CR20190156A - Derivados de bipirazol como inhibidores jak - Google Patents
Derivados de bipirazol como inhibidores jakInfo
- Publication number
- CR20190156A CR20190156A CR20190156A CR20190156A CR20190156A CR 20190156 A CR20190156 A CR 20190156A CR 20190156 A CR20190156 A CR 20190156A CR 20190156 A CR20190156 A CR 20190156A CR 20190156 A CR20190156 A CR 20190156A
- Authority
- CR
- Costa Rica
- Prior art keywords
- jak
- activity
- jak inhibitors
- diseases
- cancer
- Prior art date
Links
- YGAILVDTGIMZAB-UHFFFAOYSA-N 3-pyrazol-3-ylidenepyrazole Chemical class N1=NC=CC1=C1N=NC=C1 YGAILVDTGIMZAB-UHFFFAOYSA-N 0.000 title 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 6
- 108010024121 Janus Kinases Proteins 0.000 abstract 6
- 201000010099 disease Diseases 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 4
- 208000023275 Autoimmune disease Diseases 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000027866 inflammatory disease Diseases 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
Classifications
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- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- C07D403/14—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
-
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P31/20—Antivirals for DNA viruses
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Biotechnology (AREA)
- Dermatology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente invención proporciona compuestos de la Fórmula I: o sales farmacéuticamente aceptables de este, así como sus composiciones y métodos de uso, que inhiben la actividad de la Janus quinasa (JAK) y son útiles en el tratamiento de enfermedades relacionadas con la actividad de JAK, que incluyen, por ejemplo, trastornos inflamatorios, trastornos autoinmunitarios, cáncer, y otras enfermedades.The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361824683P | 2013-05-17 | 2013-05-17 | |
| PCT/US2014/038388 WO2014186706A1 (en) | 2013-05-17 | 2014-05-16 | Bipyrazole derivatives as jak inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20190156A true CR20190156A (es) | 2019-05-16 |
Family
ID=50983151
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20190156A CR20190156A (es) | 2013-05-17 | 2014-05-16 | Derivados de bipirazol como inhibidores jak |
| CR20150633A CR20150633A (es) | 2013-05-17 | 2015-12-03 | Derivados del bipirazol como inhibidores jak |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20150633A CR20150633A (es) | 2013-05-17 | 2015-12-03 | Derivados del bipirazol como inhibidores jak |
Country Status (36)
| Country | Link |
|---|---|
| US (8) | US9382231B2 (es) |
| EP (6) | EP3231801B1 (es) |
| JP (5) | JP6415543B2 (es) |
| KR (4) | KR102442747B1 (es) |
| CN (2) | CN107698569B (es) |
| AR (2) | AR096330A1 (es) |
| AU (5) | AU2014265279B2 (es) |
| BR (1) | BR112015028501B8 (es) |
| CA (1) | CA2911536C (es) |
| CL (1) | CL2015003355A1 (es) |
| CR (2) | CR20190156A (es) |
| CY (3) | CY1119105T1 (es) |
| DK (4) | DK3786162T3 (es) |
| EA (2) | EA039660B1 (es) |
| ES (5) | ES2626793T3 (es) |
| FI (2) | FI3786162T3 (es) |
| HK (1) | HK1245769B (es) |
| HR (5) | HRP20231048T1 (es) |
| HU (5) | HUE073609T2 (es) |
| IL (4) | IL242453B (es) |
| LT (5) | LT3527263T (es) |
| ME (2) | ME02763B (es) |
| MX (2) | MX385187B (es) |
| MY (1) | MY174788A (es) |
| PE (2) | PE20200527A1 (es) |
| PH (2) | PH12015502563B1 (es) |
| PL (5) | PL3527263T3 (es) |
| PT (5) | PT2997023T (es) |
| RS (5) | RS64591B1 (es) |
| SG (2) | SG10201709469SA (es) |
| SI (5) | SI3527263T1 (es) |
| SM (5) | SMT202500397T1 (es) |
| TR (1) | TR201905814T4 (es) |
| TW (4) | TWI719401B (es) |
| UA (1) | UA117830C2 (es) |
| WO (1) | WO2014186706A1 (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103214484B (zh) | 2005-12-13 | 2016-07-06 | 因塞特控股公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
| HUE029236T2 (en) | 2007-06-13 | 2017-02-28 | Incyte Holdings Corp | (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor |
| MY156727A (en) | 2009-05-22 | 2016-03-15 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP2432472B1 (en) | 2009-05-22 | 2019-10-02 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| EP2845856A1 (en) | 2009-06-29 | 2015-03-11 | Incyte Corporation | Pyrimidinones as PI3K inhibitors |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| AR084691A1 (es) | 2010-05-21 | 2013-06-05 | Incyte Corp | Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| TW201249844A (en) | 2010-12-20 | 2012-12-16 | Incyte Corp | N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| 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 |
| UA121539C2 (uk) | 2011-09-02 | 2020-06-25 | Інсайт Холдинґс Корпорейшн | Гетероцикліламіни як інгібітори рі3к |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| JP6359546B2 (ja) | 2012-11-01 | 2018-07-18 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害薬としての三環式縮合チオフェン誘導体 |
| TWI761825B (zh) | 2012-11-15 | 2022-04-21 | 美商英塞特控股公司 | 盧梭利替尼之緩釋性劑型 |
| MX384910B (es) | 2013-03-06 | 2025-03-14 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak. |
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| SG11201600815WA (en) | 2013-08-07 | 2016-03-30 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| SG10201807952PA (en) * | 2014-02-28 | 2018-10-30 | Incyte Corp | Jak1 inhibitors for the treatment of myelodysplastic syndromes |
| CN106413716B (zh) | 2014-04-08 | 2020-03-27 | 因赛特公司 | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 |
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| 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 |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| WO2016172712A2 (en) | 2015-04-23 | 2016-10-27 | Sydnexis, Inc. | Ophthalmic composition |
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| WO2016130501A1 (en) | 2015-02-09 | 2016-08-18 | Incyte Corporation | Aza-heteroaryl compounds as pi3k-gamma inhibitors |
| UA122332C2 (uk) | 2015-02-27 | 2020-10-26 | Інсайт Корпорейшн | Солі інгібітора pi3k і способи їх отримання |
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| WO2016183063A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Crystalline forms of a pi3k inhibitor |
| EP3302426A4 (en) | 2015-05-29 | 2018-12-05 | Sydnexis, Inc. | D2o stabilized pharmaceutical formulations |
| TWI744256B (zh) | 2015-11-06 | 2021-11-01 | 美商英塞特公司 | 作為PI3K-γ抑制劑之雜環化合物 |
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| KR20190045302A (ko) * | 2016-09-06 | 2019-05-02 | 에프. 호프만-라 로슈 아게 | 8-(아제티딘-1-일)-[1,2,4]트라이아졸로[1,5-a]피리딘일 화합물 및 이의 조성물 및 사용 방법 |
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| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| JP7393348B2 (ja) | 2018-01-30 | 2023-12-06 | インサイト・コーポレイション | (1-(3-フルオロ-2(トリフルオロメチル)イソニコチニル)ピぺリジン―4-オン)を作製するためのプロセス及び中間体 |
| UA127519C2 (uk) | 2018-02-16 | 2023-09-20 | Інсайт Корпорейшн | Інгібітори шляху jak1, призначені для лікування порушень, пов'язаних із цитокінами |
| JP7565798B2 (ja) | 2018-03-30 | 2024-10-11 | インサイト・コーポレイション | 炎症性皮膚疾患のバイオマーカー |
| CN113768934A (zh) | 2018-03-30 | 2021-12-10 | 因赛特公司 | 使用jak抑制剂治疗化脓性汗腺炎 |
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