JP5574957B2 - Janusキナーゼのチロシンキナーゼ活性の阻害剤としてのキノキサリン誘導体 - Google Patents
Janusキナーゼのチロシンキナーゼ活性の阻害剤としてのキノキサリン誘導体 Download PDFInfo
- Publication number
- JP5574957B2 JP5574957B2 JP2010510815A JP2010510815A JP5574957B2 JP 5574957 B2 JP5574957 B2 JP 5574957B2 JP 2010510815 A JP2010510815 A JP 2010510815A JP 2010510815 A JP2010510815 A JP 2010510815A JP 5574957 B2 JP5574957 B2 JP 5574957B2
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- morpholin
- ylmethyl
- methyl
- quinoxalin
- 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.)
- Expired - Fee Related
Links
- 0 C*(CC1)CC*1C(c1c(C)cc(C(F)(F)F)cc1)O Chemical compound C*(CC1)CC*1C(c1c(C)cc(C(F)(F)F)cc1)O 0.000 description 16
- MFCLMHMMNCWEOW-UHFFFAOYSA-N CC(C)(c(cc1)c(C)cc1S1OC(C)(C)C(C)(C)O1)N(CC1)CCS1(=O)=O Chemical compound CC(C)(c(cc1)c(C)cc1S1OC(C)(C)C(C)(C)O1)N(CC1)CCS1(=O)=O MFCLMHMMNCWEOW-UHFFFAOYSA-N 0.000 description 1
- SFNGVDUQTBKPDC-UHFFFAOYSA-N CC(C1)=C(CBr)C=CC1Br Chemical compound CC(C1)=C(CBr)C=CC1Br SFNGVDUQTBKPDC-UHFFFAOYSA-N 0.000 description 1
- OIJJJRHYCBDGKY-UHFFFAOYSA-N CC(CN(CC1)CCC1[n]1ncc(Br)c1)=O Chemical compound CC(CN(CC1)CCC1[n]1ncc(Br)c1)=O OIJJJRHYCBDGKY-UHFFFAOYSA-N 0.000 description 1
- CFMOXIOBLDZPCO-UHFFFAOYSA-N CC1(C)OB(c(cc2OC)ccc2OCCOC)OC1(C)C Chemical compound CC1(C)OB(c(cc2OC)ccc2OCCOC)OC1(C)C CFMOXIOBLDZPCO-UHFFFAOYSA-N 0.000 description 1
- QINFDPZSZHPUSC-UHFFFAOYSA-N CC1(C)OB(c2cc(F)c(CN3CCOCC3)cc2)OC1(C)C Chemical compound CC1(C)OB(c2cc(F)c(CN3CCOCC3)cc2)OC1(C)C QINFDPZSZHPUSC-UHFFFAOYSA-N 0.000 description 1
- XUHWXYCIGAKTMU-UHFFFAOYSA-N CC1(C)OS(c(cc2)cc(C)c2C(N2CCOCC2)=O)OC1(C)C Chemical compound CC1(C)OS(c(cc2)cc(C)c2C(N2CCOCC2)=O)OC1(C)C XUHWXYCIGAKTMU-UHFFFAOYSA-N 0.000 description 1
- DXBCHDBTNAFFQQ-UHFFFAOYSA-N CCOC(CNc1ccccc1[N+]([O-2])=O)=O Chemical compound CCOC(CNc1ccccc1[N+]([O-2])=O)=O DXBCHDBTNAFFQQ-UHFFFAOYSA-N 0.000 description 1
- WQMSTZPVPAGCMV-UHFFFAOYSA-N CN(C)CCN(C)C(c(cc1)ncc1Br)=O Chemical compound CN(C)CCN(C)C(c(cc1)ncc1Br)=O WQMSTZPVPAGCMV-UHFFFAOYSA-N 0.000 description 1
- JNCINWSVQSYQNG-UHFFFAOYSA-N CNS(c(cc1)ccc1-c1c2nc(C(CC(OC)=C3OC)C=C3OC)cnc2ccc1)(=O)=O Chemical compound CNS(c(cc1)ccc1-c1c2nc(C(CC(OC)=C3OC)C=C3OC)cnc2ccc1)(=O)=O JNCINWSVQSYQNG-UHFFFAOYSA-N 0.000 description 1
- SHEFFLURGBYZLS-UHFFFAOYSA-N COCCOc(ccc(-c1nc(c(-c2ccc(CN(CC3)CCS3(=O)=O)c(F)c2)ccc2)c2nc1)c1)c1OC Chemical compound COCCOc(ccc(-c1nc(c(-c2ccc(CN(CC3)CCS3(=O)=O)c(F)c2)ccc2)c2nc1)c1)c1OC SHEFFLURGBYZLS-UHFFFAOYSA-N 0.000 description 1
- PWKQJLSDOPXYQW-UHFFFAOYSA-N CS(C(C(C1)F)=CC=C1Br)(=O)=O Chemical compound CS(C(C(C1)F)=CC=C1Br)(=O)=O PWKQJLSDOPXYQW-UHFFFAOYSA-N 0.000 description 1
- CHTJETYJVFKELN-UHFFFAOYSA-N O=C1NCCN(Cc(c(F)cc(-c2cccc(nc3)c2nc3-c2c[n](C3CCOCC3)nc2)c2)c2F)C1 Chemical compound O=C1NCCN(Cc(c(F)cc(-c2cccc(nc3)c2nc3-c2c[n](C3CCOCC3)nc2)c2)c2F)C1 CHTJETYJVFKELN-UHFFFAOYSA-N 0.000 description 1
Classifications
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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
- A61K31/495—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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P35/00—Antineoplastic agents
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- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
- C07D241/40—Benzopyrazines
- C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D401/10—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 carbon chain containing aromatic rings
-
- 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
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07109880.0 | 2007-06-08 | ||
| EP07109880 | 2007-06-08 | ||
| EP07150266 | 2007-12-20 | ||
| EP07150266.0 | 2007-12-20 | ||
| PCT/EP2008/057058 WO2008148867A2 (en) | 2007-06-08 | 2008-06-06 | Quinoxaline derivatives as inhibitors of the tyrosine kinase activity of janus kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529088A JP2010529088A (ja) | 2010-08-26 |
| JP2010529088A5 JP2010529088A5 (enExample) | 2012-07-05 |
| JP5574957B2 true JP5574957B2 (ja) | 2014-08-20 |
Family
ID=39720643
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010510815A Expired - Fee Related JP5574957B2 (ja) | 2007-06-08 | 2008-06-06 | Janusキナーゼのチロシンキナーゼ活性の阻害剤としてのキノキサリン誘導体 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8193189B2 (enExample) |
| EP (1) | EP2155201B1 (enExample) |
| JP (1) | JP5574957B2 (enExample) |
| KR (1) | KR20100020465A (enExample) |
| CN (1) | CN101678020B (enExample) |
| AR (1) | AR066879A1 (enExample) |
| AU (1) | AU2008258486B2 (enExample) |
| BR (1) | BRPI0812893A2 (enExample) |
| CA (1) | CA2690288A1 (enExample) |
| CL (1) | CL2008001659A1 (enExample) |
| EA (1) | EA200901608A1 (enExample) |
| ES (1) | ES2392570T3 (enExample) |
| MX (1) | MX2009013218A (enExample) |
| PA (1) | PA8783501A1 (enExample) |
| TW (1) | TW200904814A (enExample) |
| UY (1) | UY31126A1 (enExample) |
| WO (1) | WO2008148867A2 (enExample) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102015710B (zh) | 2008-02-20 | 2013-04-24 | 埃科特莱茵药品有限公司 | 氮杂三环抗菌化合物 |
| EP2282995B1 (en) * | 2008-05-23 | 2015-08-26 | Novartis AG | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| US20110130384A1 (en) * | 2008-06-25 | 2011-06-02 | Takeda Pharmaceutical Company Limited | Amide compound |
| WO2010041194A1 (en) | 2008-10-07 | 2010-04-15 | Actelion Pharmaceuticals Ltd | Tricyclic oxazolidinone antibiotic compounds |
| CA2752150A1 (en) * | 2009-02-11 | 2010-08-19 | Reaction Biology Corp. | Selective kinase inhibitors |
| US20140128392A1 (en) | 2009-03-19 | 2014-05-08 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| AU2010289397B2 (en) * | 2009-09-03 | 2016-05-26 | Bioenergenix | Heterocyclic compounds for the inhibition of PASK |
| KR101461767B1 (ko) | 2010-03-30 | 2014-11-13 | 노파르티스 아게 | 만성 활성 b-세포-수용체 신호전달이 있는 b-세포 림프종의 치료를 위한 pkc 억제제 |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| EP2661431B1 (en) * | 2011-01-05 | 2018-07-11 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| US8263298B1 (en) | 2011-02-24 | 2012-09-11 | Xerox Corporation | Electrically tunable and stable imaging members |
| WO2013018733A1 (ja) | 2011-07-29 | 2013-02-07 | 富士フイルム株式会社 | 1,5-ナフチリジン誘導体又はその塩 |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| US20140343128A1 (en) | 2011-11-15 | 2014-11-20 | Novartis Ag | Combination of a phosphoinositide 3-kinase inhibitor and a modulator of the Janus Kinase 2 - Signal Transducer and Activator of Transcription 5 pathway |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| ES2625744T3 (es) | 2013-06-04 | 2017-07-20 | Bayer Pharma Aktiengesellschaft | Imidazo[1,2-a]piridinas sustituidas con 3-arilo y su uso |
| WO2015059088A1 (de) | 2013-10-23 | 2015-04-30 | Bayer Cropscience Ag | Substituierte chinoxalin-derivate als schädlingsbekämpfungsmittel |
| JP2017507140A (ja) | 2014-02-19 | 2017-03-16 | バイエル・ファルマ・アクティエンゲゼルシャフト | 3−(ピリミジン−2−イル)イミダゾ[1,2−a]ピリジン |
| EP3122358B1 (en) | 2014-03-26 | 2020-12-16 | Astex Therapeutics Ltd. | Combinations of fgfr- and cmet-inhibitors for the treatment of cancer |
| BR112016022062B1 (pt) | 2014-03-26 | 2023-04-11 | Astex Therapeutics Limited | Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| US10292970B2 (en) | 2014-12-02 | 2019-05-21 | Bayer Pharma Aktiengesellschaft | Heteroaryl-substituted imidazo[1,2-A]pyridines and their use |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| US10517870B2 (en) | 2015-07-30 | 2019-12-31 | Bristol-Myers Squibb Company | Aryl substituted bicycle heteroaryl compounds |
| US11155555B2 (en) | 2015-09-23 | 2021-10-26 | Janssen Pharmaceutica Nv | Compounds |
| HRP20220012T1 (hr) | 2015-09-23 | 2022-04-01 | Janssen Pharmaceutica Nv | Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka |
| CN108472298B (zh) | 2015-11-24 | 2021-04-20 | 深圳阿拉丁医疗科技有限公司 | 选择性激酶抑制剂 |
| HUE049305T2 (hu) * | 2016-02-24 | 2020-09-28 | Pfizer | Pirazolo[1,5-a]pirazin-4-il származékok mint JAK-inhibitorok |
| WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
| JP7503850B2 (ja) | 2018-10-10 | 2024-06-21 | アルベルト・アインシュタイン・カレッジ・オブ・メディシン | シャペロン介在性オートファジー調節剤として有用なベンゾオキサゾールおよび関連化合物 |
| WO2020200291A1 (en) * | 2019-04-02 | 2020-10-08 | Cullgen (Shanghai) , Inc. | Compounds and methods of treating cancers |
| WO2020201362A2 (en) | 2019-04-02 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| WO2020212395A1 (en) | 2019-04-16 | 2020-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
| TWI865563B (zh) | 2019-07-30 | 2024-12-11 | 德商拜耳動物保健有限公司 | 新穎異喹啉衍生物 |
| CN110698418B (zh) * | 2019-09-11 | 2022-07-01 | 广西师范大学 | 一种3-芳胺基喹喔啉-2-甲酰胺类衍生物及其制备方法和应用 |
| 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 |
| CN110981819B (zh) * | 2019-12-24 | 2022-07-01 | 广西师范大学 | 一种喹喔啉类信号通路抑制剂及其制备方法和应用 |
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| US20250283174A1 (en) | 2022-05-16 | 2025-09-11 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation |
| CN115385863A (zh) * | 2022-08-17 | 2022-11-25 | 河南师范大学 | 一种3-(二乙氧基甲基)-1-烷基-2(1h)-喹喔啉酮衍生物的合成方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4321030A1 (de) * | 1993-06-24 | 1995-01-05 | Bayer Ag | 4-bicyclisch substituierte Dihydropyridine, Verfahren zu ihrer Herstellung und ihre Verwendung in Arzneimittel |
| SE9800836D0 (sv) | 1998-03-13 | 1998-03-13 | Astra Ab | New Compounds |
| WO2002083138A1 (en) * | 2001-04-10 | 2002-10-24 | Merck & Co., Inc. | Inhibitors of akt activity |
| CN1902193B (zh) | 2003-12-04 | 2011-07-13 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的喹喔啉 |
| WO2007044729A2 (en) * | 2005-10-07 | 2007-04-19 | Exelixis, Inc. | N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors |
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| CA2690288A1 (en) | 2008-12-11 |
| CL2008001659A1 (es) | 2009-02-20 |
| EA200901608A1 (ru) | 2010-06-30 |
| AR066879A1 (es) | 2009-09-16 |
| CN101678020B (zh) | 2012-08-15 |
| EP2155201B1 (en) | 2012-08-01 |
| ES2392570T3 (es) | 2012-12-11 |
| JP2010529088A (ja) | 2010-08-26 |
| US20100168062A1 (en) | 2010-07-01 |
| MX2009013218A (es) | 2010-01-15 |
| PA8783501A1 (es) | 2009-01-23 |
| AU2008258486B2 (en) | 2011-11-10 |
| WO2008148867A3 (en) | 2009-04-09 |
| UY31126A1 (es) | 2009-01-30 |
| BRPI0812893A2 (pt) | 2014-12-09 |
| CN101678020A (zh) | 2010-03-24 |
| WO2008148867A2 (en) | 2008-12-11 |
| AU2008258486A1 (en) | 2008-12-11 |
| EP2155201A2 (en) | 2010-02-24 |
| KR20100020465A (ko) | 2010-02-22 |
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