CN101068783A - 用于制备半胱氨酸蛋白酶抑制剂的方法和中间体 - Google Patents

用于制备半胱氨酸蛋白酶抑制剂的方法和中间体 Download PDF

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Publication number
CN101068783A
CN101068783A CNA2005800389964A CN200580038996A CN101068783A CN 101068783 A CN101068783 A CN 101068783A CN A2005800389964 A CNA2005800389964 A CN A2005800389964A CN 200580038996 A CN200580038996 A CN 200580038996A CN 101068783 A CN101068783 A CN 101068783A
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chemical formula
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alkyl
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Chinese (zh)
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李家瑶
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Bayer Pharma AG
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Bayer Schering Pharma AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—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 nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/24—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 nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/25—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 nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/64—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00—Preparation of sulfones; Preparation of sulfoxides
    • C07C315/02—Preparation of sulfones; Preparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C315/00—Preparation of sulfones; Preparation of sulfoxides
    • C07C315/04—Preparation of sulfones; Preparation of sulfoxides by reactions not involving the formation of sulfone or sulfoxide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/28—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C321/00—Thiols, sulfides, hydropolysulfides or polysulfides
    • C07C321/12—Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms
    • C07C321/16—Sulfides, hydropolysulfides, or polysulfides having thio groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—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 carboxyl groups bound to the same carbon skeleton
    • C07C323/51—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—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 carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen 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
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/32—Sulfur 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
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/32—Sulfur atoms
    • C07D213/34—Sulfur atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Pyridine Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNA2005800389964A 2004-09-17 2005-09-16 用于制备半胱氨酸蛋白酶抑制剂的方法和中间体 Pending CN101068783A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US61080604P 2004-09-17 2004-09-17
US60/610,806 2004-09-17

Publications (1)

Publication Number Publication Date
CN101068783A true CN101068783A (zh) 2007-11-07

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ID=35899659

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CNA2005800389964A Pending CN101068783A (zh) 2004-09-17 2005-09-16 用于制备半胱氨酸蛋白酶抑制剂的方法和中间体

Country Status (15)

Country Link
US (1) US7737300B2 (https=)
EP (1) EP1799645A2 (https=)
JP (1) JP2008513472A (https=)
KR (1) KR20070061877A (https=)
CN (1) CN101068783A (https=)
AU (1) AU2005287046A1 (https=)
BR (1) BRPI0515470A (https=)
CA (1) CA2580065A1 (https=)
CR (1) CR8993A (https=)
EC (1) ECSP077321A (https=)
IL (1) IL181792A0 (https=)
MX (1) MX2007003118A (https=)
NO (1) NO20071937L (https=)
WO (1) WO2006034004A2 (https=)
ZA (1) ZA200703102B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106478564A (zh) * 2015-08-29 2017-03-08 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
WO2017036357A1 (zh) * 2015-08-29 2017-03-09 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途

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DK1663958T3 (da) 2003-09-18 2015-04-07 Virobay Inc Haloalkylholdige forbindelser som cysteinproteasehæmmere
WO2006060810A1 (en) 2004-12-02 2006-06-08 Schering Aktiengesellschaft Sulfonamide compounds as cysteine protease inhibitors
US7488848B2 (en) 2005-03-21 2009-02-10 Virobay, Inc. Alpha ketoamide compounds as cysteine protease inhibitors
JP5215167B2 (ja) * 2005-03-22 2013-06-19 ビロベイ，インコーポレイティド システインプロテアーゼ阻害剤としてのスルホニル基含有化合物
EP2064178A4 (en) * 2006-09-08 2011-10-05 Merck Canada Inc PRODRUGS OF INHIBITORS OF CATHEPSIN S
WO2008037072A1 (en) 2006-09-25 2008-04-03 Merck Frosst Canada Ltd. Cathepsin b inhibitors
EP2079683B1 (en) 2006-10-04 2015-01-21 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
CA2672494A1 (en) 2006-12-14 2008-06-19 Nps Pharmaceuticals, Inc. Use of d-serine derivatives for the treatment of anxiety disorders
US8273913B2 (en) 2007-04-02 2012-09-25 Merck Canada Inc. Amidation process for the preparation of cathepsin K inhibitors
CN105218565A (zh) 2008-10-17 2016-01-06 泽农医药公司 螺羟吲哚化合物及其作为治疗剂的用途
EP2445872A4 (en) * 2009-06-22 2012-12-05 Merck Canada Inc CATHEPSIN CYSTEIN PROTEASE FOR THE TREATMENT OF VARIOUS DISEASES
US8324417B2 (en) 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
WO2012119941A1 (en) 2011-03-04 2012-09-13 Prozymex A/S Peptidyl nitrilcompounds as peptidase inhibitors
WO2012174552A2 (en) * 2011-06-17 2012-12-20 Virobay, Inc. Cathepsin inhibitors for treating microglia-mediated neuron loss in the central nervous system
AU2020250933A1 (en) 2019-04-05 2021-10-28 Centre Hospitalier Régional Et Universitaire De Brest Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning

Family Cites Families (6)

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TR200001189T2 (tr) * 1997-11-05 2000-09-21 Novartis Ag. Dipeptid nitriller.
GB9723407D0 (en) * 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
EP1155010A1 (en) * 1999-02-20 2001-11-21 AstraZeneca AB Acetamido acetonitrile derivatives as inhibitors of cathepsin l and/or cathepsin s
AU2002340031A1 (en) * 2001-10-02 2003-04-14 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
US7375134B2 (en) * 2002-03-05 2008-05-20 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
DE60232547D1 (de) * 2002-03-11 2009-07-16 Kao Corp Kosmetika

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106478564A (zh) * 2015-08-29 2017-03-08 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
WO2017036357A1 (zh) * 2015-08-29 2017-03-09 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
CN107922315A (zh) * 2015-08-29 2018-04-17 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
CN106478564B (zh) * 2015-08-29 2021-11-12 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途

Also Published As

Publication number Publication date
WO2006034004A3 (en) 2006-11-23
ECSP077321A (es) 2007-04-26
MX2007003118A (es) 2007-05-24
JP2008513472A (ja) 2008-05-01
US7737300B2 (en) 2010-06-15
NO20071937L (no) 2007-06-15
EP1799645A2 (en) 2007-06-27
CA2580065A1 (en) 2006-03-30
CR8993A (es) 2007-10-04
AU2005287046A1 (en) 2006-03-30
WO2006034004A2 (en) 2006-03-30
IL181792A0 (en) 2007-07-04
KR20070061877A (ko) 2007-06-14
BRPI0515470A (pt) 2008-07-22
ZA200703102B (en) 2009-09-30
US20080114175A1 (en) 2008-05-15

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