CN1950362B - 类胰蛋白酶抑制剂的制备方法 - Google Patents

类胰蛋白酶抑制剂的制备方法 Download PDF

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Publication number
CN1950362B
CN1950362B CN2005800140491A CN200580014049A CN1950362B CN 1950362 B CN1950362 B CN 1950362B CN 2005800140491 A CN2005800140491 A CN 2005800140491A CN 200580014049 A CN200580014049 A CN 200580014049A CN 1950362 B CN1950362 B CN 1950362B
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China
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formula
amino
compound
salt
alkyl
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Expired - Fee Related
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CN2005800140491A
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English (en)
Chinese (zh)
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CN1950362A (zh
Inventor
C-D·格拉夫
C·塔佩尔佐芬
A·W·斯莱德斯基
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Aventis Pharmaceuticals Inc
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Aventis Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/52—Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • C07D213/24—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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • 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
    • C07D213/24—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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • C07D213/24—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
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/53—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/08—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN2005800140491A 2004-03-02 2005-02-18 类胰蛋白酶抑制剂的制备方法 Expired - Fee Related CN1950362B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP04004799.5 2004-03-02
EP04004799A EP1571150A1 (en) 2004-03-02 2004-03-02 Process for the preparation of tryptase inhibitors
US58574504P 2004-07-06 2004-07-06
US60/585,745 2004-07-06
PCT/EP2005/001676 WO2005095385A1 (en) 2004-03-02 2005-02-18 Process for the preparation of tryptase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2008101787837A Division CN101429194B (zh) 2004-03-02 2005-02-18 类胰蛋白酶抑制剂的制备方法

Publications (2)

Publication Number Publication Date
CN1950362A CN1950362A (zh) 2007-04-18
CN1950362B true CN1950362B (zh) 2010-08-04

Family

ID=34745976

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2005800140491A Expired - Fee Related CN1950362B (zh) 2004-03-02 2005-02-18 类胰蛋白酶抑制剂的制备方法
CN2008101787837A Expired - Fee Related CN101429194B (zh) 2004-03-02 2005-02-18 类胰蛋白酶抑制剂的制备方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2008101787837A Expired - Fee Related CN101429194B (zh) 2004-03-02 2005-02-18 类胰蛋白酶抑制剂的制备方法

Country Status (19)

Country Link
US (1) US20130225825A1 (enExample)
EP (2) EP1571150A1 (enExample)
JP (1) JP4851440B2 (enExample)
CN (2) CN1950362B (enExample)
AT (1) ATE447567T1 (enExample)
AU (1) AU2005229319B2 (enExample)
BR (1) BRPI0508430A (enExample)
CA (1) CA2557391C (enExample)
DK (1) DK1723140T3 (enExample)
ES (1) ES2334245T3 (enExample)
NZ (1) NZ549224A (enExample)
PL (1) PL1723140T3 (enExample)
PT (1) PT1723140E (enExample)
RS (1) RS51144B (enExample)
RU (1) RU2378271C2 (enExample)
SI (1) SI1723140T1 (enExample)
TN (1) TNSN06260A1 (enExample)
UA (1) UA85701C2 (enExample)
WO (1) WO2005095385A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200840566A (en) * 2006-12-22 2008-10-16 Esteve Labor Dr Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments
EP2224803B1 (en) * 2007-11-21 2014-04-02 Janssen Pharmaceutica N.V. Spiropiperidines for use as tryptase inhibitors
CN103508936A (zh) * 2008-08-22 2014-01-15 赛诺菲-安万特 用于制备吲哚苄胺化合物的中间体
WO2011037947A1 (en) * 2009-09-24 2011-03-31 Sanofi-Aventis U.S. Llc Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof
JP2013515723A (ja) * 2009-12-23 2013-05-09 サノフイ 炎症性腸疾患の処置
US20140113934A1 (en) 2011-06-20 2014-04-24 E I Du Pont De Nemours And Company Heterocyclic compounds for treating helminth infections
JP2015502936A (ja) 2011-11-28 2015-01-29 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニーＥ．Ｉ．Ｄｕ Ｐｏｎｔ Ｄｅ Ｎｅｍｏｕｒｓ Ａｎｄ Ｃｏｍｐａｎｙ スルホンアミド駆虫薬
WO2014099837A1 (en) 2012-12-18 2014-06-26 E. I. Du Pont De Nemours And Company Sulfonamide anthelmintics
CN111793101B (zh) 2020-07-17 2022-09-30 四川大学 C-核苷化合物的合成方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0401166B1 (de) * 1989-06-01 1995-02-22 Ciba-Geigy Ag Neue, stickstoffhaltige Titanocene und deren Verwendung
US5252753A (en) * 1991-11-01 1993-10-12 Ortho Pharmaceutical Corporation Process for the preparation of certain substituted biphenyl tetrazoles and compounds thereof
IL122072A (en) * 1996-11-14 2001-03-19 Akzo Nobel Nv Piperidine derivatives their preparation and pharmaceutical compositions containing them
WO1999018053A1 (en) * 1997-10-02 1999-04-15 The University Of Western Ontario Preparation of radiolabelled haloaromatics via polymer-bound intermediates
US20020045613A1 (en) * 2000-04-27 2002-04-18 Heinz Pauls 1-aroyl-piperidinyl benzamidines
DZ3347A1 (fr) * 2000-05-22 2001-11-29 Aventis Pharma Inc Dérivés d'arylméthylamine pour leur utilisation comme inhibiteurs de la tryptase
JP4846238B2 (ja) * 2002-10-18 2011-12-28 マクマスター ユニバーシティー 放射線標識した化合物の精製方法
GB0308613D0 (en) * 2002-12-26 2003-05-21 Aventis Pharma Inc 4-(3-Aminomethylphenyl) piperidin-1-yl- 5-(2-fluorophenylethynyl) furan-2-yl- methanone as an inhibitor of mast cell tryptase

Also Published As

Publication number Publication date
ATE447567T1 (de) 2009-11-15
RS51144B (sr) 2010-10-31
EP1723140A1 (en) 2006-11-22
CA2557391C (en) 2011-06-28
CN1950362A (zh) 2007-04-18
BRPI0508430A (pt) 2007-07-24
CN101429194B (zh) 2011-12-14
AU2005229319A1 (en) 2005-10-13
US20130225825A1 (en) 2013-08-29
PT1723140E (pt) 2010-01-13
JP4851440B2 (ja) 2012-01-11
NZ549224A (en) 2010-10-29
RU2378271C2 (ru) 2010-01-10
CN101429194A (zh) 2009-05-13
EP1571150A1 (en) 2005-09-07
RU2006134623A (ru) 2008-04-10
EP1723140B1 (en) 2009-11-04
ES2334245T3 (es) 2010-03-08
SI1723140T1 (sl) 2010-02-26
UA85701C2 (ru) 2009-02-25
AU2005229319B2 (en) 2011-10-20
WO2005095385A1 (en) 2005-10-13
DK1723140T3 (da) 2010-03-22
PL1723140T3 (pl) 2010-02-26
CA2557391A1 (en) 2005-10-13
JP2007526264A (ja) 2007-09-13
TNSN06260A1 (en) 2007-12-03

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