o es fenilo opcionalmente sustituido por uno o más sustituyentes seleccionados entre halógeno, ciano o alcoxi inferior sustituido por halógeno, o es piridinilo opcionalmente sustituido por halógeno o alquilo inferior sustituido por halógeno, o es pirimidinilo, opcionalmente sustituido por alquilo inferior sustituido por halógeno, o es pirazinilo, opcionalmente sustituido por halógeno, ciano o alquilo inferior sustituido por halógeno, R4 es hidrógeno, alquilo inferior o fenilo; Z es un enlace, -CH2- u -O-; o a una sal de adición de ácido farmacéuticamente aceptable de los mismos. Ahora se ha encontrado que los compuestos de las fórmulas lA e IB tienen buena afinidad con los receptores asociados con las aminas traza (TAARs), en especial con el TAAR1. Estos compuestos pueden utilizarse para el tratamiento de depresión, trastornos de ansiedad, trastorno bipolar, trastorno de hiperactividad con déficit de atención (por sus siglas en inglés, ADHD), trastornos relacionados con el estrés, trastornos psicóticos como son esquizofrenia, enfermedades neurológicas, por ejemplo enfermedad de Parkinson, trastornos neurodegenerativos, por ejemplo enfermedad de Alzheimer, epilepsia, migraña, hipertensión, abuso de sustancias y trastornos metabólicos, por ejemplo trastornos de ingestión de comida, diabetes, complicaciones diabéticas, obesidad, dislipidemia, trastornos de consumo y asimilación de energía, trastornos y malfunción de la temperatura corporal, homeostasis, trastornos del sueño y ritmo circadiano y trastornos cardiovasculares.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11169217 | 2011-06-09 | ||
| PCT/EP2012/060627 WO2012168260A1 (en) | 2011-06-09 | 2012-06-06 | Pyrazole derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2013013853A MX2013013853A (es) | 2014-01-20 |
| MX347239B true MX347239B (es) | 2017-04-20 |
Family
ID=46298390
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013013853A MX347239B (es) | 2011-06-09 | 2012-06-06 | Derivados de pirazol. |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US9073911B2 (es) |
| EP (1) | EP2717873B1 (es) |
| JP (1) | JP5914642B2 (es) |
| KR (1) | KR101574905B1 (es) |
| CN (1) | CN103596567B (es) |
| AR (1) | AR088741A1 (es) |
| AU (1) | AU2012266457B2 (es) |
| BR (1) | BR112013031324B1 (es) |
| CA (1) | CA2837255C (es) |
| CL (1) | CL2013003484A1 (es) |
| CO (1) | CO6801764A2 (es) |
| CY (1) | CY1116778T1 (es) |
| DK (1) | DK2717873T3 (es) |
| EA (1) | EA024648B1 (es) |
| EC (1) | ECSP13013072A (es) |
| ES (1) | ES2546438T3 (es) |
| HK (1) | HK1191862A1 (es) |
| HR (1) | HRP20151077T1 (es) |
| IL (1) | IL229549B (es) |
| MA (1) | MA35192B1 (es) |
| MX (1) | MX347239B (es) |
| MY (1) | MY162160A (es) |
| PE (1) | PE20140934A1 (es) |
| PL (1) | PL2717873T3 (es) |
| PT (1) | PT2717873E (es) |
| RS (1) | RS54183B1 (es) |
| SG (1) | SG195156A1 (es) |
| SI (1) | SI2717873T1 (es) |
| TW (1) | TWI440636B (es) |
| UA (1) | UA110525C2 (es) |
| WO (1) | WO2012168260A1 (es) |
| ZA (1) | ZA201308939B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029370B2 (en) | 2011-06-10 | 2015-05-12 | Hoffmann-La Roche Inc. | Substituted benzamide derivatives |
| ES2554843T3 (es) * | 2012-01-12 | 2015-12-23 | F. Hoffmann-La Roche Ag | Derivados heterocíclicos como receptores asociados de trazas de amina (TAARs) |
| MX363362B (es) * | 2012-09-14 | 2019-03-21 | Hoffmann La Roche | Derivados de pirazol carboxamida como moduladores de los receptores asociados con las aminas traza (taar) para uso en el tratamiento de varios trastornos, tales como depresión, diabetes y enfermedades de parkinson. |
| US9580407B2 (en) * | 2012-12-07 | 2017-02-28 | Merck Sharp & Dohme Corp. | Regioselective N-2 arylation of indazoles |
| WO2015165085A1 (en) | 2014-04-30 | 2015-11-05 | F.Hoffmann-La Roche Ag | Morpholin-pyridine derivatives |
| RU2731095C2 (ru) * | 2016-03-17 | 2020-08-28 | Ф. Хоффманн-Ля Рош Аг | Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar |
| ES2926255T3 (es) | 2017-04-24 | 2022-10-24 | Tesaro Inc | Métodos de fabricación de niraparib |
| CN112480079B (zh) * | 2017-11-08 | 2022-03-11 | 北京嘉林药业股份有限公司 | 化合物及其治疗癌症的用途 |
| KR20210024548A (ko) * | 2018-06-18 | 2021-03-05 | 얀센 파마슈티카 엔.브이. | Malt1 억제제로서의 피라졸 유도체 |
| KR102161787B1 (ko) * | 2018-07-02 | 2020-10-06 | 한국기초과학지원연구원 | 수면 장애의 예방 또는 치료용 약학적 조성물 |
| EP3856737B1 (en) | 2018-09-27 | 2023-05-17 | F. Hoffmann-La Roche AG | Heterocyclyl compounds for the treatment of autoimmune disease |
| WO2020175957A1 (ko) * | 2019-02-28 | 2020-09-03 | 주식회사 마더스제약 | 피라졸 아마이드 유도체 화합물 및 이의 용도 |
| CA3136083A1 (en) * | 2019-05-14 | 2020-11-19 | Metabomed Ltd | Acss2 inhibitors and methods of use thereof |
| WO2023283369A1 (en) * | 2021-07-08 | 2023-01-12 | Vibliome Therapeutics, Llc | Modulators of protein kinases |
| WO2023183444A1 (en) * | 2022-03-24 | 2023-09-28 | Vibliome Therapeutics, Llc | Modulators of protein kinases |
| WO2024033459A1 (en) * | 2022-08-12 | 2024-02-15 | F. Hoffmann-La Roche Ag | Pharmaceutical compositions comprising 5-ethyl-4-methyl- n-[4-[(2 s) morpholin-2-yl]phenyl]-1h-pyrazole-3-carboxamide |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9425211D0 (en) | 1994-12-14 | 1995-02-15 | Ucb Sa | Substituted 1H-imidazoles |
| GB9520150D0 (en) * | 1995-10-03 | 1995-12-06 | Orion Yhtymae Oy | New imidazole derivatives |
| US6841684B2 (en) * | 1997-12-04 | 2005-01-11 | Allergan, Inc. | Imidiazoles having reduced side effects |
| ATE266643T1 (de) | 1997-12-04 | 2004-05-15 | Allergan Inc | Substituierte imidazole derivate mit agonistischähnlicher wirkung auf die alpha 2b oder 2b/2c adrenergischen rezeptoren |
| KR101222412B1 (ko) | 2007-02-15 | 2013-01-15 | 에프. 호프만-라 로슈 아게 | Ｔａａｒ1 리간드로서의 2-아미노옥사졸린 |
| US8354441B2 (en) | 2009-11-11 | 2013-01-15 | Hoffmann-La Roche Inc. | Oxazoline derivatives |
| US9452980B2 (en) * | 2009-12-22 | 2016-09-27 | Hoffmann-La Roche Inc. | Substituted benzamides |
| US9132136B2 (en) * | 2010-08-02 | 2015-09-15 | Hoffmann-La Roche Inc. | Pharmaceutical combination |
| US9029370B2 (en) | 2011-06-10 | 2015-05-12 | Hoffmann-La Roche Inc. | Substituted benzamide derivatives |
| CN102899314A (zh) | 2011-07-29 | 2013-01-30 | 江汉大学 | 一种批量基因克隆的方法 |
-
2012
- 2012-06-01 US US13/485,969 patent/US9073911B2/en active Active
- 2012-06-06 MX MX2013013853A patent/MX347239B/es active IP Right Grant
- 2012-06-06 CN CN201280027873.0A patent/CN103596567B/zh active Active
- 2012-06-06 TW TW101120350A patent/TWI440636B/zh active
- 2012-06-06 DK DK12727632.7T patent/DK2717873T3/en active
- 2012-06-06 SG SG2013087234A patent/SG195156A1/en unknown
- 2012-06-06 PE PE2013002748A patent/PE20140934A1/es active IP Right Grant
- 2012-06-06 JP JP2014514042A patent/JP5914642B2/ja active Active
- 2012-06-06 BR BR112013031324-2A patent/BR112013031324B1/pt active IP Right Grant
- 2012-06-06 EP EP12727632.7A patent/EP2717873B1/en active Active
- 2012-06-06 ES ES12727632.7T patent/ES2546438T3/es active Active
- 2012-06-06 CA CA2837255A patent/CA2837255C/en active Active
- 2012-06-06 SI SI201230279T patent/SI2717873T1/sl unknown
- 2012-06-06 MY MYPI2013004400A patent/MY162160A/en unknown
- 2012-06-06 PL PL12727632T patent/PL2717873T3/pl unknown
- 2012-06-06 RS RS20150549A patent/RS54183B1/en unknown
- 2012-06-06 UA UAA201400123A patent/UA110525C2/ru unknown
- 2012-06-06 EA EA201391787A patent/EA024648B1/ru not_active IP Right Cessation
- 2012-06-06 AU AU2012266457A patent/AU2012266457B2/en active Active
- 2012-06-06 KR KR1020147000462A patent/KR101574905B1/ko active IP Right Grant
- 2012-06-06 WO PCT/EP2012/060627 patent/WO2012168260A1/en active Application Filing
- 2012-06-06 PT PT127276327T patent/PT2717873E/pt unknown
- 2012-06-07 AR ARP120102009A patent/AR088741A1/es unknown
-
2013
- 2013-10-31 CO CO13258855A patent/CO6801764A2/es active IP Right Grant
- 2013-11-21 IL IL229549A patent/IL229549B/en active IP Right Grant
- 2013-11-27 ZA ZA2013/08939A patent/ZA201308939B/en unknown
- 2013-12-05 CL CL2013003484A patent/CL2013003484A1/es unknown
- 2013-12-09 EC ECSP13013072 patent/ECSP13013072A/es unknown
- 2013-12-18 MA MA36583A patent/MA35192B1/fr unknown
-
2014
- 2014-05-30 HK HK14105124.2A patent/HK1191862A1/zh unknown
-
2015
- 2015-10-06 CY CY20151100893T patent/CY1116778T1/el unknown
- 2015-10-12 HR HRP20151077TT patent/HRP20151077T1/hr unknown
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| FG | Grant or registration |