MX2012004020A - Analogos de heterociclilo pirazolopirimidina como inhibidores de jak. - Google Patents
Analogos de heterociclilo pirazolopirimidina como inhibidores de jak.Info
- Publication number
- MX2012004020A MX2012004020A MX2012004020A MX2012004020A MX2012004020A MX 2012004020 A MX2012004020 A MX 2012004020A MX 2012004020 A MX2012004020 A MX 2012004020A MX 2012004020 A MX2012004020 A MX 2012004020A MX 2012004020 A MX2012004020 A MX 2012004020A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- compounds
- jak inhibitors
- heterocyclyl
- analogues
- Prior art date
Links
- 229940122245 Janus kinase inhibitor Drugs 0.000 title abstract 2
- -1 Heterocyclyl pyrazolopyrimidine analogues Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000000172 allergic effect Effects 0.000 abstract 1
- 208000010668 atopic eczema Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000001900 immune effect Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
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- 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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Diabetes (AREA)
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- Endocrinology (AREA)
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- Pulmonology (AREA)
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- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Nutrition Science (AREA)
Abstract
La presente invención se refiere a compuestos de fórmula (I) (ver fórmula (I)) donde X1 a X5, Y, Z1 a Z3, y R tienen el significado indicado en la descripción y las reivindicaciones. Dichos compuestos son útiles como inhibidores de JAK para el tratamiento o la profilaxis de trastornos inmunológicos, inflamatorios, autoinmunes, alérgicos, y enfermedades mediadas por el sistema inmunológico. La invención también se refiere a composiciones farmacéuticas que incluyen dichos compuestos, la preparación de dichos compuestos al igual que su uso como medicamentos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09173535 | 2009-10-20 | ||
| US37535810P | 2010-08-20 | 2010-08-20 | |
| PCT/EP2010/065700 WO2011048082A1 (en) | 2009-10-20 | 2010-10-19 | Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012004020A true MX2012004020A (es) | 2012-05-08 |
Family
ID=41531257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012004020A MX2012004020A (es) | 2009-10-20 | 2010-10-19 | Analogos de heterociclilo pirazolopirimidina como inhibidores de jak. |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9242987B2 (es) |
| EP (1) | EP2491039A1 (es) |
| JP (1) | JP5744887B2 (es) |
| KR (1) | KR20120102601A (es) |
| CN (1) | CN102666545B (es) |
| AR (1) | AR078675A1 (es) |
| AU (1) | AU2010309882B2 (es) |
| BR (1) | BR112012009327A2 (es) |
| CA (1) | CA2775009A1 (es) |
| EA (1) | EA022120B1 (es) |
| IL (1) | IL218751A0 (es) |
| MX (1) | MX2012004020A (es) |
| NZ (1) | NZ598907A (es) |
| TW (1) | TW201125867A (es) |
| WO (1) | WO2011048082A1 (es) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI3184526T1 (sl) | 2005-12-13 | 2019-03-29 | Incyte Holdings Corporation | Derivati pirolo(2,3-D)pirimidina kot inhibitorji Janus kinaze |
| MX2009013402A (es) | 2007-06-13 | 2010-02-24 | Incyte Corp | Sales de inhibidor de janus cinasa (r)-3-(4-(7h-pirrolo[2,3-d]piri midin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo. |
| PE20110828A1 (es) | 2008-10-31 | 2011-11-22 | Genentech Inc | Compuestos de pirazolopirimidina como inhibidores de jak |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| PT2448938E (pt) | 2009-06-29 | 2014-07-31 | Incyte Corp | Pirimidinonas como inibidoras de pi3k |
| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| WO2011075643A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted heteroaryl fused derivatives as pi3k inhibitors |
| PE20130038A1 (es) | 2010-03-10 | 2013-01-28 | Incyte Corp | Derivados de piperidin-4-il azetidina como inhibidores de jak1 |
| WO2011130342A1 (en) | 2010-04-14 | 2011-10-20 | Incyte Corporation | FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS |
| SG10201503983QA (en) | 2010-05-21 | 2015-06-29 | Incyte Corp | Topical Formulation for a JAK Inhibitor |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| JP2013534233A (ja) * | 2010-08-20 | 2013-09-02 | セルゾーム リミティッド | 選択的jak阻害剤としてのヘテロシクリルピラゾロピリミジン類似体 |
| BR112013006016A2 (pt) | 2010-09-15 | 2016-06-07 | Hoffmann La Roche | compostos de azabenzotiazol, composições e métodos de uso |
| BR112013012502A2 (pt) | 2010-11-19 | 2019-03-06 | Incyte Corporation | pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak |
| BR112013011520A2 (pt) | 2010-11-19 | 2019-09-24 | Hoffmann La Roche | pirazolo piridinas e pirazolo piridinas e seu uso como inibidores de tyk2 |
| JP5961187B2 (ja) | 2010-12-20 | 2016-08-02 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| WO2012143320A1 (en) | 2011-04-18 | 2012-10-26 | Cellzome Limited | (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors |
| EP2721028B1 (en) | 2011-06-20 | 2015-11-04 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| KR20140047092A (ko) * | 2011-07-28 | 2014-04-21 | 셀좀 리미티드 | Jak 억제제로서의 헤테로시클릴 피리미딘 유사체 |
| WO2013017479A1 (en) | 2011-07-29 | 2013-02-07 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors |
| WO2013017480A1 (en) | 2011-07-29 | 2013-02-07 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors |
| EP3196202B1 (en) | 2011-09-02 | 2019-02-27 | Incyte Holdings Corporation | Heterocyclylamines as pi3k inhibitors |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| EP2760863A1 (en) * | 2011-09-20 | 2014-08-06 | Cellzome Limited | Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors |
| CN104169272A (zh) | 2011-12-23 | 2014-11-26 | 赛尔佐姆有限公司 | 作为激酶抑制剂的嘧啶-2,4-二胺衍生物 |
| CN103193600B (zh) * | 2012-01-07 | 2016-04-06 | 浙江九洲药物科技有限公司 | 卡巴拉汀中间体的制备方法 |
| EP2807161B1 (en) * | 2012-01-28 | 2017-10-04 | Merck Patent GmbH | Triazolo[4,5-d]pyrimidine derivatives |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| US9296725B2 (en) | 2012-05-24 | 2016-03-29 | Cellzome Limited | Heterocyclyl pyrimidine analogues as TYK2 inhibitors |
| PL2919766T3 (pl) | 2012-11-15 | 2021-10-04 | Incyte Holdings Corporation | Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu |
| MX361136B (es) | 2013-01-23 | 2018-11-28 | Astrazeneca Ab | Compuestos quimicos. |
| EP3489239B1 (en) | 2013-03-06 | 2021-09-15 | Incyte Holdings Corporation | Processes and intermediates for making a jak inhibitor |
| LT3030227T (lt) | 2013-08-07 | 2020-06-10 | Incyte Corporation | Prailginto atpalaidavimo jak1 inhibitoriaus dozavimo formos |
| WO2015038417A1 (en) * | 2013-09-10 | 2015-03-19 | Asana Biosciences, Llc | Compounds for regulating fak and/or src pathways |
| CA2925953C (en) | 2013-10-17 | 2021-11-02 | Dow Agrosciences Llc | Processes for the preparation of pesticidal compounds |
| AU2015261812B2 (en) | 2014-05-23 | 2019-11-21 | F. Hoffmann-La Roche Ag | 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds which are JAK inhibitors |
| US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
| TW201613916A (en) | 2014-06-03 | 2016-04-16 | Gilead Sciences Inc | TANK-binding kinase inhibitor compounds |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| MX2017003930A (es) | 2014-09-26 | 2017-06-30 | Gilead Sciences Inc | Derivados de aminotriazina utiles como compuestos inhibidores de la cinasa de union a tank. |
| PL3262046T3 (pl) | 2015-02-27 | 2021-05-04 | Incyte Corporation | Sole inhibitora pi3k i sposoby ich wytwarzania |
| EP3287463A4 (en) * | 2015-04-24 | 2018-07-11 | Guangzhou Maxinovel Pharmaceuticals Co., Ltd. | Condensed-ring pyrimidylamino derivative, preparation method therefor, and intermediate, pharmaceutical composition and applications thereof |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| WO2016183063A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Crystalline forms of a pi3k inhibitor |
| EA201891024A1 (ru) | 2015-12-17 | 2018-12-28 | Джилид Сайэнс, Инк. | Соединения-ингибиторы tank-связывающей киназы |
| JP6985388B2 (ja) * | 2016-07-29 | 2021-12-22 | ラプト・セラピューティクス・インコーポレイテッド | ケモカイン受容体調節剤及びそれの使用 |
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2010
- 2010-10-19 CA CA2775009A patent/CA2775009A1/en not_active Abandoned
- 2010-10-19 WO PCT/EP2010/065700 patent/WO2011048082A1/en not_active Ceased
- 2010-10-19 MX MX2012004020A patent/MX2012004020A/es not_active Application Discontinuation
- 2010-10-19 NZ NZ598907A patent/NZ598907A/en not_active IP Right Cessation
- 2010-10-19 US US13/503,083 patent/US9242987B2/en not_active Expired - Fee Related
- 2010-10-19 AU AU2010309882A patent/AU2010309882B2/en not_active Ceased
- 2010-10-19 EA EA201270572A patent/EA022120B1/ru not_active IP Right Cessation
- 2010-10-19 TW TW099135495A patent/TW201125867A/zh unknown
- 2010-10-19 CN CN201080058290.5A patent/CN102666545B/zh not_active Expired - Fee Related
- 2010-10-19 KR KR1020127009821A patent/KR20120102601A/ko not_active Ceased
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- 2010-10-19 EP EP10775748A patent/EP2491039A1/en not_active Withdrawn
- 2010-10-19 BR BR112012009327A patent/BR112012009327A2/pt not_active IP Right Cessation
- 2010-10-19 AR ARP100103813A patent/AR078675A1/es unknown
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2012
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| WO2011048082A1 (en) | 2011-04-28 |
| NZ598907A (en) | 2014-03-28 |
| AR078675A1 (es) | 2011-11-23 |
| KR20120102601A (ko) | 2012-09-18 |
| JP5744887B2 (ja) | 2015-07-08 |
| BR112012009327A2 (pt) | 2017-06-06 |
| CN102666545B (zh) | 2016-04-06 |
| AU2010309882A1 (en) | 2012-04-12 |
| CA2775009A1 (en) | 2011-04-28 |
| US20120252779A1 (en) | 2012-10-04 |
| TW201125867A (en) | 2011-08-01 |
| AU2010309882B2 (en) | 2016-01-28 |
| JP2013508332A (ja) | 2013-03-07 |
| EA201270572A1 (ru) | 2012-12-28 |
| US9242987B2 (en) | 2016-01-26 |
| IL218751A0 (en) | 2012-06-28 |
| CN102666545A (zh) | 2012-09-12 |
| EA022120B1 (ru) | 2015-11-30 |
| EP2491039A1 (en) | 2012-08-29 |
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