ECSP13013072A - Derivados de pirazol - Google Patents
Derivados de pirazolInfo
- Publication number
- ECSP13013072A ECSP13013072A ECSP13013072A ECSP13013072A EC SP13013072 A ECSP13013072 A EC SP13013072A EC SP13013072 A ECSP13013072 A EC SP13013072A EC SP13013072 A ECSP13013072 A EC SP13013072A
- Authority
- EC
- Ecuador
- Prior art keywords
- halogen
- disorders
- lower alkyl
- optionally substituted
- substituted
- Prior art date
Links
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
-
- 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
-
- 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)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La invención se refiere a compuestos de la fórmula IA o IBen las que:R1 es hidrógeno o fenilo opcionalmente sustituido por haló-geno, 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 elegidos 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 IA 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 la depresión, los trastornos de ansiedad, el trastorno bipolar, el trastorno de hiperactividad con déficit de atención (ADHD), los trastornos relacionados con el estrés, los trastornos psicóticos como son la esquizofrenia, las enfermedades neurológicas, por ejemplo la enfermedad de Parkinson, los trastornos neurodegenerativos, por ejemplo la enfermedad de Alzheimer, la epilepsia, la migraña, la hipertensión, el abuso de sustancias y los trastornos metabólicos, por ejemplo los trastornos de ingestión de comida, la diabetes, las complicaciones diabéticas, la obesidad, la dislipidemia, los trastornos de consumo y asimilación de energía, los trastornos y malfunción de la temperatura corporal, la homeostasis, los trastornos del sueño y del ritmo circadiano y los trastornos cardiovasculares.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11169217 | 2011-06-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP13013072A true ECSP13013072A (es) | 2014-01-31 |
Family
ID=46298390
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP13013072 ECSP13013072A (es) | 2011-06-09 | 2013-12-09 | 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 |
| KR101631003B1 (ko) | 2012-01-12 | 2016-06-15 | 에프. 호프만-라 로슈 아게 | 미량 아민 결합 수용체(taar)로서 헤테로환형 유도체 |
| HUE037689T2 (hu) | 2012-09-14 | 2018-09-28 | Hoffmann La Roche | Pirazol-karboxamid származékok mint TAAR-modulátorok különféle rendellenességek, mint például depresszió, cukorbetegség és Parkinson-kór kezelésében történõ alkalmazásra |
| 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 |
| SG10201913878YA (en) * | 2016-03-17 | 2020-03-30 | Hoffmann La Roche | 5-ethyl-4-methyl-pyrazole-3-carboxamide derivative having activity as agonist of taar |
| IL270068B (en) | 2017-04-24 | 2022-06-01 | Tesaro Inc | Manufacturing methods of Niraprib |
| CN112480005B (zh) * | 2017-11-08 | 2022-08-19 | 北京嘉林药业股份有限公司 | 化合物及其治疗癌症的用途 |
| CA3104053A1 (en) * | 2018-06-18 | 2019-12-26 | Janssen Pharmaceutica Nv | Pyrazole derivatives as malt1 inhibitors |
| KR102161787B1 (ko) * | 2018-07-02 | 2020-10-06 | 한국기초과학지원연구원 | 수면 장애의 예방 또는 치료용 약학적 조성물 |
| CN112752755A (zh) | 2018-09-27 | 2021-05-04 | 豪夫迈·罗氏有限公司 | 用于治疗自身免疫性疾病的杂环基化合物 |
| KR102396602B1 (ko) * | 2019-02-28 | 2022-05-11 | 주식회사 마더스제약 | 피라졸 아마이드 유도체 화합물 및 이의 용도 |
| AU2020274645A1 (en) * | 2019-05-14 | 2021-12-16 | 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 |
| ES2216339T3 (es) | 1997-12-04 | 2004-10-16 | Allergan, Inc. | Derivados sustituidos de imidazol que tienen actividad de tipo agonista hacia los receptores adrenergicos alfa 2b o 2b/2c. |
| CN101616902B (zh) | 2007-02-15 | 2013-03-27 | 弗·哈夫曼-拉罗切有限公司 | 作为taar1配体的2-氨基*唑啉类化合物 |
| 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 WO PCT/EP2012/060627 patent/WO2012168260A1/en active Application Filing
- 2012-06-06 SG SG2013087234A patent/SG195156A1/en unknown
- 2012-06-06 BR BR112013031324-2A patent/BR112013031324B1/pt active IP Right Grant
- 2012-06-06 MX MX2013013853A patent/MX347239B/es active IP Right Grant
- 2012-06-06 JP JP2014514042A patent/JP5914642B2/ja active Active
- 2012-06-06 UA UAA201400123A patent/UA110525C2/ru unknown
- 2012-06-06 RS RS20150549A patent/RS54183B1/en unknown
- 2012-06-06 EP EP12727632.7A patent/EP2717873B1/en active Active
- 2012-06-06 TW TW101120350A patent/TWI440636B/zh active
- 2012-06-06 CA CA2837255A patent/CA2837255C/en active Active
- 2012-06-06 AU AU2012266457A patent/AU2012266457B2/en active Active
- 2012-06-06 MY MYPI2013004400A patent/MY162160A/en unknown
- 2012-06-06 KR KR1020147000462A patent/KR101574905B1/ko active IP Right Grant
- 2012-06-06 DK DK12727632.7T patent/DK2717873T3/en active
- 2012-06-06 ES ES12727632.7T patent/ES2546438T3/es active Active
- 2012-06-06 PE PE2013002748A patent/PE20140934A1/es active IP Right Grant
- 2012-06-06 SI SI201230279T patent/SI2717873T1/sl unknown
- 2012-06-06 CN CN201280027873.0A patent/CN103596567B/zh active Active
- 2012-06-06 PL PL12727632T patent/PL2717873T3/pl unknown
- 2012-06-06 EA EA201391787A patent/EA024648B1/ru not_active IP Right Cessation
- 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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