RU2012148246A - 5, 7- замещенные-имидазо[1, 2-с]пиримидины как ингибиторы jak-киназ - Google Patents
5, 7- замещенные-имидазо[1, 2-с]пиримидины как ингибиторы jak-киназ Download PDFInfo
- Publication number
- RU2012148246A RU2012148246A RU2012148246/04A RU2012148246A RU2012148246A RU 2012148246 A RU2012148246 A RU 2012148246A RU 2012148246/04 A RU2012148246/04 A RU 2012148246/04A RU 2012148246 A RU2012148246 A RU 2012148246A RU 2012148246 A RU2012148246 A RU 2012148246A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- formula
- compound
- ring
- hetar
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims abstract 160
- 150000001875 compounds Chemical class 0.000 claims abstract 110
- 125000001424 substituent group Chemical group 0.000 claims abstract 34
- -1 pyridinonyl Chemical group 0.000 claims abstract 33
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 29
- 229910052799 carbon Inorganic materials 0.000 claims abstract 21
- 125000001153 fluoro group Chemical group F* 0.000 claims abstract 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 14
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 11
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 9
- 150000003839 salts Chemical class 0.000 claims abstract 8
- 239000012453 solvate Substances 0.000 claims abstract 8
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 7
- 125000005842 heteroatom Chemical group 0.000 claims abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 7
- 125000002619 bicyclic group Chemical group 0.000 claims abstract 4
- 229910052731 fluorine Inorganic materials 0.000 claims abstract 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims abstract 3
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 3
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 claims abstract 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims abstract 2
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- PQIOSYKVBBWRRI-UHFFFAOYSA-N methylphosphonyl difluoride Chemical group CP(F)(F)=O PQIOSYKVBBWRRI-UHFFFAOYSA-N 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 8
- 238000006243 chemical reaction Methods 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 241000124008 Mammalia Species 0.000 claims 6
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000003566 oxetanyl group Chemical group 0.000 claims 4
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 3
- 239000003638 chemical reducing agent Substances 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 239000003054 catalyst Substances 0.000 claims 2
- 239000003153 chemical reaction reagent Substances 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 239000012025 fluorinating agent Substances 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 229910052763 palladium Inorganic materials 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- WJKHJLXJJJATHN-UHFFFAOYSA-N triflic anhydride Chemical compound FC(F)(F)S(=O)(=O)OS(=O)(=O)C(F)(F)F WJKHJLXJJJATHN-UHFFFAOYSA-N 0.000 claims 2
- 125000004521 1,3,4-thiadiazol-2-yl group Chemical group S1C(=NN=C1)* 0.000 claims 1
- HNEGJTWNOOWEMH-UHFFFAOYSA-N 1-fluoropropane Chemical group [CH2]CCF HNEGJTWNOOWEMH-UHFFFAOYSA-N 0.000 claims 1
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- KLNXUTSCUIBQGB-UHFFFAOYSA-N 2-bromo-2-fluoroacetaldehyde Chemical compound FC(Br)C=O KLNXUTSCUIBQGB-UHFFFAOYSA-N 0.000 claims 1
- AVAHZUUYBFUOPN-UHFFFAOYSA-N 2-chloro-2-fluoroacetaldehyde Chemical compound FC(Cl)C=O AVAHZUUYBFUOPN-UHFFFAOYSA-N 0.000 claims 1
- QSKPIOLLBIHNAC-UHFFFAOYSA-N 2-chloro-acetaldehyde Chemical compound ClCC=O QSKPIOLLBIHNAC-UHFFFAOYSA-N 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- RCPFKNIWFCVDLQ-UHFFFAOYSA-N 4-oxa-3-azabicyclo[3.2.1]octane Chemical compound C1C2CCC1ONC2 RCPFKNIWFCVDLQ-UHFFFAOYSA-N 0.000 claims 1
- NLHHRLWOUZZQLW-UHFFFAOYSA-N Acrylonitrile Chemical compound C=CC#N NLHHRLWOUZZQLW-UHFFFAOYSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- JRNVZBWKYDBUCA-UHFFFAOYSA-N N-chlorosuccinimide Chemical compound ClN1C(=O)CCC1=O JRNVZBWKYDBUCA-UHFFFAOYSA-N 0.000 claims 1
- LQZMLBORDGWNPD-UHFFFAOYSA-N N-iodosuccinimide Chemical compound IN1C(=O)CCC1=O LQZMLBORDGWNPD-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims 1
- 125000002777 acetyl group Chemical class [H]C([H])([H])C(*)=O 0.000 claims 1
- 150000001299 aldehydes Chemical class 0.000 claims 1
- 125000006177 alkyl benzyl group Chemical group 0.000 claims 1
- 150000008064 anhydrides Chemical class 0.000 claims 1
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 125000006380 bromopyridyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000000068 chlorophenyl group Chemical group 0.000 claims 1
- DOBRDRYODQBAMW-UHFFFAOYSA-N copper(i) cyanide Chemical compound [Cu+].N#[C-] DOBRDRYODQBAMW-UHFFFAOYSA-N 0.000 claims 1
- 239000012024 dehydrating agents Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 150000004820 halides Chemical class 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 229910052744 lithium Inorganic materials 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 238000007363 ring formation reaction Methods 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000004496 thiazol-5-yl group Chemical group S1C=NC=C1* 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 0 Cc1cnc2[n]1c(I)nc(*)c2 Chemical compound Cc1cnc2[n]1c(I)nc(*)c2 0.000 description 2
Classifications
-
- 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
-
- 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
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32418610P | 2010-04-14 | 2010-04-14 | |
| US61/324,186 | 2010-04-14 | ||
| PCT/US2011/031896 WO2011130146A1 (en) | 2010-04-14 | 2011-04-11 | 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2012148246A true RU2012148246A (ru) | 2014-05-20 |
Family
ID=43984073
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012148246/04A RU2012148246A (ru) | 2010-04-14 | 2011-04-11 | 5, 7- замещенные-имидазо[1, 2-с]пиримидины как ингибиторы jak-киназ |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8962596B2 (enExample) |
| EP (1) | EP2558468B1 (enExample) |
| JP (2) | JP2013523884A (enExample) |
| KR (1) | KR20130094710A (enExample) |
| CN (1) | CN102985424B (enExample) |
| AR (1) | AR081075A1 (enExample) |
| AU (1) | AU2011240808B2 (enExample) |
| CA (1) | CA2796388A1 (enExample) |
| CL (1) | CL2012002882A1 (enExample) |
| CO (1) | CO6630187A2 (enExample) |
| CR (1) | CR20120572A (enExample) |
| MX (1) | MX2012011941A (enExample) |
| NZ (1) | NZ603446A (enExample) |
| PH (1) | PH12012502046A1 (enExample) |
| RU (1) | RU2012148246A (enExample) |
| SG (1) | SG184870A1 (enExample) |
| TW (1) | TWI494314B (enExample) |
| UA (1) | UA109131C2 (enExample) |
| UY (1) | UY33328A (enExample) |
| WO (1) | WO2011130146A1 (enExample) |
| ZA (1) | ZA201208544B (enExample) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1966202E (pt) | 2005-12-13 | 2012-01-03 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
| RS53245B2 (sr) | 2007-06-13 | 2022-10-31 | Incyte Holdings Corp | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila |
| TW201100429A (en) | 2009-05-22 | 2011-01-01 | 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 |
| PL2432472T3 (pl) | 2009-05-22 | 2020-03-31 | Incyte Holdings Corporation | 3-[4-(7H-Pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo]oktano- lub heptano-nitryle jako inhibitory JAK |
| KR101903354B1 (ko) | 2009-06-17 | 2018-10-04 | 버텍스 파마슈티칼스 인코포레이티드 | 인플루엔자 바이러스 복제의 억제제 |
| 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 |
| MX354212B (es) | 2010-03-10 | 2018-02-19 | Incyte Corp | Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1). |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| EP2651940A1 (en) | 2010-12-16 | 2013-10-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| 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 |
| BR112014008865A2 (pt) * | 2011-10-12 | 2017-04-25 | Array Biopharma Inc | imidazo[1,2-c]pirimidinas 5,7-substituídas |
| MX2014005565A (es) * | 2011-11-07 | 2014-05-30 | Vertex Pharma | Metodos para tratar enfermedades inflamatorias y composiciones farmaceuticas utiles para los mismos. |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| JP6196678B2 (ja) | 2012-10-24 | 2017-09-13 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｃ型肝炎ウイルス阻害剤 |
| NZ708157A (en) | 2012-11-15 | 2019-07-26 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| US20160123982A1 (en) | 2013-02-04 | 2016-05-05 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for assaying jak2 activity in red blood cells and uses thereof |
| TWI634121B (zh) * | 2013-03-06 | 2018-09-01 | 英塞特控股公司 | 用於製備ｊａｋ抑制劑之方法及中間物 |
| WO2014146249A1 (en) | 2013-03-19 | 2014-09-25 | Merck Sharp & Dohme Corp. | Geminally substituted cyanoethylpyrazolo pyridones as janus kinase inhibitors |
| EA201591881A1 (ru) * | 2013-03-28 | 2016-04-29 | Такеда Фармасьютикал Компани Лимитед | Гетероциклическое соединение |
| WO2014172639A1 (en) * | 2013-04-19 | 2014-10-23 | Ruga Corporation | Raf kinase inhibitors |
| WO2014186706A1 (en) * | 2013-05-17 | 2014-11-20 | Incyte Corporation | Bipyrazole derivatives as jak inhibitors |
| MX394928B (es) | 2013-08-07 | 2025-03-24 | Incyte Holdings Corp | Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1). |
| DK3068776T3 (da) | 2013-11-13 | 2019-07-29 | Vertex Pharma | Inhibitorer af replikation af influenzavira |
| ES2684755T3 (es) | 2013-11-13 | 2018-10-04 | Vertex Pharmaceuticals Incorporated | Métodos para preparar inhibidores de la replicación de virus de la gripe |
| US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
| US10155727B2 (en) | 2014-08-15 | 2018-12-18 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| HUE054371T2 (hu) * | 2014-12-05 | 2021-09-28 | Array Biopharma Inc | 4,6-szubsztituált pirazolo[l,5-A]pirazinok mint janus kináz inhibitorok |
| CN105777754B (zh) * | 2014-12-16 | 2019-07-26 | 北京赛林泰医药技术有限公司 | 吡咯并嘧啶化合物 |
| HUE064003T2 (hu) | 2015-01-20 | 2024-02-28 | Wuxi Fortune Pharmaceutical Co Ltd | JAK-gátló |
| JP6600365B2 (ja) | 2015-04-29 | 2019-10-30 | 无▲錫▼福祈制▲薬▼有限公司 | Ｊａｋ阻害剤 |
| WO2016183116A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
| WO2016183120A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| UA118822C2 (uk) | 2015-05-29 | 2019-03-11 | Вуксі Фортуне Фармасьютікал Ко., Лтд | Інгібітор янус-кінази |
| AR104918A1 (es) * | 2015-06-19 | 2017-08-23 | Lilly Co Eli | Procesos e intermediarios para la preparación de {1-(etilsulfonil)-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrilo |
| CN105294699B (zh) * | 2015-12-04 | 2019-06-11 | 上海勋和医药科技有限公司 | 巴瑞替尼的制备方法 |
| JP6770580B2 (ja) * | 2016-01-26 | 2020-10-14 | 杭州華東医薬集団生物医薬有限公司Ｈａｎｇｚｈｏｕ Ｈｕａｄｏｎｇ Ｍｅｄｉｃｉｎｅ Ｇｒｏｕｐ Ｂｉｏｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏ．， Ｌｔｄ． | ピロロピリミジン５員環アザ環状誘導体およびその利用 |
| AU2017222417B2 (en) * | 2016-02-24 | 2020-07-09 | Pfizer Inc. | Pyrazolo[1,5-a]pyrazin-4-yl derivatives as JAK-inhibitors |
| CA3055233C (en) | 2017-01-23 | 2022-08-09 | Shanghai Longwood Biopharmaceuticals Co., Ltd. | Jak kinase inhibitor and preparation method and use thereof |
| 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 |
| US20200088732A1 (en) | 2017-04-13 | 2020-03-19 | INSERM (Institut National de la Santé et de la Recherche Mèdicale) | Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma |
| EP3666770A4 (en) | 2017-08-07 | 2021-04-07 | Joint Stock Company "Biocad" | NEW HETEROCYCLIC COMPOUNDS AS CDK8 / 19 INHIBITORS |
| EP3668858A1 (en) | 2017-08-14 | 2020-06-24 | Pfizer Inc | Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives |
| AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
| WO2019152374A1 (en) | 2018-01-30 | 2019-08-08 | Incyte Corporation | Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| WO2019161098A1 (en) | 2018-02-16 | 2019-08-22 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of cytokine-related disorders |
| HUE067471T2 (hu) | 2018-03-30 | 2024-10-28 | Incyte Corp | Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával |
| JP2022503932A (ja) * | 2018-09-27 | 2022-01-12 | フォチョン・ファーマシューティカルズ・リミテッド | Ｒｅｔキナーゼ阻害剤としての置換イミダゾ［１，２－ａ］ピリジン及び［１，２，４］トリアゾロ［１，５－ａ］ピリジン化合物 |
| US11071730B2 (en) | 2018-10-31 | 2021-07-27 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| US11203591B2 (en) | 2018-10-31 | 2021-12-21 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| CN111320624B (zh) * | 2018-12-14 | 2023-05-12 | 中国医药研究开发中心有限公司 | 三唑并吡啶类和咪唑并吡啶类化合物及其制备方法和医药用途 |
| MX2021012487A (es) * | 2019-04-12 | 2021-11-12 | Primegene Beijing Co Ltd | Compuestos derivados de pirazolopirazina, composicion farmaceutica y uso de la misma. |
| WO2020237025A1 (en) | 2019-05-23 | 2020-11-26 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| CN111039963B (zh) * | 2019-12-31 | 2021-03-19 | 卓和药业集团有限公司 | Wxfl10203614水溶性类似物及其合成方法 |
| JP2023528868A (ja) | 2020-06-02 | 2023-07-06 | インサイト・コーポレイション | Ｊａｋ１阻害剤の調製プロセス |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| EP3944859A1 (en) | 2020-07-30 | 2022-02-02 | Assistance Publique Hôpitaux de Paris | Method for treating immune toxicities induced by immune checkpoint inhibitors |
| JP2023552452A (ja) | 2020-12-08 | 2023-12-15 | インサイト・コーポレイション | 白斑治療用のｊａｋ１経路阻害薬 |
| US12268667B2 (en) | 2021-05-03 | 2025-04-08 | Incyte Corporation | JAK1 pathway inhibitors for the treatment of prurigo nodularis |
| CA3237632A1 (en) * | 2021-11-12 | 2023-05-19 | Changqing WEI | Pyrazolo fused ring compound and use thereof |
| CA3250151A1 (en) * | 2022-04-25 | 2023-11-02 | Eli Lilly And Company | FGFR2 INHIBITOR COMPOUNDS |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5728536A (en) | 1993-07-29 | 1998-03-17 | St. Jude Children's Research Hospital | Jak kinases and regulation of Cytokine signal transduction |
| EP1105378B1 (en) | 1998-08-21 | 2005-03-30 | Parker Hughes Institute | Quinazoline derivatives |
| JP2001302667A (ja) * | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
| US7713973B2 (en) * | 2004-10-15 | 2010-05-11 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| PT1966202E (pt) * | 2005-12-13 | 2012-01-03 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
| EP2497470B8 (en) | 2006-11-22 | 2015-12-02 | Incyte Holdings Corporation | Imidazotriazines and imidazopyrimidines as kinase inhibitors |
| DE102007012645A1 (de) * | 2007-03-16 | 2008-09-18 | Bayer Healthcare Ag | Substituierte Imidazo- und Triazolopyrimidine |
| 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. |
| BRPI0909040B8 (pt) | 2008-03-11 | 2021-05-25 | Incyte Holdings Corp | derivados de azetidina e ciclobutano, seus usos, e composição |
| JOP20190231A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
-
2011
- 2011-04-11 UA UAA201212901A patent/UA109131C2/ru unknown
- 2011-04-11 PH PH1/2012/502046A patent/PH12012502046A1/en unknown
- 2011-04-11 CN CN201180029128.5A patent/CN102985424B/zh not_active Expired - Fee Related
- 2011-04-11 AU AU2011240808A patent/AU2011240808B2/en not_active Ceased
- 2011-04-11 MX MX2012011941A patent/MX2012011941A/es active IP Right Grant
- 2011-04-11 WO PCT/US2011/031896 patent/WO2011130146A1/en not_active Ceased
- 2011-04-11 RU RU2012148246/04A patent/RU2012148246A/ru not_active Application Discontinuation
- 2011-04-11 JP JP2013504972A patent/JP2013523884A/ja not_active Ceased
- 2011-04-11 KR KR1020127029826A patent/KR20130094710A/ko not_active Withdrawn
- 2011-04-11 CA CA2796388A patent/CA2796388A1/en not_active Abandoned
- 2011-04-11 US US13/640,099 patent/US8962596B2/en not_active Expired - Fee Related
- 2011-04-11 NZ NZ603446A patent/NZ603446A/en not_active IP Right Cessation
- 2011-04-11 SG SG2012076493A patent/SG184870A1/en unknown
- 2011-04-11 EP EP11715818.8A patent/EP2558468B1/en active Active
- 2011-04-13 AR ARP110101268A patent/AR081075A1/es not_active Application Discontinuation
- 2011-04-13 UY UY0001033328A patent/UY33328A/es not_active Application Discontinuation
- 2011-04-14 TW TW100113047A patent/TWI494314B/zh not_active IP Right Cessation
-
2012
- 2012-10-12 CL CL2012002882A patent/CL2012002882A1/es unknown
- 2012-11-09 CR CR20120572A patent/CR20120572A/es unknown
- 2012-11-13 ZA ZA2012/08544A patent/ZA201208544B/en unknown
- 2012-11-13 CO CO12203751A patent/CO6630187A2/es active IP Right Grant
-
2015
- 2015-06-26 JP JP2015128369A patent/JP2015205905A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| JP2013523884A (ja) | 2013-06-17 |
| ZA201208544B (en) | 2015-04-29 |
| CA2796388A1 (en) | 2011-10-20 |
| US20130131039A1 (en) | 2013-05-23 |
| CO6630187A2 (es) | 2013-03-01 |
| SG184870A1 (en) | 2012-11-29 |
| WO2011130146A1 (en) | 2011-10-20 |
| NZ603446A (en) | 2014-05-30 |
| TWI494314B (zh) | 2015-08-01 |
| UY33328A (es) | 2012-10-31 |
| EP2558468B1 (en) | 2015-04-01 |
| TW201134827A (en) | 2011-10-16 |
| AU2011240808B2 (en) | 2015-01-22 |
| CN102985424A (zh) | 2013-03-20 |
| CN102985424B (zh) | 2015-03-11 |
| CL2012002882A1 (es) | 2013-02-08 |
| PH12012502046A1 (en) | 2017-07-26 |
| UA109131C2 (ru) | 2015-07-27 |
| JP2015205905A (ja) | 2015-11-19 |
| AR081075A1 (es) | 2012-06-06 |
| KR20130094710A (ko) | 2013-08-26 |
| MX2012011941A (es) | 2013-08-27 |
| US8962596B2 (en) | 2015-02-24 |
| AU2011240808A1 (en) | 2012-11-29 |
| EP2558468A1 (en) | 2013-02-20 |
| CR20120572A (es) | 2013-02-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2012148246A (ru) | 5, 7- замещенные-имидазо[1, 2-с]пиримидины как ингибиторы jak-киназ | |
| AU2019283921B2 (en) | Indole carboxamide compounds useful as kinase inhibitors | |
| KR102702236B1 (ko) | Ror 감마 조절제로서의 치환된 테트라하이드로퀴놀리논 화합물 | |
| JP2022506887A (ja) | 窒素含有縮合複素環系ｓｈｐ２阻害剤化合物、製造方法及び使用 | |
| JP2009524670A5 (enExample) | ||
| JP2013523884A5 (enExample) | ||
| CN102388055B (zh) | 咪唑并[2,1-b][1,3,4]噻二唑衍生物 | |
| RU2012119488A (ru) | Конденсированные азиновые производные для лечения заболеваний, связанных с ацетилхолиновым рецептором | |
| ES2781867T3 (es) | 4-Azaindoles sustituidos y su utilización como moduladores del receptor GluN2B | |
| CN105308036A (zh) | 用于激酶调节的化合物和方法及其适应症 | |
| KR102556742B1 (ko) | 키나제 억제제로서의 헤테로아릴 화합물 | |
| RU2014118954A (ru) | 5,7-ЗАМЕЩЕННЫЕ-ИМИДАЗО[1,2-c]ПИРИМИДИНЫ | |
| JP2023525126A (ja) | イミダゾール３－オキシド誘導体系ａｃｓｓ２阻害剤及びその使用方法 | |
| KR20180052702A (ko) | Perk 억제제로서의 1-페닐피롤리딘-2-온 유도체 | |
| JP7627008B2 (ja) | ピロール化合物 | |
| JP2018521119A5 (enExample) | ||
| TW202115054A (zh) | 經取代的雜芳族吡唑并－吡啶及其作為ｇｌｕｎ２ｂ受體調節劑的用途 | |
| JP2024505732A (ja) | ピリドピリミジノン系誘導体及びその製造方法と使用 | |
| JP2025534917A (ja) | Ｎｌｒｐ３インフラマソーム阻害剤及びその応用 | |
| JP2010502576A5 (enExample) | ||
| BR112016007563A2 (pt) | tiazolopirimidinonas como moduladores de atividade de nmda | |
| BR112021005960A2 (pt) | composto, método de fabricação do mesmo, uso do mesmo, composição farmacêutica e formulação farmacêutica | |
| JP2022539208A (ja) | チロシンキナーゼ非受容体１（ｔｎｋ１）阻害剤およびその使用 | |
| WO2023150681A1 (en) | Inhibitors of raf kinases | |
| JP2022534501A (ja) | 三環式化合物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20150818 |