CA3002850A1 - Substituted indazole compounds as rorgammat inhibitors and uses thereof - Google Patents

Substituted indazole compounds as rorgammat inhibitors and uses thereof Download PDF

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Publication number
CA3002850A1
CA3002850A1 CA3002850A CA3002850A CA3002850A1 CA 3002850 A1 CA3002850 A1 CA 3002850A1 CA 3002850 A CA3002850 A CA 3002850A CA 3002850 A CA3002850 A CA 3002850A CA 3002850 A1 CA3002850 A1 CA 3002850A1
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CA
Canada
Prior art keywords
chloro
indazol
ene
tetrahydro
carboxylic acid
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA3002850A
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English (en)
French (fr)
Inventor
Blair T. Lapointe
Peter H. Fuller
Hakan GUNAYDIN
Kun Liu
Mark E. Scott
B. Wesley Trotter
Hongjun Zhang
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Merck Sharp & Dohme LLC
Original Assignee
Merck Sharp & Dohme LLC
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 Merck Sharp & Dohme LLC filed Critical Merck Sharp & Dohme LLC
Publication of CA3002850A1 publication Critical patent/CA3002850A1/en
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA3002850A 2015-10-27 2016-10-27 Substituted indazole compounds as rorgammat inhibitors and uses thereof Abandoned CA3002850A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562246921P 2015-10-27 2015-10-27
US62/246,921 2015-10-27
US201662372544P 2016-08-09 2016-08-09
US62/372,544 2016-08-09
PCT/US2016/059063 WO2017075182A1 (en) 2015-10-27 2016-10-27 Substituted indazole compounds as rorgammat inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
CA3002850A1 true CA3002850A1 (en) 2017-05-04

Family

ID=58631831

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3002850A Abandoned CA3002850A1 (en) 2015-10-27 2016-10-27 Substituted indazole compounds as rorgammat inhibitors and uses thereof

Country Status (11)

Country Link
US (2) US10287272B2 (enExample)
EP (1) EP3368539B1 (enExample)
JP (1) JP2018535958A (enExample)
KR (1) KR20180070697A (enExample)
CN (1) CN108431009A (enExample)
AU (1) AU2016344115A1 (enExample)
CA (1) CA3002850A1 (enExample)
IL (1) IL258870A (enExample)
MX (1) MX2018005004A (enExample)
RU (1) RU2018117503A (enExample)
WO (1) WO2017075182A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
JP2018531958A (ja) 2015-10-27 2018-11-01 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ＲＯＲγＴ阻害薬としてのヘテロアリール置換安息香酸及びその使用
US10287272B2 (en) 2015-10-27 2019-05-14 Merck Sharp & Dohme Corp. Substituted indazole compounds as RORgammaT inhibitors and uses thereof
US10584133B2 (en) 2018-03-30 2020-03-10 Biotheryx, Inc. Thienopyrimidinone compounds
WO2020229398A1 (de) 2019-05-14 2020-11-19 Bayer Aktiengesellschaft (1-alkenyl)-substituierte pyrazole und triazole als schädlingsbekämpfungsmittel
AU2021409234A1 (en) * 2020-12-22 2023-06-29 Merck Sharp & Dohme Llc Preparation of tetrahydroindazole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors

Family Cites Families (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4670447A (en) 1983-08-22 1987-06-02 Hoechst-Roussel Pharmaceuticals Inc. Antipsychotic 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles
GB8607294D0 (en) 1985-04-17 1986-04-30 Ici America Inc Heterocyclic amide derivatives
US4751235A (en) 1986-12-23 1988-06-14 Sandoz Pharm. Corp. Anti-atherosclerotic indolizine derivatives
PT95899A (pt) 1989-11-17 1991-09-13 Glaxo Group Ltd Processo para a preparacao de derivados indole
TW263508B (enExample) 1991-02-12 1995-11-21 Pfizer
JP3414433B2 (ja) 1993-03-01 2003-06-09 日本化薬株式会社 電子写真用トナー
US5639780A (en) 1995-05-22 1997-06-17 Merck Frosst Canada, Inc. N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase inhibitors
DE19523446A1 (de) 1995-06-28 1997-01-02 Bayer Ag Benzotriazole
AU6490396A (en) 1995-07-14 1997-02-18 Smithkline Beecham Corporation Substituted-pent-4-ynoic acids
JPH11514969A (ja) 1995-08-10 1999-12-21 バイエル・アクチエンゲゼルシヤフト ハロベンゾイミダゾール類および殺微生物剤としてのそれらの使用
EP0882718B1 (en) 1995-12-28 2005-08-31 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
CA2258728C (en) 1996-06-19 2011-09-27 Rhone Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
HUP9903330A2 (hu) 1996-11-19 2000-03-28 Amgen Inc. Gyulladásgátló hatású, aril- és heteroaril csoporttal szubsztituált kondenzált pirrolszármazékok, valamint ezeket tartalmazó gyógyászati készítmények
US6828344B1 (en) 1998-02-25 2004-12-07 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6133290A (en) 1998-07-31 2000-10-17 Eli Lilly And Company 5-HT1F agonists
CZ2001959A3 (cs) 1998-09-18 2001-12-12 Basf Aktiengesellschaft 4-Aminopyrrolopyrimidiny jako inhibitory kinasy
US6348032B1 (en) 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
WO2001012600A1 (en) 1999-08-12 2001-02-22 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
US7115750B1 (en) 1999-09-20 2006-10-03 Takeda Pharmaceutical Company Limited Melanin concentrating hormone antagonist
GB0117577D0 (en) 2001-02-16 2001-09-12 Aventis Pharm Prod Inc Novel heterocyclic substituted carbonyl derivatives and their use as dopamine D receptor ligands
TWI239942B (en) 2001-06-11 2005-09-21 Dainippon Pharmaceutical Co N-arylphenylacetamide derivative and pharmaceutical composition containing the same
MXPA04001014A (es) 2001-08-03 2004-05-27 Schering Corp Novedosos inhibidores de la gama secretasa.
US7355042B2 (en) 2001-10-16 2008-04-08 Hypnion, Inc. Treatment of CNS disorders using CNS target modulators
DE10229777A1 (de) 2002-07-03 2004-01-29 Bayer Ag Indolin-Phenylsulfonamid-Derivate
FR2845382A1 (fr) 2002-10-02 2004-04-09 Sanofi Synthelabo Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique
UA80171C2 (en) 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
JP4601038B2 (ja) 2003-03-26 2010-12-22 第一三共株式会社 インドリルマレイミド類
NZ546611A (en) 2003-09-18 2010-02-26 Conforma Therapeutics Corp Novel heterocyclic compounds as HSP90-inhibitors
SE0302760D0 (sv) 2003-10-20 2003-10-20 Biovitrum Ab New compounds
US7420059B2 (en) 2003-11-20 2008-09-02 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
BRPI0418026A (pt) 2003-12-22 2007-04-17 Ajinomoto Kk derivados de fenilalanina ou sais farmaceuticamente aceitáveis destes, composição farmacêutica, antagonista de alfa4 integrina, e, agente terapêutico ou agente preventivo para doenças
JP2007517052A (ja) 2003-12-23 2007-06-28 ノバルティス アクチエンゲゼルシャフト 二環式ヘテロ環式ｐ−３８キナーゼ阻害剤
EP1771204A4 (en) 2004-07-01 2008-08-13 Univ New York COMPOSITIONS AND METHOD FOR MODULATING ROR-GAMMA-T
GT200500208A (es) 2004-08-03 2006-03-02 Indazoles ùtiles para tratar enfermedades cardiovasculares
US20070010537A1 (en) 2004-08-20 2007-01-11 Kazumasa Hamamura Fused pyramidine derivative and use thereof
CN101048407A (zh) 2004-09-03 2007-10-03 普莱希科公司 双环杂芳基pde4b抑制剂
SE0402762D0 (sv) 2004-11-11 2004-11-11 Astrazeneca Ab Indazole sulphonamide derivatives
CN100516049C (zh) 2004-11-16 2009-07-22 永信药品工业股份有限公司 抗血管生成药n2-(取代的芳基甲基)-3-(取代的苯基)吲唑的合成
AR051780A1 (es) 2004-11-29 2007-02-07 Japan Tobacco Inc Compuestos en anillo fusionados que contienen nitrogeno y utilizacion de los mismos
EP1828180A4 (en) 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
RU2008110908A (ru) 2005-08-25 2009-09-27 Шеринг Корпорейшн (US) Производные имидазола в качестве функционально селективных агонистов альфа2с адренорецепторов
US8003624B2 (en) 2005-08-25 2011-08-23 Schering Corporation Functionally selective ALPHA2C adrenoreceptor agonists
JP2009509928A (ja) 2005-09-01 2009-03-12 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ カリウムチャンネル開口剤としての新規ベンゾピラン誘導体
JP4843040B2 (ja) 2005-09-15 2011-12-21 エフ．ホフマン−ラ ロシュ アーゲー 肝カルニチンパルミトイルトランスフェラーゼのインヒビターとして有用な新規ヘテロ二環式誘導体
AU2007214594B2 (en) 2006-02-13 2010-11-11 F. Hoffmann-La Roche Ag Heterobicyclic sulfonamide derivatives for the treatment of diabetes
KR101411695B1 (ko) 2006-02-17 2014-07-03 리겔 파마슈티칼스, 인크. 자가면역 질환의 치료 또는 예방을 위한 2,4-피리미딘디아민 화합물
EP1984351A1 (en) 2006-02-17 2008-10-29 Memory Pharmaceuticals Corporation Compounds having 5-ht6 receptor affinity
JP4675801B2 (ja) 2006-03-06 2011-04-27 日本メナード化粧品株式会社 Ｒｏｒ活性化剤
US7723330B2 (en) 2006-03-07 2010-05-25 Array Biopharma Inc. Heterobicyclic pyrazole compounds and methods of use
WO2007125405A2 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
US20080305169A1 (en) 2006-05-26 2008-12-11 Japan Tobacco Inc. Pharmaceutical Compositions Comprising Nitrogen-Containing Fused Ring Coumpounds
EP2029550A2 (en) 2006-06-01 2009-03-04 Wyeth a Corporation of the State of Delaware 1-sulfonylindazolylamine and -amide derivatives as 5-hydroxytryptamine-6 ligands
GB0611587D0 (en) 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
WO2008003703A1 (en) 2006-07-03 2008-01-10 Biovitrum Ab (Publ) Indoles as 5-ht6 modulators
TWI315304B (en) 2006-08-31 2009-10-01 Univ Taipei Medical Indoline-sulfonamides compounds
WO2008045664A2 (en) 2006-10-06 2008-04-17 Kalypsys, Inc. Heterocyclic pde4 inhibitors as antiinflammatory agents
WO2008062740A1 (fr) 2006-11-20 2008-05-29 Japan Tobacco Inc. Composé azoté à anneaux fusionnés et son utilisation
US7799933B2 (en) 2006-12-21 2010-09-21 Hoffman-La Roche Inc. Sulfonamide derivatives
US20080186971A1 (en) 2007-02-02 2008-08-07 Tarari, Inc. Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic
MX2009011210A (es) 2007-04-16 2009-10-30 Abbott Lab Inhibidores de mcl1 de indol 7-no sustituido.
GB0708141D0 (en) 2007-04-26 2007-06-06 Syngenta Participations Ag Improvements in or relating to organic compounds
AR067326A1 (es) 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
EP2154965A4 (en) 2007-05-29 2011-08-17 Glaxosmithkline Llc NAPHTHYRIDINE DERIVATIVES AS P13 KINASE INHIBITORS
AR068046A1 (es) 2007-06-05 2009-11-04 Schering Corp Derivados policiclicos de indazol y su uso como inhibidores de erk para el tratamiento del cancer
US7776877B2 (en) 2007-06-22 2010-08-17 Chemocentryx, Inc. N-(2-(hetaryl)aryl) arylsulfonamides and N-(2-(hetaryl) hetaryl arylsulfonamides
JP2010534665A (ja) 2007-07-25 2010-11-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング グルココルチコイドミメチックス、それらの製造方法、医薬組成物、及びこれらの使用
EP2197876A1 (en) 2007-08-29 2010-06-23 Glaxosmithkline LLC Thiazole and oxazole kinase inhibitors
US7960376B2 (en) 2007-09-14 2011-06-14 Cara Therapeutics, Inc. Benzo-fused heterocycles
RU2364597C1 (ru) 2007-12-14 2009-08-20 Андрей Александрович Иващенко ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ Hh-СИГНАЛЬНОГО КАСКАДА, ЛЕКАРСТВЕННЫЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С АББЕРАНТНОЙ АКТИВНОСТЬЮ Hh СИГНАЛЬНОЙ СИСТЕМЫ
US7960377B2 (en) 2008-03-28 2011-06-14 Cara Therapeutics, Inc. Substituted pyridoxazines
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
EP2280946B1 (en) 2008-06-05 2016-02-10 Glaxo Group Limited 4-carboxamide indazole derivatives useful as inhibitors of p13-kinases
WO2009147188A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Benzpyrazol derivatives as inhibitors of pi3 kinases
NZ589694A (en) 2008-06-09 2012-05-25 Sanofi Aventis Annelated n-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
WO2009149819A1 (en) 2008-06-09 2009-12-17 Sanofi-Aventis Annelated pyrrolidin sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals
EP2298731A4 (en) 2008-06-25 2011-09-21 Takeda Pharmaceutical AMIDE COMPOUND
WO2010017827A1 (en) 2008-08-14 2010-02-18 European Molecular Biology Laboratory 6-substituted 1-sulfonyl-2, 3-dihydro-indole derivatives for the treatment of proliferative diseases
SI2344471T1 (sl) 2008-10-02 2013-11-29 Taisho Pharmaceutical Co., Ltd. Derivat 7-piperidinoalkil-3,4-dihidrokvinolona
EP2181710A1 (en) 2008-10-28 2010-05-05 Phenex Pharmaceuticals AG Ligands for modulation of orphan receptor-gamma (NR1F3) activity
WO2010050837A1 (ru) 2008-10-28 2010-05-06 Haskin Lev Yakovlevich Ветроэнергетическая установка
WO2010057101A2 (en) 2008-11-17 2010-05-20 Schering Corporation Compounds useful as hiv blockers
EP2367598B1 (en) 2008-11-19 2014-04-09 Merck Sharp & Dohme Corp. Inhibitors of diacylglycerol acyltransferase
CN102264743B (zh) 2008-11-25 2015-02-11 罗彻斯特大学 Mlk抑制剂及其使用方法
CN102388054B (zh) 2008-12-19 2015-03-04 西特里斯药业公司 噻唑并吡啶沉默调节蛋白调节剂的化合物
TW201030007A (en) 2009-02-06 2010-08-16 Gruenenthal Gmbh Substituted spiro-amides as b1r modulators
US8524751B2 (en) 2009-03-09 2013-09-03 GlaxoSmithKline Intellecutual Property Development 4-oxadiazol-2-YL-indazoles as inhibitors of P13 kinases
TW201102391A (en) 2009-03-31 2011-01-16 Biogen Idec Inc Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use
WO2010123139A1 (ja) 2009-04-24 2010-10-28 持田製薬株式会社 スルファモイル基を有するアリールカルボキサミド誘導体
RS53830B1 (sr) 2009-04-30 2015-06-30 Glaxo Group Limited Indazoli supstituisani oksazolom kao inhibitori pi3-kinaze
WO2010150837A1 (ja) 2009-06-25 2010-12-29 第一三共株式会社 インドリン誘導体
EP2459184A1 (en) 2009-07-31 2012-06-06 The Brigham and Women's Hospital, Inc. Modulation of sgk1 expression in th17 cells to modulate th17-mediated immune responses
US8119683B2 (en) 2009-08-10 2012-02-21 Taipei Medical University Aryl substituted sulfonamide compounds and their use as anticancer agents
WO2011059839A1 (en) 2009-10-29 2011-05-19 Sirtris Pharmaceuticals, Inc. Bicyclic pyridines and analogs as sirtuin modulators
WO2011067365A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
WO2011067364A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Novel compounds
EP2507231A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
AU2010330894A1 (en) 2009-12-18 2012-07-05 Janssen Pharmaceutica Nv Substituted aminothiazolone indazoles as estrogen related receptor-aalpha modulators
US9260382B2 (en) 2010-02-16 2016-02-16 Uwm Research Foundation Methods of reducing virulence in bacteria
CA2791738C (en) 2010-03-01 2020-06-09 Gtx, Inc. Aryl imidazolyl compounds for the treatment of cancer
EP2571361A4 (en) 2010-05-19 2013-11-13 Univ North Carolina PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
EP2613781B1 (en) 2010-09-08 2016-08-24 GlaxoSmithKline Intellectual Property Development Limited Indazole derivatives for use in the treatment of influenza virus infection
HRP20151017T1 (hr) 2010-09-08 2015-10-23 Glaxosmithkline Intellectual Property Development Limited Polimorfi i soli n-[5-[4-(5-{[(2r,6s)-2,6-dimetil-4-morfolinil]metil}-1,3-oksazol-2-il)-1h-indazol-6-il]-2-(metiloksi)-3-piridinil]metansulfonamida
WO2012037108A1 (en) 2010-09-13 2012-03-22 Glaxosmithkline Llc Aminoquinoline derivatives as antiviral agents
JP6063870B2 (ja) 2010-11-08 2017-01-18 ライセラ・コーポレイション ＲＯＲγ活性の阻害用のＮ−スルホニル化テトラヒドロキノリンおよび関連二環化合物および病気の治療
KR20120063283A (ko) 2010-12-07 2012-06-15 제일약품주식회사 신규한 피라졸로 피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 약학적 조성물
WO2012085168A1 (en) 2010-12-22 2012-06-28 Ludwig-Maximilians-Universität München Organozinc complexes and processes for making and using the same
EP2487159A1 (en) 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
EP2511263A1 (en) 2011-04-14 2012-10-17 Phenex Pharmaceuticals AG Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORgamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
JP2014166961A (ja) 2011-06-20 2014-09-11 Dainippon Sumitomo Pharma Co Ltd 新規インダゾール誘導体
CA2871504C (en) 2012-05-08 2020-07-21 Merck Sharp & Dohme Corp. Bicyclic sulfone compounds for inhibition of rorgamma activity and the treatment of disease
RU2014149136A (ru) 2012-05-08 2016-07-10 Мерк Шарп И Доум Корп. ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ
WO2014026327A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 4-heteroaryl substituted benzoic acid compounds as rorgammat inhibitors and uses thereof
WO2014026328A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-cyclohexenyl substituted indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026329A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
WO2014026330A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2015008234A1 (en) 2013-07-17 2015-01-22 Glenmark Pharmaceuticals S.A. Bicyclic heterocyclic compounds as ror gamma modulators
TW201605797A (zh) 2013-12-10 2016-02-16 葛蘭馬克製藥公司 作為ror伽馬調節物的雙環雜芳基化合物
WO2015095788A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2015095792A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2015139621A1 (zh) * 2014-03-18 2015-09-24 北京韩美药品有限公司 4-杂芳基取代的苯甲酸或苯甲酰胺类化合物
JP2016141632A (ja) * 2015-01-30 2016-08-08 第一三共株式会社 縮合二環式ヘテロ環誘導体
CA2975997A1 (en) * 2015-02-11 2016-08-18 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as rorgammat inhibitors and uses thereof
WO2016128908A1 (en) 2015-02-12 2016-08-18 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
JP2018531958A (ja) 2015-10-27 2018-11-01 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ＲＯＲγＴ阻害薬としてのヘテロアリール置換安息香酸及びその使用
US10287272B2 (en) 2015-10-27 2019-05-14 Merck Sharp & Dohme Corp. Substituted indazole compounds as RORgammaT inhibitors and uses thereof
EP3368516B1 (en) 2015-10-27 2020-07-15 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF

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