CN109415330A - 作为htra1抑制剂的新型二氟酮酰胺衍生物 - Google Patents

作为htra1抑制剂的新型二氟酮酰胺衍生物 Download PDF

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Publication number
CN109415330A
CN109415330A CN201780039927.8A CN201780039927A CN109415330A CN 109415330 A CN109415330 A CN 109415330A CN 201780039927 A CN201780039927 A CN 201780039927A CN 109415330 A CN109415330 A CN 109415330A
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CN
China
Prior art keywords
alkyl
substituted
alkoxy
carbonyl
methyl
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.)
Pending
Application number
CN201780039927.8A
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English (en)
Chinese (zh)
Inventor
汉斯·P·梅尔基
佰努瓦·霍恩斯普格
彼得·莫尔
米夏埃尔·罗伊特林格
马库斯·鲁道夫
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CN109415330A publication Critical patent/CN109415330A/zh
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)
CN201780039927.8A 2016-07-18 2017-07-12 作为htra1抑制剂的新型二氟酮酰胺衍生物 Pending CN109415330A (zh)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
CN109415330A true CN109415330A (zh) 2019-03-01

Family

ID=56418466

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780039927.8A Pending CN109415330A (zh) 2016-07-18 2017-07-12 作为htra1抑制剂的新型二氟酮酰胺衍生物

Country Status (5)

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

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE064412T2 (hu) 2016-06-21 2024-03-28 Orion Ophthalmology LLC Heterociklusos prolinamid-származékok
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
WO2025006856A1 (en) * 2023-06-28 2025-01-02 The Board Of Trustees Of The Leland Stanford Junior University Htra1 inhibitors and uses thereof

Citations (5)

* 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
WO1996002499A1 (en) * 1994-07-15 1996-02-01 Merrell Pharmaceuticals Inc. Difluorostatone antiviral agents
WO2000061542A1 (en) * 1999-04-09 2000-10-19 Cytovia, Inc. Caspase inhibitors and the use thereof
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
CN103328436A (zh) * 2011-01-24 2013-09-25 霍夫曼-拉罗奇有限公司 新芳基-苯并环烷基酰胺衍生物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1012180B1 (en) 1997-08-11 2004-12-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor peptide analogues
US7244815B2 (en) 2001-05-23 2007-07-17 The Curators Of The University Of Missouri Attachment and elaboration strategies for inverse peptide synthesis
UY28500A1 (es) 2003-09-05 2005-04-29 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc.
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
PE20081795A1 (es) 2007-02-16 2009-01-08 Genentech Inc Moduladores de htra1-pdz y htra3-pdz
EP2661433B1 (en) 2011-01-04 2017-08-16 Novartis AG Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
ES2644700T3 (es) 2012-06-28 2017-11-30 Novartis Ag Derivados de pirrolidina y su uso como moduladores de la ruta del complemento
EP3262026B1 (en) 2015-02-25 2020-03-18 H. Hoffnabb-La Roche Ag New trifluoromethylpropanamide derivatives
TW201713613A (zh) 2015-05-11 2017-04-16 赫孚孟拉羅股份公司 新二氟酮醯胺衍生物

Patent Citations (5)

* 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
WO1996002499A1 (en) * 1994-07-15 1996-02-01 Merrell Pharmaceuticals Inc. Difluorostatone antiviral agents
WO2000061542A1 (en) * 1999-04-09 2000-10-19 Cytovia, Inc. Caspase inhibitors and the use thereof
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
CN103328436A (zh) * 2011-01-24 2013-09-25 霍夫曼-拉罗奇有限公司 新芳基-苯并环烷基酰胺衍生物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
LINDA TRUEBESTEIN等: "Substrate-induced remodeling of the active site regulates human HTRA1 activity", 《NATURE STRUCTURAL & MOLECULAR BIOLOGY》 *
刘绚丽等: "年龄相关黄斑变性亚临床炎症机制的研究现状", 《国际眼科杂志》 *
李娟等: "年龄相关性黄斑变性的病因研究", 《国际眼科杂志》 *

Also Published As

Publication number Publication date
JP2019522673A (ja) 2019-08-15
US20190152895A1 (en) 2019-05-23
EP3484859A1 (en) 2019-05-22
WO2018015240A1 (en) 2018-01-25
EP3484859B1 (en) 2021-09-15
US10865182B2 (en) 2020-12-15

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