PL2350075T3 - Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk - Google Patents

Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk

Info

Publication number
PL2350075T3
PL2350075T3 PL09792796T PL09792796T PL2350075T3 PL 2350075 T3 PL2350075 T3 PL 2350075T3 PL 09792796 T PL09792796 T PL 09792796T PL 09792796 T PL09792796 T PL 09792796T PL 2350075 T3 PL2350075 T3 PL 2350075T3
Authority
PL
Poland
Prior art keywords
kinase inhibitors
substituted imidazo
pyridazine compounds
trk kinase
trk
Prior art date
Application number
PL09792796T
Other languages
English (en)
Polish (pl)
Inventor
Steven W Andrews
Julia Haas
Yutong Jiang
Gan Zhang
Original Assignee
Array Biopharma Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of PL2350075T3 publication Critical patent/PL2350075T3/pl

Links

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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/16—Halogenated acetic acids
    • C07C53/18—Halogenated acetic acids containing fluorine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
PL09792796T 2008-09-22 2009-09-21 Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk PL2350075T3 (pl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US9903008P 2008-09-22 2008-09-22
PCT/US2009/057729 WO2010033941A1 (en) 2008-09-22 2009-09-21 Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
EP09792796.6A EP2350075B1 (en) 2008-09-22 2009-09-21 Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors

Publications (1)

Publication Number Publication Date
PL2350075T3 true PL2350075T3 (pl) 2014-07-31

Family

ID=41328652

Family Applications (1)

Application Number Title Priority Date Filing Date
PL09792796T PL2350075T3 (pl) 2008-09-22 2009-09-21 Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk

Country Status (16)

Country Link
US (6) US8450322B2 (en:Method)
EP (1) EP2350075B1 (en:Method)
JP (5) JP5503655B2 (en:Method)
CN (2) CN103965200B (en:Method)
CA (2) CA2952692C (en:Method)
CY (1) CY1115107T1 (en:Method)
DK (1) DK2350075T3 (en:Method)
ES (1) ES2464461T3 (en:Method)
HR (1) HRP20140481T1 (en:Method)
PL (1) PL2350075T3 (en:Method)
PT (1) PT2350075E (en:Method)
RS (1) RS53350B (en:Method)
SI (1) SI2350075T1 (en:Method)
SM (1) SMT201400123B (en:Method)
TW (1) TWI433849B (en:Method)
WO (1) WO2010033941A1 (en:Method)

Families Citing this family (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2007316417B2 (en) * 2006-11-06 2013-08-22 Tolero Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
ES2548135T3 (es) 2008-05-13 2015-10-14 Novartis Ag Heterociclos condensados que contienen nitrógeno y composiciones de los mismos como inhibidores de quinasa
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
PT2725028T (pt) 2008-10-22 2016-08-31 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011146336A1 (en) 2010-05-20 2011-11-24 Array Biopharma Inc. Macrocyclic compounds as trk kinase inhibitors
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
CN103649076B (zh) 2011-05-13 2015-09-09 阵列生物制药公司 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物
US9102673B2 (en) 2011-07-12 2015-08-11 Merck Sharp & Dohme Corp. Substituted pyrrolo[3,2-c]pyridines as TrkA kinase inhibitors
US9416132B2 (en) 2011-07-21 2016-08-16 Tolero Pharmaceuticals, Inc. Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
MX347917B (es) * 2012-03-09 2017-05-17 Lexicon Pharmaceuticals Inc Compuestos a base de imidazo[1,2-b]piridazina, composiciones que los comprenden, y metodos para su uso.
US9181261B2 (en) 2012-05-22 2015-11-10 Merck Sharp & Dohme Corp. TrkA kinase inhibitors, compositions and methods thereof
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物
WO2014078378A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078331A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
NZ708028A (en) 2012-11-13 2018-12-21 Array Biopharma Inc N-pyrrolidinyl, n’-pyrazolyl- urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9981959B2 (en) 2012-11-13 2018-05-29 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
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
WO2014078325A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9546156B2 (en) 2012-11-13 2017-01-17 Array Biopharma Inc. N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors
US9790178B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
JP6345684B2 (ja) 2012-11-13 2018-06-20 アレイ バイオファーマ、インコーポレイテッド 疼痛の治療に有用な二環式尿素、チオ尿素、グアニジン、およびシアノグアニジン化合物
WO2015039333A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2015039334A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
MX2016009588A (es) 2014-01-24 2017-05-15 Tp Therapeutics Inc Macrociclos de diarilo como moduladores de la proteina quinasa.
WO2015143653A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143652A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143654A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
SG11201609550PA (en) 2014-05-15 2016-12-29 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
ES2941630T3 (es) 2014-11-16 2023-05-24 Array Biopharma Inc Forma cristalina de sulfato de hidrógeno de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida
CN104672121B (zh) * 2015-02-16 2017-10-24 上海华默西医药科技有限公司 2r‑(2,5‑二氟苯基)吡咯烷盐酸盐的制备方法
WO2016161572A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
CN107849615A (zh) 2015-06-01 2018-03-27 洛克索肿瘤学股份有限公司 诊断和治疗癌症的方法
CN107735399B (zh) * 2015-07-02 2021-01-26 特普医药公司 作为蛋白质激酶的调节剂的手性二芳基大环
BR112018000297A2 (pt) 2015-07-06 2018-09-04 Tp Therapeutics Inc polimorfo de macrociclo de diarila
JP6816100B2 (ja) 2015-07-16 2021-01-20 アレイ バイオファーマ、インコーポレイテッド ＲＥＴキナーゼ阻害物質としての置換ピラゾロ［１，５−ａ］ピリジン化合物
US20180325901A1 (en) 2015-07-21 2018-11-15 Tp Therapeutics, Inc. Chiral diaryl macrocycles and uses thereof
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
DK3439663T3 (da) 2016-04-04 2024-08-26 Loxo Oncology Inc Fremgangsmåder til behandling af pædiatriske cancere
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX386416B (es) 2016-04-04 2025-03-18 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida.
PE20190437A1 (es) 2016-05-18 2019-03-27 Loxo Oncology Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo
CN109715165A (zh) 2016-07-28 2019-05-03 Tp生物医药公司 巨环激酶抑制剂
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
CN108003161B (zh) * 2016-10-28 2020-10-09 正大天晴药业集团股份有限公司 神经营养因子酪氨酸激酶受体抑制剂
PT3533796T (pt) 2016-10-28 2021-11-18 Lianyungang Runzhong Pharmaceutical Co Ltd Composto de amino pirazolopirimidina utilizado como inibidor do recetor do fator neurotrófico tirosina quinase
CN106632353A (zh) * 2016-11-18 2017-05-10 山东友帮生化科技有限公司 3‑硝基‑6‑氯咪唑并[1,2‑b]哒嗪的合成方法
CN110267960B (zh) 2017-01-18 2022-04-26 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CN107286070B (zh) * 2017-07-19 2019-07-16 浙江师范大学 (r)-2-(2,5-二氟苯基)吡咯烷的合成方法及中间体
PT3658148T (pt) 2017-07-28 2024-08-26 Turning Point Therapeutics Inc Compostos macrocíclicos e utilizações dos mesmos
EP3661935B1 (en) * 2017-08-11 2022-10-12 Teligene Ltd Substituted pyrazolopyrimidines useful as kinases inhibitors
PL3674307T3 (pl) 2017-08-23 2023-11-27 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Związek makrocykliczny zawierający ugrupowanie aminopirazolu i pirymidyny oraz kompozycja farmaceutyczna i i ch zastosowanie
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
WO2019084285A1 (en) 2017-10-26 2019-05-02 Qian Zhao FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR
RS63787B1 (sr) 2017-12-19 2022-12-30 Turning Point Therapeutics Inc Makrociklična jedinjenja za lečenje bolesti
WO2019143977A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-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
CN108218754B (zh) * 2018-01-23 2021-05-07 广东赛烽医药科技有限公司 一种2-(2,5-二氟苯基)吡咯烷的制备方法
EP3765462B1 (en) 2018-03-14 2023-10-18 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
EP3773725A1 (en) 2018-03-29 2021-02-17 Loxo Oncology Inc. Treatment of trk-associated cancers
ES2989075T3 (es) 2018-04-25 2024-11-25 Primegene Beijing Co Ltd Compuesto macrocíclico diarílico y composición farmacéutica y uso del mismo
GB201811825D0 (en) * 2018-07-19 2018-09-05 Benevolentai Bio Ltd Organic compounds
CA3224985C (en) 2018-07-31 2025-11-18 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
CN110857304B (zh) * 2018-08-24 2021-05-18 北京富龙康泰生物技术有限公司 Trk抑制剂、其制备方法和用途
WO2020048455A1 (zh) 2018-09-03 2020-03-12 泰励生物科技（上海）有限公司 用作抗癌药的trk抑制剂
EP3849986B1 (en) 2018-09-10 2022-06-08 Array Biopharma, Inc. Fused heterocyclic compounds as ret kinase inhibitors
CN111039947A (zh) * 2018-10-15 2020-04-21 上海轶诺药业有限公司 一类蛋白受体激酶抑制剂的制备和应用
CN111171019A (zh) * 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
CN111269233A (zh) * 2018-12-05 2020-06-12 上海轶诺药业有限公司 一类咪唑并芳环类化合物的制备和应用
CN109354578A (zh) * 2018-12-06 2019-02-19 浙江师范大学 一种替尼中间体以及替尼的合成方法
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体
EP3924351B1 (en) 2019-02-12 2025-05-21 Sumitomo Pharma America, Inc. Crystalline form of the hydrochloride salt of 2-((1r,4r)-4-((3-(3-(trifluoromethyl)phenyl) imidazo[1,2-b]pyridazin-6-yl)amino)cyclohexyl)propan-2-ol
EP3932923B1 (en) 2019-03-19 2023-05-03 Central China Normal University Pyrazolopyrimidine compound, pharmaceutical composition, and application therefor
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CA3142088C (en) 2019-05-08 2023-02-28 Tyk Medicines, Inc. Compound used as kinase inhibitor and application thereof
CN114630829A (zh) * 2019-09-11 2022-06-14 重庆复创医药研究有限公司 作为TRK激酶抑制剂的取代的(2-氮杂双环[3.1.0]己-2-基)吡唑[1,5-a]嘧啶和咪唑[1,2-b]哒嗪化合物
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
CN112812118A (zh) * 2019-11-18 2021-05-18 上海轶诺药业有限公司 一类蛋白受体激酶抑制剂的制备和应用
KR20220130164A (ko) * 2020-01-22 2022-09-26 베네볼런트에이아이 바이오 리미티드 이미다조[1,2-b]피리다진 화합물을 포함하는 국소 약제학적 조성물
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113563343B (zh) * 2020-07-27 2022-05-24 杭州邦顺制药有限公司 取代的吡唑并[1,5-a]嘧啶化合物及其用途
BR112023021215A2 (pt) * 2021-04-13 2023-12-19 Shenzhen Newdel Biotech Co Ltd Compostos de alquinilfenilbenzamida, usos dos mesmos e composição farmacêutica compreendendo os referidos compostos
CA3223035A1 (en) * 2021-07-01 2023-01-05 Anheart Therapeutics (Hangzhou) Co., Ltd. Crystalline forms of 3-{4-[(2r)-2-aminopropoxy]phenyl}-n-[(1r)- 1-(3-fluorophenyl) ethyl]imidazo[1,2-b]pyridazin-6-amine and salts thereof

Family Cites Families (188)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2180233T3 (es) 1993-11-30 2003-02-01 Searle & Co Pirazolil bencenosulfonamidas sustituidas para uso en el tratamiento de la inflamacion.
US5430021A (en) 1994-03-18 1995-07-04 Pharmavene, Inc. Hydrophobic drug delivery systems
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
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
US6248740B1 (en) 1997-04-25 2001-06-19 Takeda Chemical Industries, Ltd. Condensed pyridazine derivatives, their production and use
US6534085B1 (en) 1999-09-23 2003-03-18 Bioresponse L.L.C. Phytochemicals for promoting weight loss
AU2001271422B2 (en) 2000-06-22 2005-12-22 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
BR0210231A (pt) 2001-05-30 2004-09-14 Genentech Inc Método de controle de uma disfunção relacionada ao fator de crescimento dos nervos (ngf), composição farmacêutica, artigo manufaturado e uso de anticorpo monoclonal anti-ngf
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
ITMI20021620A1 (it) 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
JP4024624B2 (ja) 2002-08-26 2007-12-19 富士通株式会社 半導体装置の製造方法及び製造装置
EP1537116B1 (en) 2002-09-04 2010-06-02 Schering Corporation Pyrazolopyrimidines suitable for the treatment of cancer diseases
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
WO2004052286A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
DE602004021472D1 (en) 2003-02-20 2009-07-23 Smithkline Beecham Corp Pyrimiidinverbindungen
US20070037150A1 (en) 2003-02-21 2007-02-15 The Johns Hopkins University Tyrosine kinome
JP2004277337A (ja) 2003-03-14 2004-10-07 Sumitomo Pharmaceut Co Ltd ピラゾロ［１，５−ａ］ピリミジン誘導体
EP1608652A1 (en) 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
JP2006522744A (ja) 2003-04-11 2006-10-05 ノボ　ノルディスク　アクティーゼルスカブ グルココルチコイド受容体アゴニスト療法に伴う副作用を最小化するための、１１β−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤およびグルココルチコイド受容体アゴニストを使用する併用療法
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
WO2004089471A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF
US20070042941A1 (en) 2003-04-28 2007-02-22 Mitsuomi Hirashima Galectin 9-inducing factors
PA8603801A1 (es) 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
JP2005008581A (ja) 2003-06-20 2005-01-13 Kissei Pharmaceut Co Ltd 新規なピラゾロ［１，５−ａ］ピリミジン誘導体、それを含有する医薬組成物およびそれらの用途
EA009517B1 (ru) 2003-06-27 2008-02-28 Байер Кропсайенс Аг Пиразолопиримидины
TWI635096B (zh) 2003-07-15 2018-09-11 安美基公司 作為選擇性神經生長因子（ｎｇｆ）通道抑制劑之人類抗-ｎｇｆ中和抗體
US7491794B2 (en) 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
WO2005058913A1 (en) 2003-12-18 2005-06-30 Janssen Pharmaceutica N.V. Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents
PT1696920E (pt) 2003-12-19 2015-01-14 Plexxikon Inc Compostos e métodos para o desenvolvimento de moduladores de ret
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 (ru) 2004-03-30 2010-08-25 Интермюн, Инк. Макроциклические соединения как ингибиторы вирусной репликации
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
CN101094853B (zh) 2004-11-04 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吡唑并[1,5-a]嘧啶
JO3088B1 (ar) 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
CN101119996A (zh) 2005-02-16 2008-02-06 阿斯利康(瑞典)有限公司 化学化合物
BRPI0608160A2 (pt) * 2005-02-16 2010-11-09 Astrazeneca Ab anticorpo isolado, célula hospedeira, método de inibir o crescimento de células psma+, e, uso de um anticorpo anti-psma defucosilado
JP4971300B2 (ja) 2005-03-21 2012-07-11 イーライ リリー アンド カンパニー イミダゾピリダジン化合物
EP1877057A1 (en) 2005-04-27 2008-01-16 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 (zh) 2005-06-05 2008-07-30 徐斌 一种抗特大变位的模块式梳型桥梁伸缩缝装置
ITRM20050290A1 (it) 2005-06-07 2006-12-08 Lay Line Genomics Spa Uso di molecole in grado di inibire il legame tra ngf e il suo recettore trka come analgesici ad effetto prolungato.
US20070025540A1 (en) 2005-07-07 2007-02-01 Roger Travis Call center routing based on talkativeness
EA019888B1 (ru) 2005-07-25 2014-07-30 Интермьюн, Инк. Промежуточное соединение для получения макроциклических ингибиторов репликации вируса гепатита с и способ его синтеза
US20100216798A1 (en) 2005-07-29 2010-08-26 Astellas Pharma Inc Fused heterocycles as lck inhibitors
WO2007019058A1 (en) 2005-08-03 2007-02-15 Eastman Chemical Company Tocopheryl polyethylene glycol succinate powder and process for preparing same
CA2619365A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
ES2444003T5 (es) 2005-08-25 2017-07-05 Creabilis Therapeutics S.P.A. Conjugados poliméricos de K-252A y sus derivados
US20070049591A1 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
DE102005042742A1 (de) 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
WO2007044441A2 (en) 2005-10-06 2007-04-19 Schering Corporation Use of pyrazolo [1 , 5 -a] pyrimidine derivatives for inhibiting protein kinases methods for inhibiting protein kinases
CA2624500A1 (en) 2005-10-06 2007-04-19 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
KR20080056295A (ko) 2005-10-11 2008-06-20 인터뮨, 인크. Ｃ형 간염 바이러스 복제를 억제하기 위한 화합물 및 방법
JP5030961B2 (ja) 2005-10-11 2012-09-19 サーントゥル ナシオナル ドゥ ラ ルシェルシュ シャーンティフィク 細胞のアポトーシスの検出および定量化用の化合物およびキット
US8101625B2 (en) 2005-10-21 2012-01-24 Exelixis, Inc. Pyrimidinones as Casein Kinase II (CK2) modulators
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
WO2007077435A1 (en) 2005-12-30 2007-07-12 Astex Therapeutics Limited Pharmaceutical compounds
WO2007084815A2 (en) 2006-01-19 2007-07-26 Janssen Pharmaceutica, N.V. Substituted thienopyrimidine kinase inhibitors
WO2007102679A1 (en) 2006-03-06 2007-09-13 Je Il Pharmaceutical Co., Ltd. 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
GB0606805D0 (en) 2006-04-04 2006-05-17 Novartis Ag Organic compounds
PT2024372E (pt) 2006-04-26 2010-09-16 Hoffmann La Roche Derivado de tieno[3,2-d]pirimidina útil como inibidor de pi3k
AU2007252506C1 (en) 2006-05-18 2012-07-19 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 (zh) 2006-07-05 2013-11-16 Mitsubishi Tanabe Pharma Corp 吡唑并〔１，５-ａ〕嘧啶化合物
US20100029619A1 (en) * 2006-08-04 2010-02-04 Takeda Pharmaceutical Company Limted Fused heterocyclic compound
US7531539B2 (en) 2006-08-09 2009-05-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
CN101594909A (zh) 2006-09-07 2009-12-02 比奥根艾迪克Ma公司 用于治疗炎性病症、细胞增殖性失调、免疫失调的irak调节剂
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘
BRPI0718266A2 (pt) 2006-10-30 2014-01-07 Novartis Ag Compostos heterocíclicos como agentes anti-inflamatórios.
AU2007316417B2 (en) 2006-11-06 2013-08-22 Tolero Pharmaceuticals, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
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
US20080255153A1 (en) 2007-03-28 2008-10-16 Biovitrum Ab (Publ) New compounds
RU2467008C2 (ru) 2007-04-03 2012-11-20 Эррэй Биофарма Инк. СОЕДИНЕНИЯ ИМИДАЗО[1,2-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ РЕЦЕПТОРНЫХ ТИРОЗИНКИНАЗ
CA2686382C (en) 2007-05-04 2013-09-17 Irm Llc Phenylaminopyrimidine derivatives and compositions thereof as c-kit and pdgfr kinase inhibitors
EP2170827B1 (en) 2007-06-21 2013-08-14 Janssen Pharmaceutica, N.V. Indolin-2-ones and aza-indolin-2-ones
BRPI0814628B1 (pt) 2007-07-20 2022-04-05 Nerviano Medical Sciences S.R.L. Derivados ativos de indazol substituídos como inibidores da quinase
JP5632744B2 (ja) 2007-08-10 2014-11-26 リジェネロン・ファーマシューティカルズ・インコーポレイテッド ヒト神経成長因子に対する高親和性ヒト抗体
AP2010005234A0 (en) 2007-10-16 2010-04-30 Wyeth Llc Thienopyrimidine and pyrazolopyrimidline compoundsand their use as MTOR kinase and P13 kinase inhib itors
US20100297115A1 (en) 2007-10-23 2010-11-25 Novartis Ag Use of trkb antibodies for the treatment of respiratory disorders
EP2217601A1 (en) * 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
AU2009205937B2 (en) 2008-01-17 2013-02-07 Novartis Ag 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
ES2548135T3 (es) * 2008-05-13 2015-10-14 Novartis Ag Heterociclos condensados que contienen nitrógeno y composiciones de los mismos como inhibidores de quinasa
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
GEP20125502B (en) 2008-05-23 2012-04-25 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
WO2010012733A1 (en) 2008-07-29 2010-02-04 Nerviano Medical Sciences S.R.L. Use of a cdk inhibitor for the treatment of glioma
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
PT2725028T (pt) 2008-10-22 2016-08-31 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk
RU2539568C2 (ru) 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
JP2012509859A (ja) 2008-11-24 2012-04-26 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 中皮腫の治療のためのｃｄｋ阻害物質
JO3265B1 (ar) 2008-12-09 2018-09-16 Novartis Ag مثبطات بيريديلوكسى اندولات vegf-r2 واستخدامها لعلاج المرض
PT2881402T (pt) 2009-02-12 2017-08-23 Cell Signaling Technology Inc Expressão de ros mutante em cancro de fígado humano
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
DK2536414T3 (en) 2010-02-18 2016-10-03 Inserm (Institut Nat De La Santé Et De La Rech Médicale) METHOD FOR PREVENTING cancer metastasis
US9469876B2 (en) 2010-04-06 2016-10-18 Caris Life Sciences Switzerland Holdings Gmbh Circulating biomarkers for metastatic prostate cancer
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
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
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
WO2011146336A1 (en) 2010-05-20 2011-11-24 Array Biopharma Inc. Macrocyclic compounds as trk kinase inhibitors
HUE058226T2 (hu) 2010-08-19 2022-07-28 Zoetis Belgium S A NGF elleni antitestek és alkalmazásuk
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
MX359070B (es) 2010-12-01 2018-09-13 Alderbio Holdings Llc Composiciones anti-ngf y uso de las mismas.
WO2012116217A1 (en) 2011-02-25 2012-08-30 Irm Llc Compounds and compositions as trk inhibitors
CN103649076B (zh) 2011-05-13 2015-09-09 阵列生物制药公司 作为trka激酶抑制剂的吡咯烷基脲和吡咯烷基硫脲化合物
WO2013059740A1 (en) 2011-10-21 2013-04-25 Foundation Medicine, Inc. Novel alk and ntrk1 fusion molecules and uses thereof
WO2013074518A1 (en) 2011-11-14 2013-05-23 Tesaro, Inc. Modulating certain tyrosine kinases
EA025352B1 (ru) 2011-12-12 2016-12-30 Др. Редди'С Лабораториз Лтд. ЗАМЕЩЕННЫЕ СОЕДИНЕНИЯ ПИРАЗОЛО[1,5-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ТРОПОМИОЗИН-РЕЦЕПТОРНОЙ КИНАЗЫ (Trk)
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
WO2013161919A1 (ja) 2012-04-26 2013-10-31 小野薬品工業株式会社 Ｔｒｋ阻害化合物
WO2013174876A1 (en) 2012-05-23 2013-11-28 Nerviano Medical Sciences S.R.L. 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 (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物
WO2014036387A2 (en) 2012-08-31 2014-03-06 The Regents Of The University Of Colorado Methods for diagnosis and treatment of cancer
CN104703600A (zh) 2012-09-07 2015-06-10 埃克塞里艾克西斯公司 用于治疗肺腺癌的met、vegfr和ret的抑制剂
US20140084039A1 (en) 2012-09-24 2014-03-27 Electro Scientific Industries, Inc. Method and apparatus for separating workpieces
JP2014082984A (ja) 2012-10-23 2014-05-12 Astellas Pharma Inc 新規ｎｔｒｋ２活性化変異の検出法
EP4223770A3 (en) 2012-11-05 2023-10-18 Foundation Medicine, Inc. Novel fusion molecules and uses thereof
HK1214830A1 (zh) 2012-11-05 2016-08-05 Foundation Medicine, Inc. 新型ntrk1融合分子及其应用
US9546156B2 (en) 2012-11-13 2017-01-17 Array Biopharma Inc. N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors
JP6345684B2 (ja) 2012-11-13 2018-06-20 アレイ バイオファーマ、インコーポレイテッド 疼痛の治療に有用な二環式尿素、チオ尿素、グアニジン、およびシアノグアニジン化合物
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078331A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
NZ708028A (en) 2012-11-13 2018-12-21 Array Biopharma Inc N-pyrrolidinyl, n’-pyrazolyl- 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
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9790178B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
US20150290233A1 (en) 2012-11-29 2015-10-15 Yeda Research And Development Co.Ltd. At The Weizmann Institute Of Science 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
BR112015019921A2 (pt) 2013-02-19 2017-07-18 Ono Pharmaceutical Co composto inibidor de trk
WO2014130975A1 (en) 2013-02-22 2014-08-28 Bastian Boris C 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
EP3795696B1 (en) 2013-03-15 2023-04-26 The Board of Trustees of the Leland Stanford Junior University Identification and use of circulating nucleic acid tumor markers
AR095308A1 (es) 2013-03-15 2015-10-07 Glaxosmithkline Ip Dev Ltd Compuesto de 2-piridona, composición farmacéutica que lo comprende y su uso para preparar un medicamento
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
CA2907152A1 (en) 2013-03-15 2014-09-25 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
AU2014254394B2 (en) 2013-04-17 2020-06-18 Life Technologies Corporation Gene fusions and gene variants associated with cancer
US10072298B2 (en) 2013-04-17 2018-09-11 Life Technologies Corporation Gene fusions and gene variants associated with cancer
RU2656591C2 (ru) 2013-07-11 2018-06-06 Бетта Фармасьютикалз Ко., Лтд Модуляторы протеин-тирозинкиназы и способы их применения
US10705087B2 (en) 2013-07-26 2020-07-07 Japanese Foundation For Cancer Research Detection method for NTRK3 fusion
EP3027655B1 (en) 2013-07-30 2019-08-21 Blueprint Medicines Corporation Ntrk2 fusions
AU2014340398A1 (en) 2013-10-24 2016-06-09 Georgetown University Methods and compositions for treating cancer
WO2015064621A1 (ja) 2013-10-29 2015-05-07 公益財団法人がん研究会 新規融合体及びその検出法
MX2016009588A (es) 2014-01-24 2017-05-15 Tp Therapeutics Inc Macrociclos de diarilo como moduladores de la proteina quinasa.
AU2015214185B2 (en) 2014-02-05 2016-08-04 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
SG11201609550PA (en) 2014-05-15 2016-12-29 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
WO2015183837A1 (en) 2014-05-27 2015-12-03 Brian Haynes Compositions, methods, and uses related to ntrk2-tert fusions
US20170114415A1 (en) 2014-05-30 2017-04-27 The Regents Of The University Of Colorado, A Body Corporate Activating ntrk1 gene fusions predictive of kinase inhibitor therapy
MX2017001302A (es) 2014-08-01 2017-10-11 Pharmacyclics Llc Biomarcadores para predecir la respuesta del dlbcl al tratamiento con un inhibidor de la btk.
HUE045237T2 (hu) 2014-08-18 2019-12-30 Ono Pharmaceutical Co TRK-inhibitáló vegyület savaddíciós sója
CA2964367C (en) 2014-10-14 2024-01-30 Novartis Ag Antibody molecules to pd-l1 and uses thereof
ES2941630T3 (es) 2014-11-16 2023-05-24 Array Biopharma Inc Forma cristalina de sulfato de hidrógeno de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida
ES2983908T3 (es) 2014-12-15 2024-10-28 Cmg Pharmaceutical Co Ltd Compuestos heteroarílicos de anillo condensado y su uso como inhibidores de TRK
CR20230191A (es) 2015-05-20 2023-07-06 Dana Farber Cancer Inst Inc NEOANTIGENOS COMPARTIDOS (Div. exp 2017-584)
WO2016196141A1 (en) 2015-05-29 2016-12-08 Ignyta, Inc. Compositions and methods for treating patients with rtk mutant cells
CN107849615A (zh) 2015-06-01 2018-03-27 洛克索肿瘤学股份有限公司 诊断和治疗癌症的方法
AU2015101722A4 (en) 2015-06-19 2016-05-19 Macau University Of Science And Technology Oncogenic ros1 and alk kinase inhibitor
US9782400B2 (en) 2015-06-19 2017-10-10 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
CN107735399B (zh) 2015-07-02 2021-01-26 特普医药公司 作为蛋白质激酶的调节剂的手性二芳基大环
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents 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
JPWO2017155018A1 (ja) 2016-03-11 2019-01-17 小野薬品工業株式会社 Ｔｒｋ阻害剤抵抗性の癌治療剤
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX386416B (es) 2016-04-04 2025-03-18 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida.
WO2017184597A1 (en) 2016-04-19 2017-10-26 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
PE20190437A1 (es) 2016-05-18 2019-03-27 Loxo Oncology Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
WO2019084285A1 (en) 2017-10-26 2019-05-02 Qian Zhao FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR

Also Published As

Publication number Publication date
US10011604B2 (en) 2018-07-03
PT2350075E (pt) 2014-06-09
JP2020050665A (ja) 2020-04-02
CN102224153B (zh) 2014-04-30
CN103965200B (zh) 2016-06-08
US20110166122A1 (en) 2011-07-07
JP2018044010A (ja) 2018-03-22
WO2010033941A1 (en) 2010-03-25
CA2952692A1 (en) 2010-03-25
HRP20140481T1 (hr) 2014-07-04
JP5503655B2 (ja) 2014-05-28
ES2464461T3 (es) 2014-06-02
US9796723B2 (en) 2017-10-24
TWI433849B (zh) 2014-04-11
CA2738026A1 (en) 2010-03-25
JP2014111663A (ja) 2014-06-19
US10590139B2 (en) 2020-03-17
US20170112849A1 (en) 2017-04-27
US8450322B2 (en) 2013-05-28
JP2012503018A (ja) 2012-02-02
US9227975B2 (en) 2016-01-05
JP2016147911A (ja) 2016-08-18
JP5941938B2 (ja) 2016-06-29
DK2350075T3 (da) 2014-05-26
SI2350075T1 (sl) 2014-06-30
CN102224153A (zh) 2011-10-19
US20190169193A1 (en) 2019-06-06
CY1115107T1 (el) 2016-12-14
SMT201400123B (it) 2014-11-10
US20130217662A1 (en) 2013-08-22
EP2350075A1 (en) 2011-08-03
JP6267741B2 (ja) 2018-01-24
TW201016701A (en) 2010-05-01
CA2952692C (en) 2020-04-28
CN103965200A (zh) 2014-08-06
CA2738026C (en) 2017-01-24
US20170114068A1 (en) 2017-04-27
EP2350075B1 (en) 2014-03-05
US20160251357A1 (en) 2016-09-01
JP6858240B2 (ja) 2021-04-14
RS53350B (sr) 2014-10-31
US9795611B2 (en) 2017-10-24

Similar Documents

Publication Publication Date Title
IL278119B (en) Disubstituted pyrazolo[5.1–a]pyrimidine compounds as trk kinase inhibitors
PL2350075T3 (pl) Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk
ZA201200982B (en) Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors
IL201300A0 (en) Imidazo [1, 2 - a] pyridine compounds as receptor tyrosine kinase inhibitors
IL217798A0 (en) Pyrrolo [1,2-b]pyridazine derivatives as janus kinase inhibitors
ZA201105896B (en) [1,2,4] triazolo [1,5-a] pyridines as kinase inhibitors
ZA201100437B (en) 3-(3-pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazine derivatives as met kinase inhibitors
HK1160846A (en) [1, 2, 4] triazolo [1, 5 -a] pyridines as kinase inhibitors