WO1998003540A3 - 1,2-substituted cycloalkane derivatives as thrombine inhibitors, a process for the preparation thereof and the use thereof in pharmaceutical formulations - Google Patents

1,2-substituted cycloalkane derivatives as thrombine inhibitors, a process for the preparation thereof and the use thereof in pharmaceutical formulations Download PDF

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Publication number
WO1998003540A3
WO1998003540A3 PCT/EP1997/003774 EP9703774W WO9803540A3 WO 1998003540 A3 WO1998003540 A3 WO 1998003540A3 EP 9703774 W EP9703774 W EP 9703774W WO 9803540 A3 WO9803540 A3 WO 9803540A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
pharmaceutical formulations
substituted cycloalkane
cycloalkane derivatives
thrombine
Prior art date
Application number
PCT/EP1997/003774
Other languages
French (fr)
Other versions
WO1998003540A2 (en
Inventor
Bugno Cristina Di
Raffaello Giorgi
Nicholas Harmat
Original Assignee
Menarini Farma Ind
Bugno Cristina Di
Raffaello Giorgi
Nicholas Harmat
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Menarini Farma Ind, Bugno Cristina Di, Raffaello Giorgi, Nicholas Harmat filed Critical Menarini Farma Ind
Priority to AU35437/97A priority Critical patent/AU3543797A/en
Publication of WO1998003540A2 publication Critical patent/WO1998003540A2/en
Publication of WO1998003540A3 publication Critical patent/WO1998003540A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/10Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by doubly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compounds containing a 1,2-disubstituted cycloalkane or cycloalkene ring with inhibitory activity on serinoproteases of general formula (I) wherein A is selected from the (CH2)n group with n = -3, CH=CH and Ar, L, X, Q, Y, W are as defined; processes for the preparation thereof, pharmaceutical compositions containing them and the use thereof as therapeutical agents.
PCT/EP1997/003774 1996-07-19 1997-07-15 1,2-substituted cycloalkane derivatives as thrombine inhibitors, a process for the preparation thereof and the use thereof in pharmaceutical formulations WO1998003540A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU35437/97A AU3543797A (en) 1996-07-19 1997-07-15 1,2-substituted cycloalkane derivatives as thrombine inhibitors, a process for the preparation thereof and the use thereof in pharmaceutical formulations

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT96MI001512A IT1283467B1 (en) 1996-07-19 1996-07-19 DERIVATIVES OF 1,2 SUBSTITUTED CYCLOALKANES AS THROMBIN INHIBITORS, PROCEDURE FOR THEIR PREPARATION AND THEIR USE IN FORMULATIONS
ITMI96A001512 1996-07-19

Publications (2)

Publication Number Publication Date
WO1998003540A2 WO1998003540A2 (en) 1998-01-29
WO1998003540A3 true WO1998003540A3 (en) 1998-04-09

Family

ID=11374623

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1997/003774 WO1998003540A2 (en) 1996-07-19 1997-07-15 1,2-substituted cycloalkane derivatives as thrombine inhibitors, a process for the preparation thereof and the use thereof in pharmaceutical formulations

Country Status (3)

Country Link
AU (1) AU3543797A (en)
IT (1) IT1283467B1 (en)
WO (1) WO1998003540A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1066247B1 (en) * 1998-03-31 2006-11-22 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US6462076B2 (en) * 2000-06-14 2002-10-08 Hoffmann-La Roche Inc. Beta-amino acid nitrile derivatives as cathepsin K inhibitors
US6759428B2 (en) 2001-12-04 2004-07-06 Roche Palo Alto Llc Indole nitriles
JP2005517640A (en) 2001-12-04 2005-06-16 エフ.ホフマン−ラ ロシュ アーゲー Substituted 2-amino-cycloalkanecarboxamides and their use as cysteine protease inhibitors
WO2005000793A1 (en) * 2003-06-26 2005-01-06 Taisho Pharmaceutical Co., Ltd. 2-substituted cycloalkylcarboxylic acid derivative
KR102147420B1 (en) * 2012-12-07 2020-08-25 베나토알엑스 파마슈티컬스, 인크. Beta-lactamase inhibitors
CN114437119B (en) * 2020-10-30 2024-08-09 苏州开拓药业股份有限公司 C-Myc protein inhibitor and preparation method and application thereof

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4478745A (en) * 1981-01-13 1984-10-23 Richter Gedeon Vegyeszeti Gyar R.T. T-Butyloxy-carbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate, D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and process for the preparation thereof
US4499079A (en) * 1982-11-18 1985-02-12 E. R. Squibb & Sons, Inc. Carboxy and substituted carboxy alkanoyl and cycloalkanoyl peptides

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4478745A (en) * 1981-01-13 1984-10-23 Richter Gedeon Vegyeszeti Gyar R.T. T-Butyloxy-carbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate, D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate and process for the preparation thereof
US4499079A (en) * 1982-11-18 1985-02-12 E. R. Squibb & Sons, Inc. Carboxy and substituted carboxy alkanoyl and cycloalkanoyl peptides

Also Published As

Publication number Publication date
ITMI961512A1 (en) 1998-01-19
ITMI961512A0 (en) 1996-07-19
IT1283467B1 (en) 1998-04-21
AU3543797A (en) 1998-02-10
WO1998003540A2 (en) 1998-01-29

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