Nitrogen Attached Indirectly To The Phosphorus By Nonionic Bonding Patents (Class 558/190)
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Publication number: 20040176331Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases.Type: ApplicationFiled: March 1, 2004Publication date: September 9, 2004Inventors: Carl Berthelette, Lianhai Li, Claudio Sturino, Zhaoyin Wang
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Publication number: 20040102418Abstract: This invention relates to compounds of the Formula (I): 1Type: ApplicationFiled: November 19, 2003Publication date: May 27, 2004Inventors: Zhoaning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
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Publication number: 20040077873Abstract: The present invention relates to a process for the preparation of &bgr;-phosphorated nitroxide radicals which consist in preparing, in a first step, an aminophosphonate by reaction of a carbonyl compound, of a primary amine and of a phosphorous compound in the presence of a Lewis acid and then, in a second step, in oxidizing the said crude aminophosphonate using nonhalogenated organic peracids in a water/organic solvent two-phase medium with an aqueous phase buffered at a pH ranging from 5 to 12.Type: ApplicationFiled: November 4, 2003Publication date: April 22, 2004Inventors: Olivier Guerret, Jean-Luc Couturier, Christophe Le Mercier
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Publication number: 20040019232Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: ApplicationFiled: November 6, 2002Publication date: January 29, 2004Inventors: Karl Y. Hostetler, James R. Beadle, Ganesh D. Kini
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Publication number: 20030212289Abstract: A bis(aminostyryl)naphthalene compound represented by the general formula [I] or the like below.Type: ApplicationFiled: March 17, 2003Publication date: November 13, 2003Inventors: Mari Ichimura, Tadashi Ishibashi, Shinichiro Tamura
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Publication number: 20030212067Abstract: Compounds of the formula (I) 1Type: ApplicationFiled: April 16, 2003Publication date: November 13, 2003Inventors: Arlindo Lucas Castelhano, Steven Lee Bender, Judith Gail Deal, Stephen Horne, Teng J. Liak, Zhengyu Yuan
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Publication number: 20030195173Abstract: The invention related to colchinol derivatives of the formula (I): Wherein: R1, R2 and R3 are each independently hydroxy, phosphoryloxy (—OPO3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkyl); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl,aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when bis O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyType: ApplicationFiled: January 7, 2003Publication date: October 16, 2003Inventor: Jean Claude Arnould
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Publication number: 20030186944Abstract: Disclosed are compounds of formula I 1Type: ApplicationFiled: March 21, 2003Publication date: October 2, 2003Inventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck
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Publication number: 20030171338Abstract: Novel amides of polyunsaturated fatty acids with cysteamine-S-phosphate have been synthesized. Combinations of the all-trans-retinoic acid and/or amides of the 13-cis-retinoic acid with O-phospho-L-tyrosine, and N-docosahex-aenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphate, N-arachidonoyl-cysteamine-S-phosphate, N-&agr;-linolenoyl-cysteamine-S-phosphate, and N-&ggr;-linolenoyl-cysteamine-S-phosphate and their analogues N-docosahex-aenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl-O-phospho-2-aminoethanol, N-arachidonoyl-O-phospho-2-aminoethanol, N-&agr;-linolenoyl-O-phospho-2-aminoethanol, N-&ggr;-linolenoyl-O-phospho-2-aminoethanol in different compositions exhibit a marked cell-growth inhibiting effect and display anti-tumour activity.Type: ApplicationFiled: May 6, 2003Publication date: September 11, 2003Inventor: Oleg Strelchenok
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Publication number: 20030158152Abstract: The present invention refers to synthetic protease inhibitors having an axis of symmetry C2 or pseudo-C2 characterised by possessing, in the central portion: (1) preferably, a dihydroxyethylene function, which is isosteric with a peptidic bond; (2) a peptidemimetic bridge between the two nitrogens of the main chain and (3) radicals capable of mimetising amino acids. These new protease inhibitors are a base for the preparation of anti-viral formulations capable of inhibiting HIV virus proliferation.Type: ApplicationFiled: November 15, 2002Publication date: August 21, 2003Inventors: Emerson Poley Pecanha, Luciana J.O. Figueiredo, Vera Bongertz, Octavio Augusto Ceva Antunes, Amilcar Tanuri, Rodrigo de Moraes Brindeiro
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Publication number: 20030149003Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.Type: ApplicationFiled: October 28, 2002Publication date: August 7, 2003Inventors: David J. Chaplin, Charles Manly Garner, Robert Ronald Kane, Kevin G. Pinney, Joseph Anthony Prezioso, Klaus Edvardsen
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Patent number: 6583182Abstract: This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy.Type: GrantFiled: November 30, 2001Date of Patent: June 24, 2003Assignee: Chelator LLCInventors: Harry S Winchell, Joseph Y Klein, Elliot D Simhon, Rosa L Cyjon, Ofer Klein, Haim Zaklad
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Publication number: 20020165412Abstract: N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also useful as radioprotective agents.Type: ApplicationFiled: February 28, 2002Publication date: November 7, 2002Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
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Publication number: 20020137941Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds.Type: ApplicationFiled: May 11, 2001Publication date: September 26, 2002Inventors: William C. Shakespeare, Michael G. Yang, Rajeswari Sundaramoorthi, Regine Bohacek, Charles Joseph Eyermann, Tomi K. Sawyer
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Patent number: 6417176Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: February 7, 2001Date of Patent: July 9, 2002Assignee: Tularik, Inc.Inventor: Jonathan B. Houze
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Publication number: 20020068722Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.Type: ApplicationFiled: February 8, 2001Publication date: June 6, 2002Inventors: Jacques Banville, Serge Plamondon, Yonghua Gai, Neelakantan Balasubramanian
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Publication number: 20020065246Abstract: Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.Type: ApplicationFiled: March 23, 2001Publication date: May 30, 2002Inventors: Jacques Banville, Anne Marinier, Yonghua Gai, Serge Plamondon, Stephan Roy, Neelakantan Balasubramanian
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Publication number: 20020062031Abstract: This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds.Type: ApplicationFiled: November 21, 2001Publication date: May 23, 2002Inventors: William C. Shakespeare, Michael G. Yang, Rajeswari Sundaramoorthi, Regine Bohacek, Charles Joseph Eyermann, Tomi K. Sawyer
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Patent number: 6344558Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: April 20, 2001Date of Patent: February 5, 2002Assignee: Gruenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
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Publication number: 20020013294Abstract: A method for treating hair loss in mammals uses compositions containing 2-decarboxy-2-phosphinico prostaglandin derivatives. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth. Compositions containing 2-decarboxy-2-phosphinico prostaglandin derivatives can also be used to lower intraocular pressure and treat bone disorders.Type: ApplicationFiled: January 31, 2001Publication date: January 31, 2002Inventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
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Publication number: 20020010178Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I 1Type: ApplicationFiled: April 20, 2001Publication date: January 24, 2002Applicant: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
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Publication number: 20010018430Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: ApplicationFiled: February 7, 2001Publication date: August 30, 2001Applicant: Tularik, Inc.Inventor: Jonathan B. Houze
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Patent number: 6248737Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.Type: GrantFiled: June 6, 1995Date of Patent: June 19, 2001Assignee: Gruenenthal GmbHInventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
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Patent number: 6211167Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infrections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: June 14, 2000Date of Patent: April 3, 2001Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6197825Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.Type: GrantFiled: May 28, 1998Date of Patent: March 6, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 5747513Abstract: Compounds of the formula: ##STR1## wherein R is a hydrogen atom or an OY group; R.sub.1 is a hydrogen atom or in OY' group; R.sub.2 is a hydrogen atom or an OY" group; provided that at lent one among R, R.sub.1 and R.sub.2 is hydrogen but R, R.sub.1, and R.sub.2 are not contemporaneously hydrogen atoms and R.sub.1 and R.sub.2 are not contemporaneously OY' or OY" groups respectively; m is an integer 1 or 2; n is an integer 3 to 8; p is an integer 2, 3, or 4; R.sub.3 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl; R.sub.4 is a phenyl optionally substituted by halogen atom or a C.sub.1 -C.sub.3 alkyl or alkoxy group or a 5- or 6- membered heteroaryl containing one or more heteroatoms selected from oxygen, nitrogen and sulphur, optionally substituted by halogen atoms, hydroxy groups, C.sub.1 -C.sub.3 alkyl or alkoxy groups; X is CH.sub.2, NH, S, SO, SO.sub.2, CO, CF.sub.2, O and, when R.sub.4 is a 5- or 6- membered heteroaryl, X can be also a single bond. Pharmaceutically acceptable salts are described.Type: GrantFiled: April 30, 1996Date of Patent: May 5, 1998Assignee: Zambon Group, S.P.A.Inventors: Stefania Montanari, Paolo Cavalleri, Francesco Santangelo
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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: 5716944Abstract: The present invention relates to a compound of the general formula (I): ##STR1## wherein ring A is a benzene ring that may be substituted; Y is a divalent group as a constituent member of ring B forming a 5- to 8-membered ring; Q.sub.1 is a group of the formula --X--P(O)(OR.sup.1)(OR.sup.2) wherein X is a bond or a divalent group; R.sup.1 and R.sup.2, identical or different, are hydrogen or a lower alkyl, or may be combined together to form a ring; Q.sub.2 is hydrogen, a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; and the group of the formula --CON(Q.sub.1)(Q.sub.2) is connected to the a- or b-position carbon atom, or a salt thereof, which is useful as prophylactic and therapeutic agents of various metabolic bone diseases such as osteoporosis.Type: GrantFiled: August 11, 1995Date of Patent: February 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5658897Abstract: The present invention relates to cyclopentane (or cyclopentane) heptanoic or cyclopentane (or cyclopentene) heptenoic acid, 2-hydrocarbyl phosphinyloxyalkyl or phosphonamidoalkyl, 1-esters, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: April 8, 1996Date of Patent: August 19, 1997Assignee: AllerganInventor: Robert M. Burk
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Patent number: 5489717Abstract: Novel naphthyl-substituted .alpha.-amino acid derivatives, pharmaceutical compositions containing the same and a method of using the same, for the blockade of aspartate and glutamate receptors, are described. Novel intermediates of the napthyl-substituted .alpha.-amino acid derivatives are disclosed.Type: GrantFiled: July 8, 1994Date of Patent: February 6, 1996Assignee: Warner-Lambert CompanyInventors: Christopher F. Bigge, James J. Li
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Patent number: 5475129Abstract: The disclosure is concerned with providing phosphonic acid-containing derivatives of phenylalanine and optically active isomers thereof, which are functionalized in a manner which makes them suitable for facile incorporation into peptides using standard solid-phase or solution-phase techniques.Type: GrantFiled: June 8, 1993Date of Patent: December 12, 1995Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Terrence R. Burke, Jr., Mark S. Smyth, Benjamin B. Lim
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Patent number: 5453524Abstract: The present invention provides a phosphorus-containing isoprenoid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is useful as a preventive and therapeutic agent for diseases for which a squalene synthetase inhibiting action is efficacious: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group: R.sup.3 and R.sup.4 each represent a hydrogen atom, a lower alkyl group or an alkali metal; Y represents a group represented by the formula: ##STR2## (wherein R.sup.5 and R.sup.6 each represent a hydrogen atom, a lower alkyl group or an alkali metal or a group represented by the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group or an alkali metal); Z represents a group represented by the Formula: --(CH.Type: GrantFiled: February 22, 1994Date of Patent: September 26, 1995Assignee: Eisai Co., Ltd.Inventors: Katsuya Tagami, Ichirou Yoshida, Naoki Kobayashi, Yoshio Fukuda, Yoshihito Eguchi, Makoto Nakagawa, Hironobu Hiyoshi, Hironori Ikuta, Makoto Kaino, Kenji Hayashi, Issei Ohtsuka, Shinya Abe, Shigeru Souda
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Patent number: 5424303Abstract: The present invention relates to novel aminophosphonate derivatives substituted in .alpha. position by phenol groups, of formula (I): ##STR1## in which: X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, A, B, Z and n are defined in claim 1, as well as their preparations and the pharmaceutical compositions comprising them.Type: GrantFiled: February 26, 1993Date of Patent: June 13, 1995Assignee: Symphar SAInventors: Hieu T. Phan, Lan M. Nguyen, Eric Niesor, Yves Guyon-Gellin, Craig L. Bentzen
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Patent number: 5410056Abstract: The present invention is directed to a novel process for the production of folic acid in high yield utilizing a novel diimine as an intermediate. This diimine is formed by reacting 2-substituted malondialdehyde with p-aminobenzoyl-L-glutamic acid. This diimine may be converted into folic acid by reacting said diimine with triaminopyrimidinone in the presence of sulphite.Type: GrantFiled: January 6, 1994Date of Patent: April 25, 1995Assignee: Hoffman-La Roche Inc.Inventor: Christof Wehrli
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Patent number: 5395827Abstract: The present invention pertains to antagonists of excitatory amino acid neurotransmitter receptor antagonists, their method of preparation as well as compositions containing them which have the general formula: ##STR1## wherein n and m independently are 0, 1, 2, or 3; R.sub.1 is selected from the group consisting of hydrogen and R.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl, C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl, wherein if R.sub.2 is hydrogen, R.sub.1 is not hydrogen; R.sub.3 is selected from the group consisting of hydrogen and C.sub.1 to C.sub.6 lower alkyl; the stereoisomers thereof in their resolved or racemic form, and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 22, 1993Date of Patent: March 7, 1995Assignee: Guilford Pharmaceuticals Inc.Inventors: Waclaw J. Rzeszotarski, Suzanne R. Ellenberger, Maria E. Guzewska, John W. Ferkany, Gregory S. Hamilton, Raymond J. Patch, Edward W. Karbon, Jr
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Patent number: 5298644Abstract: Aryl phosphinites of the formula (I) ##STR1## can be prepared in a simple manner and in high yields by reacting 2,4-di-tert.-butylphenylphosphonous dihalides with alkyl- or arylmagnesium bromides or alkyl- or arylmagnesium chlorides.Aryl phosphinites serve for the preparation of secondary phosphine oxides which are used as starting materials for the preparation of phosphine ligands in catalyst systems.Type: GrantFiled: May 19, 1993Date of Patent: March 29, 1994Assignee: Hoechst AktiengesellschaftInventors: Dieter Regnat, Hans-Jerg Kleiner
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Patent number: 5281640Abstract: Diarylphosphinous acid aryl esters are made by the disclosed process. These compounds are useful for stabilizing plastics, in particular polymerization plastics, and hence can be incorporated into a plastic molding composition.Type: GrantFiled: July 24, 1992Date of Patent: January 25, 1994Assignee: Hoechst AktiengesellschaftInventors: Dieter Regnat, Manfred Bohshar, Hans-Jerg Kleiner, Gerhard Pfahler
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Patent number: 5278152Abstract: The compound of the formula I ##STR1## in which R is an aldehyde group or a group which can be converted into an aldehyde, R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, hydrogen, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium or triethylamnonium, orR.sup.1 and R.sup.2 together form a cyclic diester,R.sup.3 and R.sup.4 are alkyl, alkenyl, alkynyl, cycloalkyl, hydrogen, alkoxy or halogen, R.sup.5 and R.sup.8 are alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, alkoxy, phenyl, cyanide, hydroxyl or hydrogen, and X, Y or Z are oxygen or sulfur, or prodrug forms of the compound of the formula I can be used for the treatment of diseases caused by viruses.The preparation of these compounds and pharmaceutical preparations containing them and their use is described.Type: GrantFiled: February 18, 1993Date of Patent: January 11, 1994Assignee: Hoechst AktiengesellschaftInventors: Anuschirwan Peyman, Eugen Uhlmann, Irvin Winkler, Matthias Helsberg, Christoph Meichsner
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Patent number: 5212163Abstract: Novel compounds of formula (I) and salts, solvates and hydrates thereof, processes for their preparation and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R is hydrogen, C.sub.1-6 alkyl or optionally substituted benzyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2 is C.sub.3-6 alkyl; R.sub.3 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.3 is a group ##STR2## where R.sub.7 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl and R.sub.8 is hydrogen or alkyl; and R.sub.4 is --CH.sub.2 --(CH.sub.2).sub.n OR.sub.5 or --CH.sub.2 --(CH.sub.2).sub.n OCOR.sub.6 or --CH(R.sub.9)COR.sub.10, where n is an integer from 1 to 6; R.sub.5, R.sub.6 and R.sub.9 are hydrogen or C.sub.1-6 alkyl; and R.sub.10 is hydroxy or --O--C.sub.1-6 alkyl or --NR.sub.5 R.sub.6 (where R.sub.5 and R.sub.Type: GrantFiled: September 9, 1991Date of Patent: May 18, 1993Assignee: Beecham Group p.l.c.Inventors: Robert W. Ward, Roger E. Markwell, David J. Hunter
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Patent number: 5210263Abstract: The present invention provides novel inositol phosphate analogs and a method for their use for detecting the phosphatidylinositol cycle-dependent calcium of a cell.Type: GrantFiled: May 15, 1990Date of Patent: May 11, 1993Assignees: University of Pittsburgh, Mayo Foundation For Medical Education and ResearchInventors: Alan P. Kozikowski, Garth Powis
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Patent number: 5200546Abstract: There are disclosed novel compounds of the formula: ##STR1## wherein, x is --CH.sub.2 --, --CHF--, --CF.sub.2, --CHOH-- or --C(O)--;R.sup.6 is hydrogen, benzyl, pentafluorophenyl, nitrophenyl, 1-benzotriazolyl or 1-succinimidoyl;Fmoc is 9-fluorenylmethyloxycarbonyl; and* indicates a chiral carbon atom.The Formula (I) compounds are useful in synthesizing peptides. There are also disclosed novel synthesis methods which include the step of hydrogenating a compound of the Formula ##STR2## wherein R.sup.4 and R.sup.5 are C.sub.1-8 lower alkyl, to give a compound of the formula ##STR3## wherein R.sup.4 and R.sup.5 are as defined above. The compounds of formula (II) are useful as intermediates in preparing certain formula (I) compounds.Type: GrantFiled: September 30, 1991Date of Patent: April 6, 1993Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Terrence R. Burke, Jr., Benjamin B. Lim
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Patent number: 5177240Abstract: A class of phosphono-hydroisoquinoline compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phosphono-hydroisoquinoline compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of Formula I: ##STR1## wherein each of R.sup.1 through R.sup.4 is hydrido, wherein each of Z.sup.1 and Z.sup.2 is hydroxyl, wherein W is a single bond connecting the phosphorus atom with the aromatic ring and wherein the A ring is aromatic. Also disclosed are two classes of intermediate compounds having a fully unsaturated A ring, which intermediate compounds are useful in methods to make product compounds of Formula I.Type: GrantFiled: December 31, 1990Date of Patent: January 5, 1993Assignee: G. D. Searle & Co.Inventors: Alexis A. Cordi, Michael L. Vazquez
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Patent number: 5175153Abstract: The present invention is novel substituted .alpha.-amino acids, pharmaceutical compositions, method of use, and preparations therefore having utility for treating disorders which benefit from blockade of aspartate and glutamate receptors.Type: GrantFiled: October 14, 1988Date of Patent: December 29, 1992Assignee: Warner-Lambert CompanyInventors: Christopher F. Bigge, James T. Drummond, Vlad E. Gregor, Graham Johnson, Michael R. Pavia
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Patent number: 5162311Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.Type: GrantFiled: August 19, 1991Date of Patent: November 10, 1992Assignee: Sandoz Pharmaceuticals Corp.Inventors: Paul L. Herrling, Werner Muller
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Patent number: 5153347Abstract: Novel angiotensin II receptor antagonists of the formula ##STR1## wherein X, X.sub.1, X.sub.2, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein, are disclosed. These compounds are useful, for example, in the treatment of hypertension, congestive heart failure and cardiac hypertrophy.Type: GrantFiled: January 31, 1991Date of Patent: October 6, 1992Assignee: E. R. Squibb & Sons, Inc.Inventor: John E. Lloyd
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Patent number: 5151414Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3, n, m and p have the meanings reported in the specification), their preparation and the compositions for pharmaceutical use containing them as active ingredient are described.The compounds of formula I have dopaminergic vasodilator activity and they may be used in pharmaceutical field.Type: GrantFiled: July 31, 1991Date of Patent: September 29, 1992Assignee: SIMES Societa Italiana Medicinali e Sintetici S.p.A.Inventors: Cesare Casagrande, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
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Patent number: 5130053Abstract: Concentrated solutions of hydrogen peroxide tend to decompose on storage, thereby losing their effectiveness, amongst other reasons by virtue of interaction with contaminating transition metals.Peroxygen compounds are stabilized by contact with a stabilizing amount of compound of general formula: ##STR1## in which X represents a methylene phosphonic acid group of formula --CH.sub.2 --(--PO.sub.3 H.sub.2) or salt thereof, R represents a tetra methylene diradical, optionally alkyl-substituted, that completes a cyclo-aliphatic ring and thereby establishes the two NX.sub.2 groups in a substantially fixed configuration and Y represents a hydrogen or lower alkyl group.Preferably, the solutions contain additionally one or more co-stabilizers, including stannate, phosphates, hydroxybenzoic acid, citric acid and nitrate.The stabilizer system can enable the solution to be diluted, even with municipal water.Type: GrantFiled: July 17, 1990Date of Patent: July 14, 1992Assignee: Interox Chemicals LimitedInventors: Neil D. Feasey, Gareth W. Morris
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Patent number: 5104579Abstract: It has now been discovered that oligomers of C.sub.6 - C.sub.20 alpha-olefins, such as 1-decene, with branch ratios below 0.19 and high viscosity indices (HVI) can be functionalized to provide unique phosphite derivatives. Functionalized polyalpha-olefin lubricants compositions are prepared with superior properties by adding functionalized organophosphites to the olefinic bond of HVI-PAO. The invention encompasses a process for the preparation of lubricant range hydrocarbons containing phosphonate functional groups, comprising;reacting olefinic C.sub.20 + polyalpha-olefin oligomers having a branch ratio of less than 0.19 and phosphite ester in a mixture with peroxide catalyst at elevated temperature whereby phosphite ester adduct of said polyalpha-olefin is formed;separating said reaction mixture products and recovering said adduct.Type: GrantFiled: June 24, 1988Date of Patent: April 14, 1992Assignee: Mobil Oil CorporationInventors: Linda A. Benjamin, Derek A. Law, Andrew G. Horodysky
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Patent number: 5089046Abstract: Cyclic 1-one-2-ene-3-ol compounds substituted in 2-position by an aroyl or heteroaroyl group bearing a hydrocarbylsulfonyloxy or hydrocarbylsulfonylamino substituent exhibiting herbicidal activity.Type: GrantFiled: October 2, 1989Date of Patent: February 18, 1992Assignee: Sandoz Ltd.Inventors: Shy-Fuh Lee, Richard J. Anderson, Gary W. Luehr, G. Wayne Craig, Joel L. Kirkpatrick, Takashi Nishizaka, Kenichi Komatsubara
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Phosphite derived propylene based multifunctional lubricants and multifunctional lubricant additives
Patent number: 5071577Abstract: Novel phosphite derivatives of propylene based lube olefins are novel lubricating fluid media with internal synergistic multifunctional extreme pressure, antiwear and antioxidant properties. These compounds exhibit the same multifunctional characteristics when used in minor additive amounts in either mineral or synthetic lubricating oils as well as fuels.Type: GrantFiled: December 30, 1988Date of Patent: December 10, 1991Assignee: Mobil Oil CorporationInventors: Linda A. Benjamin, Andrew G. Horodysky, Derek A. Law, Nancy M. Page