CN1237961A - 用作蛋白酶抑制剂的氨基胍和烷氧基胍类化合物 - Google Patents

用作蛋白酶抑制剂的氨基胍和烷氧基胍类化合物 Download PDF

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CN1237961A
CN1237961A CN97199940A CN97199940A CN1237961A CN 1237961 A CN1237961 A CN 1237961A CN 97199940 A CN97199940 A CN 97199940A CN 97199940 A CN97199940 A CN 97199940A CN 1237961 A CN1237961 A CN 1237961A
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alkyl
group
hydrogen
methyl
aryl
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B·E·汤姆苏克
R·M·索尔
鲁天保
C·L·菲德
C·R·伊里格
T·P·马科坦
T·P·斯塔格纳罗
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3 Dimensional Pharmaceuticals Inc
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3 Dimensional Pharmaceuticals Inc
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    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
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    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/17—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
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    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
    • C07C323/66—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton
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    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
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  • Chemical & Material Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Materials For Medical Uses (AREA)
CN97199940A 1996-11-26 1997-11-26 用作蛋白酶抑制剂的氨基胍和烷氧基胍类化合物 Pending CN1237961A (zh)

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US3182296P 1996-11-26 1996-11-26
US60/031,822 1996-11-26

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102353569A (zh) * 2002-05-13 2012-02-15 贝克顿·迪金森公司 蛋白酶抑制剂样品采集系统
CN102850451A (zh) * 2011-06-29 2013-01-02 辽宁诺康生物制药有限责任公司 具有抑制纤溶酶活性的重组textilinin-1及其制备方法和应用
CN107382869A (zh) * 2017-08-01 2017-11-24 李凯 一种治疗中风后遗症的化合物及制备方法和应用
CN111655737A (zh) * 2017-11-21 2020-09-11 开普敦大学 合成含6-脱氧-6-氨基-β-D-吡喃葡萄糖苷的聚合物及其前体的方法
CN116234799A (zh) * 2020-07-20 2023-06-06 深圳迈瑞生物医疗电子股份有限公司 一种组合物的血小板解聚用途、解聚试剂及解聚方法

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1036063B1 (en) 1997-11-26 2006-11-02 Ortho-McNeil Pharmaceuticals, Inc. Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
US6344486B1 (en) 1998-04-03 2002-02-05 3-Dimensional Pharmaceuticals, Inc. Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors
WO1999055355A1 (en) 1998-04-24 1999-11-04 3-Dimensional Pharmaceuticals, Inc. Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors
ATE461210T1 (de) 1998-06-11 2010-04-15 Ortho Mcneil Pharm Inc Pyrazine protease inhibitore
AU3731400A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Methods and compositions useful in inhibiting apoptosis
US6544541B1 (en) * 1999-06-02 2003-04-08 Cardiovascular Solutions, Inc. Devices and compounds for treating arterial restenosis
MXPA03000512A (es) 2000-07-17 2003-10-06 Dimensional Pharm Inc Oxiguanidina-pirazinonas ciclicas como inhibidores de proteasas.
KR20030022353A (ko) 2000-08-04 2003-03-15 3-디멘져널 파마슈티칼즈 인코오포레이티드 사이클릭 옥시구아니딘 프로테아제 저해제
KR100371008B1 (ko) * 2000-08-05 2003-02-06 조동련 혈소판 응집 억제제 부착 스텐트의 그 제조 방법
UA75093C2 (en) 2000-10-06 2006-03-15 Dimensional Pharm Inc Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors
EP1419172A4 (en) * 2001-08-03 2007-10-03 Univ Leland Stanford Junior BIDIRECTIONAL SYNTHESIS OF OLIGOGUANIDINTRANSPORTING MEANS
US20060264608A1 (en) * 2001-08-03 2006-11-23 Wender Paul A Bi-directional synthesis of oligoguanidine transport agents
CA2536918A1 (en) 2003-08-26 2005-03-03 Leland Shapiro Compositions of, and methods for, alpha-1 antitrypsin fc fusion molecules
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
WO2007005454A2 (en) * 2005-06-30 2007-01-11 Bayer Cropscience Ag Improved process for preparing insecticidal (disubstitutedpropenyl) phenylalkyl substituted heterocycles
JP2009521472A (ja) * 2005-12-22 2009-06-04 シェーリング コーポレイション 心肺手術の合併症の予防としてのトロンビンレセプターアンタゴニスト
US8491868B2 (en) 2006-12-26 2013-07-23 Lantheus Medical Imaging, Inc. Ligands for imaging cardiac innervation
EP3018481B1 (en) * 2009-05-20 2018-02-21 Sekisui Medical Co., Ltd. Blood coagulation time prolonging agent
KR102136503B1 (ko) 2010-05-11 2020-07-21 랜티우스 메디컬 이메징, 인크. 영상화제의 합성 및 사용을 위한 조성물, 방법 및 시스템
JP2014506253A (ja) 2010-12-31 2014-03-13 コリドー ファーマシューティカルズ インコーポレイテッド アルギナーゼ阻害剤およびその使用法
US9788539B2 (en) 2011-05-17 2017-10-17 Velico Medical, Inc. Platelet protection solution having beta-galactosidase and sialidase inhibitors
CN103702556A (zh) 2011-05-17 2014-04-02 维利科医疗公司 使用唾液酸酶抑制剂改进的血小板保存
AU2013245729B2 (en) 2012-04-12 2016-09-29 The Trustees Of The University Of Pennsylvania Filovirus consensus antigens, nucleic acid constructs and vaccines made therefrom, and methods of using same
CA2887083A1 (en) 2012-10-05 2014-04-10 Velico Medical, Inc. Platelet additive solution having a beta-galactosidase inhibitor
WO2014120886A1 (en) 2013-01-30 2014-08-07 Velico Medical, Inc. Platelet additive solution having a self-assembling hydrogel-forming peptide
US9555016B2 (en) 2013-06-10 2017-01-31 Covidien Lp Lytic agents for use in treating intravascular clots
GB202108544D0 (en) * 2021-06-15 2021-07-28 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3131218A (en) * 1961-02-15 1964-04-28 Smith Kline French Lab N-amino guanidine derivatives
US3271448A (en) 1961-11-21 1966-09-06 Pfizer & Co C Phenoxyalkyl aminoguanidines
BE663481A (cg-RX-API-DMAC10.html) * 1964-05-05
US3413303A (en) * 1965-09-27 1968-11-26 Ciba Geigy Corp Aralkenyloxyguanidines
JPS57178739A (en) 1981-04-27 1982-11-04 Mitsubishi Heavy Ind Ltd Bead supplying device for tire molding machine
US4429146A (en) * 1982-04-15 1984-01-31 Gaf Corporation Substituted diphenyl ether herbicides and process for use
JPS6229566A (ja) 1985-07-30 1987-02-07 Taiyo Yakuhin Kogyo Kk 新規グアニジノメチル安息香酸誘導体
DE3929582A1 (de) 1989-09-06 1991-03-07 Hoechst Ag Benzoylguanidine, verfahren zu ihrer herstellung, ihre verwendung als medikament sowie sie enthaltendes medikament
EP0604022A1 (en) 1992-12-22 1994-06-29 Advanced Cardiovascular Systems, Inc. Multilayered biodegradable stent and method for its manufacture
TW257757B (cg-RX-API-DMAC10.html) 1993-03-03 1995-09-21 Boehringer Mannheim Gmbh
GB9318637D0 (en) 1993-09-08 1993-10-27 Ferring Res Ltd Enzyme inhibitors
US6087479A (en) 1993-09-17 2000-07-11 Nitromed, Inc. Localized use of nitric oxide-adducts to prevent internal tissue damage
US5466811A (en) 1994-07-18 1995-11-14 Merck & Co., Inc. Dioxolenylmethyl carbamates pro moieties for amine drugs
US5643580A (en) 1994-10-17 1997-07-01 Surface Genesis, Inc. Biocompatible coating, medical device using the same and methods
AU699821B2 (en) 1994-10-17 1998-12-17 Kabushikikaisha Igaki Iryo Sekkei Stent for liberating drug
US5637113A (en) 1994-12-13 1997-06-10 Advanced Cardiovascular Systems, Inc. Polymer film for wrapping a stent structure
DE19514104C2 (de) 1995-04-13 1997-05-28 Behringwerke Ag Beschichtung für in den Blutstrom oder in das Gewebe des menschlichen Körpers einbringbares Biomaterial
HU211262A9 (hu) 1995-05-12 1995-11-28 Hoechst Ag Benzoil-guanidinek
US5792769A (en) 1995-09-29 1998-08-11 3-Dimensional Pharmaceuticals, Inc. Guanidino protease inhibitors
HUP9802764A3 (en) 1995-09-29 2000-03-28 Dimensional Pharm Inc Guanidino protease inhibitors
GB9525620D0 (en) 1995-12-15 1996-02-14 Glaxo Group Ltd Chemical compounds
DE69631692T2 (de) 1995-12-29 2004-12-02 3-Dimensional Pharmaceuticals, Inc. Amidino proteaseinhibitoren
WO1997036580A1 (en) 1996-03-29 1997-10-09 3-Dimensional Pharmaceuticals, Inc. Amidinohydrazones as protease inhibitors
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102353569A (zh) * 2002-05-13 2012-02-15 贝克顿·迪金森公司 蛋白酶抑制剂样品采集系统
CN102850451A (zh) * 2011-06-29 2013-01-02 辽宁诺康生物制药有限责任公司 具有抑制纤溶酶活性的重组textilinin-1及其制备方法和应用
CN102850451B (zh) * 2011-06-29 2014-05-07 辽宁诺康生物制药有限责任公司 具有抑制纤溶酶活性的重组textilinin-1及其制备方法和应用
CN107382869A (zh) * 2017-08-01 2017-11-24 李凯 一种治疗中风后遗症的化合物及制备方法和应用
CN111655737A (zh) * 2017-11-21 2020-09-11 开普敦大学 合成含6-脱氧-6-氨基-β-D-吡喃葡萄糖苷的聚合物及其前体的方法
CN111655737B (zh) * 2017-11-21 2022-03-25 开普敦大学 合成含6-脱氧-6-氨基-β-D-吡喃葡萄糖苷的聚合物及其前体的方法
CN116234799A (zh) * 2020-07-20 2023-06-06 深圳迈瑞生物医疗电子股份有限公司 一种组合物的血小板解聚用途、解聚试剂及解聚方法

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