JP2019522673A - Ｈｔｒａ１阻害剤としての新規なジフルオロケトアミド誘導体 - Google Patents

Ｈｔｒａ１阻害剤としての新規なジフルオロケトアミド誘導体 Download PDF

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Publication number
JP2019522673A
JP2019522673A JP2019502161A JP2019502161A JP2019522673A JP 2019522673 A JP2019522673 A JP 2019522673A JP 2019502161 A JP2019502161 A JP 2019502161A JP 2019502161 A JP2019502161 A JP 2019502161A JP 2019522673 A JP2019522673 A JP 2019522673A
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Prior art keywords
substituted
alkyl
methyl
halo
compound according
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JP2019502161A
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Japanese (ja)
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JP2019522673A5 (enExample
Inventor
メルキ，ハンス・ペー
ホルンスペルガー，ブノワ
モール，ペーター
レアットリンガー，ミヒャエル
ルドルフ，マルクス
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2019522673A publication Critical patent/JP2019522673A/ja
Publication of JP2019522673A5 publication Critical patent/JP2019522673A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
JP2019502161A 2016-07-18 2017-07-12 Ｈｔｒａ１阻害剤としての新規なジフルオロケトアミド誘導体 Pending JP2019522673A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16180013.1 2016-07-18
EP16180013 2016-07-18
PCT/EP2017/067519 WO2018015240A1 (en) 2016-07-18 2017-07-12 New difluoroketamide derivatives as htra1 inhibitors

Publications (2)

Publication Number Publication Date
JP2019522673A true JP2019522673A (ja) 2019-08-15
JP2019522673A5 JP2019522673A5 (enExample) 2020-08-20

Family

ID=56418466

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019502161A Pending JP2019522673A (ja) 2016-07-18 2017-07-12 Ｈｔｒａ１阻害剤としての新規なジフルオロケトアミド誘導体

Country Status (5)

Country Link
US (1) US10865182B2 (enExample)
EP (1) EP3484859B1 (enExample)
JP (1) JP2019522673A (enExample)
CN (1) CN109415330A (enExample)
WO (1) WO2018015240A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7179721B2 (ja) 2016-06-21 2022-11-29 オリオン・オフサルモロジー・エルエルシー 複素環式プロリンアミド誘導体
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
EP4735466A1 (en) * 2023-06-28 2026-05-06 The Board of Trustees of the Leland Stanford Junior University Htra1 inhibitors and uses thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10505582A (ja) * 1994-07-15 1998-06-02 メリル・フアーマシユウテイカルズ・インコーポレイテツド ジフルオロスタトン抗ウイルス剤
JP2002541237A (ja) * 1999-04-09 2002-12-03 サイトビア インコーポレイテッド カスパーゼインヒビターおよびその使用
US20060121039A1 (en) * 2004-12-07 2006-06-08 Alcon, Inc. Use of agents that prevent the generation of amyloid-like proteins and/or drusen, and/or use of agents that promote sequestration and/or degradation of, and/or prevent the neurotoxic effects of such proteins in the treatment of macular degeneration
JP6757336B2 (ja) * 2015-05-11 2020-09-16 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規なジフルオロケトアミド誘導体

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1986006379A1 (en) * 1985-04-19 1986-11-06 The Upjohn Company Dihalo-statine substituted renin inhibitors
PT1012180E (pt) 1997-08-11 2005-04-29 Boehringer Ingelheim Ca Ltd Analogos de peptidos inibidores da hepatite c
US7244815B2 (en) 2001-05-23 2007-07-17 The Curators Of The University Of Missouri Attachment and elaboration strategies for inverse peptide synthesis
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
CN101248046A (zh) * 2005-07-11 2008-08-20 德福根有限公司 作为激酶抑制剂的酰胺衍生物
EP2111413A2 (en) 2007-02-16 2009-10-28 Genetech, Inc. Htra1-pdz and htra3-pdz modulators
CN103402996B (zh) 2011-01-04 2015-02-11 诺瓦提斯公司 可用于治疗年龄相关性黄斑变性(amd)的吲哚化合物或其类似物
US8592426B2 (en) * 2011-01-24 2013-11-26 Hoffmann—La Roche Inc. Aryl-benzocycloalkyl amide derivatives
JP6209605B2 (ja) 2012-06-28 2017-10-04 ノバルティス アーゲー ピロリジン誘導体、および補体経路調節因子としてのその使用
AR103742A1 (es) 2015-02-25 2017-05-31 Hoffmann La Roche Derivados de trifluorometilpropanamida

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10505582A (ja) * 1994-07-15 1998-06-02 メリル・フアーマシユウテイカルズ・インコーポレイテツド ジフルオロスタトン抗ウイルス剤
JP2002541237A (ja) * 1999-04-09 2002-12-03 サイトビア インコーポレイテッド カスパーゼインヒビターおよびその使用
US20060121039A1 (en) * 2004-12-07 2006-06-08 Alcon, Inc. Use of agents that prevent the generation of amyloid-like proteins and/or drusen, and/or use of agents that promote sequestration and/or degradation of, and/or prevent the neurotoxic effects of such proteins in the treatment of macular degeneration
JP6757336B2 (ja) * 2015-05-11 2020-09-16 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新規なジフルオロケトアミド誘導体

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
NATURE STRUCTURAL & MOLECULAR BIOLOGY, vol. 18(3), JPN6021019884, 2011, pages 386 - 388, ISSN: 0004513078 *

Also Published As

Publication number Publication date
EP3484859A1 (en) 2019-05-22
US20190152895A1 (en) 2019-05-23
US10865182B2 (en) 2020-12-15
EP3484859B1 (en) 2021-09-15
CN109415330A (zh) 2019-03-01
WO2018015240A1 (en) 2018-01-25

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