Polycyclo Ring System Patents (Class 562/466)
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Patent number: 6093799Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.Type: GrantFiled: October 20, 1999Date of Patent: July 25, 2000Assignee: Pharmacopeia, Inc.Inventors: Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
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Patent number: 6093517Abstract: A lithographic photoresist composition is provided containing novel calixarene compounds, particularly calix[4]resorcinarenes that are partially or wholly protected with acid-labile functionalities, as dissolution inhibitors. Also provided is a process for using the composition to generate resist images on a substrate is provided, i.e., in the manufacture of integrated circuits or the like.Type: GrantFiled: July 31, 1998Date of Patent: July 25, 2000Assignee: International Business Machines CorporationInventors: Hiroshi Ito, Tomonari Nakayama, Mitsuru Ueda
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Patent number: 6093830Abstract: The invention relates to a novel non-catalytic enantioselective resolution process for the separation of enantiomer of arylpropionic acid drugs from the racemic mixture, which comprises dissolving the racemic mixture of the said drug an organic solvent, reacting this solution with an aqueous phase containing an ionic surfactant with or without a suitable co-surfactant, and an electrolyte in microemulsion/micellar/biphasic medium, reacting this mixture with an appropriate chiral amine at a temperature in the range of 0 to 70 degrees Celsius to obtain a diastereomeric salt, acid hydrolysing the diastereomeric salt to result in the pure enantiomer of the drug which is extracted by known methods.Type: GrantFiled: March 15, 1999Date of Patent: July 25, 2000Assignee: Council of Scientific and Industrial ResearchInventors: Nirmal Kishor Yadav, Bhaskar Dattatraya Kulkarni, Ramdas Bhagvan Khomane
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Patent number: 6087395Abstract: The present invention provides an apoptosis inhibitor containing a 15R-isocarbacyclin derivative or a 15-deoxy-isocarbacyclin derivative, which can be manufactured easily and economically by means of chemical synthesis.Type: GrantFiled: October 16, 1998Date of Patent: July 11, 2000Assignees: Japan Science and Technology Corporation, Atsuo HazatoInventors: Yasuyoshi Watanabe, Atsuo Hazato, Masaaki Suzuki, Yumiko Watanabe, Takumi Sato
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Patent number: 6008321Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.Type: GrantFiled: March 16, 1998Date of Patent: December 28, 1999Assignee: Pharmacopeia, Inc.Inventors: Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
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Derivatives of dihydro or tetrahydronaphthalene, and the pharmaceutical compositions containing them
Patent number: 6005003Abstract: A subject of the invention is the compounds of general formula (I): ##STR1## in which R1=H, alkyl, acyl, R2 and R3=H, alkyl, R4=aryl, heteroaryl, X=O, CH2, Y=OH, O-alkyl or NRaRb, as well as the salts, their preparation processes, the intermediates of these processes, their use as medicaments and the pharmaceutical compositions containing them.Type: GrantFiled: May 5, 1999Date of Patent: December 21, 1999Assignee: Hoechst Marion RousselInventor: Francois Nique -
Patent number: 5998471Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification.Type: GrantFiled: August 11, 1998Date of Patent: December 7, 1999Assignee: Allergan Sales, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5985928Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: January 9, 1998Date of Patent: November 16, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5968908Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.Type: GrantFiled: November 14, 1995Date of Patent: October 19, 1999Assignee: American Cyanamid CompanyInventors: Joseph William Epstein, Feng Ling Qing, Gary Harold Birnberg, Adam Matthew Gilbert
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Patent number: 5958972Abstract: Tricyclic compounds are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.Type: GrantFiled: May 20, 1997Date of Patent: September 28, 1999Assignee: Warner-Lambert CompanyInventors: Donald Hupe, Linda Lea Johnson, Joseph Armand Picard, Andrew David White, Qi-Zhuang Ye
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Patent number: 5955492Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 24, 1998Date of Patent: September 21, 1999Assignee: SmithKline Beecham CorporationInventors: Scott K. Thompson, Stacie M. Halbert, Katherine L. Widdowson
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Patent number: 5952382Abstract: Pharmaceutically/cosmetically-active adamantyl-substituted retinoid compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formula (a) - (d): ##STR2## and are useful for the treatment of disorders and/or ailments manifesting an overregulation of RAR receptors and/or a hypervitaminosis A.Type: GrantFiled: May 3, 1996Date of Patent: September 14, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5919464Abstract: Biomodulators, which regulate cellular differentiation and proliferation, as well as methods of use thereof, e.g., for treating various conditions, e.g., cancer, senescence, immunological disorders and vascular disease; for stimulating normal tissue architecture after injury; for vaccination; for stimulating the production of biologically important molecules by cells or organs in culture; for maintaining organs or tissues outside of a body after removal from the body and prior to transplantation; and for producing of vascular grafts for transplantation; are provided.Type: GrantFiled: September 23, 1993Date of Patent: July 6, 1999Assignee: University of New MexicoInventors: Paul L. Mann, Eugene Mash
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Patent number: 5916916Abstract: The instant invention provides a series of naphthyl compounds having an oxygen linker at the 1-position which are useful as selective estrogen receptor modulators.Type: GrantFiled: September 29, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Kenneth Lee Hauser, Alan David Palkowitz
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Patent number: 5910508Abstract: Novel pharmaceutically/cosmetically-active polycyclic polyenic compounds have the structural formula (I): ##STR1## and are useful for modulating cellular hormone receptors.Type: GrantFiled: September 2, 1997Date of Patent: June 8, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventors: Etienne Thoreau, Braham Shroot
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Patent number: 5874614Abstract: Novel and very useful forms of sodium (S)-2-(6-methoxy-2-naphthyl)propionate are provided. These forms are sodium (S)-2-(6-methoxy-2-naphthyl)propionate monohydrate having an average particle size significantly larger than about 70 microns--the size of conventional sodium (S)-2-(6-methoxy-2-naphthyl)propionate--and a chiral purity of at least 98% (S)-enantiomer. Process technology enabling the production of such novel products is also described. The provision of such novel products makes possible significant improvements in processing time, plant capacity and product handling operations.Type: GrantFiled: December 11, 1997Date of Patent: February 23, 1999Assignee: Albemarle CorporationInventors: Hao V. Phan, Robert H. Allen, Richard A. Coats
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Patent number: 5859293Abstract: A process for the extraction and isolation of concentrated carnosic acid from plant matter of the Labiatae family including contacting the plant matter with a water-miscible solvent to form a plant extract and adjusting the pH of the plant extract to a level between 7 and 10 while adding water in an amount sufficient to cause precipitation of impurities while retaining the carnosic acid salt in solution. The impurities are separated and the remaining aqueous solution is acidified to precipitate a highly purified carnosic acid product which is essentially odorless, flavorless and colorless.Type: GrantFiled: July 14, 1997Date of Patent: January 12, 1999Assignee: Hauser, Inc.Inventors: David T. Bailey, Steven L. Richheimer, Virginia R. Bank, Benjamin T. King
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Patent number: 5808124Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: June 21, 1996Date of Patent: September 15, 1998Assignee: AllerganInventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5792886Abstract: In producing (.+-.)-2-(6-methoxy-2-naphthyl)propionic acid or precursor thereof from 2-bromo-6-methoxynaphthalene, use is made of 2-bromo-6-methoxynaphthalene formed by (a) methylating 6-bromo-2-naphthol with methyl chloride in a solvent comprising one or more compounds, RZ, where R is a hydrogen atom or an alkyl group, and Z is --OH or --CN provided that if Z is --CN, R is alkyl, and in the presence of a strong base; and (b) recovering and purifying 2-bromo-6-methoxynaphthalene so formed.Type: GrantFiled: January 8, 1997Date of Patent: August 11, 1998Assignee: Albemarle CorporationInventors: Mahmood Sabahi, Kevin J. Theriot, Brian F. Becnel
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Patent number: 5773651Abstract: Process for the preparation of fluorine-containing compounds by reduction in a container provided with a stirrer, the stirrer being constructed entirely or partly of a carbon material.Type: GrantFiled: November 27, 1996Date of Patent: June 30, 1998Assignee: Hoechst AktiengesellschaftInventors: Ralf Pfirmann, Friedrich Seitz
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Patent number: 5766610Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 26, 1995Date of Patent: June 16, 1998Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5767310Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula (I) have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: November 8, 1995Date of Patent: June 16, 1998Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy Jo Kevin, Douglas J. Pettibone, Ralph A. Rivero, James R. Tata, Thomas F. Walsh, David L. Williams, Jr.
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Patent number: 5760287Abstract: Naproxene ((+)-6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid) is recovered from the corresponding racemic acid by treatment of the latter with N-substituted R-(-)-2-amino-1-butanols and recovery of the resulting diastereomeric salt.Type: GrantFiled: April 16, 1996Date of Patent: June 2, 1998Assignee: Farchemia S.R.L.Inventors: Pierre Loosen, Gabriele Breviglieri, Bruno Giagomo, Sergio Contrini, Cineia Assanelli
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Patent number: 5739352Abstract: This invention relates to a process for preparing carboxylic acids by oxidizing an aldehyde with a peracid in the presence of an amine and/or amine N-oxide catalyst selected from the group consisting of a substituted or unsubstituted alkyl amine, alkyl amine N-oxide, aromatic amine, aromatic amine N-oxide, heterocyclic amine, heterocyclic amine N-oxide and mixtures thereof, to produce the carboxylic acid. Such carboxylic acids have utility for example as chemical intermediates.Type: GrantFiled: October 19, 1995Date of Patent: April 14, 1998Assignee: United Carbide Chemicals & Plastics Technology CorporationInventors: Bruce Armin Barner, Jonathan Joshua Kurland
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5698733Abstract: Disclosed are 9-deoxyprostaglandins which are useful in the treatment of glaucoma and ocular hypertension. Some of these 9-deoxyprostaglandins are novel. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Thomas R. Dean, Paul W. Zinke, Robert D. Selliah, John E. Bishop
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Patent number: 5688998Abstract: The disclosure describes a surface reforming agent comprising a cone-type calix ?4! resorcinarene compound represented by the formula (I): ##STR1## wherein R is an alkyl group having 3 to 18 carbon atoms, an alkenyl group having 3 to 18 carbon atoms, an aralkyl group having 3 to 18 carbon atoms or a substituted or non-substituted aryl group; R.sup.1 is a hydrogen atom, a carboxyalkyl group in which the alkyl group has 1 to 3 carbon atoms, or a hydroxyalkyl group having 2 to 4 carbon atoms.Type: GrantFiled: March 10, 1995Date of Patent: November 18, 1997Assignee: Toda Kogyo CorporationInventors: Kunihiro Ichimura, Eiichi Kurita, Masahide Ueda
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Patent number: 5677469Abstract: A process for the full or partial resolution of a mixture of enantiomers of a genus of chiral carboxylic acids is disclosed. The process uses a pure enantiomer of 1-aminoindan-2-ol as the resolving agent and achieves separation of the diastereomeric salts by fractional crystallization followed by liberation of the chiral acid from the salt by treatment with mineral acid. Diastereomeric salts and solyates of those salts are disclosed. The production of ketoprofen, flurbiprofen and other chiral medicaments and precursors thereto is disclosed.Type: GrantFiled: May 18, 1995Date of Patent: October 14, 1997Assignee: Sepracor, Inc.Inventors: Paul van Eikeren, Francis X. McConville, Jorge L. Lopez
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Patent number: 5668176Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: October 18, 1996Date of Patent: September 16, 1997Assignee: Merck & Co. Inc.Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy Jo Kevin, Gerard R. Kieczykowski, Douglas J. Pettibone, James R. Tata, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Jay M. Matthews, Richard B. Toupence
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Patent number: 5663337Abstract: The present invention relates to benzoquinazoline thymidylate synthase inhibitors, processes for preparing them and pharmaceutical formulations containing them.Type: GrantFiled: May 25, 1995Date of Patent: September 2, 1997Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson
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Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5618931Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification have retinoid-like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: April 8, 1997Assignee: AllerganInventors: Richard L. Beard, Min Teng, Alan T. Johnson, Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5612479Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.Type: GrantFiled: August 17, 1994Date of Patent: March 18, 1997Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5574036Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted polycyclic acetylene compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(f): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 26, 1995Date of Patent: November 12, 1996Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Bruno Charpenter
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Patent number: 5563129Abstract: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.Type: GrantFiled: April 24, 1995Date of Patent: October 8, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirotomo Masuya, Masayoshi Yamaoka
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Patent number: 5543534Abstract: Compounds of Formula 1 ##STR1## wherein X is S or O; R.sub.1 -R.sub.5, m, o, X, Y, A, B are as defined in the specification.Type: GrantFiled: December 29, 1994Date of Patent: August 6, 1996Assignee: AllerganInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5538986Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.Type: GrantFiled: December 6, 1993Date of Patent: July 23, 1996Assignee: Schering CorporationInventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
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Patent number: 5532408Abstract: Provided are .alpha.-chain-modified isocarbacyclins of which the .alpha.-chain is modified with a phenylene group, a cycloalkylene group or a thiophendiyl group, and these .alpha.-chain-modified isocarbacyclins show the activity for inhibiting the DNA synthesis of human smooth muscle cell and are expected to be capable of inhibiting the hypertrophy of a blood vessel.Type: GrantFiled: April 5, 1995Date of Patent: July 2, 1996Assignee: Teijin LimitedInventors: Masahiro Koga, Toshio Tanaka, Takao Fujii, Tsukio Masegi
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Patent number: 5514683Abstract: The compounds of the formula I ##STR1## and their pharmaceutical acceptable salts, which are defined herein, are ligands for cholecystokinin and/or gastrin receptors.Type: GrantFiled: August 9, 1994Date of Patent: May 7, 1996Assignee: James Black Foundation LimitedInventors: Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley, Ildiko M. Buck, Katherine I. M. Steel, Jonathan M. R. Davies, David J. Dunstone, Elaine A. Harper, Michael J. Pether, Michael J. Bodkin, Matthew J. Tozer, Martin L. Hudson
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Patent number: 5484935Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.3 are each C.sub.1-4 alkyl or C.sub.1-4 alkyl-carbonyl, and R.sup.2 is carboxy, tetrazolyl, C.sub.1-4 alkyl-sulphonamido or --CR.sup.4 R.sup.5 CO.sub.2 H where R.sup.4 and R.sup.5 are each hydrogen or C.sub.1-4 alkyl; provided that when R.sup.1 and R.sup.3 are both methyl and when R.sup.1 and R.sup.3 are both methylcarbonyl, R.sup.2 is not carboxy; and salts and esters thereof.Type: GrantFiled: August 11, 1994Date of Patent: January 16, 1996Assignee: Lilly Industries LimitedInventors: Peter T. Gallagher, Terence A. Hicks, William M. Owton
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Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
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Patent number: 5462954Abstract: Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and synthesis are disclosed. Also, pharmaceutical formulations are disclosed for use in applications treating diseases or conditions characterized by excessive release of leukotriene B.sub.4, one of the metabolites of arachidonic acid.The primary LTB.sub.Type: GrantFiled: November 1, 1994Date of Patent: October 31, 1995Assignee: Eli Lilly and CompanyInventors: S. Richard Baker, Robert D. Dillard, Paul E. Floreancig, J. Scott Sawyer, Michael J. Sofia
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Patent number: 5405870Abstract: Compounds of formula (Ic): ##STR1## having valuable platelet-aggregation inhibitory activities useful for the prophylaxis and treatment of such diseases as thrombosis and pharmaceutical compositions containing said compounds.Type: GrantFiled: November 4, 1993Date of Patent: April 11, 1995Assignee: Sankyo Company, LimitedInventors: Kazuo Koyama, Shigeo Amemiya, Koichi Kojima, Shinsaku Kobayashi
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Patent number: 5403953Abstract: Compound of formula (I): ##STR1## in which: R.sub.1 represents halogen, or hydroxy, alkyl, alkoxy, cyano, amino, mercapto, alkylthio or phenoxy,R.sub.2 and R'.sub.2 represent two hydrogen when the ring is unsaturated, or alternatively identical or different, represent hydrogen or halogen, or hydroxy, alkyl, alkoxy, cyano, amino or oxo when the ring is saturated,R.sub.3 represents any one of the following groups: ##STR2## in which: m represents 1, 2 or 3,X represents oxygen or sulfur or N-R, R.sub.5 or R.sub.6, which are identical or different, represent hydrogen or alkyl or trifluoromethyl or form (C.sub.3 -C.sub.6) cycloalkyl,n represents 0, 1 or 2,R.sub.7 represents hydroxy, alkoxy, amino, or --O--CH.sub.2 --CO--NRR',R.sub.4 represents hydrogen or halogen or alkyl, alkoxy or trihaloalkyl.Type: GrantFiled: November 23, 1993Date of Patent: April 4, 1995Assignee: Adir et CompagnieInventors: Guillaume de Nanteuil, Michel Vincent, Christine Lila, Jacqueline Bonnet, Armel Fradin
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Patent number: 5395918Abstract: The invention describes new biphenyl dianhydrides, and new polyimides and copolyimides made from the dianhydrides. The synthesized polyimides exhibit significantly enhanced solubility when the biphenyl dianhydrides are substituted, particularly at the 2 and 2' positions on the phenyl rings.Type: GrantFiled: April 21, 1994Date of Patent: March 7, 1995Assignee: The University of AkronInventors: Frank W. Harris, Sheng-Hsien Lin
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Patent number: 5374654Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 is a hydrogen atom, their salts with physiologically compatible bases, their cyclodextrin clathrates, and their use as medicinal agents.Type: GrantFiled: April 21, 1993Date of Patent: December 20, 1994Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Ulrich Klar, Bob Nieuweboer, Claus-Steffen Sturzebecher
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Patent number: 5344959Abstract: Compounds of the formula ##STR1## wherein m is 1-4; R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R.sub.5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I, lower alkoxy or lower thioalkoxy of 1-6 carbons; R.sub.6 is hydrogen, lower alkyl, Cl, Br, I, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 OR NR.sub.11 --COR.sub.11 ; R.sub.20 is independently hydrogen or lower alkyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.Type: GrantFiled: May 18, 1993Date of Patent: September 6, 1994Assignee: Allergan, Inc.Inventor: Roshantha A. Chandraratna
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Patent number: 5344970Abstract: A ruthenium-phosphite complex having the formula ##STR1## wherein a is from 1 to 3; b is 1 or 2; c is from 0 to 3; and R is hydrogen, alkyl, aryl, halo, amino, acetylamino, or sulfo; and X is ##STR2## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl.This complex can be used to effect the reduction of unsaturated organic compounds or, when comprised of ligands having optical activity, can be used as the catalyst for effecting the asymmetric reduction of unsaturated organic compounds.Type: GrantFiled: December 22, 1993Date of Patent: September 6, 1994Assignee: Albemarle CorporationInventor: Charles H. Kolich
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Patent number: 5340931Abstract: Allene compounds have the formula:(CH.sub.2 .dbd.C.dbd.CH--O).sub.n --R--(A).sub.m (I)in which R is a substituted or unsubstituted mono- or polyvalent benzene, naphthalene, anthracene, azobenzene, bisphenol or polyphenyl (containing 2 to 10 benzene rings connected in line) nucleus, or a group--Ph--R.sup.1 --Ph-- (II)(in which each group Ph is a phenylene, halophenylene, alkylphenylene, cyanophenylene or alkoxyphenylene group, and the chain R.sup.1 linking the two group Ph is a C.sub.1 -C.sub.6 aliphatic hydrocarbon or an alicyclic hydrocarbon group, the chain optionally being interrupted by one or more oxygen atoms); A is a carboxyl or sulphonyl group or a group --CH.dbd.C.dbd.CH.sub.2 ; n is an integer of from 1 to 10; m is 0, 1, 2 or 3; and the sum of m and n is equal to the valence of the group R.They may be prepared by isomerization of corresponding propargyloxy compounds.Type: GrantFiled: March 15, 1989Date of Patent: August 23, 1994Assignee: Nippon Paint Co., Ltd.Inventors: Mitsuo Yamada, Hiromichi Kayano, Kei Aoki, Keizou Ishii