ES2542884T3 - Inhibidores de JAK de carbamato tricíclico - Google Patents
Inhibidores de JAK de carbamato tricíclico Download PDFInfo
- Publication number
- ES2542884T3 ES2542884T3 ES09818261.1T ES09818261T ES2542884T3 ES 2542884 T3 ES2542884 T3 ES 2542884T3 ES 09818261 T ES09818261 T ES 09818261T ES 2542884 T3 ES2542884 T3 ES 2542884T3
- Authority
- ES
- Spain
- Prior art keywords
- substituted
- oxo
- pyrimidinediamine
- tetrahydro
- oxazol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000003112 inhibitor Substances 0.000 title description 16
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 245
- -1 amino, substituted amino, carboxyl Chemical group 0.000 claims abstract description 185
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 98
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 91
- 125000003118 aryl group Chemical group 0.000 claims abstract description 76
- 150000003839 salts Chemical class 0.000 claims abstract description 60
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 59
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 46
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract description 46
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 43
- 125000000392 cycloalkenyl group Chemical group 0.000 claims abstract description 42
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 42
- 239000001257 hydrogen Substances 0.000 claims abstract description 41
- 125000000547 substituted alkyl group Chemical group 0.000 claims abstract description 40
- 125000003107 substituted aryl group Chemical group 0.000 claims abstract description 34
- 125000000304 alkynyl group Chemical group 0.000 claims abstract description 32
- 125000003342 alkenyl group Chemical group 0.000 claims abstract description 30
- 125000004426 substituted alkynyl group Chemical group 0.000 claims abstract description 27
- 125000005017 substituted alkenyl group Chemical group 0.000 claims abstract description 26
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims abstract description 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract description 23
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- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 21
- 125000004104 aryloxy group Chemical group 0.000 claims abstract description 21
- 125000005553 heteroaryloxy group Chemical group 0.000 claims abstract description 21
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract description 21
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract description 20
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims abstract description 19
- 125000004429 atom Chemical group 0.000 claims abstract description 17
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- 125000002252 acyl group Chemical group 0.000 claims abstract description 14
- 125000005133 alkynyloxy group Chemical group 0.000 claims abstract description 12
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- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims abstract description 7
- 229910052700 potassium Inorganic materials 0.000 claims abstract description 7
- 125000003282 alkyl amino group Chemical group 0.000 claims abstract description 6
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Classifications
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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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
- A61K31/41—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
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic 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
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/62—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems having two or more ring systems containing condensed 1,3-oxazole rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
- C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9950708P | 2008-09-23 | 2008-09-23 | |
| US99507P | 2008-09-23 | ||
| PCT/US2009/057972 WO2010039518A2 (en) | 2008-09-23 | 2009-09-23 | Tricyclic carbamate jak inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2542884T3 true ES2542884T3 (es) | 2015-08-12 |
Family
ID=42074107
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09818261.1T Active ES2542884T3 (es) | 2008-09-23 | 2009-09-23 | Inhibidores de JAK de carbamato tricíclico |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US8846908B2 (https=) |
| EP (1) | EP2344476B1 (https=) |
| JP (1) | JP5518076B2 (https=) |
| CA (1) | CA2736258C (https=) |
| ES (1) | ES2542884T3 (https=) |
| WO (1) | WO2010039518A2 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2792278C (en) * | 2010-04-13 | 2019-05-14 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses |
| EP2951590A1 (en) | 2013-02-04 | 2015-12-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
| KR101665301B1 (ko) | 2013-08-07 | 2016-10-11 | 카딜라 핼쓰캐어 리미티드 | 야누스 키나제의 억제제로서 n-시아노메틸아미드 |
| WO2018167283A1 (en) | 2017-03-17 | 2018-09-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling |
| WO2018189335A1 (en) | 2017-04-13 | 2018-10-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| KR20210131316A (ko) * | 2019-02-27 | 2021-11-02 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Sumo-활성화 효소 저해제 및 관문 저해제의 투여 |
| CN114761013A (zh) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | 治疗骨髓纤维化和相关病症的方法 |
| WO2021231798A1 (en) | 2020-05-13 | 2021-11-18 | Disc Medicine, Inc. | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| WO2021257857A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Naphthyridinone compounds as jak2 v617f inhibitors |
| WO2021257863A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Pyrrolotriazine compounds as jak2 v617f inhibitors |
| SMT202500271T1 (it) | 2020-07-02 | 2025-09-12 | Incyte Corp | Composti di urea triciclici come inibitori di v617f di jak2 |
| US11767323B2 (en) | 2020-07-02 | 2023-09-26 | Incyte Corporation | Tricyclic pyridone compounds as JAK2 V617F inhibitors |
| US11661422B2 (en) | 2020-08-27 | 2023-05-30 | Incyte Corporation | Tricyclic urea compounds as JAK2 V617F inhibitors |
| WO2022140231A1 (en) | 2020-12-21 | 2022-06-30 | Incyte Corporation | Deazaguaine compounds as jak2 v617f inhibitors |
| AR125273A1 (es) | 2021-02-25 | 2023-07-05 | Incyte Corp | Lactamas espirocíclicas como inhibidores de jak2 v617f |
| CN119173514A (zh) | 2022-03-17 | 2024-12-20 | 因赛特公司 | 作为jak2 v617f抑制剂的三环脲化合物 |
| CN119431398A (zh) * | 2023-07-31 | 2025-02-14 | 中国科学院上海有机化学研究所 | R406及其衍生物协同trail的抗肿瘤应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| ES2445208T3 (es) * | 2002-07-29 | 2014-02-28 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidindiamina para uso en métodos para tratar o prevenir enfermedades autoinmunitarias |
| EP1883302A4 (en) * | 2005-05-03 | 2009-05-20 | Rigel Pharmaceuticals Inc | JAK KINASE HEMMER AND ITS USE |
| WO2006133426A2 (en) * | 2005-06-08 | 2006-12-14 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| CA2642229C (en) * | 2006-02-24 | 2015-05-12 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| EP2089369B1 (en) * | 2006-10-19 | 2011-02-02 | Rigel Pharmaceuticals, Inc. | 2,4 -pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases |
-
2009
- 2009-09-23 ES ES09818261.1T patent/ES2542884T3/es active Active
- 2009-09-23 JP JP2011528087A patent/JP5518076B2/ja not_active Expired - Fee Related
- 2009-09-23 WO PCT/US2009/057972 patent/WO2010039518A2/en not_active Ceased
- 2009-09-23 US US13/119,950 patent/US8846908B2/en active Active
- 2009-09-23 EP EP20090818261 patent/EP2344476B1/en not_active Not-in-force
- 2009-09-23 CA CA2736258A patent/CA2736258C/en active Active
-
2014
- 2014-08-22 US US14/466,697 patent/US20140363443A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP2344476B1 (en) | 2015-04-29 |
| US8846908B2 (en) | 2014-09-30 |
| CA2736258C (en) | 2016-11-29 |
| EP2344476A2 (en) | 2011-07-20 |
| CA2736258A1 (en) | 2010-04-08 |
| JP5518076B2 (ja) | 2014-06-11 |
| WO2010039518A3 (en) | 2010-07-22 |
| EP2344476A4 (en) | 2012-08-15 |
| JP2012503604A (ja) | 2012-02-09 |
| US20140363443A1 (en) | 2014-12-11 |
| WO2010039518A2 (en) | 2010-04-08 |
| US20110269749A1 (en) | 2011-11-03 |
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