CO6630187A2 - 5.7-sustituido -imidazol[1.2-c]pirimidinas como inhibidores de cinasas jak - Google Patents
5.7-sustituido -imidazol[1.2-c]pirimidinas como inhibidores de cinasas jakInfo
- Publication number
- CO6630187A2 CO6630187A2 CO12203751A CO12203751A CO6630187A2 CO 6630187 A2 CO6630187 A2 CO 6630187A2 CO 12203751 A CO12203751 A CO 12203751A CO 12203751 A CO12203751 A CO 12203751A CO 6630187 A2 CO6630187 A2 CO 6630187A2
- Authority
- CO
- Colombia
- Prior art keywords
- pyrimidines
- imidazol
- substituted
- kinase inhibitors
- jak kinase
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Abstract
Los compuestos de la Fórmula I:y estereoisómeros y sales y solvatos de los mismos farmacéuticamente aceptables en los cuales R, R, R, R4, R, R, R, Xy Xtienen los significados dados en la especificación, son inhibidores de una o más cinasas JAK y son útiles en el tratamiento de enfermedades autoinmunitarias, enfermedades inflamatorias, rechazo de órganos, tejidos y células transplantados, así como también trastornos hematolágicos y malignidades y sus comorbilidades.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US32418610P | 2010-04-14 | 2010-04-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
CO6630187A2 true CO6630187A2 (es) | 2013-03-01 |
Family
ID=43984073
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CO12203751A CO6630187A2 (es) | 2010-04-14 | 2012-11-13 | 5.7-sustituido -imidazol[1.2-c]pirimidinas como inhibidores de cinasas jak |
Country Status (20)
Country | Link |
---|---|
US (1) | US8962596B2 (es) |
EP (1) | EP2558468B1 (es) |
JP (2) | JP2013523884A (es) |
KR (1) | KR20130094710A (es) |
CN (1) | CN102985424B (es) |
AR (1) | AR081075A1 (es) |
AU (1) | AU2011240808B2 (es) |
CA (1) | CA2796388A1 (es) |
CL (1) | CL2012002882A1 (es) |
CO (1) | CO6630187A2 (es) |
CR (1) | CR20120572A (es) |
MX (1) | MX2012011941A (es) |
NZ (1) | NZ603446A (es) |
RU (1) | RU2012148246A (es) |
SG (1) | SG184870A1 (es) |
TW (1) | TWI494314B (es) |
UA (1) | UA109131C2 (es) |
UY (1) | UY33328A (es) |
WO (1) | WO2011130146A1 (es) |
ZA (1) | ZA201208544B (es) |
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TWI468162B (zh) | 2005-12-13 | 2015-01-11 | 英塞特公司 | 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶 |
SG10201509887UA (en) | 2007-06-13 | 2016-01-28 | Incyte Corp | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
SG176111A1 (en) | 2009-05-22 | 2011-12-29 | Incyte Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
EA025520B1 (ru) | 2009-05-22 | 2017-01-30 | Инсайт Холдингс Корпорейшн | N-(ГЕТЕРО)АРИЛПИРРОЛИДИНОВЫЕ ПРОИЗВОДНЫЕ ПИРАЗОЛ-4-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ И ПИРРОЛ-3-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
PE20120508A1 (es) | 2009-06-17 | 2012-05-09 | Vertex Pharma | Inhibidores de la replicacion de los virus de la gripe |
WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
MX347851B (es) | 2010-03-10 | 2017-05-16 | Incyte Corp | Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1). |
EP2574168B9 (en) | 2010-05-21 | 2016-10-05 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
WO2012068450A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
CN103492381A (zh) | 2010-12-16 | 2014-01-01 | 沃泰克斯药物股份有限公司 | 流感病毒复制的抑制剂 |
CA2839767A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
WO2013055645A1 (en) * | 2011-10-12 | 2013-04-18 | Array Biopharma Inc. | 5,7-substituted-imidazo[1,2-c]pyrimidines |
CA2854879A1 (en) * | 2011-11-07 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Methods for treating inflammatory diseases and pharmaceutical combinations useful therefor |
US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
JP6196678B2 (ja) | 2012-10-24 | 2017-09-13 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | C型肝炎ウイルス阻害剤 |
BR112015010663B1 (pt) | 2012-11-15 | 2022-12-06 | Incyte Holdings Corporation | Formas de dosagem oral de liberação sustentada, e uso de ruxolitinib ou de sal farmaceuticamente aceitável do mesmo |
US20160123982A1 (en) | 2013-02-04 | 2016-05-05 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
CN105189509B (zh) * | 2013-03-06 | 2017-12-19 | 因赛特公司 | 用于制备jak抑制剂的方法及中间体 |
WO2014146249A1 (en) | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors |
US9637483B2 (en) | 2013-03-28 | 2017-05-02 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
WO2014172639A1 (en) * | 2013-04-19 | 2014-10-23 | Ruga Corporation | Raf kinase inhibitors |
TR201905814T4 (tr) * | 2013-05-17 | 2019-05-21 | Incyte Corp | Jak inhibitörü olarak bipirazol tuzu. |
RS60469B1 (sr) | 2013-08-07 | 2020-07-31 | Incyte Corp | Dozni oblici sa produženim oslobađanjem za jak1 inhibitor |
EP3068776B1 (en) | 2013-11-13 | 2019-05-29 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
SG10201804021TA (en) | 2013-11-13 | 2018-07-30 | Vertex Pharma | Methods of preparing inhibitors of influenza viruses replication |
WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
JP6618525B2 (ja) | 2014-08-15 | 2019-12-11 | ヤンセン ファーマシューティカルズ,インコーポレーテッド | ピラゾール類 |
PT3227297T (pt) | 2014-12-05 | 2021-04-09 | Array Biopharma Inc | Pirazol[1,5-a]pirazinas, substituídas nas posições 4 e 6, como inibidores de cinases janus |
CN105777754B (zh) * | 2014-12-16 | 2019-07-26 | 北京赛林泰医药技术有限公司 | 吡咯并嘧啶化合物 |
UA118149C2 (uk) | 2015-01-20 | 2018-11-26 | Вуксі Фортуне Фармасьютікал Ко., Лтд | Інгібітор jak |
EA036058B1 (ru) * | 2015-04-29 | 2020-09-21 | Уси Форчун Фармасьютикал Ко., Лтд | Ингибитор jak |
WO2016183116A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
JP6857617B2 (ja) | 2015-05-13 | 2021-04-14 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | インフルエンザウイルスの複製の阻害剤 |
PL3305788T3 (pl) | 2015-05-29 | 2021-03-08 | Wuxi Fortune Pharmaceutical Co., Ltd | Inhibitor kinazy janusowej |
AR104918A1 (es) * | 2015-06-19 | 2017-08-23 | Lilly Co Eli | Procesos e intermediarios para la preparación de {1-(etilsulfonil)-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrilo |
CN105294699B (zh) * | 2015-12-04 | 2019-06-11 | 上海勋和医药科技有限公司 | 巴瑞替尼的制备方法 |
WO2017129116A1 (zh) | 2016-01-26 | 2017-08-03 | 杭州华东医药集团新药研究院有限公司 | 吡咯嘧啶五元氮杂环衍生物及其应用 |
NZ744349A (en) | 2016-02-24 | 2023-06-30 | Pfizer | Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors |
WO2018133875A1 (zh) | 2017-01-23 | 2018-07-26 | 上海长森药业有限公司 | Jak酶抑制剂及其制备方法和用途 |
WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
WO2018189335A1 (en) | 2017-04-13 | 2018-10-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
BR112020002674A2 (pt) | 2017-08-07 | 2020-07-28 | Joint Stock Company Biocad | compostos heterocíclicos inovadores como inibidores de cdk8/19 |
WO2019034973A1 (en) * | 2017-08-14 | 2019-02-21 | Pfizer Inc. | PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES |
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CA3091339A1 (en) | 2018-02-16 | 2019-08-22 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of cytokine-related disorders |
MX2022012285A (es) | 2018-03-30 | 2023-08-15 | Incyte Corp | Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak). |
WO2020063751A1 (en) * | 2018-09-27 | 2020-04-02 | Fochon Pharmaceuticals, Ltd. | Substituted imidazo [1, 2-a] pyridine and [1, 2, 4] triazolo [1, 5-a] pyridine compounds as ret kinase inhibitors |
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WO2020092528A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
CN111320624B (zh) * | 2018-12-14 | 2023-05-12 | 中国医药研究开发中心有限公司 | ***并吡啶类和咪唑并吡啶类化合物及其制备方法和医药用途 |
WO2020207476A1 (zh) * | 2019-04-12 | 2020-10-15 | 北京普祺医药科技有限公司 | 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途 |
EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
CN111039963B (zh) * | 2019-12-31 | 2021-03-19 | 卓和药业集团有限公司 | Wxfl10203614水溶性类似物及其合成方法 |
BR112022024632A2 (pt) | 2020-06-02 | 2023-02-28 | Incyte Corp | Processos para preparar um inibidor de jak1 |
US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
EP3944859A1 (en) | 2020-07-30 | 2022-02-02 | Assistance Publique Hôpitaux de Paris | Method for treating immune toxicities induced by immune checkpoint inhibitors |
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WO2023083200A1 (zh) * | 2021-11-12 | 2023-05-19 | 南京明德新药研发有限公司 | 吡唑并环化合物及其应用 |
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US5728536A (en) | 1993-07-29 | 1998-03-17 | St. Jude Children's Research Hospital | Jak kinases and regulation of Cytokine signal transduction |
CA2342503A1 (en) | 1998-08-21 | 2000-03-02 | Parker Hughes Institute | Quinazoline derivatives |
JP2001302667A (ja) * | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
WO2006044687A2 (en) * | 2004-10-15 | 2006-04-27 | Takeda San Diego, Inc. | Kinase inhibitors |
TWI468162B (zh) | 2005-12-13 | 2015-01-11 | 英塞特公司 | 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶 |
ES2689444T3 (es) * | 2006-11-22 | 2018-11-14 | Incyte Holdings Corporation | Imidazotriazinas e imidazopirimidinas como inhibidores de la quinasa |
DE102007012645A1 (de) * | 2007-03-16 | 2008-09-18 | Bayer Healthcare Ag | Substituierte Imidazo- und Triazolopyrimidine |
CL2008001709A1 (es) * | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
ES2602577T3 (es) | 2008-03-11 | 2017-02-21 | Incyte Holdings Corporation | Derivados de azetidina y ciclobutano como inhibidores de JAK |
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-
2011
- 2011-04-11 NZ NZ603446A patent/NZ603446A/en not_active IP Right Cessation
- 2011-04-11 MX MX2012011941A patent/MX2012011941A/es active IP Right Grant
- 2011-04-11 JP JP2013504972A patent/JP2013523884A/ja not_active Ceased
- 2011-04-11 EP EP11715818.8A patent/EP2558468B1/en active Active
- 2011-04-11 KR KR1020127029826A patent/KR20130094710A/ko not_active Application Discontinuation
- 2011-04-11 US US13/640,099 patent/US8962596B2/en not_active Expired - Fee Related
- 2011-04-11 UA UAA201212901A patent/UA109131C2/ru unknown
- 2011-04-11 WO PCT/US2011/031896 patent/WO2011130146A1/en active Application Filing
- 2011-04-11 RU RU2012148246/04A patent/RU2012148246A/ru not_active Application Discontinuation
- 2011-04-11 SG SG2012076493A patent/SG184870A1/en unknown
- 2011-04-11 CA CA2796388A patent/CA2796388A1/en not_active Abandoned
- 2011-04-11 AU AU2011240808A patent/AU2011240808B2/en not_active Ceased
- 2011-04-11 CN CN201180029128.5A patent/CN102985424B/zh not_active Expired - Fee Related
- 2011-04-13 AR ARP110101268A patent/AR081075A1/es not_active Application Discontinuation
- 2011-04-13 UY UY0001033328A patent/UY33328A/es not_active Application Discontinuation
- 2011-04-14 TW TW100113047A patent/TWI494314B/zh not_active IP Right Cessation
-
2012
- 2012-10-12 CL CL2012002882A patent/CL2012002882A1/es unknown
- 2012-11-09 CR CR20120572A patent/CR20120572A/es unknown
- 2012-11-13 ZA ZA2012/08544A patent/ZA201208544B/en unknown
- 2012-11-13 CO CO12203751A patent/CO6630187A2/es active IP Right Grant
-
2015
- 2015-06-26 JP JP2015128369A patent/JP2015205905A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
US20130131039A1 (en) | 2013-05-23 |
UA109131C2 (ru) | 2015-07-27 |
JP2015205905A (ja) | 2015-11-19 |
CL2012002882A1 (es) | 2013-02-08 |
SG184870A1 (en) | 2012-11-29 |
AU2011240808B2 (en) | 2015-01-22 |
TW201134827A (en) | 2011-10-16 |
US8962596B2 (en) | 2015-02-24 |
CN102985424A (zh) | 2013-03-20 |
EP2558468B1 (en) | 2015-04-01 |
MX2012011941A (es) | 2013-08-27 |
EP2558468A1 (en) | 2013-02-20 |
JP2013523884A (ja) | 2013-06-17 |
ZA201208544B (en) | 2015-04-29 |
UY33328A (es) | 2012-10-31 |
TWI494314B (zh) | 2015-08-01 |
AR081075A1 (es) | 2012-06-06 |
KR20130094710A (ko) | 2013-08-26 |
RU2012148246A (ru) | 2014-05-20 |
NZ603446A (en) | 2014-05-30 |
CN102985424B (zh) | 2015-03-11 |
CA2796388A1 (en) | 2011-10-20 |
WO2011130146A1 (en) | 2011-10-20 |
CR20120572A (es) | 2013-02-20 |
AU2011240808A1 (en) | 2012-11-29 |
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