ES2132432T3 - Compuestos de azetidinona hidroxi-sustituidos utiles como agentes hipocolesterolemicos. - Google Patents

Compuestos de azetidinona hidroxi-sustituidos utiles como agentes hipocolesterolemicos.

Info

Publication number
ES2132432T3
ES2132432T3 ES94928563T ES94928563T ES2132432T3 ES 2132432 T3 ES2132432 T3 ES 2132432T3 ES 94928563 T ES94928563 T ES 94928563T ES 94928563 T ES94928563 T ES 94928563T ES 2132432 T3 ES2132432 T3 ES 2132432T3
Authority
ES
Spain
Prior art keywords
sup
sub
aryl
substituted
coor
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES94928563T
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English (en)
Inventor
Stuart B Rosenblum
Sundeep Dugar
Duane A Burnett
John W Clader
Brian A Mckittrick
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Schering Corp
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.)
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26799377&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2132432(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Application granted granted Critical
Publication of ES2132432T3 publication Critical patent/ES2132432T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Dental Preparations (AREA)
  • Pyrrole Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE PRESENTAN AGENTES HIPOCOLESTEROLEMICOS DE AZETIDINONAS SUSTITUIDAS CON HIDROXI DE LA FORMULA (IA) O DE UNA SAL FARMACEUTICAMENTE ACEPTABLE DE LAS MISMAS, EN LA QUE: AR{SUP,1} Y AR{SUP,2} SON ARILO O ARILO SUSTITUIDO CON R{SUP,4}; AR{SUP,3} ES ARILO O ARILO SUSTITUIDO CON R{SUP,5}; X, Y Y Z SON CH{SUB,2}-, -CH(ALQUILO INFERIOR)- O -C(DIALQUILO INFERIOR)-; R Y R{SUP,2} SON -OR{SUP,6}, -O(CO)R{SUP,6}, -O(CO)OR{SUP,9} O O(CO)NR{SUP,6}R{SUP,7}; R{SUP,1} Y R{SUP,2} SON H O ALQUILO INFERIOR; Q ES 0 O 1; R ES 0 O 1; M, N Y P SON DE 0 A 4; CON LA CONDICION DE QUE AL MENOS UNO DE ENTRE Q Y R SEA 1, Y LA SUMA DE M, N, P, Q Y R SEA DE 1 A 6; Y CON LA CONDICION DE QUE CUANDO P SEA 0 Y R SEA 1, LA SUMA DE M, Q Y N SEA DE 1 A 5; R{SUP,4} SE SELECCIONA DEL ALQUILO INFERIOR, R{SUP,5}, -CF{SUB,3}, -CN, NO{SUB,2} Y HALOGENO; R{SUP,5} SE SELECCIONA DEL -OR{SUP,6}, O(CO)R{SUP,6}, -O(CO)OR{SUP,9}, -O(CH{SUB,2}){SUB,1-5}OR{SUP,6}, -O(CO)NR{SUP,6}R{SUP,7}, -NR{SUP,6}R{SUP,7}, NR{SUP,6}(CO)R{SUP,7}, -NR{SUP,6}(CO)OR{SUP,9}, NR{SUP,6}(CO)NR{SUP,7}R{SUP,8}, -NR{SUP,6}SO{SUB,2}R{SUP,9}, COOR{SUP,6}, -CONR{SUP,6}R{SUP,7}, -COR{SUP,6}, SO{SUB,2}NR{SUP,6}R{SUP,7}, S(O){SUB,0-2}R{SUP,9}, O(CH{SUB,2}){SUB,1-10}-COOR{SUP,6}, -O(CH{SUB,2}){SUB,110}CONR{SUP,6}R{SUP,7}, -(ALQUILENO INFERIOR)COOR{SUP,6} Y CH=CH-COOR{SUP,6}; R{SUP,6}, R{SUP,7} Y R{SUP,8} SON H, ALQUILO INFERIOR, ARILO O ALQUILO INFERIOR SUSTITUIDO CON ARILO; R{SUP,9} ES ALQUILO INFERIOR, ARILO O ALQUILO INFERIOR SUSTITUIDO CON ARILO; ASI COMO UN METODO PARA REDUCIR EL COLESTEROL DEL SUERO MEDIANTE LA ADMINISTRACION DE DICHOS COMPUESTOS, POR SI SOLOS O EN COMBINACION CON UN INHIBIDOR DE LA BIOSINTESIS DEL COLESTEROL, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y UN PROCESO PARA LA PREPARACION DE LOS MISMOS.
ES94928563T 1993-09-21 1994-09-14 Compuestos de azetidinona hidroxi-sustituidos utiles como agentes hipocolesterolemicos. Expired - Lifetime ES2132432T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US10244093A 1993-09-21 1993-09-21
US08/257,593 US5631365A (en) 1993-09-21 1994-06-09 Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents

Publications (1)

Publication Number Publication Date
ES2132432T3 true ES2132432T3 (es) 1999-08-16

Family

ID=26799377

Family Applications (1)

Application Number Title Priority Date Filing Date
ES94928563T Expired - Lifetime ES2132432T3 (es) 1993-09-21 1994-09-14 Compuestos de azetidinona hidroxi-sustituidos utiles como agentes hipocolesterolemicos.

Country Status (35)

Country Link
US (5) US5631365A (es)
EP (1) EP0720599B1 (es)
JP (1) JP2803908B2 (es)
KR (1) KR100186853B1 (es)
CN (1) CN1050830C (es)
AT (1) ATE180249T1 (es)
AU (1) AU681445C (es)
BE (1) BE2014C056I2 (es)
BR (1) BR1100159A (es)
CA (1) CA2172149C (es)
CZ (2) CZ288861B6 (es)
DE (3) DE10399001I2 (es)
DK (1) DK0720599T3 (es)
ES (1) ES2132432T3 (es)
FI (1) FI110321B (es)
FR (1) FR05C0040I2 (es)
GE (1) GEP20043149B (es)
GR (1) GR3030312T3 (es)
HU (1) HU221185B1 (es)
IL (1) IL110956A (es)
LU (4) LU91050I2 (es)
MA (1) MA23332A1 (es)
MY (1) MY111314A (es)
NL (2) NL300132I2 (es)
NO (6) NO305902B1 (es)
NZ (1) NZ274041A (es)
PL (1) PL182617B1 (es)
RU (1) RU2138480C1 (es)
SG (1) SG46208A1 (es)
SK (1) SK281067B6 (es)
TN (1) TNSN94094A1 (es)
TW (1) TW427974B (es)
UA (1) UA41948C2 (es)
WO (1) WO1995008532A1 (es)
ZA (1) ZA947086B (es)

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