PE20171789A1 - Inhibidores del factor beta de crecimiento de transformacion (tgf-beta) - Google Patents

Inhibidores del factor beta de crecimiento de transformacion (tgf-beta)

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Publication number
PE20171789A1
PE20171789A1 PE2017001481A PE2017001481A PE20171789A1 PE 20171789 A1 PE20171789 A1 PE 20171789A1 PE 2017001481 A PE2017001481 A PE 2017001481A PE 2017001481 A PE2017001481 A PE 2017001481A PE 20171789 A1 PE20171789 A1 PE 20171789A1
Authority
PE
Peru
Prior art keywords
beta
tgf
growth factor
haloalkyl
alkyl
Prior art date
Application number
PE2017001481A
Other languages
English (en)
Inventor
Todd Kinsella
Marina Gelman
Hui Hong
Ihab S Darwish
Rajinder Singh
Jiaxin Yu
Robert M Borzilleri
Upender Velaparthi
Peiying Liu
Chetan Darne
Hasibur Rahaman
Jayakumar Sankara Warrier
Original Assignee
Bristol Myers Squibb Co
Rigel Pharmaceuticals 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 Bristol Myers Squibb Co, Rigel Pharmaceuticals Inc filed Critical Bristol Myers Squibb Co
Publication of PE20171789A1 publication Critical patent/PE20171789A1/es

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    • 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
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    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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

Abstract

Referido a un compuesto que tiene la estructura de formula (I°) donde X es -S- o -N(R´)-; R´es hidrogeno, alquilo C1-C6, haloalquilo C1-C6, entre otros, R1 es hidrogeno, alquilo C1-C6, haloalquilo C1-C6, alcoxi C1-C6; A es fenilo opcionalmente sustituido con uno a cinco grupos R2, en donde cada R2 es independientemente hidrogeno, -alquilo C1-C6, haloalquilo C1-C6, entre otros; Z es un anillo biciclico fusionado. Dicho compuesto puede ser una sal, profarmaco, o N-oxido. Estas composiciones farmaceuticas inhiben al Factor-beta de crecimiento de Transformacion (TGF-Beta). Dichas composiciones son utiles como quimioterapeuticos, artritis, enfermedad renal cronica u otra enfermedad o condicion que sea mediada o involucra a TGF-Beta.
PE2017001481A 2015-03-02 2016-02-26 Inhibidores del factor beta de crecimiento de transformacion (tgf-beta) PE20171789A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562127109P 2015-03-02 2015-03-02

Publications (1)

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PE20171789A1 true PE20171789A1 (es) 2017-12-28

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PE2017001481A PE20171789A1 (es) 2015-03-02 2016-02-26 Inhibidores del factor beta de crecimiento de transformacion (tgf-beta)

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US (3) US9884868B2 (es)
EP (1) EP3265454B1 (es)
JP (1) JP6836998B2 (es)
KR (1) KR20170122799A (es)
CN (1) CN107406412B (es)
AR (1) AR103828A1 (es)
AU (1) AU2016226468B2 (es)
BR (1) BR112017017135A2 (es)
CA (1) CA2973602A1 (es)
CL (1) CL2017002207A1 (es)
CO (1) CO2017009891A2 (es)
EA (1) EA037112B1 (es)
ES (1) ES2789331T3 (es)
HK (1) HK1244785A1 (es)
IL (1) IL254187A0 (es)
MX (1) MX371167B (es)
MY (1) MY186133A (es)
PE (1) PE20171789A1 (es)
PH (1) PH12017501326A1 (es)
SG (1) SG11201705821XA (es)
TN (1) TN2017000374A1 (es)
TW (1) TW201639827A (es)
WO (1) WO2016140884A1 (es)
ZA (1) ZA201705527B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2789331T3 (es) 2015-03-02 2020-10-26 Rigel Pharmaceuticals Inc Inhibidores de TGF-beta
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
CA3045947A1 (en) 2016-12-08 2018-06-14 Michael J. Soth Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease
US10961239B2 (en) 2017-01-05 2021-03-30 Bristol-Myers Squibb Company TGF beta receptor antagonists
NZ755835A (en) 2017-01-17 2023-12-22 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
JP2020512400A (ja) * 2017-03-23 2020-04-23 クラヴィウス ファーマシューティカルズ，エルエルシー ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法
CN109293652B (zh) * 2017-07-24 2021-10-22 四川科伦博泰生物医药股份有限公司 一种取代的噻唑衍生物及其用途
GB201718285D0 (en) 2017-11-03 2017-12-20 Discuva Ltd Antibacterial Compounds
AU2019246220B2 (en) 2018-03-29 2020-10-08 Masarykova Univerzita 4—(1h— imidazol— 5— yl) -1h-pyrrolo (2, 3-b) pyridines for use in the treatment of leukaemias, lymphomas and solid tumors
EP3840748A4 (en) 2018-08-22 2022-06-29 Clavius Pharmaceuticals, LLC Substituted imidazoles for the inhibition of tgf-beta and methods of treatment
AU2019396360A1 (en) * 2018-12-11 2021-05-27 Theravance Biopharma R&D Ip, Llc Naphthyridine and quinoline derivatives useful as ALK5 inhibitors
CN111825658A (zh) * 2019-04-18 2020-10-27 华东理工大学 新型egfr三突变抑制剂及其应用
US11560366B2 (en) 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease
TW202132297A (zh) * 2019-11-22 2021-09-01 美商施萬生物製藥研發Ｉｐ有限責任公司 經取代吡啶及使用方法
JP2023506768A (ja) 2019-12-12 2023-02-20 ティン セラピューティックス エルエルシー 聴覚損失の予防及び治療のための組成物及び方法
TW202214623A (zh) * 2020-06-10 2022-04-16 美商施萬生物製藥研發 Ip有限責任公司 結晶型alk5抑制劑及其用途
CN112321592B (zh) * 2020-11-12 2022-03-04 山东省科学院菏泽分院 一种6-氯咪唑并[1,2-b]哒嗪-3-甲腈的合成方法
WO2022251359A1 (en) * 2021-05-26 2022-12-01 Theravance Biopharma R&D Ip, Llc Bicyclic inhibitors of alk5 and methods of use
CN117999077A (zh) * 2021-07-28 2024-05-07 株式会社蒂奥姆生物 用于预防或治疗肿瘤的药物组合物及其用途

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ513642A (en) 1999-01-21 2004-02-27 Metamorphix Inc Growth differentiation factor inhibitors and uses therefor
AU2002225730A1 (en) * 2000-11-16 2002-05-27 Smith Kline Beecham Corporation Compounds
MXPA03008142A (es) 2001-03-09 2003-12-12 Pfizer Prod Inc Nuevos compuestos antiinflamatorios de bencimidazol.
US7320789B2 (en) 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
EP1554272B1 (en) 2002-08-09 2006-10-25 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
TWI332003B (en) * 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
US7863310B2 (en) 2004-02-03 2011-01-04 Eli Lilly And Company Kinase inhibitors
TWI380996B (zh) 2004-09-17 2013-01-01 Hoffmann La Roche 抗ｏｘ４０ｌ抗體
ES2432091T5 (es) 2005-03-25 2022-03-18 Gitr Inc Moléculas de unión GITR y usos de las mismas
KR101386494B1 (ko) 2005-05-10 2014-04-24 인사이트 코포레이션 인돌아민 2,3-디옥시게나제의 조절제 및 이의 사용방법
CN104356236B (zh) 2005-07-01 2020-07-03 E.R.施贵宝&圣斯有限责任公司 抗程序性死亡配体1(pd-l1)的人单克隆抗体
US7473784B2 (en) * 2005-08-01 2009-01-06 Bristol-Myers Squibb Company Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors
JP5294874B2 (ja) 2005-12-20 2013-09-18 インサイト・コーポレイション インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロ環
MX2008008320A (es) 2005-12-23 2008-09-03 Smithkline Beecham Corp Inhibidores de azaindol de aurora cinasas.
CA2636077C (en) * 2006-01-18 2012-01-03 Amgen Inc. Thiazole compounds as protein kinase b (pkb) inhibitors
WO2008036642A2 (en) 2006-09-19 2008-03-27 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
EP1987839A1 (en) 2007-04-30 2008-11-05 I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease
BRPI0811065A2 (pt) * 2007-06-08 2014-12-02 Abbott Lab Indazóis 5-heteroaril substituídos como inibidores de quinase
US8188083B2 (en) * 2007-06-28 2012-05-29 Abbott Laboratories Triazolopyridazines
ES2591281T3 (es) 2007-07-12 2016-11-25 Gitr, Inc. Terapias de combinación que emplean moléculas de enlazamiento a GITR
EP2044949A1 (en) 2007-10-05 2009-04-08 Immutep Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
EP2227233B1 (en) 2007-11-30 2013-02-13 Newlink Genetics Ido inhibitors
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
PE20120341A1 (es) 2008-12-09 2012-04-24 Genentech Inc Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t
US8709424B2 (en) 2009-09-03 2014-04-29 Merck Sharp & Dohme Corp. Anti-GITR antibodies
WO2011056652A1 (en) 2009-10-28 2011-05-12 Newlink Genetics Imidazole derivatives as ido inhibitors
ES2722300T3 (es) 2009-12-10 2019-08-09 Hoffmann La Roche Anticuerpos que se unen preferentemente al dominio extracelular 4 de CSF1R y su uso
CA2791658C (en) 2010-03-04 2019-10-01 Macrogenics, Inc. Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof
RU2617966C2 (ru) 2010-03-05 2017-04-28 Ф.Хоффманн-Ля Рош Аг Антитела против csf-1r человека и их применение
US9169323B2 (en) 2010-03-05 2015-10-27 Hoffmann-La Roche Inc. Antibodies against human CSF-1R
WO2011140249A2 (en) 2010-05-04 2011-11-10 Five Prime Therapeutics, Inc. Antibodies that bind csf1r
US8980933B2 (en) 2010-05-05 2015-03-17 Universitat Bayreuth Combretastatin analogs for use in the treatment of cancer
SG10201506906VA (en) 2010-09-09 2015-10-29 Pfizer 4-1bb binding molecules
JP2014500277A (ja) 2010-12-09 2014-01-09 アムジエン・インコーポレーテツド Ｐｉｍ阻害剤としての二環式化合物
NO2694640T3 (es) 2011-04-15 2018-03-17
CA2833636A1 (en) 2011-04-20 2012-10-26 Amplimmune, Inc. Antibodies and other molecules that bind b7-h1 and pd-1
EP2543372A1 (en) 2011-07-08 2013-01-09 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for the treatment of liver cancer
EP3111937B1 (en) * 2011-07-08 2020-06-17 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for treatment of liver cancer
EP2751105A1 (en) 2011-09-01 2014-07-09 Irm Llc Compounds and compositions as c-kit kinase inhibitors
BR112014010368A2 (pt) 2011-10-31 2017-04-25 Xenon Pharmaceuticals Inc biaril éter sulfonamidas e seu uso como agentes terapêuticos
LT2785375T (lt) 2011-11-28 2020-11-10 Merck Patent Gmbh Anti-pd-l1 antikūnai ir jų panaudojimas
WO2013086029A1 (en) * 2011-12-05 2013-06-13 Primorigen Biosciences Inc. Compositions and methods for differentiating pluripotent stem cells into primitive blood cells and uses thereof
WO2013086397A1 (en) 2011-12-08 2013-06-13 Array Biopharma Inc. Urea compounds as gka activators
CN104159921B (zh) 2011-12-15 2018-05-04 霍夫曼-拉罗奇有限公司 针对人csf-1r的抗体及其用途
RU2014136332A (ru) 2012-02-06 2016-03-27 Дженентек, Инк. Композиции и способы применения ингибиторов csf1r
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
US10280168B2 (en) 2012-03-30 2019-05-07 Agency For Science, Technology And Research Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
RU2670743C9 (ru) 2012-05-11 2018-12-19 Файв Прайм Терапьютикс, Инк. Способы лечения состояний антителами, которые связывают рецептор колониестимулирующего фактора 1 (csf1r)
UY34887A (es) 2012-07-02 2013-12-31 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos
RU2718751C2 (ru) 2012-08-31 2020-04-14 Файв Прайм Терапьютикс, Инк. Способы лечения патологических состояний антителами, которые связываются с рецептором колониестимулирующего фактора 1 (csf1r)
EA201590693A1 (ru) * 2012-10-05 2015-08-31 Ригель Фармасьютикалс, Инк. Ингибиторы gdf-8
US9556179B2 (en) * 2012-12-21 2017-01-31 Bristol-Myers Squibb Company Substituted imidazoles as casein kinase 1 D/E inhibitors
CN103936730A (zh) 2013-01-22 2014-07-23 通化济达医药有限公司 苯磺酰胺噻唑激酶抑制剂
CN103275112A (zh) 2013-05-11 2013-09-04 济南韶远医药技术有限公司 一种利用微反应器连续合成芳基硼酸酯的方法
SG11201509338QA (en) * 2013-05-30 2015-12-30 Plexxikon Inc Compounds for kinase modulation, and indications therefor
US20160199372A1 (en) 2013-08-20 2016-07-14 Bristol-Myers Squibb Company Imidazopyridazine kinase inhibitors useful to treating a disease or disorder mediated by aak1, such as alzheimer's disease, bipolar disorder, pain, schizophrenia
ES2789331T3 (es) 2015-03-02 2020-10-26 Rigel Pharmaceuticals Inc Inhibidores de TGF-beta

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