TWI407957B - Ｃｃｒ２拮抗劑之四級鹽 - Google Patents

Ｃｃｒ２拮抗劑之四級鹽 Download PDF

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TWI407957B
TWI407957B TW094121070A TW94121070A TWI407957B TW I407957 B TWI407957 B TW I407957B TW 094121070 A TW094121070 A TW 094121070A TW 94121070 A TW94121070 A TW 94121070A TW I407957 B TWI407957 B TW I407957B
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Taiwan
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compound
group
mmol
substituted
phenyl
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TW094121070A
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Chinese (zh)
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TW200612934A (en
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Bharat Lagu
Michael Wachter
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Janssen Pharmaceutica Nv
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    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ552173A (en) 2004-06-25 2010-07-30 Janssen Pharmaceutica Nv Quaternary salt CCR2 antagonists
EP2097452A1 (en) * 2006-12-14 2009-09-09 Actogenix N.V. Delivery of binding molecules to induce immunomodulation
WO2008131481A1 (en) * 2007-04-26 2008-11-06 Fibrotech Therapeutics Pty Ltd Treatment of mesangioproliferative diseases
CA2687931C (en) 2007-05-31 2016-05-24 Boehringer Ingelheim International Gmbh Ccr2 receptor antagonists and uses thereof
US8016912B2 (en) 2007-09-14 2011-09-13 Barrick Gold Corporation Process for recovering platinum group metals using reductants
US8093428B2 (en) * 2007-10-26 2012-01-10 Janssen Pharmaceutica N.V. Synthesis of quaternary salt compounds
US8168829B2 (en) * 2007-10-26 2012-05-01 Janssen Pharmaceutica N.V. Synthesis of quaternary salt compounds
TW200927740A (en) * 2007-11-13 2009-07-01 Bial Portela & Ca Sa Process
KR100954138B1 (ko) * 2007-12-31 2010-04-20 부산대학교 산학협력단 지방조직 유래 줄기세포를 함유하는 알레르기 비염 또는천식 예방 및 치료제
CN101481323B (zh) * 2008-01-11 2013-11-20 中国人民解放军军事医学科学院毒物药物研究所 苯并环庚烯类衍生物、其制备方法及医药用途
CN103724328B (zh) 2008-12-19 2015-10-14 贝林格尔.英格海姆国际有限公司 作为ccr2受体拮抗剂用于治疗炎症、哮喘和copd的环状嘧啶-4-甲酰胺
CN105153188B (zh) 2009-10-22 2018-06-01 法博太科制药有限公司 抗纤维化剂的稠环类似物
PL2513093T3 (pl) 2009-12-17 2015-03-31 Centrexion Therapeutics Corp Nowi antagoniści receptora CCR2 i ich zastosowanie
EP2569295B1 (en) 2010-05-12 2014-11-19 Boehringer Ingelheim International GmbH New ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments
JP2013526507A (ja) 2010-05-12 2013-06-24 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 新規ｃｃｒ２受容体アンタゴニスト、その製造方法及び薬物としてのその使用
US8841313B2 (en) 2010-05-17 2014-09-23 Boehringer Ingelheim International Gmbh CCR2 antagonists and uses thereof
JP5636094B2 (ja) 2010-05-25 2014-12-03 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 Ｃｃｒ２受容体アンタゴニスト
EP2576538B1 (en) 2010-06-01 2015-10-28 Boehringer Ingelheim International GmbH New CCR2 antagonists
MX367469B (es) 2010-06-07 2019-08-23 Novomedix Llc Compuestos furanilo y su uso.
WO2012012184A2 (en) * 2010-06-30 2012-01-26 Johnson & Johnson Vision Care, Inc. Ophthalmic devices containing chemokine antagonists
EP2583965B1 (en) * 2010-07-15 2017-01-25 Takeda Pharmaceutical Company Limited Heterocyclic ring compound
US10451897B2 (en) 2011-03-18 2019-10-22 Johnson & Johnson Vision Care, Inc. Components with multiple energization elements for biomedical devices
WO2013009582A1 (en) 2011-07-12 2013-01-17 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2013010839A1 (en) 2011-07-15 2013-01-24 Boehringer Ingelheim International Gmbh Novel and selective ccr2 antagonists
US9812730B2 (en) 2011-08-02 2017-11-07 Johnson & Johnson Vision Care, Inc. Biocompatible wire battery
US20140329809A1 (en) 2011-10-28 2014-11-06 Galderma Research & Development New leukocyte infiltrate markers for rosacea and uses thereof
US8857983B2 (en) 2012-01-26 2014-10-14 Johnson & Johnson Vision Care, Inc. Ophthalmic lens assembly having an integrated antenna structure
EP3338776A1 (en) 2012-05-01 2018-06-27 Translatum Medicus Inc. Methods for treating and diagnosing blinding eye diseases
US9715130B2 (en) 2014-08-21 2017-07-25 Johnson & Johnson Vision Care, Inc. Methods and apparatus to form separators for biocompatible energization elements for biomedical devices
US9599842B2 (en) 2014-08-21 2017-03-21 Johnson & Johnson Vision Care, Inc. Device and methods for sealing and encapsulation for biocompatible energization elements
US9941547B2 (en) 2014-08-21 2018-04-10 Johnson & Johnson Vision Care, Inc. Biomedical energization elements with polymer electrolytes and cavity structures
US10361404B2 (en) 2014-08-21 2019-07-23 Johnson & Johnson Vision Care, Inc. Anodes for use in biocompatible energization elements
US10627651B2 (en) 2014-08-21 2020-04-21 Johnson & Johnson Vision Care, Inc. Methods and apparatus to form biocompatible energization primary elements for biomedical devices with electroless sealing layers
US9383593B2 (en) 2014-08-21 2016-07-05 Johnson & Johnson Vision Care, Inc. Methods to form biocompatible energization elements for biomedical devices comprising laminates and placed separators
US10381687B2 (en) 2014-08-21 2019-08-13 Johnson & Johnson Vision Care, Inc. Methods of forming biocompatible rechargable energization elements for biomedical devices
US10361405B2 (en) 2014-08-21 2019-07-23 Johnson & Johnson Vision Care, Inc. Biomedical energization elements with polymer electrolytes
US9793536B2 (en) 2014-08-21 2017-10-17 Johnson & Johnson Vision Care, Inc. Pellet form cathode for use in a biocompatible battery
AU2016287584B2 (en) 2015-07-02 2020-03-26 Centrexion Therapeutics Corporation (4-((3R,4R)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4yl)methanone citrate
PT3416962T (pt) * 2016-02-15 2021-07-23 Sanofi Sa Derivados de 6,7-di-hidro-5h-benzo[7]anuleno como moduladores do recetor de estrogénio
US10345620B2 (en) 2016-02-18 2019-07-09 Johnson & Johnson Vision Care, Inc. Methods and apparatus to form biocompatible energization elements incorporating fuel cells for biomedical devices
CN109963848B (zh) 2016-11-17 2022-07-05 赛诺菲 取代的n-(3-氟丙基)-吡咯烷化合物、其制备方法以及其治疗用途
US11014873B2 (en) 2017-02-03 2021-05-25 Certa Therapeutics Pty Ltd. Anti-fibrotic compounds
EP3434272A1 (en) 2017-07-25 2019-01-30 Sanofi Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid
AU2019252676A1 (en) 2018-04-11 2020-11-26 Ohio State Innovation Foundation Methods and compositions for sustained release microparticles for ocular drug delivery
JP2021534101A (ja) 2018-08-09 2021-12-09 ヴェルソー セラピューティクス， インコーポレイテッド Ｃｃｒ２及びｃｓｆ１ｒを標的とするためのオリゴヌクレオチド組成物ならびにその使用
KR20210057032A (ko) 2018-09-07 2021-05-20 사노피 메틸 6-(2,4-디클로로페닐)-5-[4-[(3s)-1-(3-플루오로프로필)피롤리딘-3-일]옥시페닐]-8,9-디히드로-7h-벤조[7]아눌렌-2-카르복실레이트의 염 및 이의 제조 방법
TW202146007A (zh) 2020-02-27 2021-12-16 法商賽諾菲公司 包含阿培利司（ａｌｐｅｌｉｓｉｂ）與６－（２，４－二氯苯基）－５－［４－［（３ｓ）－１－（３－氟丙基）吡咯啶－３－基］氧苯基］－８，９－二氫－７ｈ－苯并［７］輪烯－２－羧酸之組合
CN111808062B (zh) * 2020-07-28 2022-09-13 遵义医科大学 一种蛇床子素磺酸酯类化合物及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999032100A2 (en) * 1997-12-19 1999-07-01 Takeda Chemical Industries, Ltd. Pharmaceutical composition for antagonizing ccr5 comprising anilide derivative
WO2000068203A1 (en) * 1999-05-07 2000-11-16 Takeda Chemical Industries, Ltd. Cyclic compounds and uses thereof
US6166006A (en) * 1997-12-19 2000-12-26 Takeda Chemical Industries, Ltd. Anilide derivative, production and use thereof

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0873476A (ja) * 1994-07-04 1996-03-19 Takeda Chem Ind Ltd ホスホン酸誘導体およびそれを含んでなる医薬
JP4416198B2 (ja) * 1997-12-19 2010-02-17 武田薬品工業株式会社 アニリド誘導体、その製造法および用途
AU5301599A (en) 1998-08-20 2000-03-14 Takeda Chemical Industries Ltd. Quaternary ammonium salts and their use
CA2353635A1 (en) 1998-12-21 2000-06-29 Takeda Chemical Industries, Ltd. Anilide derivative, production and use thereof
JP2001058988A (ja) * 1998-12-21 2001-03-06 Takeda Chem Ind Ltd アニリド誘導体、その製造法および用途
JP2001026586A (ja) * 1999-05-07 2001-01-30 Takeda Chem Ind Ltd 環状化合物およびその用途
WO2001042224A1 (en) * 1999-12-09 2001-06-14 Mitsubishi Pharma Corporation Carboxyamido derivatives
JP2004043432A (ja) * 2002-04-19 2004-02-12 Takeda Chem Ind Ltd Ｈｉｖ感染予防剤
AU2003235205A1 (en) * 2002-04-19 2003-11-03 Takeda Pharmaceutical Company Limited Preventives for hiv infection
JP4145230B2 (ja) * 2002-11-01 2008-09-03 武田薬品工業株式会社 神経障害の予防・治療剤
AU2005256507A1 (en) * 2004-06-25 2006-01-05 Basf Aktiengesellschaft Triazolopyrimidine compounds and their use for controlling pathogenic fungi
NZ552173A (en) 2004-06-25 2010-07-30 Janssen Pharmaceutica Nv Quaternary salt CCR2 antagonists

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999032100A2 (en) * 1997-12-19 1999-07-01 Takeda Chemical Industries, Ltd. Pharmaceutical composition for antagonizing ccr5 comprising anilide derivative
US6166006A (en) * 1997-12-19 2000-12-26 Takeda Chemical Industries, Ltd. Anilide derivative, production and use thereof
WO2000068203A1 (en) * 1999-05-07 2000-11-16 Takeda Chemical Industries, Ltd. Cyclic compounds and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Shiraishi M, Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety, Journal of Medicinal Chemistry, 43, 2049-2063, 2000 *

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