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PE20160992A1 - Inhibidores de quinasa relacionada con la tropomiosina (trk) - Google Patents

Inhibidores de quinasa relacionada con la tropomiosina (trk)

Info

Publication number
PE20160992A1
PE20160992A1 PE2016000760A PE2016000760A PE20160992A1 PE 20160992 A1 PE20160992 A1 PE 20160992A1 PE 2016000760 A PE2016000760 A PE 2016000760A PE 2016000760 A PE2016000760 A PE 2016000760A PE 20160992 A1 PE20160992 A1 PE 20160992A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibitors
tropomyosin
halo
cycloalkyl
Prior art date
Application number
PE2016000760A
Other languages
English (en)
Inventor
John L Kane Jr
Michael Kothe
Andrew Scholte
Gloria Matthews
Markus Metz
Jinyu Liu
Original Assignee
Genzyme Corp
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 Genzyme Corp filed Critical Genzyme Corp
Publication of PE20160992A1 publication Critical patent/PE20160992A1/es

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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a compuestos de Formula (I) y sales farmaceuticamente aceptables de los mismos, donde n es 1, 2, 3, 4 o 5; m es 0, 1, 2, 3 o 4; Q1 es H, halo, arilo C6–C14, entre otros; Q2 es arilo C6–C14, cicloalquilo C3–C10, entre otros; X es CH o N, entre otros; R1 es H, halo, alquilo C1–C10, NH2, entre otros; R2 es H, halo, alquilo C1–C10, NH2, entre otros; R3 y R4 son independientemente H, alquilo C1–C10, O–alquilo C1–C10, NH2, entre otros; o –CR3R4 forman un anillo de 3 a 10 miembros, opcionalmente sustituido con 1 a 4 sustituyentes seleccionados entre alquilo C1–C10, cicloalquilo C3–C10, OH, NH2, entre otros; R5 y R6 son independientemente H, alquilo C1–C10, O–alquilo C1–C10, NH2, entre otros; o –CR5R6 forman un anillo de 3 a 10 miembros, opcionalmente sustituido con 1 a 4 sustituyentes seleccionados entre alquilo C1–C10, cicloalquilo C3–C10, OH, NH2, entre otros. Dichos compuestos son inhibidores de quinasa relacionada con la tropomiosina (inhibidores de Trk), por lo cual son utiles en el tratamiento de enfermedades inflamatorias, enfermedades autoinmunes, defectos del metabolismo oseo y cancer
PE2016000760A 2013-12-10 2014-12-10 Inhibidores de quinasa relacionada con la tropomiosina (trk) PE20160992A1 (es)

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Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI731317B (zh) * 2013-12-10 2021-06-21 美商健臻公司 原肌球蛋白相關之激酶(trk)抑制劑
JP6606183B2 (ja) * 2014-12-18 2019-11-13 ジェンザイム・コーポレーション トロポミオシン関連キナーゼ(trk)阻害剤の医薬製剤
IL305843B2 (en) * 2015-07-20 2025-01-01 Genzyme Corp CSF-1R receptor antibodies
CN110869349B (zh) 2017-05-04 2025-07-22 发现号收购集团 作为例如用于保护植物的害虫防治剂的2-{[2-(苯氧基甲基)吡啶-5-基]氧基}乙胺衍生物及相关化合物
CN110156813B (zh) * 2018-02-13 2023-07-25 北京诺诚健华医药科技有限公司 作为trk抑制剂的杂环化合物
CN108822103A (zh) * 2018-07-28 2018-11-16 刘凤娟 一种咪唑并[4,5-b]吡啶化合物及其制备方法和应用
EP3903828A4 (en) 2018-12-21 2022-10-05 Daiichi Sankyo Company, Limited ANTIBODY-DRUG CONJUGATE AND KINAS INHIBITOR COMBINATION
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP3974434B1 (en) 2019-05-21 2025-11-19 Zhejiang Hisun Pharmaceutical Co., Ltd. Macrolide derivatives, preparation method and application thereof
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子-1受容体(csf-1r)阻害剤
EP4180428A1 (en) 2021-11-12 2023-05-17 Genzyme Corporation Crystalline imidazo[4,5-b]pyridine compound, pharmaceutical compositions, and their use in treating medical conditions
WO2024238957A1 (en) * 2023-05-17 2024-11-21 Centrexion Therapeutics Corporation PARTICLES OF IMIDAZO [4,5-b] PYRIDINE COMPOUND, PHARMACEUTICAL COMPOSITIONS, AND THEIR USE IN TREATING MEDICAL CONDITIONS

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59181263A (ja) * 1983-03-29 1984-10-15 Nippon Nohyaku Co Ltd ベンズイミダゾ−ル誘導体
US4612323A (en) * 1983-06-27 1986-09-16 Sumitomo Chemical Company, Limited Insecticidal and acaricidal derivatives of 1-benzylbenzimidazole
JPS60158180A (ja) * 1984-01-30 1985-08-19 Sumitomo Chem Co Ltd ベンズイミダゾ−ル誘導体、その製造法およびそれを有効成分とする殺虫、殺ダニ剤
JPS6117569A (ja) * 1984-07-03 1986-01-25 Sumitomo Chem Co Ltd ベンズイミダゾ−ル誘導体およびそれを有効成分とする殺ダニ剤
JPS61151176A (ja) 1984-12-24 1986-07-09 Sumitomo Chem Co Ltd ベンズイミダゾール誘導体およびそれを有効成分とする殺虫、殺ダニ剤
CA2075627A1 (en) * 1990-02-13 1991-08-14 William J. Greenlee Angiotensin ii antagonists incorporating a substituted benzyl element
DE4219534A1 (de) 1992-02-19 1993-12-16 Thomae Gmbh Dr K Substituierte Biphenylylderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DK154092D0 (da) * 1992-12-23 1992-12-23 Neurosearch As Imidazolforbindelser, deres fremstilling og anvendelse
US5702637A (en) 1995-04-19 1997-12-30 Minnesota Mining And Manufacturing Company Liquid crystal compounds having a chiral fluorinated terminal portion
DE19718181A1 (de) * 1997-04-30 1998-11-05 Boehringer Ingelheim Pharma Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel
BR9810456A (pt) * 1997-06-27 2001-09-25 Fujisawa Pharmaceutical Co Composto de sulfonamida, método para sua obtenção e seu uso farmacêutico
SK179899A3 (en) * 1997-07-03 2001-12-03 Du Pont Pharm Co Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders
GB9825652D0 (en) * 1998-11-23 1999-01-13 Celltech Therapeutics Ltd Chemical compounds
CZ20011981A3 (cs) * 1998-12-04 2002-01-16 Fujisawa Pharmaceutical Co., Ltd. Sulfonamidové sloučeniny
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
US7030150B2 (en) 2001-05-11 2006-04-18 Trimeris, Inc. Benzimidazole compounds and antiviral uses thereof
MXPA04001253A (es) * 2001-08-09 2004-06-03 Ono Pharmaceutical Co Derivados de acidos carboxilicos y agente farmaceutico que comprende los mismos como ingrediente activo.
GB0122190D0 (en) 2001-09-14 2001-10-31 Qinetiq Ltd Novel compounds
US20040002145A1 (en) 2002-03-18 2004-01-01 Shewchuk Lisa Marie Crystal structure of liganded cFMS kinase domain
EP1505966A4 (en) 2002-05-10 2006-08-30 Bristol Myers Squibb Co 1,1-DISUBSTITUTED CYCLOALKYL DERIVATIVES AS FACTOR XA HEMMER
FR2852957B1 (fr) 2003-03-31 2005-06-10 Sod Conseils Rech Applic Nouveaux derives d'imidazo-pyridine et leur utilisation en tant que medicament
TWI332003B (en) 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
CA2560005A1 (en) 2004-03-31 2005-10-13 Kissei Pharmaceutical Co., Ltd. Phenol derivative, medicinal composition containing the same, and medicinal use thereof
SI1747210T1 (sl) * 2004-05-07 2010-09-30 Warner Lambert Co ali monosubstituirani fenolin in tiofenolni derivati uporabni kot ligandi H
AU2005307818A1 (en) 2004-11-18 2006-05-26 The Institutes For Pharmaceutical Discovery, Llc Heterocyclylbiphenyl derivates as protein Tyrosine phosphatase inhibitors
BRPI0607455A2 (pt) * 2005-02-16 2009-09-01 Astrazeneca Ab composto, processo para a preparação do mesmo, uso de um composto, e composição farmacêutica
JP2006273879A (ja) 2005-03-25 2006-10-12 Fuji Photo Film Co Ltd カラー表示素子及びカラー表示方法
US7799820B2 (en) 2005-09-30 2010-09-21 Banyu Pharmaceutical Co., Ltd. 2-Heterocycle-substituted indole derivatives for treating diabetes and associated conditions
CN1947717B (zh) 2005-10-14 2012-09-26 卓敏 选择性抑制腺苷酸环化酶1的化合物在制备用于治疗神经性疼痛和炎性疼痛的药物中的应用
US7851484B2 (en) 2007-03-30 2010-12-14 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
WO2008129255A1 (en) 2007-04-18 2008-10-30 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer
EP2426108B1 (en) 2007-08-29 2016-08-10 MethylGene Inc. Processes and intermediates for preparing fused heterocyclic kinase inhibitors
WO2010088518A2 (en) 2009-01-31 2010-08-05 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
SI2493895T1 (sl) 2009-10-29 2017-10-30 Vectura Limited Derivati heteroarila, ki vsebujejo N, kot inhibitorji JAK3 kinaze
CN102712601A (zh) * 2009-11-12 2012-10-03 赛尔维他股份公司 化合物、其制备方法、药物组合物、化合物的用途、用于调节或调控丝氨酸/苏氨酸激酶的方法以及丝氨酸/苏氨酸激酶调节剂
US8604217B2 (en) 2009-11-12 2013-12-10 Selvita S.A. Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
CA2803448A1 (en) 2010-07-06 2012-01-12 Universite De Montreal Imidazopyridine, imidazopyrimidine and imidazopyrazine derivatives as melanocortin-4 receptor modulators
MA35024B1 (fr) 2011-04-05 2014-04-03 Pfizer Ltd Dérivés de pyrrolo-[2,3-d]pyrimidine servant d'inhibiteurs des kinases apparentés à la tropomyosine
AU2012351748B2 (en) * 2011-12-12 2016-04-14 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors
EP2858501A4 (en) 2012-05-22 2015-12-09 Merck Sharp & Dohme TRKA KINASE INHIBITORS, COMPOSITIONS AND METHOD THEREFOR
JP6117569B2 (ja) 2013-02-28 2017-04-19 三甲株式会社 ボックスパレット
GB201321741D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
TWI731317B (zh) 2013-12-10 2021-06-21 美商健臻公司 原肌球蛋白相關之激酶(trk)抑制劑
JP6606183B2 (ja) * 2014-12-18 2019-11-13 ジェンザイム・コーポレーション トロポミオシン関連キナーゼ(trk)阻害剤の医薬製剤
EP4180428A1 (en) * 2021-11-12 2023-05-17 Genzyme Corporation Crystalline imidazo[4,5-b]pyridine compound, pharmaceutical compositions, and their use in treating medical conditions

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