PE20190623A1 - Formas solidas cristalinas de un inhibidor de bet - Google Patents

Formas solidas cristalinas de un inhibidor de bet

Info

Publication number
PE20190623A1
PE20190623A1 PE2018003269A PE2018003269A PE20190623A1 PE 20190623 A1 PE20190623 A1 PE 20190623A1 PE 2018003269 A PE2018003269 A PE 2018003269A PE 2018003269 A PE2018003269 A PE 2018003269A PE 20190623 A1 PE20190623 A1 PE 20190623A1
Authority
PE
Peru
Prior art keywords
crystal forms
solid crystal
xrpd
refers
whose
Prior art date
Application number
PE2018003269A
Other languages
English (en)
Inventor
Shili Chen
Zhongjiang Jia
Pingli Liu
Lei Qiao
Yongzhong Wu
Jiacheng Zhou
Qun Li
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 PE20190623A1 publication Critical patent/PE20190623A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01M—CATCHING, TRAPPING OR SCARING OF ANIMALS; APPARATUS FOR THE DESTRUCTION OF NOXIOUS ANIMALS OR NOXIOUS PLANTS
    • A01M31/00—Hunting appliances
    • A01M31/06—Decoys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biotechnology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)

Abstract

SE REFIERE A FORMAS SOLIDAS CRISTALINAS DEL COMPUESTO DE FORMULA (I) QUE ES 2,2,4-TRIMETIL-8-(6-METIL-7-OXO-6,7-DIHIDRO-1H-PIRROLO[2,3-C]PIRIDIN-4-IL)-6-(METILSULFONIL)-2H-BENZO[B][1,4]OXAZIN-3(4H)-ONA, TALES COMO A) LA FORMA I CUYO PATRON DE DIFRACCION EN POLVO DE RAYOS X (XRPD) EN ANGULO 2THETA TIENE LOS SIGUIENTES PICOS: 8.7, 9.8, 11.6, 12.7, 14.7, 15.7, 20.0, 21.4, 23.3 Y 27.1 GRADOS; Y B) LA FORMA II CUYO PATRON DE DIFRACCION EN POLVO DE RAYOS X (XRPD) EN ANGULO 2THETA TIENE LOS SIGUIENTES PICOS: 6.7, 9.5, 10.5, 14.8, 16.2, 17.0, 18.8 Y 19.3 GRADOS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION. DICHO COMPUESTO DE FORMULA (I) ES UN INHIBIDOR DE PROTEINAS BET TALES COMO BRD2, BRD3, BRD4 Y BRD-t, SIENDO UTIL PARA EL TRATAMIENTO DE CANCER
PE2018003269A 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet PE20190623A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662352220P 2016-06-20 2016-06-20
US201662397575P 2016-09-21 2016-09-21

Publications (1)

Publication Number Publication Date
PE20190623A1 true PE20190623A1 (es) 2019-04-26

Family

ID=59258384

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2023002468A PE20240236A1 (es) 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet
PE2018003269A PE20190623A1 (es) 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2023002468A PE20240236A1 (es) 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet

Country Status (32)

Country Link
US (5) US10189832B2 (es)
EP (2) EP3472157B1 (es)
JP (4) JP7096170B2 (es)
KR (3) KR102643344B1 (es)
CN (3) CN114369091A (es)
AU (3) AU2017281286B2 (es)
BR (1) BR112018076486A2 (es)
CA (3) CA3028689A1 (es)
CL (3) CL2018003702A1 (es)
CO (1) CO2018014339A2 (es)
CR (2) CR20220651A (es)
CY (1) CY1126092T1 (es)
DK (1) DK3472157T3 (es)
EC (1) ECSP19001982A (es)
ES (1) ES2945063T3 (es)
FI (1) FI3472157T3 (es)
HR (1) HRP20230466T1 (es)
HU (1) HUE062234T2 (es)
IL (3) IL263824B2 (es)
LT (1) LT3472157T (es)
MD (1) MD3472157T2 (es)
MX (3) MX2018016281A (es)
PE (2) PE20240236A1 (es)
PH (1) PH12018502709A1 (es)
PL (1) PL3472157T3 (es)
PT (1) PT3472157T (es)
RS (1) RS64274B1 (es)
SG (2) SG10201912398PA (es)
SI (1) SI3472157T1 (es)
TW (2) TWI786050B (es)
UA (2) UA124106C2 (es)
WO (1) WO2017222977A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6243003B2 (ja) 2013-03-15 2017-12-06 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｂｅｔタンパク質阻害剤としての三環式複素環
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
DK3674302T3 (da) 2014-04-23 2023-04-03 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-oner og pyrazolo[3,4-c]pyridin-7(6h)-oner som inhibitorer af bet-proteiner
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
KR102643344B1 (ko) * 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
TW202024078A (zh) * 2018-09-13 2020-07-01 加拿大商增你智表觀遺傳學公司 Bet溴結構域(bromodomain)抑制劑之固體形式之製備方法
US20230167166A1 (en) * 2020-04-24 2023-06-01 Memorial Sloan Kettering Cancer Center Targeted therapy for the treatment & prevention of life-threatening complications of infection
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CA3184633A1 (en) 2020-06-03 2021-12-09 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (165)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59170313A (ja) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd スクリ−ンゲ−ト
JPS6085739U (ja) 1983-11-18 1985-06-13 クラリオン株式会社 テ−プレコ−ダにおけるピンチロ−ラ装置
JPH0314566A (ja) 1989-06-09 1991-01-23 Sankyo Co Ltd ベンズイミダゾール誘導体
US5244912A (en) 1991-03-28 1993-09-14 Eli Lilly And Company 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof
FR2710915B1 (fr) 1993-10-04 1995-11-24 Synthelabo Dérivés de pipéridine, leur préparation et leur utilisation en thérapeutique.
GB9410469D0 (en) 1994-05-25 1994-07-13 Erba Farmitalia Imidazolylalkyl derivatives of imidazo (5,1-c) (1,4) benzoxazin-1-one and process for their preparation
FR2731708B1 (fr) 1995-03-13 1997-04-30 Synthelabo Derives de piperidine, leur procede de preparation et leur application en therapeutique
FR2747678B1 (fr) 1996-04-22 1998-05-22 Synthelabo Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique
US6287693B1 (en) 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
NZ531171A (en) 2000-04-21 2005-03-24 Upjohn Co Cabergoline-type compounds for treating fibromyalgia and chronic fatigue syndrome
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
FR2816619B1 (fr) 2000-11-15 2003-01-31 Sanofi Synthelabo Derives de benzimidazole, leur preparation et leur application en therapeutique
CZ294493B6 (cs) 2000-08-08 2005-01-12 Sanofi-Synthelabo Deriváty benzimidazolu, způsob jejich přípravy a léčebné prostředky s jejich obsahem
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
AU2003293006A1 (en) 2002-11-22 2004-06-18 Japan Tobacco Inc. Fused bicyclic nitrogen-containing heterocycles
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
AU2005214258A1 (en) 2004-02-23 2005-09-01 Dainippon Sumitomo Pharma Co., Ltd. Novel heterocyclic compound
EP1732541A4 (en) 2004-04-07 2008-03-05 Takeda Pharmaceutical CYCLIC COMPOUNDS
US7713954B2 (en) 2004-09-30 2010-05-11 Roche Palo Alto Llc Compositions and methods for treating cognitive disorders
DE102005011058A1 (de) 2005-03-10 2006-09-14 Merck Patent Gmbh Substituierte Tetrahydro-pyrrolo-chinolinderivate
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
US20080318999A1 (en) 2005-08-05 2008-12-25 Methvin Isaac Tricyclic Benzimidazoles and Their Use as Metabotropic Glutamate Receptor Modulators
US8975259B2 (en) 2007-04-27 2015-03-10 University Of Rochester Compositions and methods for inhibiting G protein signaling
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
WO2009020559A2 (en) 2007-08-03 2009-02-12 The J. David Gladstone Institutes Agents that inhibit p-tefb interactions and methods of use thereof
CA2710740C (en) 2007-12-28 2016-07-19 Shinji Miyoshi Thienotriazolodiazepine compound as antitumor agent
DE102008052618A1 (de) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclische Aldehyde und C,H-acide Verbindungen
US8669249B2 (en) 2009-03-27 2014-03-11 Takeda Pharmaceutical Company Limited Poly (ADP-ribose) polymerase (PARP) inhibitors
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201103941A (en) 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011024987A1 (ja) 2009-08-31 2011-03-03 塩野義製薬株式会社 芳香族縮合へテロ環誘導体およびそれらを含有する医薬組成物
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2446647T3 (es) 2009-11-05 2014-03-10 Glaxosmithkline Llc Inhibidor de bromodominio de benzodiazepina
WO2011054845A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP2955524A3 (en) 2009-11-05 2016-03-23 GlaxoSmithKline LLC Novel process
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
JP2013525366A (ja) 2010-04-23 2013-06-20 キネタ・インコーポレイテツド 抗ウイルス性化合物
CN104311562B (zh) 2010-05-14 2017-07-04 达那-法伯癌症研究所 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
CN103119160B (zh) 2010-05-14 2016-06-01 达那-法伯癌症研究所 用于调节代谢的组合物和方法
CN105582014B (zh) 2010-05-14 2019-06-14 达那-法伯癌症研究所 用于治疗白血病的组合物和方法
EP2585465B1 (en) 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
KR20130116358A (ko) 2011-02-09 2013-10-23 에프. 호프만-라 로슈 아게 Pi3 키나아제 억제제로서 헤테로사이클릭 화합물
WO2012116170A1 (en) 2011-02-23 2012-08-30 Ming-Ming Zhou Inhibitors of bromodomains as modulators of gene expression
WO2012126901A1 (en) 2011-03-21 2012-09-27 F. Hoffmann-La Roche Ag Benzoxazepin compounds selective for pi3k p110 delta and methods of use
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
US9422292B2 (en) 2011-05-04 2016-08-23 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012178208A2 (en) 2011-06-24 2012-12-27 The Trustees Of The Stevens Institute Of Technology Selective inhibitors of histone deacetylase isoform 6 and methods thereof
JP2013010719A (ja) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途
AU2012290261A1 (en) 2011-07-29 2014-02-20 The Children's Hospital Of Philadelphia Compositions and methods for the treatment of HIV
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, and methods of using same
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
KR101560073B1 (ko) 2011-08-31 2015-10-13 오쓰까 세이야꾸 가부시키가이샤 퀴놀론 화합물
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
EP2757887B1 (en) 2011-09-22 2017-04-26 VIIV Healthcare UK Limited Pyrrolopyridinone compounds and methods for treating hiv
CN103857391B (zh) 2011-09-30 2016-06-08 沈阳蓝桑医药生物技术研发有限公司 含有瑞利格内酯的药物组合物及其应用
WO2013060636A1 (en) 2011-10-25 2013-05-02 Sanofi 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
RS58911B1 (sr) 2011-11-01 2019-08-30 Resverlogix Corp Oralne formulacije sa trenutnim otpuštanjem za supstituisane hinazolinone
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20150133434A1 (en) 2012-03-28 2015-05-14 The J. David Gladstone Institutes Compositions and Methods for Reactivating Latent Immunodeficiency Virus
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
EP2864336B1 (en) 2012-06-06 2016-11-23 Constellation Pharmaceuticals, Inc. Benzo[b]isoxazoloazepine bromodomain inhibitors and uses thereof
BR112014031068A2 (pt) 2012-06-12 2017-06-27 Abbvie Inc derivados piridinona e piridazinona
CN105050605A (zh) 2012-06-25 2015-11-11 翁科埃蒂克斯股份公司 使用噻吩并三唑并二氮杂*化合物治疗淋巴瘤的方法
WO2014015175A1 (en) 2012-07-18 2014-01-23 Massachusetts Institute Of Technology Compositions and methods for modulating brd4 bioactivity
CN104755473B (zh) 2012-08-16 2017-03-08 拜耳医药股份有限公司 2，3‑苯并二氮杂*
EP2884983B1 (en) 2012-08-16 2017-10-04 GlaxoSmithKline LLC Benzodiazepines for treating small cell lung cancer
CN104781259B (zh) 2012-09-28 2018-06-01 拜耳制药股份公司 抑制bet蛋白的5-芳基三唑并氮杂*
WO2014068402A2 (en) 2012-09-28 2014-05-08 Oncoethix Sa Pharmaceutical formulation containing thienotriazolodiazepine compounds
CN104854090B (zh) 2012-11-09 2017-12-15 雅各布斯制药公司 杂芳基衍生物和其用途
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
WO2014078257A1 (en) 2012-11-14 2014-05-22 Glaxosmithkline Llc Thieno[3,2-c]pyridin-4(5h)-ones as bet inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US20160193206A1 (en) 2012-12-20 2016-07-07 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
US20150344444A1 (en) 2012-12-20 2015-12-03 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydroxyquinoxalinones
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
EP2961747B1 (en) 2013-02-27 2017-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
BR112015022861A8 (pt) 2013-03-11 2019-11-26 Abbvie Inc inibidores de bromodomínio
TW201444843A (zh) 2013-03-11 2014-12-01 Abbvie Inc 溴區結構域蛋白抑制劑
AU2014249192B2 (en) 2013-03-11 2017-12-21 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
EP2970276A1 (en) 2013-03-12 2016-01-20 AbbVie Inc. Dihydro-pyrrolopyridinone bromodomain inhibitors
AU2014248647A1 (en) 2013-03-12 2015-10-01 Abbvie Inc. Pyrrole amide inhibitors
AU2014231563A1 (en) 2013-03-12 2015-09-17 Abbvie Inc. Tetracyclic bromodomain inhibitors
JP6280573B2 (ja) 2013-03-14 2018-02-14 グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ ブロモドメイン阻害薬としてのフロピリジン
ES2915658T3 (es) 2013-03-14 2022-06-24 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolin-2,3-disustituida y su uso como inhibidores de bromodominio
EA201591746A1 (ru) 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
JP2016519660A (ja) 2013-03-15 2016-07-07 エピジェネティクス・インコーポレイテッド ブロモドメイン阻害剤としてのオキサゾロ［５，４−ｃ］キノリン−２−オン化合物
EP2970265B1 (en) 2013-03-15 2018-08-08 Plexxikon Inc. Heterocyclic compounds and uses thereof
JP6243003B2 (ja) 2013-03-15 2017-12-06 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｂｅｔタンパク質阻害剤としての三環式複素環
WO2014154762A1 (en) 2013-03-27 2014-10-02 Boehringer Ingelheim International Gmbh Dihydroquinazolinone analogues as brd4 inhibitors
US9102684B2 (en) 2013-03-27 2015-08-11 Boehringer Ingelheim International Gmbh Indolinone analogues
TWI530499B (zh) 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
US10435364B2 (en) 2013-04-17 2019-10-08 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
EP2989096B1 (en) 2013-04-26 2019-04-10 BeiGene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
JP6373978B2 (ja) 2013-05-27 2018-08-15 ノバルティス アーゲー イミダゾピロリジノン誘導体および疾患の処置におけるその使用
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
WO2014191911A1 (en) 2013-05-28 2014-12-04 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease
WO2014191906A1 (en) 2013-05-28 2014-12-04 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives as bet inhibitors and their use in the treatment of disease
ITMI20130991A1 (it) 2013-06-17 2014-12-18 Industrie De Nora Spa Sistema per la misurazione di correnti presenti sugli elettrodi in celle elettrolitiche interconnesse.
WO2014202578A1 (de) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituierte phenyl-2,3-benzodiazepine
JP6599852B2 (ja) 2013-06-21 2019-10-30 ゼニス・エピジェネティクス・リミテッド ブロモドメイン阻害剤としての新規の置換された二環式化合物
WO2015002754A2 (en) 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
AR096758A1 (es) * 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
MX2015017963A (es) 2013-06-28 2016-11-10 Abbvie Inc Inhibidores de bromodominio.
CA2917319A1 (en) 2013-07-08 2015-01-15 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CN105555779B (zh) 2013-07-16 2019-05-10 巴斯夫欧洲公司 除草的嗪类
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
KR101672096B1 (ko) 2013-09-30 2016-11-02 주식회사 엘지화학 헤테로환 화합물 및 이를 포함하는 유기 발광 소자
EP3640241B1 (en) 2013-10-18 2022-09-28 Celgene Quanticel Research, Inc. Bromodomain inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015081246A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
EP3089970B1 (en) 2013-12-09 2018-10-17 AbbVie Inc. Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP3083559B1 (en) * 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
SI3092227T1 (sl) 2014-01-09 2018-10-30 Orion Corporation Biciklični heterociklični derivati kot zaviralci bromodomaina
WO2015131005A1 (en) 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
DK3674302T3 (da) 2014-04-23 2023-04-03 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-oner og pyrazolo[3,4-c]pyridin-7(6h)-oner som inhibitorer af bet-proteiner
EA201692129A1 (ru) 2014-04-23 2017-03-31 Басф Се Диаминотриазины в качестве гербицидов
CA2946519C (en) 2014-04-23 2022-07-19 Takeda Pharmaceutical Company Limited Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease
EP3137085A4 (en) 2014-05-02 2017-12-27 Oncoethix GmbH Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds
JP2017514907A (ja) 2014-05-02 2017-06-08 オンコエシックス ゲーエムベーハー チエノトリアゾロジアゼピン化合物を用いる耐性非ホジキンリンパ腫、髄芽腫及び／又はａｌｋ＋非小細胞肺癌の治療方法
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
JP2017519727A (ja) 2014-05-08 2017-07-20 オンコエシックス ゲーエムベーハー チエノトリアゾロジアゼピン化合物を用いる三種陰性乳癌の治療方法
WO2015184257A2 (en) 2014-05-30 2015-12-03 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
PT3157928T (pt) 2014-06-20 2019-05-30 Constellation Pharmaceuticals Inc Formas cristalinas de 2-((4s)-6-(4-clorofenil)-1-metil-4h-benzo[c] isoxazolo[4,5-e]azepin-4-il)acetamida
US9861077B2 (en) 2014-07-11 2018-01-09 Jaan Aked-Hurditch Leash accessory
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
LT3461821T (lt) 2014-10-24 2020-08-10 Bristol-Myers Squibb Company Indolo karboksamido junginiai, naudotini kaip kinazės inhibitoriai
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
CA2974153A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins
WO2016186453A1 (en) 2015-05-20 2016-11-24 Kainos Medicine, Inc. Quinoline derivatives as bromodomain inhibitors
CA2987384A1 (en) 2015-05-29 2016-12-08 Shionogi & Co., Ltd. Nitrogen-containing tricyclic derivative having hiv replication inhibitory activity
CN105039258B (zh) 2015-07-03 2018-04-17 北京大学 将非神经元细胞重编程为神经元样细胞的方法和组合物
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
CN105254635A (zh) 2015-10-30 2016-01-20 中国药科大学 一类咪唑并吡嗪类化合物及其药物组合物和用途
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
CA3007168A1 (en) 2015-12-14 2017-06-22 Zenith Epigenetics Ltd. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
EP3412669A4 (en) 2016-02-05 2019-09-04 Chia Tai Tianqing Pharmaceutical Group Co.,Ltd TRICYCLIC COMPOUND FOR PROTEIN INHIBITOR CONTAINING BROMODOMAINE AND PREPARATION, PHARMACEUTICAL COMPOSITION AND USE THEREOF
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
CN108069958A (zh) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 一种含氮杂环类化合物、其制备方法、药物组合物及应用

Also Published As

Publication number Publication date
HRP20230466T1 (hr) 2023-07-21
JP2019524660A (ja) 2019-09-05
ECSP19001982A (es) 2019-03-29
CN109715625B (zh) 2022-04-19
US20220306628A1 (en) 2022-09-29
CL2020000408A1 (es) 2020-07-10
US20170362229A1 (en) 2017-12-21
KR20220148313A (ko) 2022-11-04
HUE062234T2 (hu) 2023-10-28
JP7096170B2 (ja) 2022-07-05
AU2021215112A1 (en) 2021-08-26
CR20220651A (es) 2023-01-23
EP3472157B1 (en) 2023-04-12
BR112018076486A2 (pt) 2019-04-09
AU2017281286A1 (en) 2019-01-24
CA3220957A1 (en) 2017-12-28
JP7375082B2 (ja) 2023-11-07
US10189832B2 (en) 2019-01-29
RS64274B1 (sr) 2023-07-31
TW201800410A (zh) 2018-01-01
IL263824B2 (en) 2023-10-01
IL263824B1 (en) 2023-06-01
MX2018016281A (es) 2019-08-22
KR102460046B1 (ko) 2022-10-31
CL2020000407A1 (es) 2020-07-10
UA124106C2 (uk) 2021-07-21
TW202330523A (zh) 2023-08-01
IL285686B (en) 2022-06-01
JP2022088527A (ja) 2022-06-14
EP4234554A2 (en) 2023-08-30
IL302528A (en) 2023-07-01
JP2024012372A (ja) 2024-01-30
US11377446B2 (en) 2022-07-05
US20200283436A1 (en) 2020-09-10
IL285686A (en) 2021-09-30
CA3028689A1 (en) 2017-12-28
FI3472157T3 (fi) 2023-06-01
CL2018003702A1 (es) 2019-04-05
DK3472157T3 (da) 2023-05-01
PT3472157T (pt) 2023-05-30
EP3472157A1 (en) 2019-04-24
US20210105998A1 (en) 2021-04-15
KR20190039086A (ko) 2019-04-10
AU2023229471A1 (en) 2023-09-28
KR20240033293A (ko) 2024-03-12
US11091480B2 (en) 2021-08-17
MX2023009524A (es) 2023-08-24
CN114366748A (zh) 2022-04-19
PH12018502709A1 (en) 2019-04-15
SI3472157T1 (sl) 2023-07-31
EP4234554A3 (en) 2023-12-27
AU2021215112B2 (en) 2023-06-15
TWI830533B (zh) 2024-01-21
CR20190027A (es) 2019-05-16
US20190169186A1 (en) 2019-06-06
US10626114B2 (en) 2020-04-21
CO2018014339A2 (es) 2019-03-08
JP2022130666A (ja) 2022-09-06
KR102643344B1 (ko) 2024-03-07
TWI786050B (zh) 2022-12-11
IL263824A (en) 2019-01-31
AU2017281286B2 (en) 2021-05-20
MX2021009776A (es) 2021-09-08
CY1126092T1 (el) 2023-11-15
ES2945063T3 (es) 2023-06-28
CN114369091A (zh) 2022-04-19
PL3472157T3 (pl) 2023-07-31
LT3472157T (lt) 2023-09-11
MD3472157T2 (ro) 2023-10-31
SG11201811416VA (en) 2019-01-30
CN109715625A (zh) 2019-05-03
WO2017222977A1 (en) 2017-12-28
UA125476C2 (uk) 2022-03-23
PE20240236A1 (es) 2024-02-16
SG10201912398PA (en) 2020-02-27
CA3220975A1 (en) 2017-12-28

Similar Documents

Publication Publication Date Title
PE20190623A1 (es) Formas solidas cristalinas de un inhibidor de bet
CY1126052T1 (el) 1η-πυρρολο[2,3-c]πυριδιν-7(6η)-ονες και πυραζολο[3,4-c]πυριδιν-7(6η)- ονες ως αναστολεις των bet πρωτεϊνων
PH12019502318A1 (en) Trycyclic heterocycles as bet protein inhibitors
CL2017000885A1 (es) Anticuerpos anti-ox40 humanizados y usos de los mismos
CL2016001629A1 (es) Compuestos tricíclicos como agentes anticancerígenos
UY37124A (es) Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos
CL2014003444A1 (es) Compuestos derivados tienopirimidina; proceso de preparacion; composicion farmaceutica que los comprende; combinacion farmaceutica; uso en el tratamiento de canceres y enfermedades autoinmunes.
NI201400125A (es) Antagonistas de st2l y métodos de uso
JOP20140141B1 (ar) استخدام 3،2- ثنائي هيدروإيميدازول-[2،1-c] كونازولينات مستبدلة لمعالجة الاورام الليمفاوية
CR20200276A (es) Sulfamoilarilamidas y su uso como medicamentos para el tratamientos de la hepatitis b (divisional exp. 2015-0059)
UY34977A (es) 2,3-benzodiazepinas
CL2014001865A1 (es) Compuestos derivados de fosfatos; procedimiento de preparacion; composiciones farmaceuticas que los contienen y uso en el tratamiento del cancer.
DOP2014000255A (es) Uracilos sustituidos bicíclicamente y uso de los mismos
CR20150426A (es) 2,3-benzodiazepinas biciclo y espirocíclico sustituidas
MX2015014181A (es) 2-acetilnafto [2,3-b]furano -4,9-diona para uso en el tratamiento del cáncer.
TW201613935A (en) Tricyclic heterocycles as BET protein inhibitors
DOP2016000064A (es) Derivados de fenilalanina sustituidos
BR112012023836A2 (pt) composto tricíclicos e inibidores de pbk contendo os mesmos
PE20191134A1 (es) Composiciones y metodos relacionados con agonistas de piridinoilpiperidina 5-ht1f
UY37139A (es) Monotartrato de vinorelbina y su uso farmacéutico
CR20190028A (es) Compuestos heterocíclicos como inmunomoduladores
AR093874A1 (es) Composicion para control de malezas