SG10201603095TA - SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS - Google Patents
SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORSInfo
- Publication number
- SG10201603095TA SG10201603095TA SG10201603095TA SG10201603095TA SG10201603095TA SG 10201603095T A SG10201603095T A SG 10201603095TA SG 10201603095T A SG10201603095T A SG 10201603095TA SG 10201603095T A SG10201603095T A SG 10201603095TA SG 10201603095T A SG10201603095T A SG 10201603095TA
- Authority
- SG
- Singapore
- Prior art keywords
- kinase inhibitors
- pyrimidine compounds
- substituted pyrazolo
- trk kinase
- trk
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
- C07D453/04—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems having a quinolyl-4, a substituted quinolyl-4 or a alkylenedioxy-quinolyl-4 radical linked through only one carbon atom, attached in position 2, e.g. quinine
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- 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
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- 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
- C07D471/22—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 systems contains four or more hetero rings
-
- 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
- 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
- C07D498/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22419609P | 2009-07-09 | 2009-07-09 | |
US34676710P | 2010-05-20 | 2010-05-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
SG10201603095TA true SG10201603095TA (en) | 2016-05-30 |
Family
ID=42732102
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG10201603095TA SG10201603095TA (en) | 2009-07-09 | 2010-07-09 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS |
SG2012001178A SG177553A1 (en) | 2009-07-09 | 2010-07-09 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SG2012001178A SG177553A1 (en) | 2009-07-09 | 2010-07-09 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS |
Country Status (22)
Country | Link |
---|---|
US (6) | US8791123B2 (en) |
EP (2) | EP3299372B1 (en) |
JP (3) | JP5716021B2 (en) |
KR (3) | KR101997055B1 (en) |
CN (3) | CN110003214B (en) |
AR (1) | AR077468A1 (en) |
AU (1) | AU2010271270C1 (en) |
CA (2) | CA3013618C (en) |
CL (1) | CL2012000059A1 (en) |
CO (1) | CO6612183A2 (en) |
CR (2) | CR20120065A (en) |
ES (2) | ES2774654T3 (en) |
IL (1) | IL217414A (en) |
MX (2) | MX2012000513A (en) |
MY (1) | MY162180A (en) |
NZ (1) | NZ598086A (en) |
RU (2) | RU2016114128A (en) |
SG (2) | SG10201603095TA (en) |
TW (1) | TWI503321B (en) |
UY (1) | UY32782A (en) |
WO (1) | WO2011006074A1 (en) |
ZA (1) | ZA201200982B (en) |
Families Citing this family (131)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL2350075T3 (en) | 2008-09-22 | 2014-07-31 | Array Biopharma Inc | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
US8513263B2 (en) | 2008-10-22 | 2013-08-20 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors |
PE20131197A1 (en) * | 2008-10-31 | 2013-11-06 | Genentech Inc | PYRAZOLOPYRIMIDINE COMPOUNDS AS JAK INHIBITORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
CN102300862B (en) | 2008-12-19 | 2016-11-23 | 沃泰克斯药物股份有限公司 | Compound as ATR inhibitors of kinases |
UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
AR077468A1 (en) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS |
MY191934A (en) | 2010-05-20 | 2022-07-19 | Array Biopharma Inc | Macrocyclic compounds as trk kinase inhibitors |
WO2012034095A1 (en) * | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
UY33597A (en) | 2010-09-09 | 2012-04-30 | Irm Llc | COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF THE TRK |
AP2013007103A0 (en) * | 2011-02-25 | 2013-09-30 | Irm Llc | Compounds and compositions as TRK inhibitors |
CA2835835C (en) | 2011-05-13 | 2019-04-02 | Array Biopharma Inc. | Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors |
RU2018108589A (en) | 2011-09-30 | 2019-02-25 | Вертекс Фармасьютикалз Инкорпорейтед | TREATMENT OF Pancreatic cancer and non-small cell lung cancer with ATR inhibitors |
CN106496173A (en) | 2011-09-30 | 2017-03-15 | 沃泰克斯药物股份有限公司 | Method for preparing the compound that can be used as ATR kinase inhibitors |
BR112014022000A8 (en) * | 2012-03-09 | 2021-06-15 | Lexicon Pharmaceuticals Inc | pyrazol[1,5-a]pyrimidine-based compounds, their use and compositions comprising them |
PT2833973T (en) | 2012-04-05 | 2017-12-21 | Vertex Pharma | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
DK3459942T3 (en) | 2012-04-24 | 2021-03-08 | Vertex Pharma | DNA-PK inhibitors |
JOP20130273B1 (en) * | 2012-09-11 | 2021-08-17 | Genzyme Corp | Glucosylceramide synthase inhibitors |
RU2677667C2 (en) * | 2012-11-13 | 2019-01-18 | Эррэй Биофарма Инк. | N-pyrrolidinyl-urea, n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
KR102181913B1 (en) * | 2012-11-13 | 2020-11-23 | 어레이 바이오파마 인크. | Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain |
WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
US9790210B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078408A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078417A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078372A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
US9969694B2 (en) | 2012-11-13 | 2018-05-15 | Array Biopharma Inc. | N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
HUE061909T2 (en) | 2012-12-07 | 2023-08-28 | Vertex Pharma | Pyrazolo[1,5-a]pyrimidines useful as inhibitors of atr kinase for the treatment of cancer diseases |
BR122017003181A2 (en) * | 2013-02-19 | 2019-09-10 | Ono Pharmaceutical Co | trk inhibitor compound, pharmaceutical composition and medicament comprising said compound and its use for prophylaxis and / or therapy of trk related disease and / or for inhibiting trk |
PL2989106T3 (en) | 2013-04-25 | 2017-08-31 | Beigene, Ltd. | Fused heterocyclic compounds as protein kinase inhibitors |
EP3628749A1 (en) | 2013-07-30 | 2020-04-01 | Blueprint Medicines Corporation | Ntrk2 fusions |
TW201542550A (en) * | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them, and methods of their use |
KR102100419B1 (en) | 2013-09-13 | 2020-04-14 | 베이진 스위찰랜드 게엠베하 | Anti-PD1 Antibodies and their Use as Therapeutics and Diagnostics |
LT3424920T (en) | 2013-10-17 | 2020-08-10 | Vertex Pharmaceuticals Incorporated | Co-crystals of (s)-n-methyl-8-(1-((2`-methyl-[4,5`-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors |
US9067914B1 (en) * | 2013-12-10 | 2015-06-30 | Genzyme Corporation | Tropomyosin-related kinase (TRK) inhibitors |
WO2015104602A2 (en) | 2014-01-08 | 2015-07-16 | Wockhardt Limited | A process for the preparation of anagliptin and its intermediates thereof |
HRP20221518T1 (en) | 2014-01-24 | 2023-02-17 | Turning Point Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
IN2014MU01191A (en) | 2014-03-29 | 2015-10-02 | Wockhardt Ltd | |
RS59286B1 (en) | 2014-05-15 | 2019-10-31 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor |
SG11201609830RA (en) | 2014-05-23 | 2016-12-29 | Hoffmann La Roche | 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds which are jak inhibitors |
PT3149001T (en) | 2014-05-28 | 2019-07-25 | Novartis Ag | Novel pyrazolo pyrimidine derivatives and their use as malt1 inhibitors |
WO2015187451A1 (en) | 2014-06-05 | 2015-12-10 | Vertex Pharmacetucals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
EP3157566B1 (en) | 2014-06-17 | 2019-05-01 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of chk1 and atr inhibitors |
CN106604742B (en) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | Anti- PD-L1 antibody and its purposes as therapeutic agent and diagnosticum |
HUE045237T2 (en) * | 2014-08-18 | 2019-12-30 | Ono Pharmaceutical Co | Acid-addition salt of trk-inhibiting compound |
AU2015316799B2 (en) * | 2014-09-17 | 2019-07-11 | Oncodesign Precision Medicine (OPM) | Macrocyclic RIP2 kinase inhibitors |
US10570135B2 (en) | 2014-11-06 | 2020-02-25 | Lysosomal Therapeutics Inc. | Substituted pyrazolo[1,5-A]pyrimidines and their use in the treatment of medical disorders |
AU2015346046B2 (en) | 2014-11-16 | 2020-06-25 | Array Biopharma, Inc. | Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
AU2015365587B2 (en) * | 2014-12-15 | 2020-07-23 | Cmg Pharmaceutical Co., Ltd. | Fused ring heteroaryl compounds and their use as TRK inhibitors |
CA2988423A1 (en) | 2015-06-01 | 2016-12-08 | Loxo Oncology, Inc. | Methods of diagnosing and treating cancer |
JP6871903B2 (en) | 2015-07-02 | 2021-05-19 | ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics,Inc. | Chiral diallyl macrocyclic molecule as a modulator of protein kinase |
DK3322706T3 (en) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | SUBSTITUTED PYRAZOLO [1,5-A] PYRIDINE COMPOUNDS AS RIGHT CHINESE INHIBITORS |
MX2018000718A (en) | 2015-07-21 | 2020-01-20 | Turning Point Therapeutics Inc | Chiral diaryl macrocycles and uses thereof. |
CN108137607B (en) | 2015-08-26 | 2021-04-06 | 缆图药品公司 | Compounds and compositions suitable for treating NTRK-related disorders |
WO2017059357A1 (en) | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna damaging agents and atr inhibitors |
AU2016344058A1 (en) | 2015-10-26 | 2018-05-17 | Array Biopharma Inc. | Point mutations in Trk inhibitor-resistant cancer and methods relating to the same |
WO2017073706A1 (en) * | 2015-10-30 | 2017-05-04 | 中外製薬株式会社 | DIHYDRONAPHTHO[2,3-b]BENZOFURAN DERIVATIVE |
US10370379B2 (en) * | 2015-11-19 | 2019-08-06 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to NTRK |
WO2017176744A1 (en) | 2016-04-04 | 2017-10-12 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
CA3019671C (en) | 2016-04-04 | 2024-02-20 | Loxo Oncology, Inc. | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
CN109311887B (en) | 2016-04-06 | 2022-09-13 | Bial研发投资股份有限公司 | Pyrazolo [1,5-a ] pyrimidinecarboxamide compounds and their use in the treatment of medical conditions |
JP7046827B2 (en) | 2016-04-06 | 2022-04-04 | リソソーマル・セラピューティクス・インコーポレイテッド | Imidazo [1,5-a] pyrimidinylcarboxamide compounds and their use in the treatment of medical disorders |
CA3020310A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
WO2017192930A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
KR102566858B1 (en) | 2016-05-18 | 2023-08-11 | 어레이 바이오파마 인크. | (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl Method for producing )-3-hydroxypyrrolidine-1-carboxamide |
WO2018007885A1 (en) | 2016-07-05 | 2018-01-11 | Beigene, Ltd. | COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER |
CN116478166A (en) | 2016-08-16 | 2023-07-25 | 百济神州(苏州)生物科技有限公司 | Crystal form of compound, preparation and application thereof |
AU2017313085A1 (en) | 2016-08-19 | 2019-03-14 | Beigene Switzerland Gmbh | Use of a combination comprising a Btk inhibitor for treating cancers |
MX2019003317A (en) | 2016-09-27 | 2019-08-05 | Vertex Pharma | Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors. |
KR101881650B1 (en) * | 2016-10-02 | 2018-07-24 | 재단법인대구경북과학기술원 | A brain derived neurotrophic factor overexpressed animal model for depression disorder and a method for producing thereof |
TWI704148B (en) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
JOP20190077A1 (en) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
JOP20190092A1 (en) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF |
PL3533796T3 (en) | 2016-10-28 | 2022-01-17 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor |
CN108003161B (en) * | 2016-10-28 | 2020-10-09 | 正大天晴药业集团股份有限公司 | Neurotrophic factor tyrosine kinase receptor inhibitors |
US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
EP3573989A4 (en) | 2017-01-25 | 2020-11-18 | Beigene, Ltd. | Crystalline forms of (s) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahy dropyrazolo [1, 5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
JOP20190213A1 (en) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | Macrocyclic compounds as ros1 kinase inhibitors |
EP3630766A1 (en) | 2017-05-22 | 2020-04-08 | H. Hoffnabb-La Roche Ag | Therapeutic compounds and compositions, and methods of use thereof |
EP3645569A4 (en) | 2017-06-26 | 2021-03-24 | BeiGene, Ltd. | Immunotherapy for hepatocellular carcinoma |
CN109824566A (en) * | 2017-07-19 | 2019-05-31 | 浙江师范大学 | The synthetic method of one kind (R) -2- (2,5- difluorophenyl) pyrrolidines |
WO2019023468A1 (en) | 2017-07-28 | 2019-01-31 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
JP6916562B2 (en) * | 2017-08-11 | 2021-08-11 | テリジーン リミテッドTeligene Ltd. | Compounds, pharmaceutically acceptable salts thereof, solvates, stereoisomers and tautomers, and drug compositions, hyperproliferative disorder therapeutic agents, hyperproliferative disorder prophylaxis agents, drugs, cancer therapeutic agents, cancer Prophylactic agents and kinase signaling regulators |
WO2019034009A1 (en) | 2017-08-12 | 2019-02-21 | Beigene, Ltd. | Btk INHIBITORS WITH IMPROVED DUAL SELECTIVITY |
TWI791053B (en) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | Crystalline forms of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile and pharmaceutical composition thereof |
TWI812649B (en) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | Formulations of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile |
MA50456A (en) | 2017-10-26 | 2020-09-02 | Array Biopharma Inc | MACROCYCLIC KINASE TRK INHIBITOR FORMULATIONS |
US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
JP7061195B2 (en) | 2018-01-18 | 2022-04-27 | アレイ バイオファーマ インコーポレイテッド | Substituted pyrazolo [3,4-d] pyrimidine compound as a RET kinase inhibitor |
JP7060694B2 (en) | 2018-01-18 | 2022-04-26 | アレイ バイオファーマ インコーポレイテッド | Substituted pyrolo [2,3-D] pyrimidine compounds as RET kinase inhibitors |
EP3740486A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
CN110156813B (en) * | 2018-02-13 | 2023-07-25 | 北京诺诚健华医药科技有限公司 | Heterocyclic compounds as TRK inhibitors |
HRP20220331T1 (en) | 2018-03-08 | 2022-05-13 | Incyte Corporation | Aminopyrazine diol compounds as pi3k-y inhibitors |
MX2020009586A (en) | 2018-03-14 | 2020-10-05 | Fochon Biosciences Ltd | SUBSTITUTED (2-AZABICYCLO [3.1.0] HEXAN-2-YL) PYRAZOLO [1, 5-a] PYRIMIDINE AND IMIDAZO [1, 2-b] PYRIDAZINE COMPOUNDS AS TRK KINASES INHIBITORS. |
MA52218A (en) | 2018-03-29 | 2021-02-17 | Loxo Oncology Inc | TREATMENT OF CANCERS ASSOCIATED WITH TRK |
CN110294761B (en) * | 2018-06-08 | 2020-09-08 | 南京雷正医药科技有限公司 | Substituted pyrazolo [1,5-a ] pyrimidine compounds as Trk kinase inhibitors |
CN110627812B (en) | 2018-06-25 | 2022-10-11 | 北京诺诚健华医药科技有限公司 | Heterocyclic compounds as TRK inhibitors |
US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
EP3829543A1 (en) | 2018-07-31 | 2021-06-09 | Loxo Oncology, Inc. | Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide |
WO2020038457A1 (en) * | 2018-08-23 | 2020-02-27 | 珠海联邦制药股份有限公司 | [1,2,4]triazolo[1,5-a]pyridine compound as jak inhibitor and application thereof |
CN110857304B (en) * | 2018-08-24 | 2021-05-18 | 北京富龙康泰生物技术有限公司 | Trk inhibitor, preparation method and application thereof |
ES2922314T3 (en) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Fused Heterocyclic Compounds as RET Kinase Inhibitors |
AU2019360941A1 (en) | 2018-10-15 | 2021-04-29 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
CN111171049B (en) * | 2018-11-09 | 2021-06-04 | 山东轩竹医药科技有限公司 | Tyrosine kinase inhibitors and uses thereof |
CN111269233A (en) * | 2018-12-05 | 2020-06-12 | 上海轶诺药业有限公司 | Preparation and application of imidazo aromatic ring compounds |
AU2019394520A1 (en) * | 2018-12-07 | 2021-07-01 | Betta Pharmaceuticals Co., Ltd | Tyrosine kinase inhibitors, compositions and methods there of |
US20220081438A1 (en) | 2018-12-19 | 2022-03-17 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
US20220041579A1 (en) | 2018-12-19 | 2022-02-10 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of fgfr tyrosine kinases |
CA3127153A1 (en) | 2019-02-22 | 2020-08-27 | Regeneron Pharmaceuticals, Inc. | Rodents having genetically modified sodium channels and methods of use thereof |
CN111718351B (en) * | 2019-03-19 | 2021-10-12 | 华中师范大学 | Oxygen-containing substituted pyrazolopyrimidine compound, pharmaceutical composition and application thereof |
JP2022526713A (en) | 2019-03-21 | 2022-05-26 | オンクセオ | Dbait molecule in combination with a kinase inhibitor for the treatment of cancer |
CN111848626B (en) * | 2019-04-30 | 2021-11-30 | 江苏柯菲平医药股份有限公司 | TRK kinase inhibitor and application thereof |
CN112867717B (en) * | 2019-05-08 | 2023-01-10 | 浙江同源康医药股份有限公司 | Compounds useful as kinase inhibitors and uses thereof |
WO2021027503A1 (en) * | 2019-08-12 | 2021-02-18 | 罗欣药业(上海)有限公司 | Tricyclic compound, preparation method therefor, and intermediate and use thereof |
CN114761006A (en) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | Methods of treating cancer resistant to kinase inhibitors |
CN111138437B (en) * | 2019-12-04 | 2021-03-05 | 杭州华东医药集团新药研究院有限公司 | Substituted pyrazolo [1,5-a ] pyrimidine amino acid derivatives and uses thereof |
CN115210232B (en) * | 2020-01-22 | 2024-03-01 | 上海齐鲁制药研究中心有限公司 | Pyrazolo heteroaromatic ring compound and application thereof |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
WO2021159372A1 (en) * | 2020-02-13 | 2021-08-19 | 珠海联邦制药股份有限公司 | Use of jak inhibitors in preparation of drugs for treating jak kinase-related diseases |
CN114437077B (en) * | 2020-11-04 | 2024-01-30 | 浙江同源康医药股份有限公司 | Compounds useful as kinase inhibitors and uses thereof |
WO2021249450A1 (en) * | 2020-06-11 | 2021-12-16 | 贝达药业股份有限公司 | Salt form, crystal form, pharmaceutical composition and use of tyrosine kinase inhibitor |
CN111777549A (en) * | 2020-07-07 | 2020-10-16 | 中瀚(齐河县)生物医药科技有限公司 | Synthesis process of 2-methoxy-3-bromo-5-fluoropyridine |
BR112023000798A2 (en) | 2020-07-24 | 2023-02-07 | Genzyme Corp | PHARMACEUTICAL COMPOSITIONS COMPRISING VENGLUTAT |
CN113563343B (en) * | 2020-07-27 | 2022-05-24 | 杭州邦顺制药有限公司 | Substituted pyrazolo [1,5-a ] pyrimidine compounds and uses thereof |
CN112645955B (en) * | 2020-12-24 | 2022-11-04 | 四川国康药业有限公司 | [1,2,4] triazolo [4,3-b ] pyridazine compound and preparation method and application thereof |
US20240092759A1 (en) * | 2021-01-08 | 2024-03-21 | Yale University | Non-Covalent Inhibitors of the Main Protease of SARS-CoV-2 and Methods of Use |
CN112979646B (en) * | 2021-03-08 | 2022-01-14 | 北京富龙康泰生物技术有限公司 | Imidazopyridine derivative |
CN114907247A (en) * | 2022-04-21 | 2022-08-16 | 上海陶术生物科技有限公司 | Preparation method of pyrrolidine intermediate and pyrrolidine salt compound |
US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
Family Cites Families (255)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ234143A (en) | 1989-06-28 | 1991-10-25 | Mcneil Ppc Inc | Aqueous pharmaceutical suspension formulation for administering substantially insoluble pharmaceutical agents |
PL180717B1 (en) | 1993-11-30 | 2001-03-30 | Searle & Co | Substituted pyrazolyl benzosulphonamides for use in treating inflammatory states |
US5877016A (en) | 1994-03-18 | 1999-03-02 | Genentech, Inc. | Human trk receptors and neurotrophic factor inhibitors |
US5430021A (en) | 1994-03-18 | 1995-07-04 | Pharmavene, Inc. | Hydrophobic drug delivery systems |
US5844092A (en) | 1994-03-18 | 1998-12-01 | Genentech, Inc. | Human TRK receptors and neurotrophic factor inhibitors |
CA2206201A1 (en) | 1996-05-29 | 1997-11-29 | Yoshiaki Isobe | Pyrazole derivatives and their pharmaceutical use |
JP3898296B2 (en) | 1996-08-28 | 2007-03-28 | ポーラ化成工業株式会社 | Pyrrolopyrazolopyrimidine compounds and pharmaceuticals containing the same as active ingredients |
DE69827786T2 (en) | 1997-04-25 | 2005-11-24 | Takeda Pharmaceutical Co. Ltd. | CONDENSED PYRIDAZINE DERIVATIVES, THEIR PREPARATION AND USE |
UA74546C2 (en) | 1999-04-06 | 2006-01-16 | Boehringer Ingelheim Ca Ltd | Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition |
US6534085B1 (en) | 1999-09-23 | 2003-03-18 | Bioresponse L.L.C. | Phytochemicals for promoting weight loss |
IL153375A0 (en) | 2000-06-22 | 2003-07-06 | Genentech Inc | Agonist anti-trk-c monoclonal antibodies |
TWI312347B (en) | 2001-02-08 | 2009-07-21 | Eisai R&D Man Co Ltd | Bicyclic nitrogen-containing condensed ring compounds |
CA2448956C (en) | 2001-05-30 | 2017-10-03 | Genentech, Inc. | Anti-ngf antibodies for the treatment of various disorders |
US7101572B2 (en) | 2001-12-07 | 2006-09-05 | Unilab Pharmatech, Ltd. | Taste masked aqueous liquid pharmaceutical composition |
US20030199525A1 (en) | 2002-03-21 | 2003-10-23 | Hirst Gavin C. | Kinase inhibitors |
KR20040097375A (en) | 2002-04-23 | 2004-11-17 | 시오노기 앤드 컴파니, 리미티드 | Pyrazolo[1, 5-a]pyrimidine derivative and NAD(P)H oxidase inhibitor containing the same |
US7449488B2 (en) | 2002-06-04 | 2008-11-11 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
ITMI20021620A1 (en) | 2002-07-23 | 2004-01-23 | Novuspharma Spa | ANTI-TUMORAL ACTIVITY COMPOUND |
JP4024624B2 (en) * | 2002-08-26 | 2007-12-19 | 富士通株式会社 | Semiconductor device manufacturing method and manufacturing apparatus |
US7196078B2 (en) * | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
CN1880317B (en) * | 2002-09-04 | 2012-10-10 | 先灵公司 | Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors |
DK1537116T3 (en) | 2002-09-04 | 2010-09-27 | Schering Corp | Pyrazolopyrimidines suitable for the treatment of cancer diseases |
US7119200B2 (en) | 2002-09-04 | 2006-10-10 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
US8580782B2 (en) | 2002-09-04 | 2013-11-12 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors |
AU2003298942A1 (en) | 2002-12-11 | 2004-06-30 | Merck And Co., Inc. | Tyrosine kinase inhibitors |
WO2004052315A2 (en) | 2002-12-11 | 2004-06-24 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
WO2004074244A2 (en) | 2003-02-20 | 2004-09-02 | Smithkline Beecham Corporation | Pyrimidine compounds |
GB0303910D0 (en) | 2003-02-20 | 2003-03-26 | Merck Sharp & Dohme | Therapeutic agents |
WO2004082458A2 (en) | 2003-02-21 | 2004-09-30 | The Johns Hopkins University | Tyrosine kinome |
JP2004277337A (en) * | 2003-03-14 | 2004-10-07 | Sumitomo Pharmaceut Co Ltd | PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE |
EP1608652A1 (en) * | 2003-03-31 | 2005-12-28 | Vernalis (Cambridge) Limited | Pyrazolopyrimidine compounds and their use in medicine |
WO2004089471A2 (en) | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF |
WO2004089415A2 (en) | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | COMBINATIONS OF AN 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR AND A GLUCOCORTICOID RECEPTOR AGONIST |
US20060094699A1 (en) | 2003-04-11 | 2006-05-04 | Kampen Gita Camilla T | Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist to minimize the side effects associated with glucocorticoid receptor agonist therapy |
AU2004234286A1 (en) | 2003-04-28 | 2004-11-11 | Galpharma Co., Ltd | Galectin 9-inducing factor |
PA8603801A1 (en) | 2003-05-27 | 2004-12-16 | Janssen Pharmaceutica Nv | DERIVATIVES OF QUINAZOLINE |
JP2005008581A (en) * | 2003-06-20 | 2005-01-13 | Kissei Pharmaceut Co Ltd | NEW PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME AND APPLICATION THEREOF |
EA009517B1 (en) | 2003-06-27 | 2008-02-28 | Байер Кропсайенс Аг | Pyrazolopyrimidines |
JP4489077B2 (en) | 2003-07-15 | 2010-06-23 | アムジェン インコーポレイテッド | Human anti-NGF neutralizing antibodies as selective NGF pathway inhibitors |
US7491794B2 (en) | 2003-10-14 | 2009-02-17 | Intermune, Inc. | Macrocyclic compounds as inhibitors of viral replication |
EP1682564A1 (en) | 2003-10-27 | 2006-07-26 | Genelabs Technologies, Inc. | METHODS FOR PREPARING 7-(2 -SUBSTITUTED-s-D-RIBOFURANO SYL)-4-(NR2R3)-5-(SUBSTITUTED ETHYN-1-YL)-PYRROLO 2,3-D|PYRIMIDINE DERIVATIVES |
MY141220A (en) | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
RU2006122853A (en) | 2003-11-28 | 2008-01-10 | Новартис АГ (CH) | DIARYM UREA DERIVATIVES FOR TREATMENT OF DISEASES DEPENDING ON PROTEINKINASE |
UA83881C2 (en) | 2003-12-18 | 2008-08-26 | Янссен Фармацевтика Н.В. | Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents |
WO2005062795A2 (en) | 2003-12-19 | 2005-07-14 | Plexxikon, Inc. | Compounds and methods for development of ret modulators |
WO2005068424A1 (en) | 2004-01-20 | 2005-07-28 | Cell Therapeutics Europe S.R.L. | Indolinone derivatives as receptor tyrosine kinase ihibitors |
US20050222171A1 (en) | 2004-01-22 | 2005-10-06 | Guido Bold | Organic compounds |
WO2005099363A2 (en) | 2004-03-26 | 2005-10-27 | Whitehead Institute For Biomedical Research | Methods of diagnosing, preventing and treating cancer metastasis |
UA91677C2 (en) | 2004-03-30 | 2010-08-25 | Интермюн, Инк. | Macrocyclic compounds as inhibitors of hcv replication |
GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
PE20060664A1 (en) | 2004-09-15 | 2006-08-04 | Novartis Ag | BICYCLE AMIDAS AS KINASE INHIBITORS |
ZA200704476B (en) | 2004-11-04 | 2008-09-25 | Vertex Pharma | Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases |
JO3088B1 (en) | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | Macrocyclic Quinazoline derivatives and their use as MTKI |
DE102005003687A1 (en) | 2005-01-26 | 2006-07-27 | Sphingo Tec Gmbh | Immunodiagnostic determination of neurotensin in mammal blood, comprises injecting immune active N-terminal mammal proneurotensin in to the serum- or plasma- sample |
PT1853602E (en) | 2005-02-16 | 2010-08-25 | Astrazeneca Ab | Chemical compounds |
CN101119996A (en) * | 2005-02-16 | 2008-02-06 | 阿斯利康(瑞典)有限公司 | Chemical compouns |
EA012393B1 (en) | 2005-03-21 | 2009-10-30 | Эли Лилли Энд Компани | Imidazopyridazine compounds |
WO2006115452A1 (en) | 2005-04-27 | 2006-11-02 | Astrazeneca Ab | Use of pyrazolyl-pyrimidine derivatives in the treatment of pain |
WO2006123113A2 (en) | 2005-05-16 | 2006-11-23 | Astrazeneca Ab | Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors |
CN100406650C (en) | 2005-06-05 | 2008-07-30 | 徐斌 | Modular comb type expansion joint installation of girder capable of resisting super displacement |
ITRM20050290A1 (en) | 2005-06-07 | 2006-12-08 | Lay Line Genomics Spa | USE OF MOLECULES ABLE TO INHIBIT THE BOND BETWEEN NGF AND ITS TRKA RECEPTOR AS AN EXTENDED EFFECT ANALGESICS. |
AU2006261993B2 (en) | 2005-06-22 | 2011-11-17 | Plexxikon, Inc. | Pyrrolo (2, 3-B) pyridine derivatives as protein kinase inhibitors |
US20070025540A1 (en) | 2005-07-07 | 2007-02-01 | Roger Travis | Call center routing based on talkativeness |
CN101263156A (en) | 2005-07-25 | 2008-09-10 | 因特蒙公司 | Novel macrocyclic inhibitors of hepatitis C virus replication |
EP1910369A1 (en) | 2005-07-29 | 2008-04-16 | Astellas Pharma Inc. | Fused heterocycles as lck inhibitors |
JP2009503071A (en) | 2005-08-03 | 2009-01-29 | イーストマン ケミカル カンパニー | Tocopheryl polyethylene glycol succinate powder and method for producing the same |
AU2006283592A1 (en) | 2005-08-22 | 2007-03-01 | Amgen Inc. | Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators |
EA017318B1 (en) | 2005-08-25 | 2012-11-30 | Креабилис Терапеутикс С.П.А. | Polymer conjugates of indolocarbazole and derivatives thereof |
WO2007025090A2 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
DE102005042742A1 (en) | 2005-09-02 | 2007-03-08 | Schering Ag | Substituted imidazo [1,2b] pyridazines as kinase inhibitors, their production and use as pharmaceuticals |
US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
JP5152922B2 (en) | 2005-10-06 | 2013-02-27 | メルク・シャープ・アンド・ドーム・コーポレーション | Use of pyrazolo [1,5-A] pyrimidine derivatives to inhibit protein kinases and methods for inhibiting protein kinases |
EP1931675B1 (en) | 2005-10-06 | 2015-01-14 | Merck Sharp & Dohme Corp. | Pyrazolo(1, 5a) pyrimidines as protein kinase inhibitors |
ATE519757T1 (en) | 2005-10-11 | 2011-08-15 | Centre Nat Rech Scient | 3 HYDROXYFLAVONE DERIVATIVES FOR DETECTION AND QUANTIFICATION OF CELL APOPTOSIS |
DK1999129T3 (en) | 2005-10-11 | 2011-02-07 | Intermune Inc | Compounds and Methods for Inhibiting the Replication of Hepatitis C Virus |
US8101625B2 (en) | 2005-10-21 | 2012-01-24 | Exelixis, Inc. | Pyrimidinones as Casein Kinase II (CK2) modulators |
WO2007057399A2 (en) | 2005-11-15 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Treatment of cancer with indole derivatives |
GB0524436D0 (en) | 2005-11-30 | 2006-01-11 | Novartis Ag | Organic compounds |
US8399442B2 (en) | 2005-12-30 | 2013-03-19 | Astex Therapeutics Limited | Pharmaceutical compounds |
WO2007084815A2 (en) | 2006-01-19 | 2007-07-26 | Janssen Pharmaceutica, N.V. | Substituted thienopyrimidine kinase inhibitors |
WO2007087245A2 (en) | 2006-01-24 | 2007-08-02 | Merck & Co., Inc. | Ret tyrosine kinase inhibition |
KR100846988B1 (en) | 2006-03-06 | 2008-07-16 | 제일약품주식회사 | Novel thienopyrimidine derivatives or pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical composition comprising the same |
CA2645137A1 (en) | 2006-03-07 | 2007-09-13 | James F. Blake | Heterobicyclic pyrazole compounds and methods of use |
NZ572202A (en) | 2006-03-27 | 2012-05-25 | Nerviano Medical Sciences Srl | Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors |
GB0606805D0 (en) | 2006-04-04 | 2006-05-17 | Novartis Ag | Organic compounds |
BRPI0710874A2 (en) | 2006-04-26 | 2012-02-14 | Hoffmann La Roche | thienopyrimidine compounds, processes for producing said compounds, pharmaceutical compositions containing them, kit, product, and uses of the compounds |
US20090209580A1 (en) | 2006-05-18 | 2009-08-20 | Eisai R & D Management Co., Ltd. | Antitumor agent for thyroid cancer |
US7389632B2 (en) | 2006-06-10 | 2008-06-24 | Uhlmann Pac-Systeme Gmbh & Co. Kg | Apparatus for distributing small objects in a fill station |
EP1873157A1 (en) | 2006-06-21 | 2008-01-02 | Bayer Schering Pharma Aktiengesellschaft | Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same |
TW201345908A (en) * | 2006-07-05 | 2013-11-16 | Mitsubishi Tanabe Pharma Corp | A pyrazolo [1,5-a] pyrimidine compound |
JPWO2008016131A1 (en) | 2006-08-04 | 2009-12-24 | 武田薬品工業株式会社 | Fused heterocyclic compounds |
US7531539B2 (en) | 2006-08-09 | 2009-05-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
US20110021513A1 (en) | 2006-09-07 | 2011-01-27 | Biogen Idec Ma Inc. | Modulators of interleukin-1 receptor-associated kinase |
US20110195072A1 (en) | 2006-09-12 | 2011-08-11 | Anne Boulay | Non-neuroendocrine cancer therapy |
CN101516885A (en) | 2006-09-29 | 2009-08-26 | 诺瓦提斯公司 | Pyrazolopyrimidines as PI3K lipid kinase inhibitors |
BRPI0718266A2 (en) | 2006-10-30 | 2014-01-07 | Novartis Ag | HETEROCYCLIC COMPOUNDS AS ANTI-INFLAMMATORY AGENTS. |
BRPI0718029A2 (en) | 2006-11-06 | 2013-11-26 | Supergen Inc | IMIDAZO (1,2-B) PYRIDAZINE AND PIRAZOLE (1,5-A) PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS |
WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
JP2010514695A (en) | 2006-12-21 | 2010-05-06 | プレキシコン,インコーポレーテッド | Compounds and methods for kinase regulation and indications therefor |
PE20121126A1 (en) | 2006-12-21 | 2012-08-24 | Plexxikon Inc | PIRROLO [2,3-B] PYRIDINES COMPOUNDS AS KINASE MODULATORS |
US20080234267A1 (en) | 2007-03-20 | 2008-09-25 | Karen Elizabeth Lackey | Compounds and Methods of Treatment |
US20080234262A1 (en) | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
EP2137187A1 (en) | 2007-03-28 | 2009-12-30 | Inovacia AB | Pyrazolo [1,5-a]pyrimidines as inhibitors of stearoyl-coa desaturase |
UA101611C2 (en) | 2007-04-03 | 2013-04-25 | Аррей Байофарма Инк. | Compounds of imidazo[1,2-a]pyridine as receptor tyrosine kinase inhibitors |
JP5160637B2 (en) | 2007-05-04 | 2013-03-13 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Compounds and compositions as c-kit and PDGFR kinase inhibitors |
DK2170827T3 (en) | 2007-06-21 | 2013-11-18 | Janssen Pharmaceutica Nv | Indoline-2-ones and aza-indoline-2-ones |
AU2008273889B2 (en) | 2007-07-09 | 2012-03-08 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
WO2009012283A1 (en) | 2007-07-17 | 2009-01-22 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
CA2693967A1 (en) | 2007-07-19 | 2009-01-29 | Schering Corporation | Heterocyclic amide compounds as protein kinase inhibitors |
CA2693901C (en) | 2007-07-20 | 2015-12-29 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
WO2009017838A2 (en) | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
ME02239B (en) | 2007-08-10 | 2015-04-30 | Regeneron Pharma | High affinity human antibodies to human nerve growth factor |
AU2008312631A1 (en) | 2007-10-16 | 2009-04-23 | Wyeth Llc | Thienopyrimidine and pyrazolopyrimidine compounds and their use as mTOR kinase and PI3 kinase inhibitors |
EA201000603A1 (en) | 2007-10-23 | 2010-12-30 | Новартис Аг | APPLICATION OF ANTIBODIES TO TRKB FOR THE TREATMENT OF RESPIRATORY DISTURBANCES |
WO2009060197A1 (en) | 2007-11-08 | 2009-05-14 | Centro Nacional De Investigaciones Oncologicas (Cnio) | Imidazopyridazines for use as protein kinase inhibitors |
CA2706946A1 (en) | 2007-11-28 | 2009-06-04 | Schering Corporation | 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
WO2009071480A2 (en) | 2007-12-04 | 2009-06-11 | Nerviano Medical Sciences S.R.L. | Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors |
EP2235062A1 (en) | 2008-01-17 | 2010-10-06 | Irm Llc | Improved anti-trkb antibodies |
US20090227556A1 (en) | 2008-01-31 | 2009-09-10 | Eisai R&D Management Co., Ltd. | Receptor tyrosine kinase inhibitors comprising pyridine and pyrimidine derivatives |
EP2254886B1 (en) | 2008-03-28 | 2016-05-25 | Nerviano Medical Sciences S.r.l. | 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
KR101324804B1 (en) | 2008-05-13 | 2013-11-01 | 아이알엠 엘엘씨 | Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors |
US8158636B2 (en) | 2008-05-19 | 2012-04-17 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
PE20091846A1 (en) | 2008-05-19 | 2009-12-16 | Plexxikon Inc | PIRROLO [2,3-d] -PYRIMIDINE DERIVATIVES AS KINE MODULATORS |
EP2282995B1 (en) | 2008-05-23 | 2015-08-26 | Novartis AG | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
AU2009257635A1 (en) | 2008-06-10 | 2009-12-17 | Plexxikon, Inc. | 5H-Pyrrolo [2,3-b] pyrazine derivatives for kinase modulation, and indications therefor |
EP2323664B1 (en) | 2008-07-29 | 2015-01-07 | Nerviano Medical Sciences S.r.l. | Use of a cdk inhibitor for the treatment of glioma |
US8394802B2 (en) | 2008-09-19 | 2013-03-12 | Nerviano Medical Sciences S.R.L. | 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases |
PL2350075T3 (en) | 2008-09-22 | 2014-07-31 | Array Biopharma Inc | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
US8513263B2 (en) | 2008-10-22 | 2013-08-20 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors |
PE20131197A1 (en) | 2008-10-31 | 2013-11-06 | Genentech Inc | PYRAZOLOPYRIMIDINE COMPOUNDS AS JAK INHIBITORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
EP2376084B1 (en) | 2008-11-24 | 2013-07-17 | Nerviano Medical Sciences S.r.l. | CDK inhibitor for the treatment of mesothelioma |
JO3265B1 (en) | 2008-12-09 | 2018-09-16 | Novartis Ag | Pyridyloxyindoles Inhibitors of VEGF-R2 and Use Thereof for Treatment of Disease |
PL2881402T3 (en) | 2009-02-12 | 2017-10-31 | Cell Signaling Technology Inc | Mutant ROS expression in human liver cancer |
WO2010111527A1 (en) | 2009-03-26 | 2010-09-30 | Plexxikon, Inc. | Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use |
EP3045457B1 (en) | 2009-06-15 | 2018-05-09 | Nerviano Medical Sciences S.r.l. | Substituted pyrimidinylpyrrolopyridinone derivatives, process for their preparation and their use as kinase inhibitors |
AR077468A1 (en) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS |
EP2528918B1 (en) | 2010-01-29 | 2014-09-10 | Nerviano Medical Sciences S.r.l. | 6,7-dihydroimidazo[1,5-a]pyrazin-8(5h)-one derivatives as protein kinase modulators |
DK2536414T3 (en) | 2010-02-18 | 2016-10-03 | Inserm (Institut Nat De La Santé Et De La Rech Médicale) | METHOD FOR PREVENTING cancer metastasis |
JP2013526852A (en) | 2010-04-06 | 2013-06-27 | カリス ライフ サイエンシズ ルクセンブルク ホールディングス | Circulating biomarkers for disease |
US8383793B2 (en) | 2010-04-15 | 2013-02-26 | St. Jude Children's Research Hospital | Methods and compositions for the diagnosis and treatment of cancer resistant to anaplastic lymphoma kinase (ALK) kinase inhibitors |
TWI619713B (en) | 2010-04-21 | 2018-04-01 | 普雷辛肯公司 | Compounds and methods for kinase modulation, and indications therefor |
US8543395B2 (en) | 2010-05-18 | 2013-09-24 | Shazam Entertainment Ltd. | Methods and systems for performing synchronization of audio with corresponding textual transcriptions and determining confidence values of the synchronization |
MY191934A (en) | 2010-05-20 | 2022-07-19 | Array Biopharma Inc | Macrocyclic compounds as trk kinase inhibitors |
PL3333188T3 (en) | 2010-08-19 | 2022-05-09 | Zoetis Belgium S.A. | Anti-ngf antibodies and their use |
UY33597A (en) | 2010-09-09 | 2012-04-30 | Irm Llc | COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF THE TRK |
WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
JP2014005206A (en) | 2010-10-22 | 2014-01-16 | Astellas Pharma Inc | Arylamino heterocyclic carboxamide compound |
US9783601B2 (en) | 2010-12-01 | 2017-10-10 | Alderbio Holdings Llc | Methods of preventing inflammation and treating pain using anti-NGF compositions |
WO2012101029A1 (en) | 2011-01-26 | 2012-08-02 | Nerviano Medical Sciences S.R.L. | Tricyclic derivatives, process for their preparation and their use as kinase inhibitors |
BR112013018515B1 (en) | 2011-01-26 | 2021-06-29 | Nerviano Medical Sciences S.R.I | TRICYCLICAL PYRROL DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE AS KINASE INHIBITORS |
AU2012214762B2 (en) | 2011-02-07 | 2015-08-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
BR112013021537B1 (en) | 2011-02-24 | 2021-08-10 | Nerviano Medical Sciences S.R.L. | THAZOLYLPENYL-BENZENOSULPONAMIDE DERIVATIVES AS KINASE INHIBITORS |
AP2013007103A0 (en) | 2011-02-25 | 2013-09-30 | Irm Llc | Compounds and compositions as TRK inhibitors |
WO2012139930A1 (en) | 2011-04-11 | 2012-10-18 | Nerviano Medical Sciences S.R.L. | Pyrazolyl-pyrimidine derivatives as kinase inhibitors |
JP5970537B2 (en) | 2011-04-19 | 2016-08-17 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | Substituted pyrimidinyl-pyrroles active as kinase inhibitors |
CA2835478C (en) | 2011-05-12 | 2019-02-05 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
CA2835835C (en) | 2011-05-13 | 2019-04-02 | Array Biopharma Inc. | Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors |
JP6016915B2 (en) | 2011-07-28 | 2016-10-26 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | Alkynyl-substituted pyrimidinylpyrroles active as kinase inhibitors |
WO2013050446A1 (en) | 2011-10-07 | 2013-04-11 | Nerviano Medical Sciences S.R.L. | SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS |
US9181258B2 (en) | 2011-10-07 | 2015-11-10 | Nerviano Medical Sciences S.R.L. | Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors |
WO2013059740A1 (en) | 2011-10-21 | 2013-04-25 | Foundation Medicine, Inc. | Novel alk and ntrk1 fusion molecules and uses thereof |
KR20140128946A (en) | 2011-11-14 | 2014-11-06 | 테사로, 인코포레이티드 | Modulating certain tyrosine kinases |
KR20140105508A (en) | 2011-12-12 | 2014-09-01 | 닥터 레디스 레보러터리즈 리미티드 | Substituted pyrazolo[1,5-a]pyridine as tropomyosin receptor kinase (trk) inhibitors |
US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
EP2842955B1 (en) | 2012-04-26 | 2016-10-05 | ONO Pharmaceutical Co., Ltd. | Trk-inhibiting compound |
JP2013226108A (en) | 2012-04-27 | 2013-11-07 | Astellas Pharma Inc | Method for detecting new ntrk2 activating mutation |
ES2751944T3 (en) | 2012-05-23 | 2020-04-02 | Nerviano Medical Sciences Srl | Process for the preparation of N- [5- (3,5-difluoro-benzyl) -1H-indazol-3-yl] -4- (4-methyl-piperazin-1-yl) -2- (tetrahydro-pyran- 4-ylamino) -benzamide |
TWI585088B (en) | 2012-06-04 | 2017-06-01 | 第一三共股份有限公司 | Imidazo[1,2-b]pyridazine analogues as kinase inhibitors |
KR102163776B1 (en) | 2012-07-11 | 2020-10-12 | 블루프린트 메디신즈 코포레이션 | Inhibitors of the fibroblast growth factor receptor |
EP2689778A1 (en) | 2012-07-27 | 2014-01-29 | Pierre Fabre Medicament | Derivatives of azaindoles or diazaindoles for treating pain |
WO2014019908A2 (en) | 2012-08-02 | 2014-02-06 | Nerviano Medical Sciences S.R.L. | Substituted pyrroles active as kinases inhibitors |
US20150218652A1 (en) | 2012-08-31 | 2015-08-06 | The Regents Of The Unversity Of Colorado, A Body Corporate | Methods for diagnosis and treatment of cancer |
EP2892532B1 (en) | 2012-09-07 | 2019-02-13 | Exelixis, Inc. | Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma |
US20140084039A1 (en) | 2012-09-24 | 2014-03-27 | Electro Scientific Industries, Inc. | Method and apparatus for separating workpieces |
JP2014082984A (en) | 2012-10-23 | 2014-05-12 | Astellas Pharma Inc | Method for detecting novel ntrk2 activating mutation |
AU2013337264B2 (en) | 2012-11-05 | 2018-03-08 | Foundation Medicine, Inc. | Novel fusion molecules and uses thereof |
CA2890207A1 (en) | 2012-11-05 | 2014-05-08 | Foundation Medicine, Inc. | Novel ntrk1 fusion molecules and uses thereof |
EP2917214B1 (en) | 2012-11-07 | 2019-08-28 | Nerviano Medical Sciences S.r.l. | Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors |
WO2014078378A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
RU2677667C2 (en) | 2012-11-13 | 2019-01-18 | Эррэй Биофарма Инк. | N-pyrrolidinyl-urea, n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
US9969694B2 (en) | 2012-11-13 | 2018-05-15 | Array Biopharma Inc. | N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
WO2014078322A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078408A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078328A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
KR102181913B1 (en) | 2012-11-13 | 2020-11-23 | 어레이 바이오파마 인크. | Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain |
US9790210B2 (en) | 2012-11-13 | 2017-10-17 | Array Biopharma Inc. | N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors |
WO2014078372A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
WO2014078417A1 (en) | 2012-11-13 | 2014-05-22 | Array Biopharma Inc. | Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors |
CN104822390A (en) | 2012-11-29 | 2015-08-05 | 耶达研究及发展有限公司 | Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors |
US9447135B2 (en) | 2012-12-14 | 2016-09-20 | University Of Kentucky Research Foundation | Semi-synthetic mithramycin derivatives with anti-cancer activity |
US9127055B2 (en) | 2013-02-08 | 2015-09-08 | Astellas Pharma Inc. | Method of treating pain with anti-human NGF antibody |
BR122017003181A2 (en) | 2013-02-19 | 2019-09-10 | Ono Pharmaceutical Co | trk inhibitor compound, pharmaceutical composition and medicament comprising said compound and its use for prophylaxis and / or therapy of trk related disease and / or for inhibiting trk |
EP2981613A4 (en) | 2013-02-22 | 2016-11-02 | Boris C Bastian | Fusion polynucleotides and fusion polypeptides associated with cancer and particularly melanoma and their uses as therapeutic and diagnostic targets |
WO2014134096A1 (en) | 2013-02-27 | 2014-09-04 | Oregon Health & Science University | Methods of treating cancers characterized by aberrent ros1 activity |
WO2014150751A2 (en) | 2013-03-15 | 2014-09-25 | Novartis Ag | Biomarkers associated with brm inhibition |
AR095308A1 (en) | 2013-03-15 | 2015-10-07 | Glaxosmithkline Ip Dev Ltd | COMPOSITE OF 2-PIRIDONA, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND ITS USE TO PREPARE A MEDICINAL PRODUCT |
EP2970231A1 (en) | 2013-03-15 | 2016-01-20 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
ES2946689T3 (en) | 2013-03-15 | 2023-07-24 | Univ Leland Stanford Junior | Identification and use of circulating nucleic acid tumor markers |
JP2016515508A (en) | 2013-03-15 | 2016-05-30 | ザ・トラスティーズ・オブ・コロンビア・ユニバーシティ・イン・ザ・シティ・オブ・ニューヨーク | Fusion protein and method thereof |
WO2014152777A2 (en) | 2013-03-15 | 2014-09-25 | Insight Genetics, Inc. | Methods and compositions for the diagnosis and treatment of cancers resistant to ros1 inhibitors |
US10072298B2 (en) | 2013-04-17 | 2018-09-11 | Life Technologies Corporation | Gene fusions and gene variants associated with cancer |
CN105378110A (en) | 2013-04-17 | 2016-03-02 | 生命技术公司 | Gene fusions and gene variants associated with cancer |
WO2014184069A1 (en) | 2013-05-14 | 2014-11-20 | Nerviano Medical Sciences S.R.L. | Pyrrolo[2,3-d]pyrimidine derivatives, process for their preparation and their use as kinase inhibitors |
MX2015015966A (en) | 2013-05-30 | 2016-04-13 | Plexxikon Inc | Compounds for kinase modulation, and indications therefor. |
CA2917735C (en) | 2013-07-11 | 2017-04-18 | Betta Pharmaceuticals Co., Ltd | Protein tyrosine kinase modulators and methods of use |
US10705087B2 (en) | 2013-07-26 | 2020-07-07 | Japanese Foundation For Cancer Research | Detection method for NTRK3 fusion |
EP3628749A1 (en) | 2013-07-30 | 2020-04-01 | Blueprint Medicines Corporation | Ntrk2 fusions |
WO2015017528A1 (en) | 2013-07-30 | 2015-02-05 | Blueprint Medicines Corporation | Pik3c2g fusions |
WO2015039006A1 (en) | 2013-09-16 | 2015-03-19 | The General Hospital Corporation | Methods of treating cancer |
AU2014337314B2 (en) | 2013-10-17 | 2018-12-13 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to KIT |
WO2015058129A1 (en) | 2013-10-17 | 2015-04-23 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
MX2016004678A (en) | 2013-10-24 | 2017-03-10 | Univ Georgetown | Methods and compositions for treating cancer. |
WO2015061572A1 (en) | 2013-10-25 | 2015-04-30 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
WO2015064621A1 (en) | 2013-10-29 | 2015-05-07 | 公益財団法人がん研究会 | Novel fusions and detection method therefor |
WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
HRP20221518T1 (en) | 2014-01-24 | 2023-02-17 | Turning Point Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
NZ721057A (en) | 2014-02-05 | 2023-04-28 | VM Oncology LLC | Compositions of compounds and uses thereof |
US10231965B2 (en) | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
US20170044622A1 (en) | 2014-04-18 | 2017-02-16 | Blueprint Medicines Corporation | Pik3ca fusions |
US20170044621A1 (en) | 2014-04-18 | 2017-02-16 | Blueprint Medicines Corporation | Met fusions |
RS59286B1 (en) | 2014-05-15 | 2019-10-31 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor |
WO2015183836A1 (en) | 2014-05-27 | 2015-12-03 | Brian Haynes | Compositions, methods, and uses related to ntrk2-tert fusions |
WO2015183837A1 (en) | 2014-05-27 | 2015-12-03 | Brian Haynes | Compositions, methods, and uses related to ntrk2-tert fusions |
WO2015184443A1 (en) | 2014-05-30 | 2015-12-03 | The Regents Of The University Of Colorado | Activating ntrk1 gene fusions predictive of kinase inhibitor therapy |
EP3155118A1 (en) | 2014-06-10 | 2017-04-19 | Blueprint Medicines Corporation | Pkn1 fusions |
EP3155131B1 (en) | 2014-06-10 | 2020-02-12 | Blueprint Medicines Corporation | Raf1 fusions |
WO2016011141A1 (en) | 2014-07-17 | 2016-01-21 | Blueprint Medicines Corporation | Fgr fusions |
US10370723B2 (en) | 2014-07-17 | 2019-08-06 | Blueprint Medicines Corporation | TERT fusions |
US10370724B2 (en) | 2014-07-17 | 2019-08-06 | Blueprint Medicines Corporation | PRKC fusions |
US20160032404A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Biomarkers for predicting response of dlbcl to treatment with a btk inhibitor |
US9688680B2 (en) | 2014-08-04 | 2017-06-27 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
HUE045237T2 (en) | 2014-08-18 | 2019-12-30 | Ono Pharmaceutical Co | Acid-addition salt of trk-inhibiting compound |
CN114920840A (en) | 2014-10-14 | 2022-08-19 | 诺华股份有限公司 | Antibody molecules against PD-L1 and uses thereof |
KR102562866B1 (en) | 2014-11-14 | 2023-08-04 | 네르비아노 메디칼 사이언시스 에스.알.엘. | 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors |
AU2015346046B2 (en) | 2014-11-16 | 2020-06-25 | Array Biopharma, Inc. | Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
US20170356052A1 (en) | 2014-11-18 | 2017-12-14 | Blueprint Medicines Corporation | Prkacb fusions |
AU2015365587B2 (en) | 2014-12-15 | 2020-07-23 | Cmg Pharmaceutical Co., Ltd. | Fused ring heteroaryl compounds and their use as TRK inhibitors |
RU2020132040A (en) | 2015-05-20 | 2020-10-12 | Те Брод Инститьют Инк. | GENERAL NEOANTIGENS |
MA43943A (en) | 2015-05-29 | 2018-12-12 | Ignyta Inc | COMPOSITIONS AND METHODS FOR TREATING PATIENTS WITH RTK MUTANT CELLS |
CA2988423A1 (en) | 2015-06-01 | 2016-12-08 | Loxo Oncology, Inc. | Methods of diagnosing and treating cancer |
US9782400B2 (en) | 2015-06-19 | 2017-10-10 | Macau University Of Science And Technology | Oncogenic ROS1 and ALK kinase inhibitor |
AU2015101722A4 (en) | 2015-06-19 | 2016-05-19 | Macau University Of Science And Technology | Oncogenic ros1 and alk kinase inhibitor |
GB201511546D0 (en) | 2015-07-01 | 2015-08-12 | Immatics Biotechnologies Gmbh | Novel peptides and combination of peptides for use in immunotherapy against ovarian cancer and other cancers |
JP6871903B2 (en) | 2015-07-02 | 2021-05-19 | ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics,Inc. | Chiral diallyl macrocyclic molecule as a modulator of protein kinase |
AU2016344058A1 (en) | 2015-10-26 | 2018-05-17 | Array Biopharma Inc. | Point mutations in Trk inhibitor-resistant cancer and methods relating to the same |
US20170224662A1 (en) | 2016-01-22 | 2017-08-10 | The Medicines Company | Aqueous Formulations and Methods of Preparation and Use Thereof |
TW201733580A (en) | 2016-03-11 | 2017-10-01 | 小野藥品工業股份有限公司 | Treating agent for cancer having TrK inhibitor resistance |
US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
CA3019671C (en) | 2016-04-04 | 2024-02-20 | Loxo Oncology, Inc. | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
US20210030737A1 (en) | 2016-04-19 | 2021-02-04 | Exelixis, Inc. | Triple Negative Breast Cancer Treatment Method |
WO2017201156A1 (en) | 2016-05-18 | 2017-11-23 | Duke University | Method of treating kras wild-type metastatic colorectal cell carcinoma using cabozantinib plus panitumumab |
KR102566858B1 (en) | 2016-05-18 | 2023-08-11 | 어레이 바이오파마 인크. | (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-A]pyrimidin-3-yl Method for producing )-3-hydroxypyrrolidine-1-carboxamide |
JOP20190092A1 (en) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | PROCESS FOR THE PREPARATION OF PYRAZOLO[1,5-a]PYRIMIDINES AND SALTS THEREOF |
JOP20190213A1 (en) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | Macrocyclic compounds as ros1 kinase inhibitors |
MA50456A (en) | 2017-10-26 | 2020-09-02 | Array Biopharma Inc | MACROCYCLIC KINASE TRK INHIBITOR FORMULATIONS |
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