HUP0203246A2 - Eljárás és köztitermékek imidazolidinon típusú alfa V integrin antagonisták előállítására - Google Patents

Eljárás és köztitermékek imidazolidinon típusú alfa V integrin antagonisták előállítására

Info

Publication number
HUP0203246A2
HUP0203246A2 HU0203246A HUP0203246A HUP0203246A2 HU P0203246 A2 HUP0203246 A2 HU P0203246A2 HU 0203246 A HU0203246 A HU 0203246A HU P0203246 A HUP0203246 A HU P0203246A HU P0203246 A2 HUP0203246 A2 HU P0203246A2
Authority
HU
Hungary
Prior art keywords
carbon atoms
group containing
alkyl
avb3
general formula
Prior art date
Application number
HU0203246A
Other languages
English (en)
Inventor
Mark S. Jensen
Michael Palucki
Nelo R. Rivera
Yaling Wang
Kenneth M. Wells
Yi Xiao
Chunhua Yang
Nobuyoshi Yasuda
Original Assignee
Merck & Co., Inc.
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 Merck & Co., Inc. filed Critical Merck & Co., Inc.
Publication of HUP0203246A2 publication Critical patent/HUP0203246A2/hu
Publication of HUP0203246A3 publication Critical patent/HUP0203246A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07D213/60—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 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A találmány tárgya javított eljárás az (I) általános képletű,avb3/avb5 integrin antagonista hatású imidazolidinon-származékokelőállítására. A találmány továbbá az eljárásban hasznosíthatóköztitermékekre vonatkozik. A találmány szerinti vegyületekantagonista hatást fejtenek ki az avb3/avb5 integrin receptoroknál,így felhasználhatók csont reszorpció gátlására, továbbá oszteoporóziskezelésére vagy megelőzésére. Ismertetésre kerül továbbá a 3-{2-oxo-3-[3- (5,6,7,8-tetrahidro-[1,8]naftiridin-2-il)-propil]imidazolidin-1-il}-3(S)-(6-metoxipiridin- 3-il)-propionsav hemihidrát formájában. Az(I) általános képletben Ar jelentése mono- vagy diszubsztituáltfenil-, naftil-, piridil-, furil-, tienil-, pirrolil-, oxazolil-,tiazolil-, izoxazolil-, izotiazolil-, imidazolil-, tetrazolil-,pirazolil-, benztiazolil-, benzoxazolil-, indolil-, izoindolil-,purinil- vagy karbazolilcsoport, ahol a szubsztituenst egymástólfüggetlenül megválasztva hidrogén- vagy halogénatomok vagy 1-6szénatomot tartalmazó alkil-, 3-6 szénatomot tartalmazó cikloalkil-,1-3 szénatomot tartalmazó acilamino-, 1-4 szénatomot tartalmazóalkoxi-, az alkoxirészben 1-5 szénatomot tartalmazó alkoxikarbonil-,ciano-, trifluormetil-, trifluormetoxi-, hidroxi-, amino-, 1-4szénatomot tartalmazó alkilamino-, az alkil<- >részekben 1-4szénatomot tartalmazó dialkilamino- vagy az alkilrészben 1-5szénatomot tartalmazó alkilkarboniloxicsoportok közül választják meg;és R1 jelentése hidrogén- vagy halogénatom vagy 1-10 szénatomottartalmazó alkil-, 3-6 szénatomot tartalmazó cikloalkil- vagy 1-3szénatomot tartalmazó alkoxicsoport. Ó
HU0203246A 1999-11-08 2000-11-03 Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists HUP0203246A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16397999P 1999-11-08 1999-11-08
PCT/US2000/030361 WO2001034602A2 (en) 1999-11-08 2000-11-03 Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists

Publications (2)

Publication Number Publication Date
HUP0203246A2 true HUP0203246A2 (hu) 2003-01-28
HUP0203246A3 HUP0203246A3 (en) 2003-12-29

Family

ID=22592461

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0203246A HUP0203246A3 (en) 1999-11-08 2000-11-03 Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists

Country Status (20)

Country Link
EP (1) EP1230240B1 (hu)
JP (1) JP2003513974A (hu)
KR (1) KR20020048427A (hu)
CN (1) CN1414966A (hu)
AR (1) AR029407A1 (hu)
AT (1) ATE245645T1 (hu)
AU (1) AU777919B2 (hu)
BR (1) BR0015384A (hu)
CA (1) CA2389999A1 (hu)
CZ (1) CZ20021508A3 (hu)
DE (1) DE60004087T2 (hu)
EA (1) EA200200548A1 (hu)
ES (1) ES2202191T3 (hu)
HU (1) HUP0203246A3 (hu)
IL (1) IL149313A0 (hu)
MX (1) MXPA02004547A (hu)
PL (1) PL355011A1 (hu)
SK (1) SK8012002A3 (hu)
WO (1) WO2001034602A2 (hu)
YU (1) YU32502A (hu)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001290884B2 (en) * 2000-09-13 2005-12-15 Merck & Co., Inc. Alpha V integrin receptor antagonists
AU9259801A (en) 2000-09-14 2002-03-26 Merck & Co Inc Alpha v integrin receptor antagonists
US6706885B2 (en) 2001-06-06 2004-03-16 Merck & Co., Inc. Process for preparing integrin antagonist intermediates
US6509347B2 (en) 2001-06-11 2003-01-21 Merck & Co., Inc. Crystalline forms of an integrin receptor antagonist
US6646130B2 (en) 2001-07-19 2003-11-11 Merck & Co., Inc. Process to chiral integrin antagonist beta-amino acid intermediate
AR038189A1 (es) * 2002-01-29 2005-01-05 Merck & Co Inc Proceso para la preparacion de intermediarios de antagonistas de integrina
CA2499149A1 (en) * 2002-09-20 2004-04-01 Merck & Co., Inc. Mannitol formulation for integrin receptor antagonist
KR101491938B1 (ko) 2010-07-14 2015-02-10 노파르티스 아게 Ｉｐ 수용체 효능제 헤테로시클릭 화합물
WO2013105057A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused pyrroles as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
WO2014125413A1 (en) 2013-02-13 2014-08-21 Novartis Ag Ip receptor agonist heterocyclic compounds
GB201305668D0 (en) 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
HRP20211836T1 (hr) 2013-09-24 2022-03-04 Fujifilm Corporation Novi spoj koji sadrži dušik ili njegova sol, ili njegov metalni kompleks
AU2014338549B2 (en) * 2013-10-25 2017-05-25 Novartis Ag Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
GB201417094D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417011D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417002D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compound
GB201417018D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
WO2016054483A1 (en) 2014-10-03 2016-04-07 Novartis Ag Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
GB201604680D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
GB201604681D0 (en) * 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
US10118929B2 (en) 2016-04-27 2018-11-06 Scifluor Life Sciences, Inc. Nonanoic and decanoic acid derivatives and uses thereof
HUE053620T2 (hu) * 2016-11-08 2021-07-28 Bristol Myers Squibb Co Pirrol amidok mint alfa-V integrin inhibitorok

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE298338T1 (de) * 1997-12-17 2005-07-15 Merck & Co Inc Integrin-rezeptor-antagonisten

Also Published As

Publication number Publication date
WO2001034602A3 (en) 2002-01-17
CN1414966A (zh) 2003-04-30
AR029407A1 (es) 2003-06-25
ATE245645T1 (de) 2003-08-15
AU777919B2 (en) 2004-11-04
EP1230240A2 (en) 2002-08-14
EA200200548A1 (ru) 2002-10-31
CZ20021508A3 (cs) 2002-10-16
CA2389999A1 (en) 2001-05-17
PL355011A1 (en) 2004-03-22
DE60004087T2 (de) 2004-04-15
SK8012002A3 (en) 2002-10-08
ES2202191T3 (es) 2004-04-01
YU32502A (sh) 2004-12-31
IL149313A0 (en) 2002-11-10
KR20020048427A (ko) 2002-06-22
WO2001034602A2 (en) 2001-05-17
MXPA02004547A (es) 2002-09-02
DE60004087D1 (de) 2003-08-28
JP2003513974A (ja) 2003-04-15
BR0015384A (pt) 2002-10-08
EP1230240B1 (en) 2003-07-23
HUP0203246A3 (en) 2003-12-29
AU1461401A (en) 2001-06-06

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