WO1994004537A3 - Dual functional anti-inflammatory and immunosuppressive agents - Google Patents

Dual functional anti-inflammatory and immunosuppressive agents Download PDF

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Publication number
WO1994004537A3
WO1994004537A3 PCT/US1993/007728 US9307728W WO9404537A3 WO 1994004537 A3 WO1994004537 A3 WO 1994004537A3 US 9307728 W US9307728 W US 9307728W WO 9404537 A3 WO9404537 A3 WO 9404537A3
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WO
WIPO (PCT)
Prior art keywords
inflammatory
paf
immunosuppressive agents
dual functional
functional anti
Prior art date
Application number
PCT/US1993/007728
Other languages
French (fr)
Other versions
WO1994004537A2 (en
Inventor
David M Goldstein
San-Bao Hwang
Ralph T Scannell
T Y Shen
Original Assignee
Cytomed 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 Cytomed Inc filed Critical Cytomed Inc
Priority to AU50167/93A priority Critical patent/AU5016793A/en
Priority to EP93920131A priority patent/EP0656004A1/en
Publication of WO1994004537A2 publication Critical patent/WO1994004537A2/en
Publication of WO1994004537A3 publication Critical patent/WO1994004537A3/en

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    • 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
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/83—Oxygen atoms
    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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

Abstract

Platelet activating factor receptor antagonists of diverse structures are imparted with 5-lipoxygenase activity by adding a moiety such as a hydroxamate, hydroxyurea, oxalkane, thioalkane, quinolylmethoxy, or amidohydroxyurea to the PAF receptor antagonist at a position on the PAF antagonist molecule that demonstrates 'bulk tolerance', i.e., the ability to accommodate functionality without the significant loss of PAF activity.
PCT/US1993/007728 1992-08-20 1993-08-16 Dual functional anti-inflammatory and immunosuppressive agents WO1994004537A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU50167/93A AU5016793A (en) 1992-08-20 1993-08-16 Dual functional anti-inflammatory and immunosuppressive agents
EP93920131A EP0656004A1 (en) 1992-08-20 1993-08-16 Dual functional anti-inflammatory and immunosuppressive agents

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US93339592A 1992-08-20 1992-08-20
US07/933,395 1992-08-20

Publications (2)

Publication Number Publication Date
WO1994004537A2 WO1994004537A2 (en) 1994-03-03
WO1994004537A3 true WO1994004537A3 (en) 1994-10-27

Family

ID=25463868

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1993/007728 WO1994004537A2 (en) 1992-08-20 1993-08-16 Dual functional anti-inflammatory and immunosuppressive agents

Country Status (5)

Country Link
EP (1) EP0656004A1 (en)
CN (1) CN1090284A (en)
AU (1) AU5016793A (en)
MX (1) MX9305063A (en)
WO (1) WO1994004537A2 (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8841307B2 (en) 2000-08-04 2014-09-23 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US8871772B2 (en) 2008-05-27 2014-10-28 Ampio Pharmaceuticals, Inc. Therapeutic methods and compounds
US8962568B2 (en) 2003-05-15 2015-02-24 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US8980834B2 (en) 2011-10-10 2015-03-17 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US9034878B2 (en) 2010-09-07 2015-05-19 Ampio Pharmaceuticals, Inc. Treatment of diseases

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5639782A (en) * 1992-03-04 1997-06-17 Center For Innovative Technology Neolignan derivatives as platelet activating factor receptor antagonists and 5-lipoxygenase inhibitors
US5434151A (en) * 1992-08-24 1995-07-18 Cytomed, Inc. Compounds and methods for the treatment of disorders mediated by platelet activating factor or products of 5-lipoxygenase
DK0650485T3 (en) 1992-07-13 2001-01-22 Millennium Pharm Inc 2,5-Diaryltetrahydrothiophenes, furans and analogues for the treatment of inflammatory and immune disorders
US5463083A (en) * 1992-07-13 1995-10-31 Cytomed, Inc. Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
ES2061406B1 (en) * 1993-05-07 1995-06-01 Uriach & Cia Sa J NEW DERIVATIVES OF 2- (QUINOLINE) WITH PHARMACOLOGICAL ACTIVITY.
US5750565A (en) 1995-05-25 1998-05-12 Cytomed, Inc. Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
US5792776A (en) * 1994-06-27 1998-08-11 Cytomed, Inc., Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
US5703093A (en) * 1995-05-31 1997-12-30 Cytomed, Inc. Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
KR20140075772A (en) 2011-10-10 2014-06-19 앰피오 파마슈티컬스 인코퍼레이티드 Implantable medical devices with increased immune tolerance, and methods for making and implanting
CN103841974A (en) 2011-10-28 2014-06-04 安皮奥制药股份有限公司 Treatment of rhinitis
MX2015010937A (en) 2013-03-15 2015-10-29 Ampio Pharmaceuticals Inc Compositions for the mobilization, homing, expansion and differentiation of stem cells and methods of using the same.
CA2958080A1 (en) 2014-08-18 2016-02-25 Ampio Pharmaceuticals, Inc. Treatment of joint conditions
EP3310375A4 (en) 2015-06-22 2019-02-20 Ampio Pharmaceuticals, Inc. Use of low molecular weight fractions of human serum albumin in treating diseases
CN117881684A (en) 2021-08-02 2024-04-12 豪夫迈·罗氏有限公司 Novel cyclopenta-thieno-diazepine derivatives as GABAA gamma 1 PAM

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0194416A1 (en) * 1985-01-25 1986-09-17 Boehringer Ingelheim Kg Thieno-triazolo-1,4-diazepino-2-carboxamides, process for their preparation and pharmaceutical compositions
EP0217204A1 (en) * 1985-09-13 1987-04-08 Merck & Co. Inc. Trans-2-(3,4,5-trimethoxyphenyl)-5-(5,6-dimethoxy-3-pyridyl)-tetrahydrothiophene, a PAF-antagonist
EP0222961A1 (en) * 1985-09-17 1987-05-27 Ciba-Geigy Ag Resorcinol ethers
EP0299761A1 (en) * 1987-07-15 1989-01-18 The Wellcome Foundation Limited Anti-inflammatory aryl derivatives
EP0351214A1 (en) * 1988-07-14 1990-01-17 The Wellcome Foundation Limited Anti-inflammatory aryl derivatives
FR2653119A1 (en) * 1989-10-18 1991-04-19 Lipha New phenoxy-ethylbenzene derivs.
EP0441515A1 (en) * 1990-02-07 1991-08-14 Pfizer Inc. Tetralin and chroman derivatives in the treatment of asthma, arthritis and related diseases
WO1991017163A1 (en) * 1990-05-09 1991-11-14 Pfizer Inc. IMIDAZO (4,5-c) PYRIDINES WITH PAF ANTAGONIST ACTIVITY
EP0475204A2 (en) * 1990-08-30 1992-03-18 Boehringer Ingelheim Kg Heteroazepinoid amides
WO1992010498A1 (en) * 1990-12-13 1992-06-25 Smithkline Beecham Corporation Novel csaids

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4757084A (en) * 1984-02-29 1988-07-12 Merck & Co., Inc. 2,5-diaryl tetrahydrothiophenes and analogs thereof as PAF-antagonists
EP0194416A1 (en) * 1985-01-25 1986-09-17 Boehringer Ingelheim Kg Thieno-triazolo-1,4-diazepino-2-carboxamides, process for their preparation and pharmaceutical compositions
EP0217204A1 (en) * 1985-09-13 1987-04-08 Merck & Co. Inc. Trans-2-(3,4,5-trimethoxyphenyl)-5-(5,6-dimethoxy-3-pyridyl)-tetrahydrothiophene, a PAF-antagonist
EP0222961A1 (en) * 1985-09-17 1987-05-27 Ciba-Geigy Ag Resorcinol ethers
EP0299761A1 (en) * 1987-07-15 1989-01-18 The Wellcome Foundation Limited Anti-inflammatory aryl derivatives
EP0351214A1 (en) * 1988-07-14 1990-01-17 The Wellcome Foundation Limited Anti-inflammatory aryl derivatives
FR2653119A1 (en) * 1989-10-18 1991-04-19 Lipha New phenoxy-ethylbenzene derivs.
EP0441515A1 (en) * 1990-02-07 1991-08-14 Pfizer Inc. Tetralin and chroman derivatives in the treatment of asthma, arthritis and related diseases
WO1991017163A1 (en) * 1990-05-09 1991-11-14 Pfizer Inc. IMIDAZO (4,5-c) PYRIDINES WITH PAF ANTAGONIST ACTIVITY
EP0475204A2 (en) * 1990-08-30 1992-03-18 Boehringer Ingelheim Kg Heteroazepinoid amides
WO1992010498A1 (en) * 1990-12-13 1992-06-25 Smithkline Beecham Corporation Novel csaids

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
C. BONNE ET AL.: "2-(2-Hydroxy-4-methylphenyl)aminothiazole Hydrochloride as a Dual Inhibitor of Cyclooxygenase/Lipoxygenase and a Free Radical Scavenger", ARZNEIM.-FORSCH./DRUG. RES., vol. 39 (II), no. 10, 1989, pages 1242 - 1245 *
C.M. HERD ET AL.: "Effect of a 5-lipoxygenase inhibitor and leukotriene antagonist (PF 5901) on PAF-induced airway responses in neonatally immunized rabbits", BR. J. PHARMACOL., vol. 107, no. 4, 1992, pages 1108 - 1115 *
D.M. GOLDSTEIN, T.Y. SHEN: "Dual Inhibitors of Platelet Activating Factor and 5-Lipoxygenase I. 2,4-Diaryl-1,3-dithiolanes", MED. CHEM. RES., vol. 2, no. 7-8, 1992, pages 443 - 450 *
D.M. GOLDSTEIN, T.Y. SHEN: "Dual Inhibitors of Platelet Activating Factor and 5-Lipoxygenase II. Novel 2,4-Diaryl-1,3-dithiolanes with Iron-chelating Functionalities", MED. CHEM. RES., vol. 2, no. 7-8, 1992, pages 451 - 456 *
G. ANDERSON, M. FENNESSY: "Effects of REV 5901, a 5-lipoxygenase inhibitor and leukotriene antagonist, on pulmonary responses to platelet activating factor in the guinea-pig", BR. J. PHARMACOL., vol. 94, no. 4, 1988, pages 1115 - 1122 *
J. CHANG ET AL.: "The antiinflammatory action of guanabenz is mediated through 5-lipoxygenase and cyclooxygenase", EUR. J. PHARMACOL., vol. 142, no. 2, 1987, pages 197 - 205 *
R.N. WILLETTE ET AL.: "SK&F 86002, a dual lipoxygenase/cyclooxygenase inhibitor prevents changes in body weight and serum tumor necrosis factor elicited by lipopolysaccharide and platelet activating factor", PHARMACOL. COMM., vol. 1, no. 4, 1992, pages 329 - 335 *
T. HIDAKA ET AL.: "Inhibition of Polymorphonuclear Leukocyte 5-Lipoxygenase and Platelet Cyclooxygenase by alpha-(3,5-Di-Tert-Butyl-4-Hydroxybenzylidene)-gamma-Butyrolactone (KME-4), a New Antiinflammatory Drug", JAPAN. J. PHARMACOL., vol. 38, 1985, pages 267 - 272 *

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8841307B2 (en) 2000-08-04 2014-09-23 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US8916568B2 (en) 2000-08-04 2014-12-23 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US9561226B2 (en) 2000-08-04 2017-02-07 Ampio Pharmaceuticals, Inc. Method of using diketopiperazines and composition containing them
US8962568B2 (en) 2003-05-15 2015-02-24 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US8969308B2 (en) 2003-05-15 2015-03-03 Ampio Pharmaceuticals, Inc. Treatment of T-cell mediated diseases
US8871772B2 (en) 2008-05-27 2014-10-28 Ampio Pharmaceuticals, Inc. Therapeutic methods and compounds
US9522893B2 (en) 2008-05-27 2016-12-20 Ampio Pharmaceuticals, Inc. Therapeutic methods and compounds
US9034878B2 (en) 2010-09-07 2015-05-19 Ampio Pharmaceuticals, Inc. Treatment of diseases
US8980834B2 (en) 2011-10-10 2015-03-17 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease
US9060968B2 (en) 2011-10-10 2015-06-23 Ampio Pharmaceuticals, Inc. Treatment of degenerative joint disease

Also Published As

Publication number Publication date
MX9305063A (en) 1994-04-29
CN1090284A (en) 1994-08-03
AU5016793A (en) 1994-03-15
WO1994004537A2 (en) 1994-03-03
EP0656004A1 (en) 1995-06-07

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