EA039660B1 - Твердая форма производного бипиразола - Google Patents
Твердая форма производного бипиразола Download PDFInfo
- Publication number
- EA039660B1 EA039660B1 EA202090291A EA202090291A EA039660B1 EA 039660 B1 EA039660 B1 EA 039660B1 EA 202090291 A EA202090291 A EA 202090291A EA 202090291 A EA202090291 A EA 202090291A EA 039660 B1 EA039660 B1 EA 039660B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- mmol
- cyanomethyl
- azetidin
- trifluoro
- mixture
- Prior art date
Links
Classifications
-
- 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
- A61K31/495—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
-
- 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
-
- 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)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- AIDS & HIV (AREA)
- Biotechnology (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361824683P | 2013-05-17 | 2013-05-17 | |
| US61/824,683 | 2013-05-17 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EA202090291A2 EA202090291A2 (ru) | 2020-05-31 |
| EA202090291A3 EA202090291A3 (ru) | 2020-06-30 |
| EA039660B1 true EA039660B1 (ru) | 2022-02-24 |
Family
ID=50983151
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202090291A EA039660B1 (ru) | 2013-05-17 | 2014-05-16 | Твердая форма производного бипиразола |
| EA201592199A EA036448B1 (ru) | 2013-05-17 | 2014-05-16 | Производные бипиразола в качестве ингибиторов jak |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201592199A EA036448B1 (ru) | 2013-05-17 | 2014-05-16 | Производные бипиразола в качестве ингибиторов jak |
Country Status (36)
Families Citing this family (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1966202T1 (sl) | 2005-12-13 | 2012-01-31 | Incyte Corp | S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze |
| EP2173752B2 (en) | 2007-06-13 | 2022-07-13 | Incyte Holdings Corporation | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| CA2762174C (en) | 2009-05-22 | 2018-02-20 | Incyte Corporation | 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 |
| CN106967070A (zh) | 2009-05-22 | 2017-07-21 | 因塞特控股公司 | 作为jak抑制剂的化合物 |
| SG177384A1 (en) | 2009-06-29 | 2012-02-28 | Incyte Corp | Pyrimidinones as pi3k inhibitors |
| AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| EP3715347B1 (en) | 2010-03-10 | 2021-12-22 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| NZ603686A (en) | 2010-05-21 | 2014-11-28 | Incyte Corp | Topical formulation for a jak inhibitor |
| PE20140146A1 (es) | 2010-11-19 | 2014-02-06 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
| CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| TWI577676B (zh) | 2011-06-20 | 2017-04-11 | 英塞特控股公司 | 作為ｊａｋ抑制劑之吖丁啶基苯基、吡啶基或吡基羧醯胺衍生物 |
| 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 |
| PL3196202T3 (pl) | 2011-09-02 | 2019-09-30 | Incyte Holdings Corporation | Heterocykloaminy jako inhibitory pi3k |
| 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 |
| MX2015005428A (es) | 2012-11-01 | 2015-07-21 | Incyte Corp | Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak). |
| SG11201503695XA (en) | 2012-11-15 | 2015-06-29 | Incyte Corp | Sustained-release dosage forms of ruxolitinib |
| JP6397831B2 (ja) | 2013-03-06 | 2018-09-26 | 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阻害剤の製造方法及びその中間体 |
| WO2014186706A1 (en) * | 2013-05-17 | 2014-11-20 | Incyte Corporation | Bipyrazole derivatives as jak inhibitors |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| PE20161388A1 (es) * | 2014-02-28 | 2016-12-28 | Incyte Corp | Inhibidores de la jak1 para el tratamiento de sindromes mielodisplasicos |
| NZ725778A (en) | 2014-04-08 | 2023-04-28 | Incyte Holdings Corp | Treatment of b-cell malignancies by a combination jak and pi3k inhibitor |
| JP2017514832A (ja) | 2014-04-30 | 2017-06-08 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ１抑制剤を調製する方法及びその新しい形態 |
| 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 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| WO2016172712A2 (en) | 2015-04-23 | 2016-10-27 | Sydnexis, Inc. | Ophthalmic composition |
| US9421199B2 (en) | 2014-06-24 | 2016-08-23 | Sydnexis, Inc. | Ophthalmic composition |
| US9586949B2 (en) | 2015-02-09 | 2017-03-07 | Incyte Corporation | Aza-heteroaryl compounds as PI3K-gamma inhibitors |
| MD3831833T2 (ro) | 2015-02-27 | 2023-04-30 | Incyte Holdings Corp | Procedee pentru prepararea unui inhibitor PI3K |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | 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 |
| CN107847432A (zh) | 2015-05-29 | 2018-03-27 | 西德奈克西斯公司 | D2o稳定化的药物制剂 |
| 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 |
| AR107293A1 (es) | 2016-01-05 | 2018-04-18 | Incyte Corp | COMPUESTOS DE PIRIDINA Y PIRIDIMINA COMO INHIBIDORES DE PI3K-g |
| US10138248B2 (en) | 2016-06-24 | 2018-11-27 | Incyte Corporation | Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors |
| CN107759623B (zh) * | 2016-08-23 | 2020-08-14 | 苏州旺山旺水生物医药有限公司 | Jak抑制剂的中间体及其制备方法 |
| MX2019002627A (es) * | 2016-09-06 | 2019-10-30 | Hoffmann La Roche | Compuestos de 8-(azetidin-1-il)-[1,2,4]triazolo[1,5-a]piridinilo, composiciones y métodos de uso del mismo. |
| MD3697789T2 (ro) | 2017-10-18 | 2022-02-28 | Incyte Corp | Derivați imidazol condensați substituiți cu grupări hidroxi terțiare ca inhibitori PI3K-GAMA |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| MD3746429T2 (ro) | 2018-01-30 | 2022-08-31 | Incyte Corp | Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă) |
| BR112020016628A2 (pt) | 2018-02-16 | 2020-12-15 | Incyte Corporation | Inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas |
| HUE067471T2 (hu) * | 2018-03-30 | 2024-10-28 | Incyte Corp | Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával |
| WO2019191679A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| CN112567247A (zh) | 2018-04-13 | 2021-03-26 | 因赛特公司 | 用于移植物抗宿主病的生物标志物 |
| CN108484468A (zh) * | 2018-05-11 | 2018-09-04 | 南京大学 | 芳基氮杂环丁烷类化合物的制备方法 |
| CA3101323A1 (en) | 2018-06-01 | 2019-12-05 | Incyte Corporation | Dosing regimen for the treatment of pi3k related disorders |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| IL282643B2 (en) | 2018-10-31 | 2025-08-01 | Incyte Corp | A selective jak1 inhibitor for use in a method of treating hematological disease |
| AU2019403304B2 (en) | 2018-12-19 | 2025-09-04 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of gastrointestinal disease |
| JP2022524997A (ja) | 2019-03-05 | 2022-05-11 | インサイト・コーポレイション | 慢性肺同種移植片機能不全の治療のためのｊａｋ１経路阻害剤 |
| JP2022526301A (ja) * | 2019-03-19 | 2022-05-24 | インサイト・コーポレイション | 尋常性白斑のバイオマーカー |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| JP2022549506A (ja) | 2019-09-27 | 2022-11-25 | ディスク・メディシン・インコーポレイテッド | 骨髄線維症および関連状態を処置するための方法 |
| US12203942B2 (en) | 2019-10-10 | 2025-01-21 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US12360120B2 (en) | 2019-10-10 | 2025-07-15 | Incyte Corporation | Biomarkers for graft-versus-host disease |
| US11992490B2 (en) | 2019-10-16 | 2024-05-28 | Incyte Corporation | Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP) |
| JP7518900B2 (ja) * | 2019-10-16 | 2024-07-18 | インサイト・コーポレイション | 皮膚エリテマトーデス及び扁平苔癬（ｌｐ）の治療のためのｊａｋ１阻害剤の使用 |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN115836089A (zh) | 2020-05-13 | 2023-03-21 | 迪斯克医药公司 | 用于治疗骨髓纤维化的抗血幼素（hjv）抗体 |
| FI4157831T3 (fi) | 2020-06-02 | 2024-12-02 | Incyte Corp | Menetelmiä jak1-estäjän valmistamiseksi |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| IL300555A (en) | 2020-08-18 | 2023-04-01 | Incyte Corp | Process and intermediates for preparing a JAK inhibitor |
| AU2021329301A1 (en) | 2020-08-18 | 2023-04-13 | Incyte Corporation | Process and intermediates for preparing a JAK1 inhibitor |
| CN112159394B (zh) * | 2020-10-09 | 2021-10-22 | 嘉兴特科罗生物科技有限公司 | 一种作为jak激酶抑制剂的小分子化合物及其用途 |
| HRP20250528T1 (hr) | 2020-12-04 | 2025-06-20 | Incyte Corporation | Jak inhibitor s analogom vitamina d za liječenje kožnih bolesti |
| US11957661B2 (en) * | 2020-12-08 | 2024-04-16 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of vitiligo |
| CN114099514A (zh) * | 2020-12-29 | 2022-03-01 | 上海岸阔医药科技有限公司 | 预防或治疗egfr功能异常相关的副作用的方法 |
| EP4274578A1 (en) | 2021-01-11 | 2023-11-15 | Incyte Corporation | Combination therapy comprising jak pathway inhibitor and rock inhibitor |
| LT4333840T (lt) | 2021-05-03 | 2026-01-12 | Incyte Corporation | Jak1 kelio inhibitoriai, skirti mazgelinio niežulio gydymui |
| US12071439B2 (en) | 2021-07-12 | 2024-08-27 | Incyte Corporation | Process and intermediates for preparing a JAK inhibitor |
| CN119768166A (zh) | 2022-08-05 | 2025-04-04 | 因赛特公司 | 使用jak抑制剂的荨麻疹治疗 |
| WO2024192350A1 (en) | 2023-03-16 | 2024-09-19 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of asthma |
| CN117186078A (zh) * | 2023-11-06 | 2023-12-08 | 药康众拓(北京)医药科技有限公司 | 氘代氮杂环丁烷类jak抑制剂药物及用途 |
| US20250325664A1 (en) | 2024-04-22 | 2025-10-23 | Incyte Corporation | Combination therapy with an anti-colony stimulating factor 1 receptor antibody and a jak inhibitor |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090233903A1 (en) * | 2008-03-11 | 2009-09-17 | Incyte Corporation | Azetidine and cyclobutane derivatives as jak inhibitors |
| US20110059951A1 (en) * | 2009-09-01 | 2011-03-10 | Rodgers James D | HETEROCYCLIC DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS |
| WO2012177606A1 (en) * | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
Family Cites Families (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS60106847U (ja) | 1983-12-27 | 1985-07-20 | 富士重工業株式会社 | 室外後写鏡 |
| JP2650681B2 (ja) | 1987-07-10 | 1997-09-03 | 株式会社ブリヂストン | 空気ばね |
| JPH0515775Y2 (enExample) | 1987-07-13 | 1993-04-26 | ||
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| PT1107964E (pt) | 1998-08-11 | 2010-06-11 | Novartis Ag | Derivados de isoquinolina com actividade inibidora da angiogénese |
| US6133031A (en) | 1999-08-19 | 2000-10-17 | Isis Pharmaceuticals Inc. | Antisense inhibition of focal adhesion kinase expression |
| GB9905075D0 (en) | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| HU230396B1 (hu) | 2000-06-28 | 2016-04-28 | Smithkline Beecham Plc | Nedves őrlési eljárás |
| BR0212760A (pt) | 2001-09-19 | 2004-12-07 | Aventis Pharma Sa | Compostos quìmicos |
| CA2462657C (en) | 2001-10-30 | 2011-04-26 | Novartis Ag | Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity |
| PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| AR042052A1 (es) | 2002-11-15 | 2005-06-08 | Vertex Pharma | Diaminotriazoles utiles como inhibidores de proteinquinasas |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| WO2006056399A2 (en) | 2004-11-24 | 2006-06-01 | Novartis Ag | Combinations of jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors |
| SI1966202T1 (sl) | 2005-12-13 | 2012-01-31 | Incyte Corp | S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze |
| EP2173752B2 (en) | 2007-06-13 | 2022-07-13 | Incyte Holdings Corporation | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| 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. |
| EA020777B1 (ru) * | 2007-11-16 | 2015-01-30 | Инсайт Корпорейшн | 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus |
| CL2009001884A1 (es) | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| JOP20190230A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| CN106967070A (zh) | 2009-05-22 | 2017-07-21 | 因塞特控股公司 | 作为jak抑制剂的化合物 |
| CA2762174C (en) | 2009-05-22 | 2018-02-20 | Incyte Corporation | 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 |
| PL2486041T3 (pl) | 2009-10-09 | 2014-01-31 | Incyte Holdings Corp | Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu |
| JP5858434B2 (ja) | 2010-02-18 | 2016-02-10 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｎｕｓキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体 |
| EP3715347B1 (en) | 2010-03-10 | 2021-12-22 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| US8962596B2 (en) * | 2010-04-14 | 2015-02-24 | Array Biopharma Inc. | 5,7-substituted-imidazo[1,2-C]pyrimidines as inhibitors of JAK kinases |
| NZ603686A (en) | 2010-05-21 | 2014-11-28 | Incyte Corp | Topical formulation for a jak inhibitor |
| PE20140146A1 (es) * | 2010-11-19 | 2014-02-06 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
| JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | 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阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
| US8828987B2 (en) * | 2010-12-10 | 2014-09-09 | Rottapharm Biotech S.R.L. | Pyridine amide derivatives as EP4 receptor antagonists |
| WO2012116248A1 (en) | 2011-02-24 | 2012-08-30 | Massachusetts Institute Of Technology | ALTERNATIVELY SPLICED mRNA ISOFORMS AS PROGNOSTIC INDICATORS FOR METASTATIC CANCER |
| 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 |
| EP2758377B1 (en) | 2011-09-22 | 2017-08-02 | Merck Sharp & Dohme Corp. | Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors |
| 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 |
| MX2015005428A (es) | 2012-11-01 | 2015-07-21 | Incyte Corp | Derivados triciclicos fusionados de tiofeno como inhibidores de la cinasa janus (jak). |
| SG11201503695XA (en) | 2012-11-15 | 2015-06-29 | Incyte Corp | Sustained-release dosage forms of ruxolitinib |
| JP6397831B2 (ja) | 2013-03-06 | 2018-09-26 | 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阻害剤の製造方法及びその中間体 |
| JO3603B1 (ar) | 2013-05-17 | 2020-07-05 | Janssen Sciences Ireland Uc | مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي |
| US9371282B2 (en) | 2013-05-17 | 2016-06-21 | Centrexion Therapeutics Corporation | Somatostatin receptor subtype 4 (SSTR4) agonists |
| SG11201509463YA (en) | 2013-05-17 | 2015-12-30 | Hoffmann La Roche | 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of hepatitis b virus infection |
| EP2803668A1 (en) | 2013-05-17 | 2014-11-19 | Boehringer Ingelheim International Gmbh | Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles |
| WO2014186706A1 (en) | 2013-05-17 | 2014-11-20 | Incyte Corporation | Bipyrazole derivatives as jak inhibitors |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| PE20161388A1 (es) | 2014-02-28 | 2016-12-28 | Incyte Corp | Inhibidores de la jak1 para el tratamiento de sindromes mielodisplasicos |
| JP2017514832A (ja) | 2014-04-30 | 2017-06-08 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ１抑制剤を調製する方法及びその新しい形態 |
| 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 |
| MA41185B1 (fr) | 2014-12-16 | 2019-12-31 | Novartis Ag | Composés d'acide isoxazole hydroxamique comme inhibiteurs de lpxc |
| BR112020016628A2 (pt) | 2018-02-16 | 2020-12-15 | Incyte Corporation | Inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas |
| FI4157831T3 (fi) | 2020-06-02 | 2024-12-02 | Incyte Corp | Menetelmiä jak1-estäjän valmistamiseksi |
| HRP20250528T1 (hr) | 2020-12-04 | 2025-06-20 | Incyte Corporation | Jak inhibitor s analogom vitamina d za liječenje kožnih bolesti |
| US11957661B2 (en) | 2020-12-08 | 2024-04-16 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of vitiligo |
-
2014
- 2014-05-16 WO PCT/US2014/038388 patent/WO2014186706A1/en not_active Ceased
- 2014-05-16 DK DK17158350.3T patent/DK3231801T3/en active
- 2014-05-16 EP EP17158350.3A patent/EP3231801B1/en active Active
- 2014-05-16 SM SM20230352T patent/SMT202300352T1/it unknown
- 2014-05-16 CN CN201711000293.3A patent/CN107698569B/zh active Active
- 2014-05-16 LT LTEP18215671.1T patent/LT3527263T/lt unknown
- 2014-05-16 PE PE2020000001A patent/PE20200527A1/es unknown
- 2014-05-16 TW TW103117400A patent/TWI664176B/zh active
- 2014-05-16 SI SI201432117T patent/SI4275756T1/sl unknown
- 2014-05-16 FI FIEP20201593.9T patent/FI3786162T3/fi active
- 2014-05-16 PT PT202015939T patent/PT3786162T/pt unknown
- 2014-05-16 US US14/279,929 patent/US9382231B2/en active Active
- 2014-05-16 TR TR2019/05814T patent/TR201905814T4/tr unknown
- 2014-05-16 EP EP20201593.9A patent/EP3786162B1/en active Active
- 2014-05-16 CA CA2911536A patent/CA2911536C/en active Active
- 2014-05-16 HR HRP20251220TT patent/HRP20251220T1/hr unknown
- 2014-05-16 UA UAA201512465A patent/UA117830C2/uk unknown
- 2014-05-16 PT PT231858895T patent/PT4275756T/pt unknown
- 2014-05-16 TW TW112149597A patent/TWI885650B/zh active
- 2014-05-16 PT PT147327050T patent/PT2997023T/pt unknown
- 2014-05-16 EA EA202090291A patent/EA039660B1/ru unknown
- 2014-05-16 ME MEP-2017-116A patent/ME02763B/me unknown
- 2014-05-16 DK DK18215671.1T patent/DK3527263T3/da active
- 2014-05-16 HU HUE18215671A patent/HUE053122T2/hu unknown
- 2014-05-16 LT LTEP14732705.0T patent/LT2997023T/lt unknown
- 2014-05-16 LT LTEP17158350.3T patent/LT3231801T/lt unknown
- 2014-05-16 ES ES23185889T patent/ES3047826T3/es active Active
- 2014-05-16 SG SG10201709469SA patent/SG10201709469SA/en unknown
- 2014-05-16 SI SI201431754T patent/SI3527263T1/sl unknown
- 2014-05-16 MX MX2020004506A patent/MX385187B/es unknown
- 2014-05-16 LT LTEP20201593.9T patent/LT3786162T/lt unknown
- 2014-05-16 ES ES14732705.0T patent/ES2626793T3/es active Active
- 2014-05-16 KR KR1020247014111A patent/KR102729910B1/ko active Active
- 2014-05-16 ME MEP-2019-79A patent/ME03355B/me unknown
- 2014-05-16 EP EP25180368.0A patent/EP4620528A3/en active Pending
- 2014-05-16 CR CR20190156A patent/CR20190156A/es unknown
- 2014-05-16 PL PL20201593.9T patent/PL3786162T3/pl unknown
- 2014-05-16 MX MX2015015738A patent/MX373238B/es active IP Right Grant
- 2014-05-16 PT PT182156711T patent/PT3527263T/pt unknown
- 2014-05-16 EP EP18215671.1A patent/EP3527263B1/en active Active
- 2014-05-16 RS RS20230782A patent/RS64591B1/sr unknown
- 2014-05-16 RS RS20251023A patent/RS67392B1/sr unknown
- 2014-05-16 ES ES17158350T patent/ES2720073T3/es active Active
- 2014-05-16 ES ES20201593T patent/ES2960731T3/es active Active
- 2014-05-16 KR KR1020157035750A patent/KR102341908B1/ko active Active
- 2014-05-16 CN CN201480032106.8A patent/CN105452239B/zh active Active
- 2014-05-16 PL PL17158350T patent/PL3231801T3/pl unknown
- 2014-05-16 HU HUE14732705A patent/HUE033587T2/hu unknown
- 2014-05-16 SI SI201431118T patent/SI3231801T1/sl unknown
- 2014-05-16 SM SM20170258T patent/SMT201700258T1/it unknown
- 2014-05-16 HU HUE17158350A patent/HUE043573T2/hu unknown
- 2014-05-16 DK DK20201593.9T patent/DK3786162T3/da active
- 2014-05-16 SI SI201430239A patent/SI2997023T1/sl unknown
- 2014-05-16 RS RS20210074A patent/RS61482B1/sr unknown
- 2014-05-16 SM SM20190223T patent/SMT201900223T1/it unknown
- 2014-05-16 PT PT17158350T patent/PT3231801T/pt unknown
- 2014-05-16 AR ARP140101971A patent/AR096330A1/es active IP Right Grant
- 2014-05-16 JP JP2016514126A patent/JP6415543B2/ja active Active
- 2014-05-16 ES ES18215671T patent/ES2845210T3/es active Active
- 2014-05-16 KR KR1020217030190A patent/KR102442747B1/ko active Active
- 2014-05-16 SM SM20210040T patent/SMT202100040T1/it unknown
- 2014-05-16 EP EP14732705.0A patent/EP2997023B9/en active Active
- 2014-05-16 AU AU2014265279A patent/AU2014265279B2/en active Active
- 2014-05-16 RS RS20190315A patent/RS58743B1/sr unknown
- 2014-05-16 DK DK23185889.5T patent/DK4275756T3/da active
- 2014-05-16 TW TW108103947A patent/TWI719401B/zh active
- 2014-05-16 EP EP23185889.5A patent/EP4275756B1/en active Active
- 2014-05-16 EA EA201592199A patent/EA036448B1/ru unknown
- 2014-05-16 RS RS20170526A patent/RS56012B1/sr unknown
- 2014-05-16 BR BR112015028501A patent/BR112015028501B8/pt active IP Right Grant
- 2014-05-16 PE PE2015002406A patent/PE20160126A1/es unknown
- 2014-05-16 HU HUE20201593A patent/HUE063817T2/hu unknown
- 2014-05-16 LT LTEP23185889.5T patent/LT4275756T/lt unknown
- 2014-05-16 FI FIEP23185889.5T patent/FI4275756T3/fi active
- 2014-05-16 SM SM20250397T patent/SMT202500397T1/it unknown
- 2014-05-16 KR KR1020227030853A patent/KR102663357B1/ko active Active
- 2014-05-16 SG SG11201509180WA patent/SG11201509180WA/en unknown
- 2014-05-16 HR HRP20170795TT patent/HRP20170795T1/hr unknown
- 2014-05-16 SI SI201432046T patent/SI3786162T1/sl unknown
- 2014-05-16 HR HRP20231048TT patent/HRP20231048T1/hr unknown
- 2014-05-16 MY MYPI2015002767A patent/MY174788A/en unknown
- 2014-05-16 PL PL18215671T patent/PL3527263T3/pl unknown
- 2014-05-16 TW TW110101630A patent/TWI840646B/zh active
- 2014-05-16 PL PL14732705T patent/PL2997023T3/pl unknown
-
2015
- 2015-11-04 IL IL24245315A patent/IL242453B/en active IP Right Grant
- 2015-11-12 PH PH12015502563A patent/PH12015502563B1/en unknown
- 2015-11-13 CL CL2015003355A patent/CL2015003355A1/es unknown
- 2015-12-03 CR CR20150633A patent/CR20150633A/es unknown
-
2016
- 2016-06-20 US US15/187,296 patent/US9926301B2/en active Active
-
2017
- 2017-06-08 CY CY20171100610T patent/CY1119105T1/el unknown
-
2018
- 2018-02-15 US US15/897,598 patent/US10435392B2/en active Active
- 2018-04-18 HK HK18105021.2A patent/HK1245769B/en unknown
- 2018-08-31 AU AU2018223058A patent/AU2018223058B2/en active Active
- 2018-10-02 PH PH12018502125A patent/PH12018502125A1/en unknown
- 2018-10-02 JP JP2018187613A patent/JP6775560B2/ja active Active
-
2019
- 2019-01-22 IL IL264409A patent/IL264409B/en active IP Right Grant
- 2019-04-16 HR HRP20190713TT patent/HRP20190713T1/hr unknown
- 2019-05-10 CY CY20191100510T patent/CY1121763T1/el unknown
- 2019-08-29 US US16/555,620 patent/US11001571B2/en active Active
-
2020
- 2020-02-17 AR ARP200100433A patent/AR118120A2/es unknown
- 2020-03-19 AU AU2020202000A patent/AU2020202000B2/en active Active
- 2020-10-06 JP JP2020168950A patent/JP7126741B2/ja active Active
-
2021
- 2021-01-22 HR HRP20210119TT patent/HRP20210119T1/hr unknown
- 2021-01-22 CY CY20211100050T patent/CY1123756T1/el unknown
- 2021-04-13 US US17/229,397 patent/US11591318B2/en active Active
- 2021-04-26 IL IL282644A patent/IL282644B/en unknown
- 2021-04-29 AU AU2021202685A patent/AU2021202685B2/en active Active
- 2021-10-17 IL IL287313A patent/IL287313B/en unknown
-
2022
- 2022-08-10 JP JP2022128042A patent/JP2022163162A/ja active Pending
- 2022-10-31 AU AU2022263454A patent/AU2022263454B2/en active Active
-
2023
- 2023-01-24 US US18/101,014 patent/US11905275B2/en active Active
-
2024
- 2024-01-02 US US18/402,493 patent/US12247020B2/en active Active
- 2024-05-15 JP JP2024079435A patent/JP2024105557A/ja active Pending
-
2025
- 2025-02-05 US US19/045,868 patent/US20250206726A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090233903A1 (en) * | 2008-03-11 | 2009-09-17 | Incyte Corporation | Azetidine and cyclobutane derivatives as jak inhibitors |
| US20110059951A1 (en) * | 2009-09-01 | 2011-03-10 | Rodgers James D | HETEROCYCLIC DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS |
| WO2012177606A1 (en) * | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA039660B1 (ru) | Твердая форма производного бипиразола | |
| HK1245769A1 (en) | Bipyrazole salt as jak inhibitor | |
| HK40049209A (en) | Bipyrazole derivatives as jak inhibitors | |
| HK40012259B (en) | Bipyrazole derivatives as jak inhibitors | |
| HK40012259A (en) | Bipyrazole derivatives as jak inhibitors | |
| HK1221466B (en) | Bipyrazole derivatives as jak inhibitors | |
| NZ753639B2 (en) | Bipyrazole derivatives as jak inhibitors | |
| NZ753636B2 (en) | Bipyrazole derivatives as jak inhibitors |