JP6549735B2 - 核内受容体調節剤 - Google Patents

核内受容体調節剤 Download PDF

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Publication number
JP6549735B2
JP6549735B2 JP2017563311A JP2017563311A JP6549735B2 JP 6549735 B2 JP6549735 B2 JP 6549735B2 JP 2017563311 A JP2017563311 A JP 2017563311A JP 2017563311 A JP2017563311 A JP 2017563311A JP 6549735 B2 JP6549735 B2 JP 6549735B2
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methyl
dichloro
dimethyl
trifluoromethyl
mmol
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JP2017563311A
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Japanese (ja)
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JP2018521020A5 (enExample
JP2018521020A (ja
Inventor
アージリアディ，マリア・エイ
ブレインリンガー，エリック・シー
キューザック，ケビン・ピー
ホブソン，エイドリアン・ディー
ポタン，ドミニク
バルサ，マルティーヌ
アモードリュ，ジェローム
プーパルダン，オリビア
ムーニエ，ロラン
コート，マイケル・イー
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アッヴィ・インコーポレイテッド
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Priority claimed from PCT/IB2015/001693 external-priority patent/WO2016198908A1/en
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
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    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
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    • 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
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    • C07D401/10—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 aromatic rings
    • 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
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    • 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
    • C07D403/10—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 aromatic 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
    • C07D405/10—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 carbon chain containing aromatic 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
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    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • C07D491/10—Spiro-condensed systems
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    • 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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017563311A 2015-06-09 2016-06-08 核内受容体調節剤 Expired - Fee Related JP6549735B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
PCT/IB2015/001693 WO2016198908A1 (en) 2015-06-09 2015-06-09 Ror nuclear receptor modulators
IBPCT/IB2015/001693 2015-06-09
US201562257806P 2015-11-20 2015-11-20
US62/257,806 2015-11-20
US201662343905P 2016-06-01 2016-06-01
US62/343,905 2016-06-01
PCT/US2016/036283 WO2016200851A1 (en) 2015-06-09 2016-06-08 Nuclear receptor modulators

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JP2018521020A JP2018521020A (ja) 2018-08-02
JP2018521020A5 JP2018521020A5 (enExample) 2019-02-28
JP6549735B2 true JP6549735B2 (ja) 2019-07-24

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021191774A (ja) * 2015-06-09 2021-12-16 アッヴィ・インコーポレイテッド 核内受容体調節剤

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201710164QA (en) 2015-06-09 2018-01-30 Bayer Pharma AG Positive allosteric modulators of muscarinic m2 receptor
GB201609601D0 (en) 2016-06-01 2016-07-13 Nucana Biomed Ltd Phosphoramidate compounds
CA3030204A1 (en) 2016-07-11 2018-01-18 Bayer Pharma Aktiengesellschaft 7-substituted 1-pyridyl-naphthyridine-3-carboxylic acid amides and use thereof
JOP20190045A1 (ar) 2016-09-14 2019-03-14 Bayer Ag مركبات أميد حمض 1- أريل-نفثيريدين-3-كربوكسيليك مستبدلة في الموضع 7 واستخدامها.
CN108689942B (zh) * 2017-04-11 2023-06-09 广东东阳光药业有限公司 含氮双环化合物及其制备方法和用途
US11427596B2 (en) * 2019-07-19 2022-08-30 Indian Institute of Technology Indore Metal-free solvent-free synthesis of fused-pyrido heterocycles and biomedical applications
CN110407863B (zh) * 2019-08-24 2021-08-17 中国科学院兰州化学物理研究所 一种通过转移硼化反应合成烯基硼酸酯类化合物的方法
CN110483561B (zh) * 2019-08-24 2021-07-23 中国科学院兰州化学物理研究所 一种烯基硼酸酯类化合物的合成方法
CN114436833B (zh) * 2021-12-27 2024-12-24 南京红太阳医药研究院有限公司 一种替米沙坦关键中间体4′-溴甲基联苯-2-羧酸酯的制备方法
WO2023232870A1 (en) 2022-05-31 2023-12-07 Immunic Ag Rorg/rorgt modulators for the treatment of virus infections like covid-19
AU2024267864A1 (en) * 2023-05-09 2025-11-06 11949098 Canada Inc. Inverse agonists of rar related orphan receptors (rors)
WO2024254218A2 (en) * 2023-06-05 2024-12-12 The Board Of Regents Of The University Of Texas System Non-peptide small molecule fgf14:nav1.6 channel complex protein-protein interaction modulators
CN117263810A (zh) * 2023-09-19 2023-12-22 上海凌凯医药科技有限公司 还原硝基苯制备苯胺类化合物以及选择性碘代苯胺类化合物的方法
CN119241538A (zh) * 2024-09-30 2025-01-03 陕西科技大学 一类三唑并吡啶结构的化合物、合成方法及其应用

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3334087B2 (ja) 1990-09-10 2002-10-15 アヴェンティス ファーマシューティカルズ インコーポレイテッド 選択的ロイコトリエンｂ▲４▼拮抗剤活性を示す置換された二環式アリール化合物
US5290798A (en) 1991-09-30 1994-03-01 Merck Frosst Canada, Inc. (hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis
ZA928276B (en) 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
JP3457694B2 (ja) 1993-02-04 2003-10-20 第一製薬株式会社 インフルエンザ感染予防・治療薬
US5589482A (en) 1994-12-14 1996-12-31 Pfizer Inc. Benzo-thiophene estrogen agonists to treat prostatic hyperplasia
US6124463A (en) 1998-07-02 2000-09-26 Dupont Pharmaceuticals Benzimidazoles as corticotropin release factor antagonists
US7157487B2 (en) 2000-12-28 2007-01-02 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitors
US20070129334A1 (en) 2001-10-30 2007-06-07 Conforma Therapeutics Corporation Orally Active Purine-Based Inhibitors of Heat Shock Protein 90
AU2003220896A1 (en) 2002-03-28 2003-11-10 Sumitomo Pharmaceuticals Co., Ltd. Novel heteroaryl compounds
CN1747949A (zh) 2002-12-20 2006-03-15 法马西亚公司 无环吡唑化合物
EP1628970A2 (en) 2003-04-30 2006-03-01 The Institutes of Pharmaceutical Discovery, LLC Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b
JP2007500703A (ja) 2003-07-28 2007-01-18 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 ベンズイミダゾール、ベンズチアゾールおよびベンゾキサゾール誘導体およびｌｔａ４ｈモジュレーターとしてのそれらの使用
UY28526A1 (es) 2003-09-24 2005-04-29 Boehringer Ingelheim Pharma Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
EA200700119A1 (ru) 2004-06-24 2007-10-26 Эли Лилли Энд Компани Соединения и способы лечения дислипидемии
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
EP1807072B1 (en) 2004-10-29 2009-01-07 Eli Lilly And Company Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
DK2395004T3 (en) * 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
FR2890071B1 (fr) 2005-08-30 2007-11-09 Fournier Sa Sa Lab Nouveaux composes de l'indole
AU2007227681A1 (en) 2006-03-15 2007-09-27 Wyeth N-substituted-azacyclylamines as histamine-3 antagonists
US8026257B2 (en) 2007-07-11 2011-09-27 Bristol-Myers Squibb Company Substituted heterocyclic ethers and their use in CNS disorders
KR101641596B1 (ko) * 2007-11-15 2016-07-21 엠에스디 이탈리아 에스.알.엘. Ｐａｒｐ 억제제로서의 피리다지논 유도체
US8450363B2 (en) 2009-02-06 2013-05-28 Elan Pharmaceuticals, Inc. Inhibitors of Jun N-terminal kinase
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
CN102762534A (zh) 2009-09-18 2012-10-31 扎里卡斯药品有限公司 作为钙通道阻断剂的芳基砜衍生物
WO2012068589A2 (en) 2010-11-19 2012-05-24 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US8466186B2 (en) * 2010-12-10 2013-06-18 Boehringer Ingelheim International Gmbh Compounds
EP2487159A1 (en) * 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
CN103781785A (zh) 2011-07-25 2014-05-07 阿勒根公司 作为α2肾上腺素能受体的调节剂的N-(咪唑烷-2-亚基)-杂环戊并[b]吡啶衍生物
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
UA111754C2 (uk) * 2011-10-06 2016-06-10 Байєр Фарма Акцієнгезелльшафт Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань
KR20140077963A (ko) 2011-10-20 2014-06-24 글락소스미스클라인 엘엘씨 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체
EP2647628A1 (en) 2012-04-02 2013-10-09 Almirall, S.A. Substituted tricyclic compounds with activity towards ep1 receptors
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
WO2014179564A1 (en) 2013-05-01 2014-11-06 Vitae Pharmaceuticals, Inc. Thiazalopyrrolidine inhibitors of ror-gamma
WO2015015378A2 (en) * 2013-08-02 2015-02-05 Pfizer Inc. Rorc2 inhibitors and methods of use thereof
HK1223933A1 (zh) * 2013-09-11 2017-08-11 F. Hoffmann-La Roche Ag 作为rorc调节剂的酮-咪唑并呲啶衍生物
RS59007B1 (sr) 2014-02-03 2019-08-30 Vitae Pharmaceuticals Llc Dihidropirolopiridinski inhibitori ror-gama
EA031967B1 (ru) 2014-10-14 2019-03-29 Вайтаи Фармасьютиклз, Инк. ДИГИДРОПИРРОЛОПИРИДИНОВЫЕ ИНГИБИТОРЫ ROR-γ
US10106501B2 (en) * 2015-06-09 2018-10-23 Abbvie Inc. Nuclear receptor modulators

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021191774A (ja) * 2015-06-09 2021-12-16 アッヴィ・インコーポレイテッド 核内受容体調節剤
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