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WO2000066577A3 - Brigded cycloalkanes as thromboxane ligands without blood clotting effects - Google Patents

Brigded cycloalkanes as thromboxane ligands without blood clotting effects Download PDF

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Publication number
WO2000066577A3
WO2000066577A3 PCT/US2000/011760 US0011760W WO0066577A3 WO 2000066577 A3 WO2000066577 A3 WO 2000066577A3 US 0011760 W US0011760 W US 0011760W WO 0066577 A3 WO0066577 A3 WO 0066577A3
Authority
WO
WIPO (PCT)
Prior art keywords
radical
group
radicals
aryl
hemorrhage
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.)
Ceased
Application number
PCT/US2000/011760
Other languages
French (fr)
Other versions
WO2000066577A2 (en
Inventor
Robert M Burk
Achim H Krauss
David F Woodward
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.)
Allergan Sales LLC
Original Assignee
Allergan Sales LLC
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 Allergan Sales LLC filed Critical Allergan Sales LLC
Priority to AU46875/00A priority Critical patent/AU4687500A/en
Publication of WO2000066577A2 publication Critical patent/WO2000066577A2/en
Publication of WO2000066577A3 publication Critical patent/WO2000066577A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/558—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
    • C07D319/08—1,3-Dioxanes; Hydrogenated 1,3-dioxanes condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A method of treating ocular hypotension, hypertension, hemorrhage, myocardial ischemia, angina pectoris, coronary contraction, cerebrovascular contraction after subarachnoidal hemorrhage, cerebral hemorrhage and asthma which comprises administering to a mammal suffering therefrom a therapeutically effective amount of a thromboxane ligand which is a compound of formula (I(a)), wherein the hatched line indicates the α configuration and the solid triangle indicates the β configuration; Y is (CH2)x; Z is selected from the group consisting of (1), O, OCH2, O-C-O and (CR2)x, x is an integer of 1 or 2; R2 is hydrogen or an alkyl radical of from 1 to 4 carbons, A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups or said alkylene or alkenylene may have one or more enchained oxo or imino radicals; B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms, or substituted derivatives of said methyl, cycloalkyl or aryl radicals wherein said substituent is selected from the group consisting of halo, nitro, amino, thiol, hydroxy, alkyloxy and alkylcarboxy; and X is selected from the group consisting of nitro, cyano, -COOR, -CH2OR1, -C(O)N(R1)2, -CH2N(R1)2 -CH=N-OH and -CH2SR1 radicals wherein R is a C1 to C10 alkyl, phenyl or benzyl and R1 is R or hydrogen; or a pharmaceutically acceptable salt thereof.
PCT/US2000/011760 1999-04-29 2000-04-27 Brigded cycloalkanes as thromboxane ligands without blood clotting effects Ceased WO2000066577A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU46875/00A AU4687500A (en) 1999-04-29 2000-04-27 Thromboxane ligands without blood clotting side effects

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30179499A 1999-04-29 1999-04-29
US09/301,794 1999-04-29

Publications (2)

Publication Number Publication Date
WO2000066577A2 WO2000066577A2 (en) 2000-11-09
WO2000066577A3 true WO2000066577A3 (en) 2001-03-01

Family

ID=23164906

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/011760 Ceased WO2000066577A2 (en) 1999-04-29 2000-04-27 Brigded cycloalkanes as thromboxane ligands without blood clotting effects

Country Status (2)

Country Link
AU (1) AU4687500A (en)
WO (1) WO2000066577A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0201837D0 (en) * 2002-06-14 2002-06-14 Astrazeneca Ab Chemical compounds
HUE067954T2 (en) 2014-05-13 2024-11-28 Novartis Ag Compounds and compositions for inducing chondrogenesis

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4438136A (en) * 1979-01-05 1984-03-20 National Research Development Corporation Prostaglandins
US4654364A (en) * 1984-11-30 1987-03-31 E. R. Squibb & Sons, Inc. Hydroxamic acids of 7-oxabicycloheptane substituted ethers
JPS63284158A (en) * 1987-05-18 1988-11-21 Shionogi & Co Ltd Phenylsulfonylaminoalkylbicycloheptylheptenoic acid derivative
US4942256A (en) * 1988-12-13 1990-07-17 National Research Development Corporation Novel intermediates in the manufacture of novel thromboxane A2 antagonists
DE4013680A1 (en) * 1989-05-01 1990-11-08 Squibb & Sons Inc THROMBOXAN-A (ARROW DOWN) 2 (ARROW ABSTRACT) RECEPTOR ANTAGONISTS FOR INHIBITING VASOSPASM AND THROMBOCYTE AGGREGATION BASED ON ANGIOPLASTY
US4973604A (en) * 1988-12-13 1990-11-27 National Research Development Corporation Thromboxane A2 antagonists and pharmaceutical compositions thereof
US4977174A (en) * 1989-06-12 1990-12-11 E. R. Squibb & Sons, Inc. 7-oxabicycloheptane imidazole prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
JPH0377862A (en) * 1989-08-18 1991-04-03 Ono Pharmaceut Co Ltd Bicyclo(2,2,1)heptane derivative, purification and its production
WO1995018103A1 (en) * 1993-12-28 1995-07-06 Allergan 7-[carboxyalkyl or alkenyl]-6-[alkyl or alkenyl] 3-oxo-2,4-dioxobicyclo-[3.2.1] octane and derivatives thereof
US5650431A (en) * 1993-12-28 1997-07-22 Allergan Thromboxane ligands without blood clotting side effects
US5741812A (en) * 1993-12-28 1998-04-21 Allergan Thromboxane ligands without blood clotting side effects
WO1999012921A1 (en) * 1997-09-09 1999-03-18 Allergan Sales, Inc. Thromboxane ligands

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4438136A (en) * 1979-01-05 1984-03-20 National Research Development Corporation Prostaglandins
US4654364A (en) * 1984-11-30 1987-03-31 E. R. Squibb & Sons, Inc. Hydroxamic acids of 7-oxabicycloheptane substituted ethers
JPS63284158A (en) * 1987-05-18 1988-11-21 Shionogi & Co Ltd Phenylsulfonylaminoalkylbicycloheptylheptenoic acid derivative
US4942256A (en) * 1988-12-13 1990-07-17 National Research Development Corporation Novel intermediates in the manufacture of novel thromboxane A2 antagonists
US4973604A (en) * 1988-12-13 1990-11-27 National Research Development Corporation Thromboxane A2 antagonists and pharmaceutical compositions thereof
DE4013680A1 (en) * 1989-05-01 1990-11-08 Squibb & Sons Inc THROMBOXAN-A (ARROW DOWN) 2 (ARROW ABSTRACT) RECEPTOR ANTAGONISTS FOR INHIBITING VASOSPASM AND THROMBOCYTE AGGREGATION BASED ON ANGIOPLASTY
US4977174A (en) * 1989-06-12 1990-12-11 E. R. Squibb & Sons, Inc. 7-oxabicycloheptane imidazole prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
JPH0377862A (en) * 1989-08-18 1991-04-03 Ono Pharmaceut Co Ltd Bicyclo(2,2,1)heptane derivative, purification and its production
WO1995018103A1 (en) * 1993-12-28 1995-07-06 Allergan 7-[carboxyalkyl or alkenyl]-6-[alkyl or alkenyl] 3-oxo-2,4-dioxobicyclo-[3.2.1] octane and derivatives thereof
US5516791A (en) * 1993-12-28 1996-05-14 Allergan 7-[carboxyakyl or alkenyl]-6-[alkyl or alkenyl]3-oxo-2,4-dioxobicyclo-[3.2.1]octane and derivatives thereof
US5650431A (en) * 1993-12-28 1997-07-22 Allergan Thromboxane ligands without blood clotting side effects
US5741812A (en) * 1993-12-28 1998-04-21 Allergan Thromboxane ligands without blood clotting side effects
WO1999012921A1 (en) * 1997-09-09 1999-03-18 Allergan Sales, Inc. Thromboxane ligands

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
PATENT ABSTRACTS OF JAPAN vol. 013, no. 107 14 March 1989 (1989-03-14) *
PATENT ABSTRACTS OF JAPAN vol. 015, no. 248 25 June 1991 (1991-06-25) *

Also Published As

Publication number Publication date
AU4687500A (en) 2000-11-17
WO2000066577A2 (en) 2000-11-09

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