EA201290957A1 - Пиразол-4-илгетероциклилкарбоксамидные соединения и способы их применения - Google Patents
Пиразол-4-илгетероциклилкарбоксамидные соединения и способы их примененияInfo
- Publication number
- EA201290957A1 EA201290957A1 EA201290957A EA201290957A EA201290957A1 EA 201290957 A1 EA201290957 A1 EA 201290957A1 EA 201290957 A EA201290957 A EA 201290957A EA 201290957 A EA201290957 A EA 201290957A EA 201290957 A1 EA201290957 A1 EA 201290957A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- pyrazol
- methods
- ilheterocyclilkarboxamide
- application
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/08—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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
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- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Пиразол-4-илгетероциклилкарбоксамидные соединения формулы I, включая их стереоизомеры, геометрические изомеры, таутомеры и фармацевтически приемлемые соли, где Х представляет собой тиазолильное, пиколинильное, пиридинильное, пиримидинильное и фторпиридильное кольцо, полезны для ингибирования киназы Pim и для лечения расстройств, таких как рак, опосредованных киназой Pim. Раскрыты способы применения соединений формулы I для in vitro, in situ и in vivo диагностики, предупреждения или лечения таких расстройств в клетках млекопитающих или ассоциированных патологических состояний.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US32158810P | 2010-04-07 | 2010-04-07 | |
PCT/EP2011/055300 WO2011124580A1 (en) | 2010-04-07 | 2011-04-06 | Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
Publications (1)
Publication Number | Publication Date |
---|---|
EA201290957A1 true EA201290957A1 (ru) | 2013-04-30 |
Family
ID=44227838
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201290957A EA201290957A1 (ru) | 2010-04-07 | 2011-04-06 | Пиразол-4-илгетероциклилкарбоксамидные соединения и способы их применения |
Country Status (20)
Country | Link |
---|---|
US (3) | US8436001B2 (ru) |
EP (1) | EP2556066B1 (ru) |
JP (2) | JP6161537B2 (ru) |
KR (1) | KR101464060B1 (ru) |
CN (1) | CN102933572B (ru) |
AU (1) | AU2011237936A1 (ru) |
BR (1) | BR112012025480A2 (ru) |
CA (1) | CA2794801C (ru) |
CL (1) | CL2012002782A1 (ru) |
CO (1) | CO6630133A2 (ru) |
CR (1) | CR20120469A (ru) |
EA (1) | EA201290957A1 (ru) |
ES (1) | ES2601004T3 (ru) |
HK (1) | HK1178149A1 (ru) |
IL (1) | IL222227A0 (ru) |
MA (1) | MA34234B1 (ru) |
MX (1) | MX2012011533A (ru) |
PE (1) | PE20130405A1 (ru) |
SG (1) | SG184475A1 (ru) |
WO (1) | WO2011124580A1 (ru) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2638552C2 (ru) * | 2011-09-27 | 2017-12-14 | Ф. Хоффманн-Ля Рош Аг | Пиразол-4-ил-гетероциклил-карбоксамидные соединения и способы применения |
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BR112014028954A2 (pt) | 2012-05-21 | 2017-07-18 | Novartis Ag | amidas de n-piridinila substituídas no anel como inibidores da quinase |
WO2014033631A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | N-(3-pyridyl) biarylamides as kinase inhibitors |
WO2014033630A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | Novel aminothiazole carboxamides as kinase inhibitors |
CN104640858B (zh) * | 2012-09-26 | 2018-11-06 | 霍夫曼-拉罗奇有限公司 | 环醚吡唑-4-基-杂环基-甲酰胺化合物及使用方法 |
US20150336960A1 (en) | 2012-12-19 | 2015-11-26 | Novartis Ag | Aryl-substituted fused bicyclic pyridazine compounds |
WO2014110574A1 (en) | 2013-01-14 | 2014-07-17 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
EA035929B1 (ru) | 2013-01-15 | 2020-09-02 | Инсайт Холдингс Корпорейшн | ТИАЗОЛКАРБОКСАМИДЫ И ПИРИДИНКАРБОКСАМИДЫ, ИСПОЛЬЗУЕМЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ Pim-КИНАЗЫ |
SG11201601259YA (en) | 2013-08-23 | 2016-03-30 | Incyte Corp | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
NZ631142A (en) * | 2013-09-18 | 2016-03-31 | Axikin Pharmaceuticals Inc | Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors |
TW201605847A (zh) * | 2013-11-08 | 2016-02-16 | 武田藥品工業股份有限公司 | 雜環化合物 |
MX2016012007A (es) | 2014-03-18 | 2016-12-05 | Hoffmann La Roche | Compuestos de oxepan-2-il-pirazol-4-il-heterociclil-carboxamida y metodos de uso. |
US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
US10227343B2 (en) | 2015-01-30 | 2019-03-12 | Vanderbilt University | Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
KR20170138457A (ko) * | 2015-04-22 | 2017-12-15 | 리겔 파마슈티칼스, 인크. | 피라졸 화합물 및 이러한 화합물을 제조하고 사용하는 방법 |
US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
CN105254624B (zh) * | 2015-09-18 | 2019-08-09 | 上海吉铠医药科技有限公司 | 异噻唑衍生物pim激酶抑制剂及其制备方法与在制药中的应用 |
TW201718546A (zh) | 2015-10-02 | 2017-06-01 | 英塞特公司 | 適用作pim激酶抑制劑之雜環化合物 |
EP3532465B1 (en) * | 2016-10-26 | 2023-03-01 | Rigel Pharmaceuticals, Inc. | Pyrazole amide compounds as irak inhibitors |
CN112739345A (zh) | 2017-11-06 | 2021-04-30 | 斯奈普生物公司 | Pim激酶抑制剂组合物,方法和其用途 |
TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
PL3762368T3 (pl) | 2018-03-08 | 2022-06-06 | Incyte Corporation | ZWIĄZKI AMINOPIRAZYNODIOLOWE JAKO INHIBITORY PI3K-γ |
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CN110452180A (zh) * | 2019-06-25 | 2019-11-15 | 南京普锐达医药科技有限公司 | 一种合成2-氯-5-氨基-6-嘧啶甲酸乙酯的方法 |
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CN111087389B (zh) * | 2019-12-03 | 2020-10-27 | 佳木斯大学 | 一种用于治疗胶质母细胞瘤的药物 |
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2011
- 2011-04-06 ES ES11713749.7T patent/ES2601004T3/es active Active
- 2011-04-06 EP EP11713749.7A patent/EP2556066B1/en not_active Not-in-force
- 2011-04-06 MA MA35372A patent/MA34234B1/fr unknown
- 2011-04-06 BR BR112012025480-4A patent/BR112012025480A2/pt not_active IP Right Cessation
- 2011-04-06 EA EA201290957A patent/EA201290957A1/ru unknown
- 2011-04-06 PE PE2012001997A patent/PE20130405A1/es not_active Application Discontinuation
- 2011-04-06 CA CA2794801A patent/CA2794801C/en not_active Expired - Fee Related
- 2011-04-06 JP JP2013503090A patent/JP6161537B2/ja not_active Expired - Fee Related
- 2011-04-06 MX MX2012011533A patent/MX2012011533A/es active IP Right Grant
- 2011-04-06 AU AU2011237936A patent/AU2011237936A1/en not_active Abandoned
- 2011-04-06 CN CN201180028158.4A patent/CN102933572B/zh not_active Expired - Fee Related
- 2011-04-06 WO PCT/EP2011/055300 patent/WO2011124580A1/en active Application Filing
- 2011-04-06 SG SG2012074324A patent/SG184475A1/en unknown
- 2011-04-06 US US13/080,762 patent/US8436001B2/en not_active Expired - Fee Related
- 2011-04-06 KR KR1020127029089A patent/KR101464060B1/ko active IP Right Grant
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2012
- 2012-09-17 CR CR20120469A patent/CR20120469A/es unknown
- 2012-09-27 IL IL222227A patent/IL222227A0/en unknown
- 2012-10-04 CL CL2012002782A patent/CL2012002782A1/es unknown
- 2012-10-09 CO CO12177921A patent/CO6630133A2/es not_active Application Discontinuation
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2013
- 2013-03-15 US US13/834,316 patent/US8669361B2/en not_active Expired - Fee Related
- 2013-04-26 HK HK13105060.9A patent/HK1178149A1/xx not_active IP Right Cessation
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2014
- 2014-01-13 US US14/153,891 patent/US9573943B2/en not_active Expired - Fee Related
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2015
- 2015-09-28 JP JP2015189690A patent/JP2016040281A/ja active Pending
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2638552C2 (ru) * | 2011-09-27 | 2017-12-14 | Ф. Хоффманн-Ля Рош Аг | Пиразол-4-ил-гетероциклил-карбоксамидные соединения и способы применения |
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EP2556066B1 (en) | 2016-10-19 |
US9573943B2 (en) | 2017-02-21 |
SG184475A1 (en) | 2012-11-29 |
WO2011124580A1 (en) | 2011-10-13 |
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CO6630133A2 (es) | 2013-03-01 |
EP2556066A1 (en) | 2013-02-13 |
IL222227A0 (en) | 2012-12-31 |
CN102933572B (zh) | 2015-01-07 |
BR112012025480A2 (pt) | 2020-08-18 |
CA2794801C (en) | 2019-01-15 |
MA34234B1 (fr) | 2013-05-02 |
PE20130405A1 (es) | 2013-04-10 |
US8669361B2 (en) | 2014-03-11 |
AU2011237936A1 (en) | 2012-10-11 |
MX2012011533A (es) | 2012-12-17 |
JP2013523798A (ja) | 2013-06-17 |
JP6161537B2 (ja) | 2017-07-12 |
JP2016040281A (ja) | 2016-03-24 |
KR101464060B1 (ko) | 2014-11-20 |
US20130203732A1 (en) | 2013-08-08 |
CN102933572A (zh) | 2013-02-13 |
HK1178149A1 (en) | 2013-09-06 |
CL2012002782A1 (es) | 2013-01-18 |
KR20130001309A (ko) | 2013-01-03 |
US20110251176A1 (en) | 2011-10-13 |
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