EA201391787A1 - Производные пиразола - Google Patents
Производные пиразолаInfo
- Publication number
- EA201391787A1 EA201391787A1 EA201391787A EA201391787A EA201391787A1 EA 201391787 A1 EA201391787 A1 EA 201391787A1 EA 201391787 A EA201391787 A EA 201391787A EA 201391787 A EA201391787 A EA 201391787A EA 201391787 A1 EA201391787 A1 EA 201391787A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- halogen
- lower alkyl
- substituted
- hydrogen
- disorders
- 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
-
- 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
-
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Addiction (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Настоящее изобретение относится к соединениям формулыгде Rпредставляет собой водород или фенил, возможно, содержащий в качестве заместителя галоген, CN или низшую алкоксигруппу или же низшую алкоксигруппу, замещенную галогеном; Rпредставляет собой водород или низший алкил; Rпредставляет собой водород или низший алкил или представляет собой фенил, возможно, содержащий один или более заместителей, выбранных из следующих: галоген, цианогруппа или низшая алкоксигруппа, замещенная галогеном, или представляет собой пиридинил, возможно, содержащий в качестве заместителя галоген или низший алкил, замещенный галогеном, или представляет собой пиримидинил, возможно, содержащий в качестве заместителя низший алкил, замещенный галогеном, или представляет собой пиразинил, возможно, содержащий в качестве заместителя галоген, цианогруппу или низший алкил, замещенный галогеном; Rпредставляет собой водород, низший алкил или фенил; Z представляет собой связь, -СН- или -О-; или к их фармацевтически приемлемым кислотно-аддитивным солям. Было показано, что соединения формулы IA и IB обладают высоким сродством по отношению к рецепторам следовых аминов (TAARs), в частности TAAR1. Эти соединения можно применять для лечения депрессии, тревожного невроза, биполярного расстройства, синдрома дефицита внимания и гиперактивности (СДВГ), расстройств, связанных со стрессом, психических расстройств, таких как шизофрения, неврологических заболеваний, таких как болезнь Паркинсона, нейродегенеративных расстройств, таких как болезнь Альцгеймера, эпилепсии, мигрени, гипертонии, наркотической зависимости и токсикомании и метаболических расстройств, таких как расстройства приема
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 |
|---|---|
| EA201391787A1 true EA201391787A1 (ru) | 2014-04-30 |
| EA024648B1 EA024648B1 (ru) | 2016-10-31 |
Family
ID=46298390
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201391787A EA024648B1 (ru) | 2011-06-09 | 2012-06-06 | Производные пиразола |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US9073911B2 (ru) |
| EP (1) | EP2717873B1 (ru) |
| JP (1) | JP5914642B2 (ru) |
| KR (1) | KR101574905B1 (ru) |
| CN (1) | CN103596567B (ru) |
| AR (1) | AR088741A1 (ru) |
| AU (1) | AU2012266457B2 (ru) |
| BR (1) | BR112013031324B1 (ru) |
| CA (1) | CA2837255C (ru) |
| CL (1) | CL2013003484A1 (ru) |
| CO (1) | CO6801764A2 (ru) |
| CY (1) | CY1116778T1 (ru) |
| DK (1) | DK2717873T3 (ru) |
| EA (1) | EA024648B1 (ru) |
| EC (1) | ECSP13013072A (ru) |
| ES (1) | ES2546438T3 (ru) |
| HK (1) | HK1191862A1 (ru) |
| HR (1) | HRP20151077T1 (ru) |
| IL (1) | IL229549B (ru) |
| MA (1) | MA35192B1 (ru) |
| MX (1) | MX347239B (ru) |
| MY (1) | MY162160A (ru) |
| PE (1) | PE20140934A1 (ru) |
| PL (1) | PL2717873T3 (ru) |
| PT (1) | PT2717873E (ru) |
| RS (1) | RS54183B1 (ru) |
| SG (1) | SG195156A1 (ru) |
| SI (1) | SI2717873T1 (ru) |
| TW (1) | TWI440636B (ru) |
| UA (1) | UA110525C2 (ru) |
| WO (1) | WO2012168260A1 (ru) |
| ZA (1) | ZA201308939B (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029370B2 (en) | 2011-06-10 | 2015-05-12 | Hoffmann-La Roche Inc. | Substituted benzamide derivatives |
| RU2621050C2 (ru) * | 2012-01-12 | 2017-05-31 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические производные в качестве рецепторов, ассоциированных со следовыми аминами (taars) |
| CN107903251A (zh) | 2012-09-14 | 2018-04-13 | 霍夫曼-拉罗奇有限公司 | 作为用于治疗数种疾病如抑郁症、糖尿病和帕金森病的taar调节剂的吡唑甲酰胺衍生物 |
| 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 |
| JP7179014B2 (ja) | 2017-04-24 | 2022-11-28 | テサロ， インコーポレイテッド | ニラパリブの製造方法 |
| 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 |
| EA202190055A1 (ru) * | 2018-06-18 | 2021-04-23 | Янссен Фармацевтика Нв | Производные пиразола в качестве ингибиторов malt1 |
| KR102161787B1 (ko) * | 2018-07-02 | 2020-10-06 | 한국기초과학지원연구원 | 수면 장애의 예방 또는 치료용 약학적 조성물 |
| WO2020064792A1 (en) | 2018-09-27 | 2020-04-02 | F. Hoffmann-La Roche Ag | Heterocyclyl compounds for the treatment of autoimmune disease |
| KR102396602B1 (ko) * | 2019-02-28 | 2022-05-11 | 주식회사 마더스제약 | 피라졸 아마이드 유도체 화합물 및 이의 용도 |
| EP3983386A4 (en) * | 2019-05-14 | 2023-01-11 | Metabomed Ltd | ACSS2 INHIBITORS AND METHODS OF USE |
| 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 |
| JP4783502B2 (ja) | 1997-12-04 | 2011-09-28 | アラーガン、インコーポレイテッド | α２Ｂまたは２Ｂ／２Ｃアドレナリン受容体において作動剤様活性を示す置換イミダゾール誘導体 |
| US6841684B2 (en) | 1997-12-04 | 2005-01-11 | Allergan, Inc. | Imidiazoles having reduced side effects |
| ES2525229T3 (es) | 2007-02-15 | 2014-12-19 | F. Hoffmann-La Roche Ag | 2-aminooxazolinas como ligandos de TAAR1 |
| 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 UA UAA201400123A patent/UA110525C2/ru unknown
- 2012-06-06 SI SI201230279T patent/SI2717873T1/sl unknown
- 2012-06-06 EP EP12727632.7A patent/EP2717873B1/en active Active
- 2012-06-06 TW TW101120350A patent/TWI440636B/zh active
- 2012-06-06 BR BR112013031324-2A patent/BR112013031324B1/pt active IP Right Grant
- 2012-06-06 PT PT127276327T patent/PT2717873E/pt unknown
- 2012-06-06 CN CN201280027873.0A patent/CN103596567B/zh active Active
- 2012-06-06 SG SG2013087234A patent/SG195156A1/en unknown
- 2012-06-06 EA EA201391787A patent/EA024648B1/ru not_active IP Right Cessation
- 2012-06-06 JP JP2014514042A patent/JP5914642B2/ja active Active
- 2012-06-06 PL PL12727632T patent/PL2717873T3/pl unknown
- 2012-06-06 PE PE2013002748A patent/PE20140934A1/es active IP Right Grant
- 2012-06-06 RS RS20150549A patent/RS54183B1/en unknown
- 2012-06-06 AU AU2012266457A patent/AU2012266457B2/en active Active
- 2012-06-06 MX MX2013013853A patent/MX347239B/es active IP Right Grant
- 2012-06-06 CA CA2837255A patent/CA2837255C/en active Active
- 2012-06-06 ES ES12727632.7T patent/ES2546438T3/es active Active
- 2012-06-06 KR KR1020147000462A patent/KR101574905B1/ko active IP Right Grant
- 2012-06-06 MY MYPI2013004400A patent/MY162160A/en unknown
- 2012-06-06 DK DK12727632.7T patent/DK2717873T3/en active
- 2012-06-06 WO PCT/EP2012/060627 patent/WO2012168260A1/en active Application Filing
- 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
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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
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |