EA026431B1 - Модуляторы x рецепторов печени - Google Patents

Модуляторы x рецепторов печени Download PDF

Info

Publication number
EA026431B1
EA026431B1 EA201491610A EA201491610A EA026431B1 EA 026431 B1 EA026431 B1 EA 026431B1 EA 201491610 A EA201491610 A EA 201491610A EA 201491610 A EA201491610 A EA 201491610A EA 026431 B1 EA026431 B1 EA 026431B1
Authority
EA
Eurasian Patent Office
Prior art keywords
isopropyl
disease
methylsulfonyl
mmol
mixture
Prior art date
Application number
EA201491610A
Other languages
English (en)
Russian (ru)
Other versions
EA201491610A1 (ru
Inventor
Чэнго Дон
И Фань
Катерина Лефтерис
Стивен Лотеста
Суреш Б. Сингх
Колин Тайс
Вэй Чжао
Яцзюнь Чжэн
Линхан Чжуан
Original Assignee
Вайтаи Фармасьютиклз, Инк.
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 Вайтаи Фармасьютиклз, Инк. filed Critical Вайтаи Фармасьютиклз, Инк.
Publication of EA201491610A1 publication Critical patent/EA201491610A1/ru
Publication of EA026431B1 publication Critical patent/EA026431B1/ru

Links

Classifications

    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Child & Adolescent Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
EA201491610A 2012-03-16 2013-03-14 Модуляторы x рецепторов печени EA026431B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261612063P 2012-03-16 2012-03-16
PCT/US2013/031250 WO2013138568A1 (en) 2012-03-16 2013-03-14 Liver x reception modulators

Publications (2)

Publication Number Publication Date
EA201491610A1 EA201491610A1 (ru) 2014-12-30
EA026431B1 true EA026431B1 (ru) 2017-04-28

Family

ID=47997958

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201491610A EA026431B1 (ru) 2012-03-16 2013-03-14 Модуляторы x рецепторов печени

Country Status (27)

Country Link
US (5) US9073931B2 (https=)
EP (1) EP2825542B1 (https=)
JP (3) JP6114815B2 (https=)
KR (1) KR102069913B1 (https=)
CN (1) CN104203950B (https=)
AU (1) AU2013232069B2 (https=)
BR (1) BR112014022780A8 (https=)
CA (1) CA2865639C (https=)
CY (1) CY1118323T1 (https=)
DK (1) DK2825542T3 (https=)
EA (1) EA026431B1 (https=)
ES (1) ES2607113T3 (https=)
HR (1) HRP20161690T1 (https=)
HU (1) HUE030785T2 (https=)
IL (2) IL234301A (https=)
LT (1) LT2825542T (https=)
ME (1) ME02660B (https=)
MX (1) MX354820B (https=)
NZ (1) NZ629189A (https=)
PL (1) PL2825542T3 (https=)
PT (1) PT2825542T (https=)
RS (1) RS55532B1 (https=)
SG (1) SG11201405323YA (https=)
SI (1) SI2825542T1 (https=)
SM (2) SMT201700009T1 (https=)
WO (1) WO2013138568A1 (https=)
ZA (1) ZA201406390B (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013138568A1 (en) * 2012-03-16 2013-09-19 Vitae Pharmaceuticals, Inc. Liver x reception modulators
CN104203951B (zh) * 2012-03-16 2016-11-02 生命医药公司 肝x受体调节剂
WO2015106164A1 (en) 2014-01-10 2015-07-16 Rgenix, Inc. Lxr agonists and uses thereof
WO2015195922A1 (en) * 2014-06-19 2015-12-23 Vitae Pharmaceuticals, Inc. Compounds for use in treating acute coronary syndrome and related conditions
BR112017002260A2 (pt) * 2014-08-07 2017-11-21 Vitae Pharmaceuticals Inc derivados de piperazina como moduladores do receptor x do fígado
EP3373935B1 (en) 2015-11-12 2021-09-01 Merck Sharp & Dohme Corp. Cyanopyridine derivatives as liver x receptor beta agonists, compositions, and their use
EP3402477A4 (en) 2016-01-11 2019-08-21 The Rockefeller University METHOD FOR THE TREATMENT OF DISEASES RELATED TO MYELOID-DERIVED SUPPRESSOR CELLS
EP3490579B1 (en) 2016-07-27 2025-09-10 Hartis-Pharma SA Therapeutic combinations to treat red blood cell disorders
CA3078981A1 (en) 2017-11-21 2019-05-31 Rgenix, Inc. Polymorphs and uses thereof
MY198220A (en) 2018-05-15 2023-08-14 Alkahest Inc Treatment Of Aging-Associated Disease With Modulators Of Leukotriene A4 Hydrolase
JP7654202B2 (ja) * 2019-02-28 2025-04-01 ザ ロックフェラー ユニバーシティー がんの予後及び治療におけるapoe遺伝子型決定
EP3999055A1 (en) 2019-07-15 2022-05-25 Novartis AG Methods for treating meibomian gland dysfunction with liver x receptor agonists
TWI888447B (zh) 2019-12-13 2025-07-01 美商因思博納公司 金屬鹽及其用途
US12575690B2 (en) * 2023-07-26 2026-03-17 Brumate, Inc. Keyed straw

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101456863A (zh) * 2007-12-14 2009-06-17 华北制药集团新药研究开发有限责任公司 新的lxr激动剂及其制备方法和用途
WO2009086129A1 (en) * 2007-12-21 2009-07-09 Wyeth Pyrazolo [1,5-a] pyrimidine compounds

Family Cites Families (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4748247A (en) 1986-10-21 1988-05-31 American Home Products Corporation 2-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]alkyl]alkyl]pyrido- and pyrazino-indole-1,3-dione derivatives as histamine H1 antagonists
CA2074163A1 (en) 1990-01-22 1991-07-23 William Thomas Zimmerman Herbicidal sulfonylureas
EP0572863A1 (de) 1992-06-05 1993-12-08 F. Hoffmann-La Roche Ag ZNS Pyrazinoindole
US5545636A (en) 1993-12-23 1996-08-13 Eli Lilly And Company Protein kinase C inhibitors
CA2179650C (en) 1993-12-23 2007-10-30 William Francis Heath, Jr. Bisindolemaleimides and their use as protein kinase c inhibitors
AU3831495A (en) 1994-10-20 1996-05-15 American Home Products Corporation Indole derivatives useful as serotonergic agents
AU709631B2 (en) 1996-06-28 1999-09-02 Merck & Co., Inc. Fibrinogen receptor antagonist prodrugs
US5854245A (en) 1996-06-28 1998-12-29 Merck & Co., Inc. Fibrinogen receptor antagonists
JP2000513375A (ja) 1996-06-28 2000-10-10 メルク エンド カンパニー インコーポレーテッド フィブリノーゲンレセプター拮抗薬プロドラッグ
WO1998000134A1 (en) 1996-06-28 1998-01-08 Merck & Co., Inc. Fibrinogen receptor antagonists
US6177440B1 (en) 1996-10-30 2001-01-23 Eli Lilly And Company Substituted tricyclics
FR2761073B1 (fr) 1997-03-20 1999-04-23 Synthelabo Derives de pyrazino[1,2-a]indole-1-one, leur preparation et leur application en therapeutique
FR2761070B1 (fr) 1997-03-20 1999-04-23 Synthelabo Derives de dihydropyrazino[1,2-a]indole-1-one, leur preparation et leur application en therapeutique
DE19802235A1 (de) 1998-01-22 1999-07-29 Bayer Ag Mit tricyclischen Indolen substituierte Oxazolidinone
IL129484A0 (en) 1998-04-17 2000-02-29 Lilly Co Eli Substituted tricyclics
DE60018274T2 (de) 1999-05-06 2005-08-04 Neurogen Corp., Branford Substituierte 4-oxo-chinolin-3-carboxamide als gaba gehirnrezeptorliganden
US7037916B2 (en) 1999-07-15 2006-05-02 Pharmacopeia Drug Discovery, Inc. Pyrimidine derivatives as IL-8 receptor antagonists
IT1313593B1 (it) * 1999-08-03 2002-09-09 Novuspharma Spa Derivati di 1,2-diidro-1-oxo-pirazino 1,2-a indolo.
WO2001030331A2 (en) 1999-10-22 2001-05-03 Eli Lilly And Company Therapeutic compositions including protein kinase c inhibitors
DE60132975T2 (de) 2000-01-06 2009-02-26 Merck Frosst Canada Inc., Kirkland Neue substanzen und verbindungen als protease-inhibitoren
JP4180365B2 (ja) 2000-07-31 2008-11-12 エフ.ホフマン−ラ ロシュ アーゲー ピペラジン誘導体
EP1343768A1 (en) 2000-12-20 2003-09-17 Bristol-Myers Squibb Pharma Company Aryl and aminoaryl substituted serotonin receptor agonist and antagonist ligands
GB0106177D0 (en) * 2001-03-13 2001-05-02 Hoffmann La Roche Piperazine derivatives
FR2829766A1 (fr) 2001-09-14 2003-03-21 Lipha Derives d'oxamates comportant un heterocycle azote diversement substitue
CA2471562A1 (en) 2001-12-21 2003-07-24 King Pharmaceuticals Research And Development, Inc. Tyrosyl derivatives and their use as p2x7 receptor modulators
US7919497B2 (en) 2002-08-02 2011-04-05 Nereus Pharmaceuticals, Inc. Analogs of dehydrophenylahistins and their therapeutic use
DE10320780A1 (de) 2003-05-09 2005-01-20 Bayer Healthcare Ag Heterocyclyl-substituierte Dihydrochinazoline
US7994196B2 (en) 2004-02-12 2011-08-09 Mitsubishi Tanabe Pharma Corporation Indazole compound and pharmaceutical use thereof
BRPI0509754A (pt) 2004-04-08 2007-10-16 Novartis Ag inibidores de proteìna quinase c para o tratamento de doenças auto-imunes e de rejeição a transplante
RU2266906C1 (ru) 2004-04-29 2005-12-27 Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") Анелированные карбамоилазагетероциклы, способы их получения (варианты), фармацевтическая композиция, фокусированная библиотека
ITMI20040874A1 (it) 2004-04-30 2004-07-30 Ist Naz Stud Cura Dei Tumori Derivati indolici ed azaindolici con azione antitumorale
WO2005113526A2 (en) 2004-05-21 2005-12-01 Pfizer Products Inc. Metabolites of 4-(3,4-dichloro-phenyl)-2-[2-(4-methyl-piperazin-1-yl)-benzylidene]-thiomorpholin-3-one
ATE457989T1 (de) * 2004-12-15 2010-03-15 Hoffmann La Roche Bi- und trizyklische substituierte phenyl- methanone als inhibitoren von glycin-i (glyt-1)- transportern zur behandlung der alzheimer- krankheit
WO2006072608A2 (en) 2005-01-03 2006-07-13 Universitá Degli Studi Di Siena Aryl piperazine derivatives for the treatment of neuropsychiatric disorders
US7790712B2 (en) 2005-03-17 2010-09-07 Boehringer Ingelheim Pharmaceutical, Inc. Substituted [1,4]diazepino[1,2-A]indoles and azepino[1,2-A]indoles as anti-cytokine inhibitors
WO2006106423A2 (en) 2005-04-07 2006-10-12 Pfizer Inc. Amino sulfonyl derivatives as inhibitors of human 11-.beta.-hydrosysteroid dehydrogenase
CA2615726C (en) 2005-07-14 2014-05-27 Caterina Bissantz Indol-3-yl-carbonyl-spiro-piperidine derivatives as v1a receptor antagonists
WO2007035841A1 (en) 2005-09-21 2007-03-29 Nereus Pharmaceuticals, Inc. Analogs of dehydrophenylahistins and their therapeutic use
EP1779848A1 (en) 2005-10-28 2007-05-02 Nikem Research S.R.L. V-ATPase inhibitors for the treatment of inflammatory and autoimmune diseases
JP4882127B2 (ja) * 2005-11-16 2012-02-22 株式会社ジェイテクト 位置調整式ステアリング装置
JP2007137810A (ja) * 2005-11-17 2007-06-07 Sankyo Co Ltd インドール化合物を含有する医薬
DE602006010433D1 (de) 2005-12-09 2009-12-24 Hoffmann La Roche Für die behandlung von obesitas geeignete tricyclische amidderivate
US7351706B2 (en) 2006-01-05 2008-04-01 Hoffmann-La Roche Inc. Indol-3-yl-carbonyl-spiro-piperidine derivatives
FR2897061B1 (fr) * 2006-02-03 2010-09-03 Sanofi Aventis Derives de n-heteroaryl-carboxamides tricycliques contenant un motif benzimidazole, leur preparation et leur application en therapeutique.
RU2318818C1 (ru) 2006-04-12 2008-03-10 Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" Азагетероциклы, комбинаторная библиотека, фокусированная библиотека, фармацевтическая композиция и способ получения (варианты)
US8129527B2 (en) 2006-11-03 2012-03-06 Nereus Pharmacuticals, Inc. Analogs of dehydrophenylahistins and their therapeutic use
WO2008122115A1 (en) 2007-04-09 2008-10-16 Methylgene Inc. Inhibitors of histone deacetylase
CA2690748A1 (en) 2007-06-25 2008-12-31 Neurogen Corporation Piperazinyl oxoalkyl tetrahydro-beta-carbolines and related analogues
EP2205085A1 (en) 2007-09-25 2010-07-14 Merck Sharp & Dohme Corp. 2-aryl or heteroaryl indole derivatives
PE20091439A1 (es) 2008-01-22 2009-10-19 Takeda Pharmaceutical Compuestos triciclicos como antagonistas de crf
US20090192147A1 (en) 2008-01-30 2009-07-30 Wyeth [a]-FUSED INDOLE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
US20100137320A1 (en) 2008-02-29 2010-06-03 Schering Corporation Gamma secretase modulators
EP2254886B1 (en) 2008-03-28 2016-05-25 Nerviano Medical Sciences S.r.l. 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
TW201031665A (en) 2009-02-04 2010-09-01 Gruenenthal Gmbh Substituted indole-compound
AU2010257856A1 (en) 2009-06-08 2011-11-03 Grünenthal GmbH Substituted benzimidazoles, benzothiazoles and benzoxazoles
WO2011005295A1 (en) 2009-06-24 2011-01-13 Arena Pharmaceuticals, Inc. Modulators of the sphingosine-1-phosphate (s1p) receptor useful for the treatment of disorders related thereto
MX2012002898A (es) 2009-09-11 2012-04-02 Sunovion Pharmaceuticals Inc Agonistas y antagonistas inversos de histamina h3 y metodos de uso para los mismos.
WO2011071725A1 (en) 2009-12-07 2011-06-16 Boehringer Ingelheim International Gmbh Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
US20130045203A1 (en) 2010-03-02 2013-02-21 Emory University Uses of Noscapine and Derivatives in Subjects Diagnosed with FAP
KR101302474B1 (ko) 2012-02-20 2013-09-02 주식회사 케이씨씨 내충격성 및 불연성이 우수한 진공단열재용 봉지부재
WO2013138568A1 (en) * 2012-03-16 2013-09-19 Vitae Pharmaceuticals, Inc. Liver x reception modulators
CN104203951B (zh) * 2012-03-16 2016-11-02 生命医药公司 肝x受体调节剂

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101456863A (zh) * 2007-12-14 2009-06-17 华北制药集团新药研究开发有限责任公司 新的lxr激动剂及其制备方法和用途
WO2009086129A1 (en) * 2007-12-21 2009-07-09 Wyeth Pyrazolo [1,5-a] pyrimidine compounds

Also Published As

Publication number Publication date
WO2013138568A8 (en) 2014-08-28
CN104203950B (zh) 2016-08-24
EP2825542B1 (en) 2016-09-14
ZA201406390B (en) 2019-11-27
PT2825542T (pt) 2016-12-20
BR112014022780A2 (pt) 2017-06-20
HK1206332A1 (en) 2016-01-08
KR20140135829A (ko) 2014-11-26
BR112014022780A8 (pt) 2021-06-15
MX2014011104A (es) 2014-12-05
AU2013232069A1 (en) 2014-09-18
US20170007603A1 (en) 2017-01-12
DK2825542T3 (en) 2017-01-09
SG11201405323YA (en) 2014-10-30
ME02660B (me) 2017-06-20
JP2017128589A (ja) 2017-07-27
US9416135B2 (en) 2016-08-16
NZ629189A (en) 2016-08-26
HRP20161690T1 (hr) 2017-02-24
US20180117041A1 (en) 2018-05-03
MX354820B (es) 2018-03-21
LT2825542T (lt) 2016-12-27
RS55532B1 (sr) 2017-05-31
JP2015514061A (ja) 2015-05-18
US20150336963A1 (en) 2015-11-26
IL251897A0 (en) 2017-06-29
US9073931B2 (en) 2015-07-07
EP2825542A1 (en) 2015-01-21
SI2825542T1 (sl) 2017-01-31
AU2013232069B2 (en) 2017-07-13
PL2825542T3 (pl) 2017-05-31
SMT201700009T1 (it) 2017-03-08
CA2865639C (en) 2020-12-22
ES2607113T3 (es) 2017-03-29
US9707232B2 (en) 2017-07-18
JP6114815B2 (ja) 2017-04-12
HUE030785T2 (en) 2017-06-28
SMT201700009B (it) 2017-03-08
CY1118323T1 (el) 2017-06-28
KR102069913B1 (ko) 2020-01-23
WO2013138568A1 (en) 2013-09-19
JP2019006813A (ja) 2019-01-17
CA2865639A1 (en) 2013-09-19
EA201491610A1 (ru) 2014-12-30
IL234301A (en) 2017-09-28
US20150065515A1 (en) 2015-03-05
US20200138812A1 (en) 2020-05-07
CN104203950A (zh) 2014-12-10

Similar Documents

Publication Publication Date Title
EA026431B1 (ru) Модуляторы x рецепторов печени
ES2987014T3 (es) Derivados carboxi con propiedades antiinflamatorias
ES2598653T3 (es) Moduladores del receptor X del hígado
EP3848367A1 (en) Tricyclic compounds acting on crbn proteins
US9000182B2 (en) 2H-imidazol-4-amine compounds and their use as BACE inhibitors
EP3929185A1 (en) Nitrogen-containing fused cyclic compound, preparation method therefor and use thereof
WO2012157746A1 (ja) 自己免疫疾患治療薬
EP3851436B1 (en) Novel heteroaromatic amide derivative and medicine containing same
JP2025541281A (ja) 炎症性疾患若しくは望ましくない免疫応答に関連する疾患の治療又は予防に使用するための置換ピリジン
TW202340207A (zh) Klf2誘導劑及其使用方法
CN112218878A (zh) Ntcp抑制剂
HK1206332B (en) Liver x receptor modulators