PE20040916A1 - PYRIMIDIN-4,6-DICARBOXYL ACID DIAMIDES AS SELECTIVE INHIBITORS OF MMP-13 - Google Patents

PYRIMIDIN-4,6-DICARBOXYL ACID DIAMIDES AS SELECTIVE INHIBITORS OF MMP-13

Info

Publication number
PE20040916A1
PE20040916A1 PE2003001280A PE2003001280A PE20040916A1 PE 20040916 A1 PE20040916 A1 PE 20040916A1 PE 2003001280 A PE2003001280 A PE 2003001280A PE 2003001280 A PE2003001280 A PE 2003001280A PE 20040916 A1 PE20040916 A1 PE 20040916A1
Authority
PE
Peru
Prior art keywords
alkyl
pyrimidin
halogen
substituted
mmp
Prior art date
Application number
PE2003001280A
Other languages
Spanish (es)
Inventor
Otmar Klingler
Reinhard Kirsch
Jorg Habermann
Klaus-Ulrich Weithmann
Christian Engel
Bernard Pirard
Original Assignee
Aventis Pharma Gmbh
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 Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Publication of PE20040916A1 publication Critical patent/PE20040916A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DIAMIDAS DE ACIDO PIRIMIDIN-4,6-DICARBOXILICO DE FORMULA I DONDE R1 ES H O ALQUILO C1-C6; R2 ES ALQUILO C1-C6 SUSTITUIDO UNA A TRES VECES POR C(O)-O-R8, ALQUIL(C1-C6)-O-R8, ENTRE OTROS; R3, R4, R5, R6 y R7 SON H, HALOGENO, ALQUILO C1-C6 NO SUSTITUIDO O SUSTITUIDO HASTA TRES VECES POR HALOGENO, O-ALQUILO C1-C6 NO SUSTITUIDO O SUSTITUIDO HASTA TRES VECES POR HALOGENO, S-ALQUILO C1-C6; R8 ES H O ALQUILO C1-C6. SON COMPUESTOS PREFERIDOS: [4-({[6-(4-FLUORO-3-METILBENCILCARBAMOIL)-PIRIMIDIN-4-CARBONIL]AMINO}METIL)FENOXI] ACETATO DE TERC-BUTILO; ACIDO [4-({[6-(4-FLUORO-3-METILBENCILCARBAMOIL)-PIRIMIDIN-4-CARBONIL]AMINO}METIL)FENOXI] ACETICO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA PREPARAR ESTOS COMPUESTOS Y UN PRODUCTO FARMACEUTICO. ESTOS COMPUESTOS SON UTILES PARA LA PROFILAXIS Y LA TERAPIA DE ENFERMEDADES CUYO CURSO IMPLICA UNA ACTIVIDAD INCREMENTADA DE METALOPROTEINASA DE MATRIZ 13 COMO SON ENFERMEDADES DEGENERATIVAS DE LAS ARTICULACIONES, ENFERMEDADES DEL TEJIDO CONECTIVO, ENFERMEDADES CANCEROSASREFERS TO DIAMIDES OF PYRIMIDIN-4,6-DICARBOXYLIC ACID OF FORMULA I WHERE R1 IS H OR C1-C6 ALKYL; R2 IS C1-C6 ALKYL SUBSTITUTED ONE TO THREE TIMES BY C (O) -O-R8, (C1-C6) -O-R8 ALKYL, AMONG OTHERS; R3, R4, R5, R6 and R7 ARE H, HALOGEN, C1-C6 ALKYL NOT REPLACED OR SUBSTITUTED UP TO THREE TIMES BY HALOGEN, OR C1-C6 ALKYL NOT REPLACED OR SUBSTITUTED UP TO THREE TIMES BY HALOGEN, S-C6 RENTAL ; R8 IS H OR C1-C6 ALKYL. PREFERRED COMPOUNDS ARE: [4 - ({[6- (4-FLUORO-3-METHYLBENZYLCARBAMOYL) -PYRIMIDIN-4-CARBONYL] AMINO} METHYL) PHENOXY] THIRD-BUTYL ACETATE; [4 - ({[6- (4-FLUORO-3-METHYLBENZYLCARBAMOIL) -PYRIMIDIN-4-CARBONYL] AMINO} METHYL) PHENOXY] ACETIC ACID, AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR PREPARING THESE COMPOUNDS AND A PHARMACEUTICAL PRODUCT. THESE COMPOUNDS ARE USEFUL FOR THE PROPHYLAXIS AND THERAPY OF DISEASES WHOSE COURSE INVOLVES AN INCREASED ACTIVITY OF MATRIX METALOPROTEINASE 13 AS THEY ARE DEGENERATIVE DISEASES OF THE JOINTS, DISEASES OF THE CONNECTED CANNER,

PE2003001280A 2003-01-03 2003-12-12 PYRIMIDIN-4,6-DICARBOXYL ACID DIAMIDES AS SELECTIVE INHIBITORS OF MMP-13 PE20040916A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10300017A DE10300017A1 (en) 2003-01-03 2003-01-03 Selective MMP 13 inhibitors

Publications (1)

Publication Number Publication Date
PE20040916A1 true PE20040916A1 (en) 2005-01-25

Family

ID=32519591

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001280A PE20040916A1 (en) 2003-01-03 2003-12-12 PYRIMIDIN-4,6-DICARBOXYL ACID DIAMIDES AS SELECTIVE INHIBITORS OF MMP-13

Country Status (11)

Country Link
EP (1) EP1587803A1 (en)
JP (1) JP2006515595A (en)
AR (1) AR042687A1 (en)
AU (1) AU2003293951A1 (en)
BR (1) BR0317834A (en)
CA (1) CA2512183A1 (en)
DE (1) DE10300017A1 (en)
MX (1) MXPA05006401A (en)
PE (1) PE20040916A1 (en)
TW (1) TW200505906A (en)
WO (1) WO2004060883A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060173183A1 (en) * 2004-12-31 2006-08-03 Alantos Pharmaceuticals, Inc., Multicyclic bis-amide MMP inhibitors
US20070155738A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20070155737A1 (en) * 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
JP2009522295A (en) * 2005-12-30 2009-06-11 アラントス・フアーマシユーテイカルズ・ホールデイング・インコーポレイテツド Substituted bis-amide metalloprotease inhibitors
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US20080221092A1 (en) * 2006-11-20 2008-09-11 Harald Bluhm Heterobicyclic metalloprotease inhibitors
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
SG184987A1 (en) 2010-04-22 2012-11-29 Vertex Pharma Process of producing cycloalkylcarboxamido-indole compounds
US10206877B2 (en) 2014-04-15 2019-02-19 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases
GB201908453D0 (en) * 2019-06-12 2019-07-24 Enterprise Therapeutics Ltd Compounds for treating respiratory disease

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3931432A1 (en) * 1989-09-21 1991-04-04 Hoechst Ag PYRIMIDIN-4,6-DICARBONSAEUREDIAMIDE, METHOD FOR THE PRODUCTION AND USE THEREOF AND MEDICINAL PRODUCTS BASED ON THESE COMPOUNDS
BR0207209A (en) * 2001-02-14 2004-01-27 Warner Lambert Co Pyrimidine Matrix Metalloproteinase Inhibitors
DE10160357A1 (en) * 2001-12-08 2003-06-18 Aventis Pharma Gmbh Use of pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides for the selective inhibition of collagenases

Also Published As

Publication number Publication date
EP1587803A1 (en) 2005-10-26
CA2512183A1 (en) 2004-07-22
JP2006515595A (en) 2006-06-01
AR042687A1 (en) 2005-06-29
MXPA05006401A (en) 2005-08-19
BR0317834A (en) 2005-11-29
DE10300017A1 (en) 2004-07-15
TW200505906A (en) 2005-02-16
AU2003293951A1 (en) 2004-07-29
WO2004060883A1 (en) 2004-07-22

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