CO2020001469A2 - Compuestos bicíclicos de pirazol y triazolo como inhibidores de las cinasas jak - Google Patents
Compuestos bicíclicos de pirazol y triazolo como inhibidores de las cinasas jakInfo
- Publication number
- CO2020001469A2 CO2020001469A2 CONC2020/0001469A CO2020001469A CO2020001469A2 CO 2020001469 A2 CO2020001469 A2 CO 2020001469A2 CO 2020001469 A CO2020001469 A CO 2020001469A CO 2020001469 A2 CO2020001469 A2 CO 2020001469A2
- Authority
- CO
- Colombia
- Prior art keywords
- inhibitors
- compounds
- jak kinases
- triazole compounds
- bicyclic pyrazole
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- 125000002619 bicyclic group Chemical group 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- -1 triazole compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 abstract 1
- 108010024121 Janus Kinases Proteins 0.000 abstract 1
- 102000015617 Janus Kinases Human genes 0.000 abstract 1
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 abstract 1
- 230000002496 gastric effect Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition 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
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762539642P | 2017-08-01 | 2017-08-01 | |
| PCT/US2018/044508 WO2019027960A1 (en) | 2017-08-01 | 2018-07-31 | BICYCLIC PYRAZOLO AND TRIAZOLO COMPOUNDS AS JAK KINASE INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2020001469A2 true CO2020001469A2 (es) | 2020-05-29 |
Family
ID=63209687
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2020/0001469A CO2020001469A2 (es) | 2017-08-01 | 2020-02-11 | Compuestos bicíclicos de pirazol y triazolo como inhibidores de las cinasas jak |
Country Status (23)
| Country | Link |
|---|---|
| US (4) | US10392368B2 (OSRAM) |
| EP (1) | EP3652169A1 (OSRAM) |
| JP (2) | JP7098716B2 (OSRAM) |
| KR (1) | KR20200036004A (OSRAM) |
| CN (1) | CN111032646B (OSRAM) |
| AR (1) | AR112348A1 (OSRAM) |
| AU (1) | AU2018312349A1 (OSRAM) |
| BR (1) | BR112020002265A2 (OSRAM) |
| CA (1) | CA3069990A1 (OSRAM) |
| CL (1) | CL2020000283A1 (OSRAM) |
| CO (1) | CO2020001469A2 (OSRAM) |
| EA (1) | EA038912B1 (OSRAM) |
| IL (1) | IL272031A (OSRAM) |
| MA (1) | MA49570A (OSRAM) |
| MX (1) | MX2020001170A (OSRAM) |
| MY (1) | MY200629A (OSRAM) |
| PE (1) | PE20201028A1 (OSRAM) |
| PH (1) | PH12020500201A1 (OSRAM) |
| SG (1) | SG11202000602YA (OSRAM) |
| TW (1) | TW201920150A (OSRAM) |
| UA (1) | UA125318C2 (OSRAM) |
| WO (1) | WO2019027960A1 (OSRAM) |
| ZA (1) | ZA202000561B (OSRAM) |
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| AU2018312349A1 (en) | 2017-08-01 | 2020-02-06 | Theravance Biopharma R&D Ip, Llc | Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors |
| WO2020154350A1 (en) * | 2019-01-23 | 2020-07-30 | Theravance Biopharma R&D Ip, Llc | Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors |
| WO2021009664A1 (en) * | 2019-07-15 | 2021-01-21 | Novartis Ag | Methods for treating meibomian gland dysfunction with liver x receptor agonists |
| CA3179566A1 (en) * | 2020-04-08 | 2021-10-14 | Pfizer Inc. | Crystalline forms of 3-cyano-1-[4-[6-(1-methyl-1h-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1h-pyrazol-1-yl]cyclobutaneacetonitrile, and use thereof |
| TW202207918A (zh) | 2020-05-14 | 2022-03-01 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | 腸道選擇性ｊａｋ３抑制劑的投與 |
| WO2022033544A1 (zh) * | 2020-08-13 | 2022-02-17 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| CN114075220A (zh) * | 2020-08-13 | 2022-02-22 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| TW202229242A (zh) * | 2020-09-10 | 2022-08-01 | 大陸商四川海思科製藥有限公司 | 一種碳環醯胺衍生物及其在醫藥上的應用 |
| WO2022199599A1 (zh) * | 2021-03-23 | 2022-09-29 | 凯复(苏州)生物医药有限公司 | 丙烯酰基取代的化合物、包含其的药物组合物及其用途 |
| CN117377667A (zh) * | 2021-03-29 | 2024-01-09 | 百时美施贵宝公司 | 6-(环丙烷甲酰胺基)-4-((2-甲氧基-3-(1-甲基-1H-1,2,4-三唑-3-基)苯基)氨基)-N-(甲基-d3)哒嗪-3-甲酰胺的晶型 |
| CN113061137B (zh) * | 2021-04-02 | 2022-08-02 | 广西医科大学 | 含氮杂环衍生物或其药学上可接受的盐和用途 |
| MX2023013052A (es) * | 2021-05-03 | 2024-01-12 | Incyte Corp | Inhibidores de la via de la cinasa jano 1 (jak1) para el tratamiento del prurigo nodularis. |
| US20250051360A1 (en) * | 2021-12-23 | 2025-02-13 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compound, and composition and use thereof |
| WO2023165562A1 (zh) * | 2022-03-02 | 2023-09-07 | 南京明德新药研发有限公司 | 含氮杂环类化合物及其应用 |
| GB202213163D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| GB202213164D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
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| KR102032418B1 (ko) * | 2017-06-15 | 2019-10-16 | 한국화학연구원 | 접합 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 브루톤티로신 키나제 활성 관련 질환의 예방 또는 치료용 약학적 조성물 |
| AU2018312349A1 (en) | 2017-08-01 | 2020-02-06 | Theravance Biopharma R&D Ip, Llc | Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors |
| BR112020008850A2 (pt) | 2017-11-03 | 2020-10-20 | Aclaris Therapeutics, Inc. | composto, composição farmacêutica e método para tratar uma doença mediada por jak1 e jak3 |
| MX2020006799A (es) | 2017-12-28 | 2020-09-03 | Daewoong Pharmaceutical Co Ltd | Derivados de oxi-fluoropiperidina como inhibidor de cinasa. |
| KR102577241B1 (ko) | 2017-12-28 | 2023-09-11 | 주식회사 대웅제약 | 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체 |
| KR102577242B1 (ko) | 2017-12-28 | 2023-09-11 | 주식회사 대웅제약 | 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체 |
| WO2020154350A1 (en) * | 2019-01-23 | 2020-07-30 | Theravance Biopharma R&D Ip, Llc | Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors |
| TW202207918A (zh) * | 2020-05-14 | 2022-03-01 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | 腸道選擇性ｊａｋ３抑制劑的投與 |
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2018
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- 2018-07-31 MA MA049570A patent/MA49570A/fr unknown
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- 2018-07-31 AR ARP180102151 patent/AR112348A1/es unknown
- 2018-07-31 US US16/050,227 patent/US10392368B2/en active Active
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- 2018-07-31 EA EA202090413A patent/EA038912B1/ru unknown
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- 2018-07-31 EP EP18755621.2A patent/EP3652169A1/en not_active Withdrawn
- 2018-07-31 PE PE2020000171A patent/PE20201028A1/es unknown
- 2018-07-31 WO PCT/US2018/044508 patent/WO2019027960A1/en not_active Ceased
- 2018-07-31 TW TW107126579A patent/TW201920150A/zh unknown
- 2018-07-31 MY MYPI2020000251A patent/MY200629A/en unknown
- 2018-07-31 KR KR1020207005956A patent/KR20200036004A/ko not_active Withdrawn
- 2018-07-31 CA CA3069990A patent/CA3069990A1/en not_active Abandoned
- 2018-07-31 UA UAA202001352A patent/UA125318C2/uk unknown
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2019
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2020
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2021
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| MX2020001170A (es) | 2020-03-12 |
| SG11202000602YA (en) | 2020-02-27 |
| BR112020002265A2 (pt) | 2020-07-28 |
| CL2020000283A1 (es) | 2020-06-12 |
| PE20201028A1 (es) | 2020-10-05 |
| UA125318C2 (uk) | 2022-02-16 |
| EA038912B1 (ru) | 2021-11-09 |
| MY200629A (en) | 2024-01-06 |
| MA49570A (fr) | 2020-05-20 |
| JP7098716B2 (ja) | 2022-07-11 |
| TW201920150A (zh) | 2019-06-01 |
| KR20200036004A (ko) | 2020-04-06 |
| CN111032646A (zh) | 2020-04-17 |
| CA3069990A1 (en) | 2019-02-07 |
| AU2018312349A1 (en) | 2020-02-06 |
| AR112348A1 (es) | 2019-10-16 |
| US10968205B2 (en) | 2021-04-06 |
| JP2021098751A (ja) | 2021-07-01 |
| US20190315724A1 (en) | 2019-10-17 |
| CN111032646B (zh) | 2023-01-03 |
| EA202090413A1 (ru) | 2020-06-24 |
| US20200216423A1 (en) | 2020-07-09 |
| US20190040043A1 (en) | 2019-02-07 |
| US20220119369A1 (en) | 2022-04-21 |
| US10538513B2 (en) | 2020-01-21 |
| EP3652169A1 (en) | 2020-05-20 |
| ZA202000561B (en) | 2022-04-28 |
| WO2019027960A1 (en) | 2019-02-07 |
| IL272031A (en) | 2020-03-31 |
| JP2020529987A (ja) | 2020-10-15 |
| PH12020500201A1 (en) | 2020-10-12 |
| US10392368B2 (en) | 2019-08-27 |
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