AR115927A2 - Derivados de tetrahidro-pirido-pirimidina - Google Patents

Derivados de tetrahidro-pirido-pirimidina

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Publication number
AR115927A2
AR115927A2 ARP190102244A ARP190102244A AR115927A2 AR 115927 A2 AR115927 A2 AR 115927A2 AR P190102244 A ARP190102244 A AR P190102244A AR P190102244 A ARP190102244 A AR P190102244A AR 115927 A2 AR115927 A2 AR 115927A2
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AR
Argentina
Prior art keywords
alkyl
alkylcarbonyl
alkoxy
hydroxy
halo
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ARP190102244A
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English (en)
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Novartis Ag
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
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    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
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    • AHUMAN NECESSITIES
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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicación 1: Un derivado de tetrahidro-pirido-pirimidina de la fórmula (1) y/o las sales farmacéuticamente aceptables del mismo, en donde: Y se selecciona a partir de O ó NR³; R¹ se selecciona a partir de fenilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, 1,2,3-triazinilo, 1,2,4-triazinilo, 1,3,5-triazinilo, o -C(O)-R⁴; en donde: R⁴ se selecciona a partir de alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, alquilo C₁₋₈-sulfonil-alquilo C₁₋₈, heterociclilo, heterocicliloxilo, heterociclil-alquilo C₁₋₈, cicloalquilo C₃₋₁₂, cicloalquilo C₃₋₁₂-alquilo C₁₋₈, heteroarilo, heteroariloxilo, heteroaril-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, o N,N-di-alquilo C₁₋₈-amino; en donde ‘alquilo C₁₋₈’ en N-alquilo C₁₋₈-amino y N,N-di-alquilo C₁₋₈-amino puede estar insustituido o sustituido por halógeno, hidroxilo, o alcoxilo C₁₋₄; en donde ‘cicloalquilo C₃₋₁₂’ en cicloalquilo C₃₋₁₂ y cicloalquilo C₃₋₁₂-alquilo C₁₋₈ puede estar insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de oxo, halógeno, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈-carbonilo; en donde ‘heterociclilo’ se selecciona a partir de oxiranilo, aziridinilo, oxetanilo, tietanilo, azetidinilo, pirrolidinilo, tetrahidro-furanilo, tetrahidro-tiofenilo, 2,3-dihidro-furanilo, 2,5-dihidro-furanilo, 2,3-dihidro-tiofenilo, 1-pirrolinilo, 2-pirrolinilo, 3-pirrolinilo, tetrahidro-piranilo, piperidinilo, tetrahidro-tiopiranilo, morfolinilo, tiomorfolinilo, piperazinilo, azepanilo, tiepanilo u oxepanilo; cada uno de los cuales está insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de oxo, halógeno, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈-carbonilo; en donde ‘heterociclilo’ se puede unir en un heteroátomo o en un átomo de carbono, y en donde los heteroátomos de N y/o S también se pueden oxidar opcionalmente hasta diferentes estados de oxidación; en donde ‘heteroarilo’ se selecciona a partir de: furanilo, tiofenilo, pirrolilo, imidazolilo, pirazolilo, tiazolilo, isotiazolilo, oxazolilo, isoxazolilo, 1,2,5-oxadiazolilo, 1,2,4-oxadiazolilo, 1,2,3-oxadiazolilo, 1,3,4-oxadiazolilo, 1,2,5-tiadiazolilo, 1,2,4-tiadiazolilo, 1,2,3-tiadiazolilo, 1,3,4-tiadiazolilo, 1,2,3-triazolilo, 1,2,4-triazolilo, 1,2,5-triazolilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, 1,2,3-triazinilo, 1,2,4-triazinilo o 1,3,5-triazinilo; cada uno de los cuales está insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de halógeno, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo, hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈-carbonilo; en donde ‘heteroarilo’ se puede unir en un heteroátomo o en un átomo de carbono, y en donde los heteroátomos de N y/o S también se pueden oxidar opcionalmente hasta diferentes estados de oxidación; R² se selecciona a partir de fenilo, naftilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, quinolinilo o isoquinolinilo, cada uno de los cuales está insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de halógeno, ciano, nitro, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈ hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo, hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈-carbonilo; R³ se selecciona a partir de H o alquilo C₁₋₄; y m se selecciona a partir de 0 ó 1.
ARP190102244A 2010-07-06 2019-08-07 Derivados de tetrahidro-pirido-pirimidina AR115927A2 (es)

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ARP110102390A AR084970A1 (es) 2010-07-06 2011-07-04 Derivados de tetrahidro-pirido-pirimidina, una composicion farmaceutica en base al compuesto y un proceso para su preparacion
ARP190102244A AR115927A2 (es) 2010-07-06 2019-08-07 Derivados de tetrahidro-pirido-pirimidina
ARP200101358A AR118919A2 (es) 2010-07-06 2020-05-12 Derivados de tetrahidro-pirido-pirimidina

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AR (3) AR084970A1 (es)
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Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8759362B2 (en) * 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
JO3733B1 (ar) 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
SG195067A1 (en) 2011-06-27 2013-12-30 Novartis Ag Solid forms and salts of tetrahydro-pyrido-pyrimidine derivatives
EP2790705B1 (en) * 2011-12-15 2017-12-06 Novartis AG Use of inhibitors of the activity or function of pi3k
IN2014CN04174A (es) 2011-12-22 2015-09-04 Novartis Ag
EA035391B1 (ru) 2012-11-08 2020-06-05 Ризен Фармасьютикалз Са Фармацевтические композиции, содержащие ингибитор pde4 и ингибитор pi3-дельта или двойной ингибитор pi3-дельта-гамма киназы
EP2920171B1 (en) 2012-11-16 2018-08-29 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
MX2015006192A (es) 2012-11-16 2015-08-10 Merck Sharp & Dohme Inhibidores de purina de fosfatidilinositol 3-quinasa delta humana.
EP2742940B1 (en) 2012-12-13 2017-07-26 IP Gesellschaft für Management mbH Fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-l-aza-bicyclo-[2.2.2]octane for adminstration once daily, twice daily or thrice daily
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
WO2015162584A1 (en) 2014-04-24 2015-10-29 Novartis Ag Crystalline forms of the sulfate salt of n-[5-(3-imidazol-1-yl-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]-acetamide
GB201506786D0 (en) * 2015-04-21 2015-06-03 Ucb Biopharma Sprl Therapeutic use
JP6462155B2 (ja) * 2015-05-04 2019-01-30 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft B型肝炎ウイルス感染症の治療用のHBsAg(HBV表面抗原)及びHBV DNA産生の阻害剤としてのテトラヒドロピリドピリミジン類及びテトラヒドロピリドピリジン類
SG10202109655VA (en) 2015-12-04 2021-10-28 Novartis Ag Compositions and methods for immunooncology
RU2749731C2 (ru) * 2016-02-10 2021-06-16 Новартис Аг Применение ингибиторов активности или функции pi3k для лечения первичного синдрома шегрена
MX2019011272A (es) 2017-03-22 2019-10-24 Novartis Ag Composiciones y metodos para inmunooncologia.
EP3630116B1 (en) 2017-05-26 2024-05-01 The Board Of Regents Of The University Of Texas System Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase
CN111867590B (zh) 2017-07-13 2023-11-17 德州大学系统董事会 Atr激酶的杂环抑制剂
JP7290627B2 (ja) 2017-08-17 2023-06-13 ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム Atrキナーゼの複素環式阻害剤
CN112218631B (zh) 2018-03-16 2023-12-22 德州大学系统董事会 Atr激酶的杂环抑制剂
CN114315826B (zh) * 2021-11-30 2023-05-16 西安交通大学 一种吡啶并嘧啶类化合物及其应用
KR20230160977A (ko) 2022-05-17 2023-11-27 에이치앤오바이오시스(주) 항암 치료에 사용되는 5종 이상의 생약 추출물

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1197466B (de) 1962-03-22 1965-07-29 Thomae Gmbh Dr K Verfahren zur Herstellung von neuen 5, 6, 7, 8-Tetrahydropyrido-[4, 3-d]pyrimidinen
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
US5300645A (en) 1993-04-14 1994-04-05 Eli Lilly And Company Tetrahydro-pyrido-indole
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
EP3103799B1 (en) 1995-03-30 2018-06-06 OSI Pharmaceuticals, LLC Quinazoline derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
CA2224435C (en) 1995-07-06 2008-08-05 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
IL126351A0 (en) 1996-04-12 1999-05-09 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
JP2000512990A (ja) 1996-06-24 2000-10-03 ファイザー・インク 過増殖性疾患を処置するためのフェニルアミノ置換三環式誘導体
NZ334821A (en) 1996-08-30 2000-12-22 Novartis Ag Method for producing epothilones
DE69724269T2 (de) 1996-09-06 2004-06-09 Obducat Ab Verfahren für das anisotrope ätzen von strukturen in leitende materialien
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
DK1367057T3 (da) 1996-11-18 2009-01-19 Biotechnolog Forschung Gmbh Epothiloner E og F
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
US5939421A (en) * 1997-07-01 1999-08-17 Signal Pharmaceuticals, Inc. Quinazoline analogs and related compounds and methods for treating inflammatory conditions
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
CA2322157C (en) 1998-02-25 2012-05-29 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
EP1135470A2 (en) 1998-11-20 2001-09-26 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
NZ535616A (en) 2000-11-07 2006-03-31 Novartis Ag Indolymaleimide derivatives as protein kinase c inhibitors
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
TWI324064B (en) 2002-04-03 2010-05-01 Novartis Ag Indolylmaleimide derivatives
PL376844A1 (pl) 2002-12-09 2006-01-09 The Board Of Regents Of The University Of Texas System Sposoby selektywnego hamowania kinazy tyrozynowej 3 z grupy Janus (JAK3)
JP4733986B2 (ja) 2002-12-27 2011-07-27 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー HIVインテグラーゼ阻害薬として有用なテトラヒドロ−4H−ピリド[1,2−a]ピリミジン類および関連する化合物
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
CN100465173C (zh) 2004-01-12 2009-03-04 西托匹亚研究有限公司 选择性激酶抑制剂
US20050165032A1 (en) * 2004-01-23 2005-07-28 Norman Mark H. Vanilloid receptor ligands and their use in treatments
CN101912400B (zh) 2004-06-11 2013-06-26 日本烟草产业株式会社 用于治疗癌症的5-氨基-2,4,7-三氧代-3,4,7,8-四氢-2H-吡啶并[2,3-d]嘧啶衍生物和相关化合物
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
CA2606760C (en) * 2005-05-04 2014-12-23 Renovis, Inc. Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds and compositions thereof useful in the treatment of conditions associated with neurological and inflammatory disorders and disfunctions
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
EP2136639B1 (en) * 2007-04-02 2016-03-09 Evotec AG Pyrid-2-yl fused heterocyclic compounds, and compositions and uses thereof
PL2139334T3 (pl) 2007-04-17 2013-11-29 Evotec Ag Skondensowane związki heterocykliczne 2-cyjanofenylu i ich kompozycje i zastosowania
US20100298289A1 (en) 2007-10-09 2010-11-25 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
ES2553340T3 (es) 2007-12-12 2015-12-07 Rigel Pharmaceuticals, Inc. Compuestos de carboxamida, sulfonamida y amina para trastornos metabólicos
US8436005B2 (en) 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
US20120028940A1 (en) 2008-09-16 2012-02-02 Merck Sharp & Dohme Corp. Functionally selective azanitrile alpha-2c adrenoreceptor agonists
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US8759362B2 (en) 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
US8546388B2 (en) 2008-10-24 2013-10-01 Purdue Pharma L.P. Heterocyclic TRPV1 receptor ligands
JP2010105951A (ja) 2008-10-29 2010-05-13 Dainippon Sumitomo Pharma Co Ltd 6−アルキル置換テトラヒドロピリド[4,3−d]ピリミジン誘導体
TW201102391A (en) 2009-03-31 2011-01-16 Biogen Idec Inc Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use
WO2010120991A1 (en) 2009-04-17 2010-10-21 Wyeth Llc 5, 6, 7, 8-tetrahydropyrido[4,3-d]pyrimidine compounds, their use as mtor, pi3, and hsmg-1 kinase inhibitors, and their syntheses
US20100280067A1 (en) 2009-04-30 2010-11-04 Pakala Kumara Savithru Sarma Inhibitors of acetyl-coa carboxylase
ES2659725T3 (es) 2009-05-05 2018-03-19 Dana-Farber Cancer Institute, Inc. Inhibidores de EGFR y procedimiento de tratamiento de trastornos
WO2010138430A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Alkoxy tetrahydro-pyridopyrimidine pde10 inhibitors
JP2013032290A (ja) 2009-11-20 2013-02-14 Dainippon Sumitomo Pharma Co Ltd 新規縮合ピリミジン誘導体
JP2013516479A (ja) 2010-01-06 2013-05-13 ジョゼフ・ピー・エリコ 標的薬物を開発する方法および組成物
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
WO2011103715A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Task channel antagonists
WO2011143495A1 (en) 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
AU2011255218B2 (en) 2010-05-21 2015-03-12 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
EP2790705B1 (en) 2011-12-15 2017-12-06 Novartis AG Use of inhibitors of the activity or function of pi3k

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