[go: up one dir, main page]

ECSP20024651A - Derivados de imidazol condensados sustituidos por grupos de hidroxilo terciario como inhibidores de gamma pi3k-y - Google Patents

Derivados de imidazol condensados sustituidos por grupos de hidroxilo terciario como inhibidores de gamma pi3k-y

Info

Publication number
ECSP20024651A
ECSP20024651A ECSENADI202024651A ECDI202024651A ECSP20024651A EC SP20024651 A ECSP20024651 A EC SP20024651A EC SENADI202024651 A ECSENADI202024651 A EC SENADI202024651A EC DI202024651 A ECDI202024651 A EC DI202024651A EC SP20024651 A ECSP20024651 A EC SP20024651A
Authority
EC
Ecuador
Prior art keywords
inhibitors
hydroxyl groups
imidazole derivatives
tertiary hydroxyl
condensed imidazole
Prior art date
Application number
ECSENADI202024651A
Other languages
English (en)
Inventor
Daniel Levy
Artem Shvartsbart
Padmaja Polam
Andrew P Combs
Nikoo Falahatpisheh
Ravi Kumar Jalluri
David M Burns
Eddy W Yue
Andrew W Buesking
Stacey Shepard
Brent Douty
Richard B Sparks
Lixin Shao
Original Assignee
Incyte 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 Incyte Corp filed Critical Incyte Corp
Publication of ECSP20024651A publication Critical patent/ECSP20024651A/es

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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención se refiere a compuestos de Fórmula (I): o sales de los mismos farmacéuticamente aceptables, los cuales son inhibidores de PI3K-gamma; los cuales son útiles para el tratamiento de trastornos tales como enfermedades autoinmunes, cáncer, enfermedades cardiovasculares, y enfermedades neurodegenerativas.
ECSENADI202024651A 2017-10-18 2020-05-04 Derivados de imidazol condensados sustituidos por grupos de hidroxilo terciario como inhibidores de gamma pi3k-y ECSP20024651A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762574057P 2017-10-18 2017-10-18
US201762608897P 2017-12-21 2017-12-21
US201862727316P 2018-09-05 2018-09-05

Publications (1)

Publication Number Publication Date
ECSP20024651A true ECSP20024651A (es) 2020-06-30

Family

ID=64110207

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI202024651A ECSP20024651A (es) 2017-10-18 2020-05-04 Derivados de imidazol condensados sustituidos por grupos de hidroxilo terciario como inhibidores de gamma pi3k-y

Country Status (35)

Country Link
US (4) US10738057B2 (es)
EP (2) EP4006034A1 (es)
JP (2) JP7244504B2 (es)
KR (2) KR20240152947A (es)
CN (2) CN118063470A (es)
AU (3) AU2018350980C1 (es)
BR (1) BR112020007593A2 (es)
CA (1) CA3084589A1 (es)
CL (1) CL2020001047A1 (es)
CR (2) CR20210442A (es)
CY (1) CY1124814T1 (es)
EC (1) ECSP20024651A (es)
ES (1) ES2902390T3 (es)
GE (2) GEP20237483B (es)
HR (1) HRP20211827T1 (es)
HU (1) HUE056615T2 (es)
IL (3) IL295978B2 (es)
JO (1) JOP20200086A1 (es)
LT (1) LT3697789T (es)
MA (1) MA50398B1 (es)
MD (1) MD3697789T2 (es)
MX (1) MX2020003862A (es)
PE (1) PE20210169A1 (es)
PH (1) PH12020550442A1 (es)
PL (1) PL3697789T3 (es)
PT (1) PT3697789T (es)
RS (1) RS62818B1 (es)
SA (1) SA520411783B1 (es)
SG (1) SG11202003428VA (es)
SI (1) SI3697789T1 (es)
SM (1) SMT202100656T1 (es)
TW (2) TWI834560B (es)
UA (1) UA128085C2 (es)
WO (1) WO2019079469A1 (es)
ZA (1) ZA202201220B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20210442A (es) * 2017-10-18 2021-12-20 Incyte Corp ALCOHOLES TERCIARIOS COMO INHIBIDORES DE PI3K-y (Divisional Exp. 2020-0214)
PT3728271T (pt) 2017-12-19 2022-10-06 Turning Point Therapeutics Inc Compostos macrocíclicos para tratar doenças
MD3762368T2 (ro) 2018-03-08 2022-07-31 Incyte Corp Compuși diol aminopirazină ca inhibitori ai PI3K-Y
MA53097A (fr) 2018-07-05 2021-05-12 Incyte Corp Dérivés de pyrazine fusionnés en tant qu'inhibiteurs d'a2a/a2b
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
CN115286521B (zh) * 2022-07-11 2023-11-03 上海医药集团(本溪)北方药业有限公司 一种盐酸左沙丁胺醇的合成方法

Family Cites Families (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4269846A (en) 1979-10-29 1981-05-26 Usv Pharmaceutical Corporation Heterocyclic compounds useful as anti-allergy agents
US5137876A (en) 1990-10-12 1992-08-11 Merck & Co., Inc. Nucleoside antiviral and anti-inflammatory compounds and compositions and methods for using same
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0011092D0 (en) 2000-05-08 2000-06-28 Black James Foundation Gastrin and cholecystokinin receptor ligands (III)
MXPA03000051A (es) 2000-06-28 2003-08-19 Smithkline Beecham Plc Procedimiento de molido en humedo.
CN100391958C (zh) 2001-09-19 2008-06-04 安万特医药股份有限公司 化合物
FR2831536A1 (fr) 2001-10-26 2003-05-02 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr
JP5039268B2 (ja) 2001-10-26 2012-10-03 アベンティス・ファーマスーティカルズ・インコーポレイテツド ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用
ATE335490T1 (de) 2001-10-30 2006-09-15 Novartis Pharma Gmbh Staurosporin-derivate als hemmer der flt3- rezeptor-tyrosinkinase-wirkung
DE10207843A1 (de) 2002-02-15 2003-09-04 Schering Ag Mikrolia-Inhibitoren zur Unterbrechung von Interleukin 12 und IFN-gamma vermittelten Immunreaktionen
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7186832B2 (en) * 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US8524899B2 (en) 2003-03-04 2013-09-03 California Institute Of Technology Alternative heterocycles for DNA recognition
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
KR20060054410A (ko) 2003-08-01 2006-05-22 제네랩스 테크놀로지스, 인코포레이티드 플라비비리다에에 대한 2고리 이미다졸 유도체
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
ES2372694T3 (es) * 2003-10-15 2012-01-25 OSI Pharmaceuticals, LLC Inhibidores de tirosina cinasa de imidazo[1,5-a]pirazina.
WO2005118580A2 (en) 2004-05-12 2005-12-15 The Government Of The United States Of America As Represented By The Secretary, Department Of Health Tricyclic compounds as inhibitors of the hypoxic signaling pathway
CN1960988B (zh) 2004-06-10 2012-01-25 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
JP2008520612A (ja) 2004-11-24 2008-06-19 ノバルティス アクチエンゲゼルシャフト ＪＡＫ阻害剤およびＢｃｒ−Ａｂｌ、Ｆｌｔ−３、ＦＡＫまたはＲＡＦキナーゼ阻害剤のうち少なくとも１個の組合せ
EP1909910A1 (en) 2005-08-04 2008-04-16 Sirtris Pharmaceuticals, Inc. Benzimidazole derivatives as sirtuin modulators
CA2620223A1 (en) 2005-09-02 2007-03-08 Abbott Laboratories Novel imidazo based heterocycles
US20080039450A1 (en) 2006-06-22 2008-02-14 Jensen Annika J Compounds
EP2139474A2 (en) 2007-03-27 2010-01-06 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
DE102007035333A1 (de) 2007-07-27 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Arylsulfonylglycine, deren Herstellung und deren Verwendung als Arzneimittel
GB0716292D0 (en) 2007-08-21 2007-09-26 Biofocus Dpi Ltd Imidazopyrazine compounds
BRPI0820544A2 (pt) 2007-11-16 2015-06-16 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase
EP2234486A4 (en) 2007-12-19 2011-09-14 Scripps Research Inst BENZIMIDAZOLES AND ANALOGS AS INHIBITORS OF RHO-KINASE
CA2712071A1 (en) 2008-01-15 2009-10-08 Siga Technologies, Inc. Antiviral drugs for treatment of arenavirus infection
ATE555116T1 (de) 2008-02-26 2012-05-15 Merck Sharp & Dohme Ahcy-hydrolasehemmer zur behandlung von hyperhomocysteinämie
DK2288610T3 (en) 2008-03-11 2016-11-28 Incyte Holdings Corp Azetidinesulfonic AND CYCLOBUTANDERIVATER AS JAK INHIBITORS
WO2009133127A1 (en) 2008-04-30 2009-11-05 Merck Serono S.A. Fused bicyclic compounds and use thereof as pi3k inhibitors
CA2763536C (en) 2008-05-30 2017-05-09 Marvin J. Miller Anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria
WO2010051245A1 (en) 2008-11-03 2010-05-06 Merck Sharp & Dohme Corp. Benzimidazole and aza-benzimidazole carboxamides
WO2010061903A1 (ja) 2008-11-27 2010-06-03 塩野義製薬株式会社 Pi3k阻害活性を有するピリミジン誘導体およびピリジン誘導体
GB0822981D0 (en) 2008-12-17 2009-01-21 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
EP2401273A1 (en) 2009-02-27 2012-01-04 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
JP5805623B2 (ja) * 2009-04-16 2015-11-04 フンダシオン セントロ ナシオナル デ インベスティガシオネス オンコロヒカス カルロス ザ サードＦｕｎｄａｃｉｏｎ Ｃｅｎｔｒｏ Ｎａｃｉｏｎａｌ ｄｅ Ｉｎｖｅｓｔｉｇａｃｉｏｎｅｓ Ｏｎｃｏｌｏｇｉｃａｓ Ｃａｒｌｏｓ ＩＩＩ キナーゼ阻害剤として使用するためのイミダゾピラジン類
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
PT2448938E (pt) 2009-06-29 2014-07-31 Incyte Corp Pirimidinonas como inibidoras de pi3k
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TW201130842A (en) 2009-12-18 2011-09-16 Incyte Corp Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
US8759359B2 (en) 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
WO2011099832A2 (en) 2010-02-12 2011-08-18 Crystalgenomics, Inc. Novel benzimidazole compound, preparation method thereof and pharmaceutical composition comprising the same
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
KR101911697B1 (ko) 2010-03-10 2018-10-25 인사이트 홀딩스 코포레이션 Ｊａｋ１ 저해제로서의 피페리딘­４­일 아제티딘 유도체
JP2013523766A (ja) 2010-03-31 2013-06-17 グラクソ グループ リミテッド キナーゼ阻害剤としてのイミダゾリル‐イミダゾール
JP5816678B2 (ja) 2010-04-14 2015-11-18 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ ＰＩ３Ｋδ阻害剤としての縮合誘導体
WO2011149856A1 (en) 2010-05-24 2011-12-01 Presidio Pharmaceuticals, Inc. Inhibitors of hcv ns5a
WO2011149874A2 (en) 2010-05-26 2011-12-01 Schering Corporation N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
BR112013009166A2 (pt) 2010-10-13 2016-07-26 Millennium Pharm Inc heteroarilas e uso das mesmas.
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
NZ611151A (en) 2010-11-19 2015-06-26 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
PE20140161A1 (es) 2010-11-30 2014-02-19 Takeda Pharmaceutical Compuesto biciclico
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US8673905B2 (en) 2011-03-17 2014-03-18 Hoffmann-La Roche Inc. Imidazo pyrazines
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
US9029389B2 (en) 2011-04-21 2015-05-12 Institut Pasteur Korea Anti-inflammation compounds
US9181214B2 (en) 2011-06-09 2015-11-10 Rhizen Pharmaceuticals Sa Bicyclic compounds as modulators of GPR-119
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
TWI673272B (zh) 2011-09-02 2019-10-01 美商英塞特控股公司 作為pi3k抑制劑之雜環基胺
WO2013104610A1 (en) * 2012-01-10 2013-07-18 Bayer Intellectual Property Gmbh Substituted imidazopyrazines as akt kinase inhibitors
WO2013129674A1 (ja) 2012-03-01 2013-09-06 学校法人兵庫医科大学 新規ベンズイミダゾール誘導体及びその用途
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
WO2013180193A1 (ja) 2012-05-31 2013-12-05 住友化学株式会社 縮合複素環化合物
EP2872508B1 (en) 2012-07-13 2018-08-29 UCB Biopharma SPRL Imidazopyridine derivatives as modulators of tnf activity
UA117572C2 (uk) 2012-11-01 2018-08-27 Інсайт Холдинґс Корпорейшн Трициклічні конденсовані похідні тіофену як інгібітори jak
TWI687220B (zh) 2013-03-01 2020-03-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
WO2014149207A2 (en) 2013-03-15 2014-09-25 Dow Agrosciences Llc Benzimidazole-based insecticidal compositions and related methods
US8999992B2 (en) 2013-03-15 2015-04-07 Vm Pharma Llc Crystalline forms of tryosine kinase inhibitors and their salts
WO2014153529A1 (en) 2013-03-22 2014-09-25 The Scripps Research Institute Substituted benzimidazoles as nociceptin receptor modulators
US9394254B2 (en) 2013-05-08 2016-07-19 The University of Denver and Regis University Antibiotic and anti-parasitic agents that modulate class II fructose 1,6-bisphosphate aldolase
RS56012B1 (sr) 2013-05-17 2017-09-29 Incyte Corp Derivati bipirazola kao inhibitori jak
MX380467B (es) 2013-07-17 2025-03-12 Otsuka Pharma Co Ltd Compuestos de cianotriazol.
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
HRP20201887T1 (hr) 2014-04-08 2021-02-05 Incyte Corporation LIJEČENJE B-STANIČNIH MALIGNITETA S KOMBINACIJOM INHIBITORA JAK i PI3K
EP2930048A1 (en) 2014-04-10 2015-10-14 Johnson Controls Automotive Electronics SAS Head up display projecting visual information onto a screen
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
JP6660060B2 (ja) 2014-09-16 2020-03-04 セルジーン クオンティセル リサーチ，インク． ヒストンデメチラーゼ阻害剤
US10023576B2 (en) * 2014-10-22 2018-07-17 Bristol-Myers Squibb Company Heteroaryl substituted pyrrolotriazine amine compounds as PI3K inhibitors
EP3209664B1 (en) * 2014-10-22 2020-06-03 Bristol-Myers Squibb Company Bicyclic heteroaryl amine compounds as pi3k inhibitors
MA40933A (fr) 2014-11-11 2017-09-19 Piqur Therapeutics Ag Difluorométhyl-aminopyridines et difluorométhyl-aminopyrimidines
WO2016106624A1 (en) * 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Tertiary alcohol imidazopyrazine btk inhibitors
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
US9968604B2 (en) * 2015-04-16 2018-05-15 Chiesi Farmaceutici S.P.A. Chromene derivatives as phoshoinositide 3-kinases inhibitors
HK1252614A1 (zh) 2015-05-12 2019-05-31 Zeno Royalties & Milestones, LLC 二環化合物
TWI744256B (zh) 2015-11-06 2021-11-01 美商英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
MA54567A (fr) 2016-01-05 2021-10-27 Incyte Corp Pyridine et composés de pyridimine en tant qu'inhibiteurs de pi3k-gamma
TW201803871A (zh) * 2016-06-24 2018-02-01 英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物
RU2019108464A (ru) 2016-08-26 2020-09-28 Мицубиси Танабе Фарма Корпорейшн Бициклическое азотсодержащее гетероциклическое соединение
WO2018136754A1 (en) 2017-01-20 2018-07-26 Massachusetts Institute Of Technology Injectable polymer micro-depots for controlled local drug delivery
TWI674261B (zh) 2017-02-17 2019-10-11 美商英能腫瘤免疫股份有限公司 Nlrp3 調節劑
EP3658539B1 (en) 2017-07-24 2024-02-21 Novartis AG Compounds and compositions for treating conditions associated with nlrp activity
US10988454B2 (en) 2017-09-14 2021-04-27 Abbvie Overseas S.À.R.L. Modulators of the cystic fibrosis transmembrane conductance regulator protein and methods of use
CR20210442A (es) 2017-10-18 2021-12-20 Incyte Corp ALCOHOLES TERCIARIOS COMO INHIBIDORES DE PI3K-y (Divisional Exp. 2020-0214)
EP3697762A4 (en) 2017-10-18 2021-04-07 Epizyme, Inc. AMINE SUBSTITUTED HETEROCYCLIC COMPOUNDS, USED AS EHMT2 INHIBITORS, SALTS THEREOF, AND THEIR METHODS OF SYNTHESIS
PT3728271T (pt) 2017-12-19 2022-10-06 Turning Point Therapeutics Inc Compostos macrocíclicos para tratar doenças
US10829487B2 (en) 2017-12-21 2020-11-10 Boehringer Ingelheim International Gmbh Benzylamino substituted pyridopyrimidinones and derivatives as SOS1 inhibitors
US11512054B2 (en) 2017-12-21 2022-11-29 Basf Se Pesticidal compounds
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)

Also Published As

Publication number Publication date
SG11202003428VA (en) 2020-05-28
GEP20237483B (en) 2023-03-27
BR112020007593A2 (pt) 2020-09-24
MA50398A (fr) 2021-05-05
CN111542526B (zh) 2024-01-09
IL295978A (en) 2022-10-01
UA128085C2 (uk) 2024-04-03
US20200385392A1 (en) 2020-12-10
AU2018350980A1 (en) 2020-04-30
AU2023203088B2 (en) 2024-10-03
IL295978B2 (en) 2024-01-01
IL273983A (en) 2020-05-31
HUE056615T2 (hu) 2022-02-28
MA50398B1 (fr) 2021-10-29
TW201927788A (zh) 2019-07-16
MD3697789T2 (ro) 2022-02-28
TWI803525B (zh) 2023-06-01
IL295978B1 (en) 2023-09-01
PT3697789T (pt) 2021-12-31
RS62818B1 (sr) 2022-02-28
PL3697789T3 (pl) 2022-02-21
US11926630B2 (en) 2024-03-12
US20220213107A1 (en) 2022-07-07
US11225486B2 (en) 2022-01-18
JP2021500340A (ja) 2021-01-07
CL2020001047A1 (es) 2020-08-28
US20190152975A1 (en) 2019-05-23
JP2023085290A (ja) 2023-06-20
SI3697789T1 (sl) 2022-04-29
AU2024287193A1 (en) 2025-01-23
KR102717072B1 (ko) 2024-10-15
WO2019079469A1 (en) 2019-04-25
GEP20257716B (en) 2025-01-27
CY1124814T1 (el) 2022-11-25
AU2018350980B2 (en) 2023-02-23
CN111542526A (zh) 2020-08-14
ZA202201220B (en) 2023-03-29
MX2020003862A (es) 2020-08-13
IL273983B2 (en) 2023-02-01
EP3697789A1 (en) 2020-08-26
SA520411783B1 (ar) 2024-05-12
TWI834560B (zh) 2024-03-01
KR20200089264A (ko) 2020-07-24
ES2902390T3 (es) 2022-03-28
CN118063470A (zh) 2024-05-24
JP7244504B2 (ja) 2023-03-22
EP3697789B1 (en) 2021-09-29
US20240228498A1 (en) 2024-07-11
CA3084589A1 (en) 2019-04-25
KR20240152947A (ko) 2024-10-22
PH12020550442A1 (en) 2021-05-31
JOP20200086A1 (ar) 2020-04-30
JP7541594B2 (ja) 2024-08-28
EP4006034A1 (en) 2022-06-01
CR20210442A (es) 2021-12-20
CR20200214A (es) 2020-07-25
PE20210169A1 (es) 2021-01-29
TW202340200A (zh) 2023-10-16
IL273983B (en) 2022-10-01
SMT202100656T1 (it) 2022-01-10
LT3697789T (lt) 2021-12-10
AU2018350980C1 (en) 2024-12-12
HRP20211827T1 (hr) 2022-03-18
US10738057B2 (en) 2020-08-11
AU2023203088A1 (en) 2023-06-15

Similar Documents

Publication Publication Date Title
ECSP20024651A (es) Derivados de imidazol condensados sustituidos por grupos de hidroxilo terciario como inhibidores de gamma pi3k-y
ECSP24026455A (es) Compuestos de pirrolotriazina como inhibidores de tam
MX2022014648A (es) Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b.
ECSP17073191A (es) Compuestos heterocíclicos como inhibidores de lsd1
CO2018001268A2 (es) Derivados de heteroarilo como inhibidores de parp
ECSP20061378A (es) COMPUESTOS DIÓLICOS DE AMINOPIRAZINA COMO INHIBIDORES DE PI3K-gamma
CY1123059T1 (el) Αναστολη του διαυλου ιοντων παροδικου δυναμικου του υποδοχεα α1
DOP2016000299A (es) Derivados de pirrolidina-2,5-diona, composiciones farmacéuticas y su uso como inhibidores ido1
DOP2015000158A (es) Inhibidores de prmt5 y sus usos
MX2018002326A (es) Analogos novedosos de nucleosidos sustituidos en el anillo aromatico biciclico 6-6 para su uso como inhibidores de prmt5.
CU20160167A7 (es) Compuestos de pirazolopiridinas y pirazolopirimidinas útiles en el tratamiento de condiciones alérgicas y respiratorias
MX2015012427A (es) Compuestos de morfolinona de acido heteroarilo como inhibidores mdm2 para el tratamiento de cancer.
MX2020010900A (es) Inhibidores de demetilasa-1 especifica de lisina.
MX2017003695A (es) Pirimidinonas como inhibidores del factor xia.
CO2017000363A2 (es) Inhibidores de la desmetilasa-1 específica de la lisina (lsd-1) derivados del [(5-carbonil)-1h-pirrol-3-il]-benzonitrilo o [(4-carbonil)imidazol-2-il]-benzonitrilo
CL2019002297A1 (es) Inhibidores de mnk sustituidos con piperidina y métodos relacionados con los mismos.
CO7280468A2 (es) Antagonistas del receptor de 5-ht3
BR112016024936A2 (pt) moduladores de gpr40 à base de pirrolidina para tratamento de doenças como diabetes
CU20160195A7 (es) Derivados de quinolizinona como inhibidores de pi3k
UY36758A (es) Inhibidores del potenciador del homólogo zeste 2
EA201792109A1 (ru) Конденсированные с тетрагидрофураном производные аминогидротиазина, пригодные для лечения болезни альцгеймера
EA201892188A1 (ru) Соединения пирролотриазина в качестве ингибиторов tam
CR20160532A (es) Derivados de pirrolidina-2,5-diona, composiciones farmacéuticas y métodos para usar como inhibidores ido1