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AR049293A1 - Derivados de aril y heteroaril sustituidos como moduladores del metabolismo y la prevencion de trastornos relacionados - Google Patents

Derivados de aril y heteroaril sustituidos como moduladores del metabolismo y la prevencion de trastornos relacionados

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Publication number
AR049293A1
AR049293A1 ARP050102283A ARP050102283A AR049293A1 AR 049293 A1 AR049293 A1 AR 049293A1 AR P050102283 A ARP050102283 A AR P050102283A AR P050102283 A ARP050102283 A AR P050102283A AR 049293 A1 AR049293 A1 AR 049293A1
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AR
Argentina
Prior art keywords
alkyl
haloalkyl
dialkyl
cycloalkyl
sulfonamide
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ARP050102283A
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English (en)
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Arena Pharm Inc
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Publication of AR049293A1 publication Critical patent/AR049293A1/es

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Abstract

Los compuestos de la presente son utiles para el tratamiento de trastornos relacionados con el metabolismo y sus complicaciones, tales como diabetes y obesidad. Reivindicacion 1: Un compuesto de formula (1), o una sal, solvato, hidrato o N-oxido aceptable para uso farmacéutico del mismo; en donde: A1 y A2 son independientemente alquileno C1-3 opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en alquilo C1-6, alcoxi C1-6, y carboxi; D es CR1R2 o NR2, en donde R1 se selecciona del grupo que consiste en H, alquilo C1-6, alcoxi C1-6, halogeno e hidroxilo; E es N, C, o CR3, en donde R3 es H o alquilo C1-6; la línea punteada es un enlace simple cuando E es N o CR3, o un doble enlace cuando E es C; K está ausente, es un grupo cicloalquileno C3-6, o alquileno C1-3, cada uno opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en alquilo C1-6, alcoxi C1-6, carboxi, ciano y halogeno; Q1 es NR4, O, S, S(O), o S(O)2, en donde R4 es H, acilo C1-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, o cicloalquil C3-7-alquileno C1-3, en donde dicho alquilo C1-6 está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1-6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, dialquil C1-6amino, alcoxi C1-6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1- 6sulfonamida, dialquil C1-6tiocarboxamida, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, hidroxilo, hidroxilamino y nitro; Q2 es NR5 u O, en donde R5 es H, acilo C1-6, alquilo C1- 6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, o cicloalquil C3-7-alquileno C1-3, en donde dicho alquilo C1-6 está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1-6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, dialquil C1-6amino, alcoxi C1-6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1-6sulfonamida, dialquil C1-6tiocarboxamida, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, hidroxilo, hidroxilamino y nitro; W es N o CH; X es N o CR6; Y es N o CR7; Z es N o CR8; V está ausente, es heteroalquileno C1-3, o alquileno C1-3 en donde cada uno está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en alquilo C1-3, alcoxi C1-6, carboxi, ciano, haloalquilo C1-3, y halogeno; R6, R7, y R8 se selecciona cada uno independientemente del grupo que consiste en H, acilo C1-6, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1-6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1- 6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, dialquil C1-6amino, alcoxi C1-6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1-6sulfonamida, dialquil C1-6tiocarboxamida, haloalcoxi C1- 6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, hidroxilo, hidroxilamino y nitro, en donde dichos alquenilo C2-6, alquilo C1-6, alquinilo C2-6 y cicloalquilo C3-6 están cada uno opcionalmente sustituidos con uno o más sustituyentes independientemente seleccionados del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1-6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, dialquil C1-6amino, alcoxi C1-6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1- 6carboxamida, dialquil C1-6sulfonamida, dialquil C1-6tiocarboxamida, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, hidroxilo, hidroxilamino y nitro; Ar es arilo o heteroarilo opcionalmente sustituido con R9, R10, R11, R12, y R13; R9 se selecciona del grupo que consiste en acilo C1-6, acil C1-6sulfonamida, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1-6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, arilo, arilcarbonilo, arilsulfonilo, dialquil C1-6amino, carbamimidoílo, alcoxi C1- 6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1-6sulfonamida, dialquil C1-6tiocarboxamida, guanidina, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, heterocíclico, heterocíclicosulfonilo, heteroarilo, hidroxilo, hidroxilamino, nitro, oxo-cicloalquilo C3-6, fenoxi, sulfonamida, ácido sulfonico y tiol; y en donde cada R9 está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en acilo C1-6, acil C1-6sulfonamida, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1- 6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, arilo, arilcarbonilo, arilsulfonilo, dialquil C1-6amino, alcoxi C1-6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1-6sulfonamida, dialquil C1-6tiocarboxamida, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, heteroarilo, heteroarilcarbonilo, heteroarilsulfonilo, heterocíclico, hidroxilo, hidroxilamino y nitro; R10, R11, R12, y R13 se seleccionan independientemente del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquilamino C1-6, alquilcarboxamida C1-6, alquinilo C2-6, alquilsulfonamida C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquiltio C1-6, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, di-alquil C1-6amino, alcoxi C1- 6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, di-alquil C1-6carboxamida, di-alquil C1-6sulfonamida, di-alquil C1-6tiocarboxamida, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, hidroxilo, hidroxilamino, nitro, y tiol; o dos grupos adyacentes R10, R11, R12 y R13 junto con los átomos con los que están unidos forman un cicloalquilo de 5, 6 o 7 miembros, cicloalquenilo de 5, 6 o 7 miembros, o un grupo heterocíclico de 5, 6 o 7 miembros en donde el grupo de 5, 6 o 7 miembros está opcionalmente sustituido con halogeno u oxo; y R2 se selecciona del grupo que consiste en H, acilo C1-6, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1-6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, arilo, arilcarbonilo, ariloxi, dialquil C1-6amino, carbamimidoílo, alcoxi C1-6carbonilo, cicloalcoxi C3-7carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1-6sulfonamida, dialquil C1-6tiocarboxamida, guanidina, haloalcoxi C1-6, haloalquilo C1- 6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, heteroarilo, heteroarilalquileno C1-3, heteroarilcarbonilo, heteroariloxi, heterocíclicocarboxamida, hidroxilo, hidroxilamino y nitro; en donde cada R2 está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-6, alcoxi C1-6, alquilo C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquinilo C2-6, alquil C1- 6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6tiocarboxamida, alquil C1-6tioureilo, alquil C1-6ureilo, amino, arilo, dialquil C1-6amino, alcoxi C1-6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1-6sulfonamida, dialquil C1-6tiocarboxamida, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, heterocíclico, heteroarilo, hidroxilo, hidroxilamino y nitro, y en donde alquilo C1-6 está además opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que consiste en acilo C1-6, alcoxi C1-6, alquil C1-6amino, alquil C1-6carboxamida, alquil C1- 6sulfonamida, alquil C1-6sulfinilo, alquil C1-6sulfonilo, alquil C1-6tio, alquil C1-6ureilo, amino, dialquil C1-6amino, alcoxi C1-6carbonilo, carboxamida, carboxi, ciano, cicloalquilo C3-6, dialquil C1-6carboxamida, dialquil C1-6sulfonamida, haloalcoxi C1-6, haloalquilo C1-6, halogeno, haloalquil C1-6sulfinilo, haloalquil C1-6sulfonilo, haloalquil C1-6tio, heterocíclico, hidroxilo, hidroxilamino y nitro; siempre que el compuesto no sea el éster isopropilo del ácido 4-[6-(2-fluoro-4- metansulfonil-fenoxi)-pirimidin-4-iloxi]-piperidin-1-carboxílico.
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Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2295816T3 (es) 2003-01-14 2008-04-16 Arena Pharmaceuticals, Inc. Derivados arilo y heteroarilo 1,2,3-trisustituidos como moduladores del metabolismo, y profilaxis y tratamiento de transtornos relacionados con los mismos, tales como la diabetes y la hiperglucemia.
AR045047A1 (es) 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
KR20070091038A (ko) * 2004-12-24 2007-09-06 프로시디온 리미티드 Ｇ-단백질 결합 수용체(ｇｐｒ116) 효능제 및 비만 및당뇨병을 치료하기 위한 이의 용도
DOP2006000008A (es) * 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
MY148521A (en) 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
AU2006255465A1 (en) * 2005-06-09 2006-12-14 Merck Frosst Canada Ltd Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
MX2007016508A (es) * 2005-06-30 2008-03-04 Prosidion Ltd Agonistas del receptor acoplado a la proteina g.
DE602006006461D1 (de) * 2005-09-16 2009-06-04 Arena Pharm Inc Stoffwechselmodulatoren und behandlung damit verbundener erkrankungen
PE20071221A1 (es) * 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
US7833730B2 (en) 2006-04-11 2010-11-16 Arena Pharmaceuticals, Inc. Methods of using GPR119 to identify compounds useful for increasing bone mass in an individual
TW200811147A (en) 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
TW200811140A (en) * 2006-07-06 2008-03-01 Arena Pharm Inc Modulators of metabolism and the treatment of disorders related thereto
CA2661371A1 (en) * 2006-08-30 2008-03-06 Biovitrum Ab (Publ) Pyrimidine compounds for treating gpr119 related disorders
DK2076508T3 (da) 2006-10-18 2011-02-21 Pfizer Prod Inc Biaryl-ether-urinstof-forbindelser
JP5330260B2 (ja) 2006-12-06 2013-10-30 スミスクライン ビーチャム コーポレーション 二環式化合物ならびに抗糖尿病薬としての使用
JP4782239B2 (ja) 2007-04-18 2011-09-28 ファイザー・プロダクツ・インク 異常細胞増殖治療のためのスルホニルアミド誘導体
EP2152707B1 (en) 2007-05-04 2012-06-20 Bristol-Myers Squibb Company [6,5]-bicyclic gpr119 g protein-coupled receptor agonists
ES2388967T3 (es) 2007-05-04 2012-10-22 Bristol-Myers Squibb Company Agonistas [6,6]- y [6,7]-bicíclicos del receptor GPR119 acoplado a la proteína G
JP5318867B2 (ja) 2007-07-17 2013-10-16 ブリストル−マイヤーズ スクイブ カンパニー ピリドンｇｐｒ１１９ｇタンパク質共役受容体アゴニスト
CN101801954B (zh) 2007-09-20 2013-10-09 Irm责任有限公司 作为gpr119活性调节剂的化合物和组合物
AU2008312948C1 (en) * 2007-10-16 2012-08-09 Daiichi Sankyo Company, Limited Pyrimidyl indoline compound
MX2010004450A (es) 2007-10-22 2010-05-05 Schering Corp Derivados heterociclo biciclicos y su uso como moduladores de la actividad de gpr119.
WO2009063364A2 (en) * 2007-11-13 2009-05-22 Encysive Pharmaceuticals Inc. Modulators of urotensin receptor and methods of use thereof
CA2714703A1 (en) * 2008-02-22 2009-08-27 Irm Llc Compounds and compositions as modulators of gpr119 activity
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
WO2009129036A1 (en) * 2008-04-14 2009-10-22 Merck & Co., Inc. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
TW201006821A (en) * 2008-07-16 2010-02-16 Bristol Myers Squibb Co Pyridone and pyridazone analogues as GPR119 modulators
WO2010048149A2 (en) * 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US20100113479A1 (en) * 2008-10-30 2010-05-06 Anusuya Choudhury Process for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives useful as gdir agonists
JP2012513470A (ja) 2008-12-23 2012-06-14 シェーリング コーポレイション 二環式複素環誘導体及びその使用方法
US8722882B2 (en) 2008-12-23 2014-05-13 Merck Sharp & Dohme Corp. Pyrimidine derivatives as GPCR modulators for use in the treatment of obesity and diabetes
CN102333528B (zh) * 2009-01-26 2013-12-18 台北医学大学 蕨素化合物用于治疗糖尿病及肥胖之用途
JP5657518B2 (ja) * 2009-02-18 2015-01-21 武田薬品工業株式会社 縮合複素環化合物
JP2012520868A (ja) * 2009-03-20 2012-09-10 ファイザー・インク ３−オキサ−７−アザビシクロ［３．３．１］ノナン
US8580807B2 (en) 2009-04-03 2013-11-12 Merck Sharp & Dohme Corp. Bicyclic piperidine and piperazine derivatives as GPCR modulators for the treatment of obesity, diabetes and other metabolic disorders
WO2010119881A1 (ja) * 2009-04-15 2010-10-21 第一三共株式会社 インドリン化合物
AR077214A1 (es) 2009-06-24 2011-08-10 Neurocrine Biosciences Inc Heterociclos nitrogenados y composiciones farmaceuticas que los contienen
NZ596445A (en) 2009-06-24 2013-04-26 Boehringer Ingelheim Int New compounds, pharmaceutical composition and methods relating thereto
US8552022B2 (en) 2009-08-13 2013-10-08 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
JP2013511571A (ja) * 2009-11-23 2013-04-04 ファイザー・インク Ｇｐｒ１１９阻害剤としてのイミダゾ−ピラゾール
SG10201500639TA (en) 2010-01-27 2015-03-30 Arena Pharm Inc Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof
WO2011113947A1 (en) 2010-03-18 2011-09-22 Boehringer Ingelheim International Gmbh Combination of a gpr119 agonist and the dpp-iv inhibitor linagliptin for use in the treatment of diabetes and related conditions
CN102933576A (zh) 2010-04-08 2013-02-13 百时美施贵宝公司 作为gpr119调节剂的嘧啶基哌啶基氧基吡啶酮类似物
BR112012028445A2 (pt) 2010-05-06 2016-07-19 Bristol Myers Squibb Co compostos de heteroarila bicíclica como moduladores de gpr119
US8729084B2 (en) 2010-05-06 2014-05-20 Bristol-Myers Squibb Company Benzofuranyl analogues as GPR119 modulators
RU2012154308A (ru) 2010-05-17 2014-06-27 Эррэй Биофарма Инк. Пиперидинил-замещенные лактамы как модуляторы gpr119
WO2012025811A1 (en) 2010-08-23 2012-03-01 Lupin Limited Indolylpyrimidines as modulators of gpr119
EP2619198A1 (en) * 2010-09-22 2013-07-31 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
AR083575A1 (es) 2010-11-08 2013-03-06 Lilly Co Eli Aminopirazoles para inhibir la proteinquinasa chk1
EP2643311A1 (en) 2010-11-26 2013-10-02 Lupin Limited Bicyclic gpr119 modulators
ES2602813T3 (es) 2011-06-09 2017-02-22 Rhizen Pharmaceuticals S.A. Nuevos compuestos como moduladores de GPR-119
CA2841757A1 (en) 2011-07-15 2013-01-24 Etzer Darout Gpr 119 modulators
US20140256756A1 (en) * 2011-11-03 2014-09-11 Array Biopharma Inc. Piperidinyl-substituted lactams as gpr119 modulators
CN104024246B (zh) * 2012-03-27 2016-03-02 广东东阳光药业有限公司 作为欧若拉激酶抑制剂的取代嘧啶衍生物
MX371331B (es) 2012-04-24 2020-01-27 Vertex Pharma Inhibidores de la proteina cinasa dependiente de acido desoxirribonucleico(adn-pk).
EP2850073B1 (en) 2012-05-16 2017-07-19 Bristol-Myers Squibb Company Pyrimidinylpiperidinyloxypyridone analogues as gpr119 modulators
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
GB2516303A (en) * 2013-07-18 2015-01-21 Redx Pharma Ltd Compounds
DK3424920T3 (da) 2013-10-17 2020-06-08 Vertex Pharma Co-krystaller af (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinolin-4-carboxamid og deuterede derivater deraf som dna-pk-inhibitorer
AR098394A1 (es) * 2013-11-25 2016-05-26 Lilly Co Eli Inhibidores de dgat2 (diacilglicerol o-aciltransferasa 2)
NZ729137A (en) * 2014-08-04 2022-07-29 Nuevolution As Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
PL3242666T3 (pl) 2015-01-06 2025-02-17 Arena Pharmaceuticals, Inc. Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1
JP6838744B2 (ja) 2015-06-22 2021-03-03 アリーナ ファーマシューティカルズ， インコーポレイテッド Ｓ１Ｐ１レセプター関連障害における使用のための（Ｒ）−２−（７−（４−シクロペンチル−３−（トリフルオロメチル）ベンジルオキシ）−１，２，３，４−テトラヒドロシクロペンタ［ｂ］インドール−３−イル）酢酸（化合物１）の結晶性Ｌ−アルギニン塩
GB201514021D0 (en) 2015-08-07 2015-09-23 Arner Elias Set Jeno Novel Pyridines and their use in the treatment of cancer
WO2017121700A1 (de) 2016-01-15 2017-07-20 Bayer Pharma Aktiengesellschaft 1,3-disubstituierte 1h-pyrazolo[3,4-b]pyridin- derivate und ihre verwendung als stimulatoren der löslichen guanylatcyclase
US10906894B2 (en) 2016-06-09 2021-02-02 Pramana Pharmaceuticals Inc. Compounds containing benzo[d][1,3]oxathiole, benzo[d][1,3]oxathiole 3-oxide or benzo[d][1,3]oxathiole 3,3-dioxide and methods/uses thereof as agonists of g protein-coupled receptor 119
JP2019529475A (ja) 2016-09-27 2019-10-17 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ損傷剤とｄｎａ−ｐｋ阻害剤との組合せ物を使用する、がんを処置するための方法
EP3580203A1 (en) 2017-02-07 2019-12-18 Oblique Therapeutics AB Hydrocarbylsulfonyl-substituted pyridines and their use in the treatment of cancer
KR20190115011A (ko) 2017-02-07 2019-10-10 오블리크 세러퓨틱스 에이비 설피닐피리딘 및 암의 치료에서 이의 용도
BR112019016223A2 (pt) 2017-02-07 2020-04-07 Oblique Therapeutics Ab piridinas substituídas por heteroarilsulfonila e uso das mesmas no tratamento de câncer
US11168069B2 (en) 2017-02-07 2021-11-09 Oblique Therapeutics Ab Heterocyclylsulfonyl-substituted pyridines and their use in the treatment of cancer
AU2018220521A1 (en) 2017-02-16 2019-09-05 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
MX2021011775A (es) 2017-04-26 2023-01-10 Basilea Pharm Int Ag Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos.
MA49456A (fr) 2017-06-19 2020-04-29 Arena Pharm Inc Composés et procédés pour le traitement de nafld et de nash
WO2019104418A1 (en) 2017-11-30 2019-06-06 Pramana Pharmaceuticals Inc. Compounds containing polysubstituted benzo[d][1,3]oxathiole, benzo[d][1,3]oxathiole 3-oxide or benzo[d][1,3]oxathiole 3,3-dioxide and methods/uses thereof as agonists of g protein-coupled receptor 119
KR102859841B1 (ko) 2018-06-06 2025-09-12 아레나 파마슈티칼스, 인크. S1p1 수용체와 관련된 병태의 치료 방법
CN114127057B (zh) 2019-05-10 2024-07-12 德西费拉制药有限责任公司 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法
EP4295846A3 (en) 2019-05-10 2024-02-28 Deciphera Pharmaceuticals, LLC Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
US11590134B2 (en) 2019-06-17 2023-02-28 Deciphera Pharmaceuticals, Llc Aminopyrimidine amide autophagy inhibitors and methods of use thereof
JP2021098692A (ja) 2019-12-20 2021-07-01 ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ 核内受容体に対して活性の化合物
JP7746259B2 (ja) 2019-12-20 2025-09-30 ヌエヴォリューション・アクティーゼルスカブ 核内受容体に対して活性の化合物
US11613532B2 (en) 2020-03-31 2023-03-28 Nuevolution A/S Compounds active towards nuclear receptors
US11780843B2 (en) 2020-03-31 2023-10-10 Nuevolution A/S Compounds active towards nuclear receptors
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Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH478818A (de) * 1965-10-22 1969-09-30 Ciba Geigy Verfahren zur Herstellung neuer N,N'-Di-(pyrimidyl-(4)-aminoalkyl)-diazacycloalkanen
CH480410A (de) * 1967-01-09 1969-10-31 Geigy Ag J R Verfahren zur Herstellung von wasserlöslichen Azopyrimidinfarbstoffen
CA961052A (en) * 1967-01-12 1975-01-14 Max Schellenbaum N-2-ethylhexyl-n'-aryl ureas and preparation containing them
US3608087A (en) * 1968-06-21 1971-09-21 Merck & Co Inc Feed compositions
US3887329A (en) * 1969-05-05 1975-06-03 Ciba Geigy Ag Hexamethyl phosphotriamide-dye compositions
US3686238A (en) * 1970-01-19 1972-08-22 Syntex Corp Glycerol esterified with 2-naphthyl-acetic acids and fatty acids
US3852434A (en) * 1970-09-11 1974-12-03 Merck & Co Inc Potentiation of ({31 ) cis-1,2-epoxypropyl)phosphonic acid and analogues thereof
US3966744A (en) * 1971-01-11 1976-06-29 Syva Company Spin labeled compounds
US3690834A (en) * 1971-01-11 1972-09-12 Syva Co Ligand determination with spin labeled compounds by receptor displacement
DE2106585A1 (de) * 1971-02-11 1972-08-24 Farbenfabriken Bayer Ag, 5090 Leverkusen Aminothiodiazole und Thiodiazol-Azofarbstoffe
US3966764A (en) * 1972-07-10 1976-06-29 Syva Company Ligand determination of spin labeled compounds by receptor displacement-amphetamine analogs
US3849420A (en) * 1972-10-20 1974-11-19 Dow Chemical Co Bis-(alkylthio-and alkylsulfonyl)-pentachloroquinolines
CH574206A5 (es) * 1972-11-16 1976-04-15 Ciba Geigy Ag
DE2340569C2 (de) * 1973-08-10 1982-12-02 Bayer Ag, 5090 Leverkusen Azofarbstoffe
AT340933B (de) * 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
US4101541A (en) * 1973-12-21 1978-07-18 Ciba-Geigy Corporation 3-Cyano-1,2,4-thiadiazolyl-5-czo dyestuffs
FR2306697A1 (fr) * 1975-04-10 1976-11-05 Sogeras Nouvelles pyrimidines utilisables comme medicaments antidiabetiques et hypocholesterolemiants
DE2731264A1 (de) * 1977-07-11 1979-02-01 Boehringer Mannheim Gmbh Neue 1-acyl-2-cyanaziridine, verfahren zu deren herstellung und diese verbindungen enthaltende pharmazeutische zubereitungen
JPS6038696B2 (ja) * 1977-12-09 1985-09-02 コニカ株式会社 ハロゲン化銀カラ−写真感光材料
US4242507A (en) * 1978-02-23 1980-12-30 Fujisawa Pharmaceutical Co., Ltd. Sulfonic acid esters
DE2831580C2 (de) * 1978-07-18 1980-09-18 Boehringer Mannheim Gmbh, 6800 Mannheim Verfahren und Reagens zur Bestimmung von Glycerin
DE2906603A1 (de) * 1979-02-21 1980-09-04 Boehringer Mannheim Gmbh N-substituierte aziridin-2-carbonsaeurederivate, verfahren zu deren herstellung sowie diese substanzen enthaltende arzneimittel
DOP1981004033A (es) * 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
DE3334455A1 (de) * 1983-03-04 1984-09-06 Bayer Ag, 5090 Leverkusen Guanidin - derivate
ZA848275B (en) * 1983-12-28 1985-08-28 Degussa New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring
DE3601196A1 (de) * 1986-01-17 1987-07-23 Merck Patent Gmbh 1,4-dihydropyridine
TW574214B (en) * 1994-06-08 2004-02-01 Pfizer Corticotropin releasing factor antagonists
NZ292269A (en) * 1994-09-09 1998-09-24 Nippon Shinyaku Co Ltd Heterocyclic amine derivatives and medicaments therefrom
US5691364A (en) * 1995-03-10 1997-11-25 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
US6403599B1 (en) * 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
US6956047B1 (en) * 1995-06-06 2005-10-18 Pfizer Inc. Corticotropin releasing factor antagonists
US5849759A (en) * 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
US5948786A (en) * 1996-04-12 1999-09-07 Sumitomo Pharmaceuticals Company, Limited Piperidinylpyrimidine derivatives
AR008789A1 (es) * 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
US6008234A (en) * 1996-09-12 1999-12-28 Berlex Laboratories, Inc. Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants
AU2298899A (en) * 1998-02-05 1999-08-23 Takeda Chemical Industries Ltd. Sulfonamide derivatives, process for producing the same and utilization thereof
US6187777B1 (en) * 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
US6239126B1 (en) * 1998-12-17 2001-05-29 American Home Products Corporation Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
HUP0202682A3 (en) * 1999-09-10 2003-03-28 Merck & Co Inc Tyrosine kinase inhibitors, pharmaceutical compositions containing them and their use
US6414002B1 (en) * 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
US20020137755A1 (en) * 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
US6545017B1 (en) * 2000-12-08 2003-04-08 3M Innovative Properties Company Urea substituted imidazopyridines
US6525064B1 (en) * 2000-12-08 2003-02-25 3M Innovative Properties Company Sulfonamido substituted imidazopyridines
US6545016B1 (en) * 2000-12-08 2003-04-08 3M Innovative Properties Company Amide substituted imidazopyridines
US6825198B2 (en) * 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
ATE316088T1 (de) * 2001-06-22 2006-02-15 Merck & Co Inc Tyrosin-kinase inhibitoren
EP1406875B1 (en) * 2001-06-26 2013-07-31 Bristol-Myers Squibb Company N-heterocyclic inhibitors of tnf-alpha expression
JP2006507302A (ja) * 2002-10-30 2006-03-02 メルク　エンド　カムパニー　インコーポレーテッド キナーゼ阻害剤
ES2295816T3 (es) * 2003-01-14 2008-04-16 Arena Pharmaceuticals, Inc. Derivados arilo y heteroarilo 1,2,3-trisustituidos como moduladores del metabolismo, y profilaxis y tratamiento de transtornos relacionados con los mismos, tales como la diabetes y la hiperglucemia.
US7265122B2 (en) * 2003-02-28 2007-09-04 Encysive Pharmaceuticals, Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
US7083933B1 (en) * 2003-05-09 2006-08-01 Prosidion Limited Methods for identification of modulators of OSGPR116 activity
AR045047A1 (es) * 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
CA2540640A1 (en) * 2003-09-30 2005-04-14 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7534798B2 (en) * 2004-02-11 2009-05-19 Amgen Inc. Vanilloid receptor ligands and their use in treatments
MY148521A (en) * 2005-01-10 2013-04-30 Arena Pharm Inc Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto

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