JP2013537210A - １７α−ヒドロキシラーゼ／Ｃ１７，２０−リアーゼ阻害剤 - Google Patents

１７α−ヒドロキシラーゼ／Ｃ１７，２０−リアーゼ阻害剤 Download PDF

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JP2013537210A
JP2013537210A JP2013528663A JP2013528663A JP2013537210A JP 2013537210 A JP2013537210 A JP 2013537210A JP 2013528663 A JP2013528663 A JP 2013528663A JP 2013528663 A JP2013528663 A JP 2013528663A JP 2013537210 A JP2013537210 A JP 2013537210A
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mmol
alkyl
pyridin
methyl
dihydro
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JP2013537210A5 (OSRAM
Inventor
マーク・ジー・ボック
クリストフ・ガウル
ベンカテシュワル・ラオ・グンマディ
ヘンリク・メビッツ
サウミトラ・セングプタ
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ノバルティス アーゲー
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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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2013528663A 2010-09-16 2011-09-14 １７α−ヒドロキシラーゼ／Ｃ１７，２０−リアーゼ阻害剤 Pending JP2013537210A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN2719/CHE/2010 2010-09-16
IN2719CH2010 2010-09-16
PCT/EP2011/065965 WO2012035078A1 (en) 2010-09-16 2011-09-14 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS

Publications (2)

Publication Number Publication Date
JP2013537210A true JP2013537210A (ja) 2013-09-30
JP2013537210A5 JP2013537210A5 (OSRAM) 2014-11-06

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JP2013528663A Pending JP2013537210A (ja) 2010-09-16 2011-09-14 １７α−ヒドロキシラーゼ／Ｃ１７，２０−リアーゼ阻害剤

Country Status (5)

Country Link
US (1) US8946260B2 (OSRAM)
EP (1) EP2627648A1 (OSRAM)
JP (1) JP2013537210A (OSRAM)
CN (1) CN103108871B (OSRAM)
WO (1) WO2012035078A1 (OSRAM)

Cited By (2)

* Cited by examiner, † Cited by third party
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JP2014533736A (ja) * 2011-11-30 2014-12-15 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規二環式ジヒドロイソキノリン−１−オン誘導体
JP2020505458A (ja) * 2017-01-22 2020-02-20 福建広生堂薬業股▲ふん▼有限公司 Ａｓｋ１阻害剤、その調製方法および使用

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EA023064B1 (ru) 2011-04-28 2016-04-29 Новартис Аг ИНГИБИТОРЫ 17α-ГИДРОКСИЛАЗЫ/C-ЛИАЗЫ
CN103958478B (zh) * 2011-11-30 2017-08-01 霍夫曼-拉罗奇有限公司 双环二氢异喹啉‑1‑酮衍生物
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
CN104370938A (zh) * 2013-01-24 2015-02-25 韩冰 一类降低眼压的化合物及其制备方法和用途
CN103086945A (zh) * 2013-01-24 2013-05-08 张家港威胜生物医药有限公司 一种重要医药化工中间体色胺合成工艺
CN104370926A (zh) * 2013-01-24 2015-02-25 韩冰 一类具有神经保护作用的化合物及其制备方法和用途
CN104370925A (zh) * 2013-01-24 2015-02-25 韩冰 一类蛋白酶抑制剂及其制备方法和用途
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CN105308045B (zh) * 2013-05-27 2017-05-17 豪夫迈·罗氏有限公司 新的3,4‑二氢‑2h‑异喹啉‑1‑酮和2,3‑二氢‑异吲哚‑1‑酮化合物
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AU2015357167B2 (en) 2014-12-03 2020-06-25 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo(1,5-alpha)pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors
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US11045562B2 (en) 2015-12-18 2021-06-29 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
CN105541712B (zh) * 2016-01-08 2018-10-09 山东金城医药集团股份有限公司 索利那新中间体的制备方法
CN108264509B (zh) * 2016-12-30 2021-05-04 复旦大学 取代的苯并噻吩并[2，3-c]四氢吡啶衍生物及其制备方法和用途
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CN108929228A (zh) * 2018-07-09 2018-12-04 上海华堇生物技术有限责任公司 一种3-甲氧基-β-硝基苯乙烯的新制备方法
CN108929229A (zh) * 2018-07-10 2018-12-04 上海华堇生物技术有限责任公司 一种4-氯-β-硝基苯乙烯的新制备方法
CN114410727B (zh) * 2022-01-25 2023-09-19 山东诺明康药物研究院有限公司 一种克拉考特酮的制备方法
KR20240165402A (ko) 2022-03-23 2024-11-22 아이디어야 바이오사이언시스 인코포레이티드 Parg의 억제제로서의 피페라진 치환된 인다졸 화합물
CN117229284B (zh) * 2023-11-10 2024-02-06 上海泽德曼医药科技有限公司 三环稠杂环类化合物、其制备方法及其在医药上的应用
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