EA202090291A3 - Производные бипиразола в качестве ингибиторов jak - Google Patents
Производные бипиразола в качестве ингибиторов jakInfo
- Publication number
- EA202090291A3 EA202090291A3 EA202090291A EA202090291A EA202090291A3 EA 202090291 A3 EA202090291 A3 EA 202090291A3 EA 202090291 A EA202090291 A EA 202090291A EA 202090291 A EA202090291 A EA 202090291A EA 202090291 A3 EA202090291 A3 EA 202090291A3
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- bipirazole
- derivatives
- jak inhibitors
- diseases
- jak
- Prior art date
Links
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 3
- 108010024121 Janus Kinases Proteins 0.000 abstract 3
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
- C07D403/14—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)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Biotechnology (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
В изобретении предложены соединения формулы Iили их фармацевтически приемлемые соли, а также их композиции и способы их применения, которые ингибируют активность Янус-киназы (JAK) и подходят для применения для лечения заболеваний, связанных с активностью JAK, включая, например, воспалительные заболевания, аутоиммунные заболевания, раковые заболевания и другие заболевания.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361824683P | 2013-05-17 | 2013-05-17 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EA202090291A2 EA202090291A2 (ru) | 2020-05-31 |
| EA202090291A3 true EA202090291A3 (ru) | 2020-06-30 |
| EA039660B1 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)
| Country | Link |
|---|---|
| US (8) | US9382231B2 (ru) |
| EP (6) | EP4275756B1 (ru) |
| JP (5) | JP6415543B2 (ru) |
| KR (4) | KR102663357B1 (ru) |
| CN (2) | CN107698569B (ru) |
| AR (2) | AR096330A1 (ru) |
| AU (5) | AU2014265279B2 (ru) |
| BR (1) | BR112015028501B8 (ru) |
| CA (1) | CA2911536C (ru) |
| CL (1) | CL2015003355A1 (ru) |
| CR (2) | CR20190156A (ru) |
| CY (3) | CY1119105T1 (ru) |
| DK (4) | DK3786162T3 (ru) |
| EA (2) | EA039660B1 (ru) |
| ES (4) | ES2720073T3 (ru) |
| FI (1) | FI3786162T3 (ru) |
| HK (1) | HK1245769B (ru) |
| HR (4) | HRP20231048T1 (ru) |
| HU (4) | HUE063817T2 (ru) |
| IL (4) | IL242453B (ru) |
| LT (4) | LT2997023T (ru) |
| ME (2) | ME02763B (ru) |
| MX (2) | MX385187B (ru) |
| MY (1) | MY174788A (ru) |
| PE (2) | PE20160126A1 (ru) |
| PH (2) | PH12015502563B1 (ru) |
| PL (4) | PL3231801T3 (ru) |
| PT (4) | PT3786162T (ru) |
| RS (4) | RS58743B1 (ru) |
| SG (2) | SG11201509180WA (ru) |
| SI (4) | SI3527263T1 (ru) |
| SM (4) | SMT201900223T1 (ru) |
| TR (1) | TR201905814T4 (ru) |
| TW (4) | TWI885650B (ru) |
| UA (1) | UA117830C2 (ru) |
| WO (1) | WO2014186706A1 (ru) |
Families Citing this family (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE041382T2 (hu) | 2005-12-13 | 2019-05-28 | Incyte Holdings Corp | Pirrolo[2,3-d]pirimidin származékok janus-kináz inhibitorként |
| RS54878B1 (sr) | 2007-06-13 | 2016-10-31 | Incyte Holdings Corp | Kristalne soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropionitril |
| UA106078C2 (ru) | 2009-05-22 | 2014-07-25 | Інсайт Корпорейшн | 3-[4-(7H-ПИРРОЛО[2,3-d] ПИРИМИДИН-4-ИЛ)-1H- ПИРАЗОЛ-1-ИЛ]ОКТАН- ИЛИ ГЕПТАННИТРИЛ КАК JAK-ИНГИБИТОРЫ |
| AR076794A1 (es) | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| WO2011008487A1 (en) | 2009-06-29 | 2011-01-20 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
| 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 |
| TWI592413B (zh) | 2010-03-10 | 2017-07-21 | 英塞特公司 | 作為ｊａｋ１抑制劑之哌啶-４-基三亞甲亞胺衍生物 |
| AU2011255443B2 (en) | 2010-05-21 | 2014-07-03 | Incyte Holdings Corporation | Topical formulation for a JAK inhibitor |
| EA026201B1 (ru) | 2010-11-19 | 2017-03-31 | Инсайт Холдингс Корпорейшн | Циклобутилзамещенные производные пирролопиридина и пирролопиримидина как ингибиторы jak |
| EP2655374B1 (en) | 2010-12-20 | 2019-10-23 | Incyte Holdings Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| CA2839767A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | 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 |
| KR102371532B1 (ko) | 2011-09-02 | 2022-03-07 | 인사이트 홀딩스 코포레이션 | Ｐｉ３ｋ 억제제로서 헤테로시클릴아민 |
| 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 |
| AR091079A1 (es) | 2012-05-18 | 2014-12-30 | Incyte Corp | Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak |
| 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 |
| PH12020551186B1 (en) | 2012-11-15 | 2024-03-20 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| SG10201707259PA (en) | 2013-03-06 | 2017-10-30 | Incyte Corp | Processes and intermediates for making a jak inhibitor |
| PL3231801T3 (pl) | 2013-05-17 | 2019-07-31 | Incyte Corporation | Sol bipirazolu jako inhibitor jak |
| DK3030227T3 (da) | 2013-08-07 | 2020-04-20 | Incyte Corp | Vedvarende frigivelses-doseringsformer for en jak1-inhibitor |
| PL3110409T3 (pl) * | 2014-02-28 | 2018-12-31 | Incyte Corporation | Inhibitory jak1 do leczenia zespołów mielodysplastycznych |
| ES2829914T3 (es) | 2014-04-08 | 2021-06-02 | Incyte Corp | Tratamiento de enfermedades malignas de células B mediante una combinación de inhibidor de JAK y PI3K |
| SG11201609016VA (en) | 2014-04-30 | 2016-11-29 | Incyte Corp | Processes of preparing a jak1 inhibitor and new forms thereto |
| 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 |
| US11382909B2 (en) | 2014-09-05 | 2022-07-12 | Sydnexis, Inc. | Ophthalmic composition |
| WO2016130501A1 (en) | 2015-02-09 | 2016-08-18 | Incyte Corporation | Aza-heteroaryl compounds as pi3k-gamma inhibitors |
| PL3262046T3 (pl) | 2015-02-27 | 2021-05-04 | Incyte Corporation | Sole inhibitora pi3k i sposoby ich wytwarzania |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
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| CN118453493A (zh) | 2015-05-29 | 2024-08-09 | 西德奈克西斯公司 | D2o稳定化的药物制剂 |
| HUE059324T2 (hu) | 2015-11-06 | 2022-11-28 | Incyte Corp | Heterociklusos vegyületek, mint PI3K-gamma inhibitorok |
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| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| PL3746429T3 (pl) | 2018-01-30 | 2022-06-20 | Incyte Corporation | Procesy do otrzymywania (1-(3-fluoro-2-(trifluorometylo)izonikotynoilo)piperydyn-4-onu) |
| US11103510B2 (en) | 2018-02-16 | 2021-08-31 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of cytokine-related disorders |
| WO2019191679A1 (en) | 2018-03-30 | 2019-10-03 | Incyte Corporation | Biomarkers for inflammatory skin disease |
| PT3773593T (pt) * | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| MX2020010815A (es) | 2018-04-13 | 2020-12-11 | Incyte Corp | Biomarcadores para enfermedad de injerto contra hospedero. |
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