Ortho Fused Patents (Class 560/28)
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Patent number: 6924082Abstract: The present application describes a method for information storage and data processing comprising the steps of thermo inducing or photo inducing double-bond shifts (DBS) in substituted (4n)-annulenes thus generating transitions between two different conjugation states with at least one substituent. The two different conjugation states are the conjugation on-state and conjugation off-state of the annulene core ?-electrons with the substituent ?-electrons. The present invention is furthermore related to novel substituted (4n)-heptalenes being optically and/or thermally switchable, based on thermal or photochemical double-bond shifts (DBS) as well as methods for their preparation. The (4n)-heptalenes can be used for information storage and data processing devices.Type: GrantFiled: December 10, 1996Date of Patent: August 2, 2005Assignee: Ciba Specialty Chemicals CorporationInventor: Hans-Jürgen Hansen
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Publication number: 20040236119Abstract: The present invention relates to a process wherein a cyclic carbonate compound bearing an electrophilic group is reacted with a compound containing a nucleophilic group, especially an amine group. Such reactions permit to obtain urethane groups useful in polymer preparation, such as polyurethanes, or other urethane-containing polymers.Type: ApplicationFiled: April 12, 2004Publication date: November 25, 2004Inventor: Jurgen Van Holen
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Publication number: 20040167211Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.Type: ApplicationFiled: October 17, 2003Publication date: August 26, 2004Inventors: Xiiaoli Chen, Keith T. Demarest, Jung Lee, Jay M. Matthews, Philip Rybczynski
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Publication number: 20040138262Abstract: The present invention provides compounds of the formula 1Type: ApplicationFiled: July 8, 2003Publication date: July 15, 2004Applicant: Pfizer Inc.Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
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Patent number: 6737547Abstract: The present invention provides novel aminoindenes having the structure: wherein n is 1 or 2, R1 is hydrogen, linear or branched chain C1-C8 alkyl or linear or branched chain C1-C8 alkoxy and R2 is hydrogen or a halogen. Such compounds may be used to treat neurodegenerative conditions such as Alzheimer's disease, head trauma, stroke, hypoxia, anoxia, epilepsy, convulsions, seizures.Type: GrantFiled: September 15, 1999Date of Patent: May 18, 2004Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Benjamin Sklarz, Sasson Cohen, Tzipora Speiser, Rachel Nachman
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Publication number: 20040063698Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: July 31, 2003Publication date: April 1, 2004Inventor: Thomas P. Maduskuie
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Patent number: 6700025Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: GrantFiled: January 5, 2001Date of Patent: March 2, 2004Assignee: United Therapeutics CorporationInventors: Robert M. Moriarty, Hitesh Batra
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Patent number: 6462222Abstract: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is 0 or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R1 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome. Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: August 31, 2001Date of Patent: October 8, 2002Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Teva Pharmaceutical Industries, Ltd., Technion Research and Development Foundation, Ltd.Inventors: Michael Chorev, Tamar Goren, Yacov Herzig, Jeffrey Sterling, Marta Weinstock-Rosin, Moussa B. H. Youdim
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Patent number: 6455725Abstract: The invention relates to substituted cinnamic acids and cinnamic acid esters of formula (I), wherein X represents F, Cl or J and R1 and R2 are the same or different and represent hydrogen, an optionally substituted C1-C10-alkyl radical or an optionally substituted benzyl radical. Substituted indanone carboxylic acid esters are produced using said substituted cinnamic acid and cinnamic acid ester in a technically simple and non-dangerous manner as far as safety is concerned.Type: GrantFiled: February 13, 2001Date of Patent: September 24, 2002Assignee: Bayer AktiengesellschaftInventors: Walter Lange, Joachim Komoschinski, Guido Steffan, Ernst Kysela
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Patent number: 6437169Abstract: 1. A 1-naphthol compound represented by formula (I) below: wherein A represents the moiety of a compound having an acidic proton the pKa of a corresponding protonated form (AH) of which is 0 to 14, R1 represents an aliphatic group, aryl group, or heterocyclic group, R2 represents a substituent, n represents an integer of 0 to 5, X represents a hydrogen atom, halogen atom, R11—, R11O—, R11S—, R11OCOO—, R12COO—, R12(R13)NCOO—, R12CON(R13)—, —NO, —NO2, or —N═N—R11, wherein R11 represents an aliphatic group, aryl group, or heterocyclic group, and each of R12 and R13 independently represents a hydrogen atom, aliphatic group, aryl group, or heterocyclic group, and Y represents an oxygen atom or sulfur atom.Type: GrantFiled: June 19, 2000Date of Patent: August 20, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Takayuki Ito, Koji Takaku
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Patent number: 6410749Abstract: Process for preparing optically active &bgr;-amino alcohols represented by a general formula (2): Ra—C*H(OH)—C*H(Rb)—Rc wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, Rb is one member selected from among groups represented by the following general formulae; (3) R1CO(R2)N—, and (4) R1CO(R1′CO)N—, and C* is an asymmetric carbon atom, characterized by reacting a racemic &agr;-aminocarbonyl compound represented by the general formula (1): Ra—CO—CH(Rb)—Rc, with hydrogen in the presence of an optically active transition metal compound represented by a general formula (7): MaXY(Px)m(Nx)n wherein Ma represents a metal atom belonging to VIII-group of the periodic law, X and Y represent each independently hydrogen, halogeno, Px represents a phosphine ligand, Nx represents an amine ligand, at least one of Px and Nx is optically active, and m and n each independently represent 0 or an integer of 1 thType: GrantFiled: July 17, 2001Date of Patent: June 25, 2002Assignee: Nippon Soda Co., Ltd.Inventors: Eiji Katayama, Daisuke Sato, Hirohito Ooka, Tsutomu Inoue
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6319930Abstract: The invention relates to compounds of formula (I): A—G1—Cy—G2—Cy—G3—B (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure and G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: March 24, 2000Date of Patent: November 20, 2001Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
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Patent number: 6310074Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: May 18, 2000Date of Patent: October 30, 2001Assignee: Adir et CompagnieInventors: Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois
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Patent number: 6242609Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.Type: GrantFiled: April 7, 1999Date of Patent: June 5, 2001Assignee: Konica CorporationInventor: Fumio Ishii
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Patent number: 6232489Abstract: A method for making arthropodicidal oxadiazines and intermediates which are racemic or enantiomerically enriched at their chiral center, the method for making the oxadiazines comprising reaction of an intermediate selected from as well as certain selected intermediates including those depicted above, and methods of making them.Type: GrantFiled: May 9, 2000Date of Patent: May 15, 2001Assignee: E. I. du Pont de Nemours and CompanyInventors: Gary David Annis, Stephen Frederick McCann, Rafael Shapiro
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Patent number: 6127414Abstract: There is provided pharmaceutically useful compounds of formula I, ##STR1## wherein Ar.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.Type: GrantFiled: October 26, 1998Date of Patent: October 3, 2000Assignee: Astra AktiebolagInventors: Nils-.ANG.ke Bergman, Thomas D'Ambra, Garry M Pilling
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Patent number: 6080856Abstract: A method for making arthropodicidal oxadiazines and intermediates which are racemic or enantiomerically enriched at their chiral center, the method for making the oxadiazines comprising reaction of an intermediate selected from ##STR1## wherein: R.sup.1 is F, Cl, or C.sub.1 -C.sub.3 fluoroalkoxy,R.sup.2 is C.sub.1 -C.sub.3 alkyl, andR.sup.4 is H or CO.sub.2 CH.sub.2 (C.sub.6 H.sub.5).as well as certain selected intermediates including those depicted above, and methods of making them.Type: GrantFiled: October 21, 1999Date of Patent: June 27, 2000Assignee: E. I. du Pont Nemours and CompanyInventors: Gary David Annis, Stephen Frederick McCann, Rafael Shapiro
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Patent number: 6028112Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.Type: GrantFiled: July 31, 1998Date of Patent: February 22, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Karen L. Leboulluec, Katherine S. Takaki
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Patent number: 6018071Abstract: A method for making arthropodicidal oxadiazines and intermediates which are racemic or enantiomerically enriched at their chiral center, the method for making the oxadiazines comprising reaction of an intermediate selected from ##STR1## wherein: R.sup.1 is F, Cl, or C.sub.1 -C.sub.3 fluoroalkoxy,R.sup.2 is C.sub.1 -C.sub.3 alkyl, andR.sup.4 is H or CO.sub.2 CH.sub.2 (C.sub.6 H.sub.5).as well as certain selected intermediates including those depicted above, and methods of making them.Type: GrantFiled: October 2, 1998Date of Patent: January 25, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Gary David Annis, Stephen Frederick McCann, Rafael Shapiro
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Patent number: 6011045Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: January 4, 2000Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5977170Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sub.4 and R.sub.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thenyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.Type: GrantFiled: June 11, 1998Date of Patent: November 2, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Susan Christman
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Patent number: 5968975Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.Type: GrantFiled: June 11, 1998Date of Patent: October 19, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Susan Christman
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Patent number: 5922771Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.Type: GrantFiled: August 19, 1996Date of Patent: July 13, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 5922899Abstract: Carbamoylcarboxamides of the general formula I ##STR1## (R.sup.1 =unsubstituted or substituted alkyl, alkenyl, alkynyl; R.sup.2 =hydrogen, halogen, cyano, nitro, or unsubstituted or substituted alkyl, alkoxy, alkylthio, or an unsubstituted or substituted phenyl group which is bonded via oxygen or sulfur) and compositions comprising them, processes for their preparation, and the use of the compounds I and of the compositions.Type: GrantFiled: February 17, 1998Date of Patent: July 13, 1999Assignee: BASF AktiengesellschaftInventors: Frank Wetterich, Oliver Wagner, Karl Eicken, Klaus Ditrich, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5874580Abstract: Compounds of formulaA(B).sub.x, (I),wherein x is an integer from 1 to 4, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2,3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m und n, are as defined in claim 1.These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.Type: GrantFiled: June 2, 1998Date of Patent: February 23, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Zhimin Hao, John S. Zambounis, Abul Iqbal
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Patent number: 5872296Abstract: A process for preparing enantiomerically pure cis-1-amino-2-hydroxyindane, which comprisesa) converting racemic trans-1-aminoindan-2-ol with acids or acid derivatives of the general formula RCOX by conventional methods into amides of type A ##STR1## b) adding seed crystals of one enantiomer to a super-saturated solution or melt of the racemic amide A,c) isolating the crystals which have separated out, and again supersaturating the remaining mother liquor or melt after dissolving racemic amide A, and adding seed crystals of the other enantiomer, leading to selective crystallization of the latter,d) converting the resulting enantiomerically pure trans amide by conventional methods into the enantiomerically pure cis-1-amino-2-hydroxyindane.Type: GrantFiled: October 28, 1997Date of Patent: February 16, 1999Assignee: BASF AktiengesellschaftInventors: Christoph Nubling, Wolfgang Ladner
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Patent number: 5869657Abstract: A method for making arthropodicidal oxadiazines and intermediates which are racemic or enantiomerically enriched at their chiral center, the method for making the oxadiazines comprising reaction of an intermediate selected from ##STR1## wherein: R.sup.1 is F, Cl, or C.sub.1 -C.sub.3 fluroalkoxy,R.sup.2 is C.sub.1 -C.sub.3 alkyl, andR.sup.4 is H or CO.sub.2 CH.sub.2 (C.sub.6 H.sub.5).as well as certain selected intermediates including those depicted above, and methods of making them.Type: GrantFiled: October 16, 1996Date of Patent: February 9, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Gary David Annis, Stephen Frederick McCann, Rafael Shapiro
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Patent number: 5852199Abstract: The present invention provides a novel carbamazepine hydrazide compound suitable for covalent attachment to a polymer particle reagent, having the general formula ##STR1## The present invention provides a novel carbamazepine acid compound suitable for attachment to proteins for the production of carbamazepine immunogens. The carbamazepine antigen of the present invention has the following general structure: ##STR2## where X is C.dbd.O, CH.sub.2 or SO.sub.2 ; Y is C.dbd.O, CH.sub.2, SO.sub.2 ; R is an alkyl and P is a protein or a hapten.Type: GrantFiled: July 25, 1997Date of Patent: December 22, 1998Assignee: Dade Behring Inc.Inventor: Chengrong Wang
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Patent number: 5849945Abstract: The present invention pertains to a process for the preparation of Compound (4) through the below-described reaction route: ##STR1## wherein R.sup.1 and R.sup.2 each represents H, halogen, OH or C.sub.1-6 alkyl group; X and Y each represents a protected amino group and n stands for 0 to 4. According to the above process, an aminotetralone derivative which is an intermediate useful for an industrial preparation of a camptothecin derivative can be obtained in a convenient manner and in a high yield.Type: GrantFiled: August 21, 1997Date of Patent: December 15, 1998Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushikikaisha Yakult HonshaInventors: Shinji Kamihara, Kazuaki Kanai, Shigeru Noguchi
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Patent number: 5847194Abstract: Carbamoylcarboxamides of the general formula I ##STR1## and their salts (R.sup.1 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or an unsubstituted or substituted nonaromatic carbo- or heterocycle;R.sup.2 is H or unhalogenated or halogenated alkyl or cycloalkyl;R.sup.3 is unsubstituted or substituted alkyl, cycloalkyl or phenylalkyl;R.sup.4 is H or one of the radicals R.sup.3 orR.sup.3 and R.sup.4, together with the C atom to which they are bonded, are an unsubstituted or substituted carbo- or heterocycle;R.sup.5 independently of these is one of the radicals R.sup.2 ;X independently of one another is hydrogen, unsubstituted or substituted alkyl and/or alkenyl;Y independently of one another and of these is one of the radicals X;p,q independently of one another are 0, 1 or 2;R.sup.Type: GrantFiled: March 3, 1997Date of Patent: December 8, 1998Assignee: BASF AktiengesellschaftInventors: Frank Wetterich, Oliver Wagner, Karl Eicken, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5843910Abstract: The present invention relates to novel colchicine derivatives of formula (1), where Y is a --CH.sub.2 --CH--NH--R.sub.3 group or a --CH--CH.sub.2 OR.sub.3 group and the other variables are as defined in claim 1, having antiproliferative, antitumoral and anti-inflammatory activities. The novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine, but, in comparison with the latter, they are less toxic and more selective, particularly on cells resistant to the usual medicaments. Some compounds have a marked activity on TNF and interleukine 2, and therefore are very potent anti-inflammatory agents. They can be included in pharmaceutical formulations useful for the parenteral, oral and topical administrations.Type: GrantFiled: March 21, 1997Date of Patent: December 1, 1998Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Bruno Gabetta
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Patent number: 5837807Abstract: This invention is directed to tetrahydronaphthalene compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, bromine, cyano, formyl, hydroxy, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, aryloxy, lower aralkoxy or aryl; R.sup.2 is an amino acid residue or a chain of 2 to 20 amino acid residues wherein reactive moieties in the side chains of the amino acid residue(s) is/are protected or unprotected, and wherein the amino group of the N-terminal amino acid is a free or protected amino group; A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each are .alpha.-amino acid residues wherein A.sup.1 and A.sup.2 are in the L configuration and A.sup.3 and A.sup.4 are in the D configuration when the .alpha.-C atom of said .alpha.-amino acid residue is asymmetric; X is oxygen or sulphur; Y is a residue of the formula ##STR2## n is 0 or 1; R.sup.3 is hydrogen or lower alkyl; R.sup.Type: GrantFiled: February 27, 1996Date of Patent: November 17, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Christine Abrecht, Alfred Grieder, Klaus Muller, Daniel Obrecht
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Patent number: 5783697Abstract: Vinyl carbamate compounds are prepared by reacting appropriate secondary amines with carbon dioxide and acetylenically unsaturated compounds in the presence of a compound of a metal from the platinum group, in particular a ruthenium compound, with either one of the two process steps (a) and (b) or, preferably, both being carried out:(a) the acetylene compound is reinjected during the reaction;(b) the reaction is carried out in the presence of a tertiary amine.Type: GrantFiled: January 21, 1997Date of Patent: July 21, 1998Assignee: BASF AktiengesellschaftInventors: Marc Heider, Jochem Henkelmann, Michael Karcher, Thomas Ruhl
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Patent number: 5773469Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.Type: GrantFiled: June 18, 1996Date of Patent: June 30, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
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Patent number: 5739160Abstract: New Cyclopentane- or cyclopentene-beta-aminoacid derivatives and their isomers, acid additional salts and metal salt complexes have strong antimicrobial and broad-spectrum antimycotic acitivity. As antimycotics they are especially active against dermatophyte, and biphasic fungi. The new compounds are also low toxicity antibacterial agents, effective against Gram positive bacteria, including antibiotic-resistant strains. The new Cyclopentane- or cyclopentene-beta-aminoacid derivatives are useful in human or veterinary medicine for combating dermatomycosis or systemic mycosis or local or systemic bacterial infections. In addition, the new compounds can also be used as preservatives, especially for water, foods, or organic materials such as polymers, lubricants, paints, fibers, leather, paper or wood.Type: GrantFiled: September 19, 1994Date of Patent: April 14, 1998Assignee: Bayer AktiengesellschaftInventors: Joachim Mittendorf, Franz Kunisch, Michael Matzke, Hans-Christian Militzer, Rainer Endermann, Karl Georg Metzger, Klaus-Dieter Bremm, Manfred Plempel
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Patent number: 5698731Abstract: A process is described for the preparation of aromatic carbamates in which an organic carbonate in a stoichiometric quantity or in a quantity higher than the stoichiometric value is reacted with an aromatic amine operating in the presence of a carbamation catalyst, wherein this catalyst is selected from N,N-substituted carbamate complexes of zinc or copper.The process gives high yields and selectivity in the useful reaction product.Type: GrantFiled: June 27, 1996Date of Patent: December 16, 1997Assignee: Ministero dell `Universita` e della Ricerca Scientifica e TecnologicaInventors: Aldo Bosetti, Pietro Cesti, Fausto Calderazzo
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Patent number: 5688817Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: November 18, 1997Assignee: Centre Int'l. De Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5676923Abstract: Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.Type: GrantFiled: June 7, 1995Date of Patent: October 14, 1997Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Ulrich Niedballa, Peter Mareski, Bernd Raduchel, Hanns-Joachim Weinmann, Andreas Muhler, Bernd Misselwitz
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Patent number: 5670505Abstract: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.Type: GrantFiled: November 28, 1994Date of Patent: September 23, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Takashi Manabe, Nobukiyo Konishi, Shinji Shigenaga, Kenji Murano, Hiroshi Matsuda, Hiroshi Miyake
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Patent number: 5637770Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.Type: GrantFiled: May 31, 1995Date of Patent: June 10, 1997Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Hirofumi Terasawa, Akio Ejima, Satoru Ohsuki, Kouichi Uoto
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Patent number: 5624957Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein X is F, Cl, OH or CH.sub.3, Y is H or F, R.sub.1 -R.sub.6 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, n is an integer of 1 to 4 and R.sub.7 is hydrogen or a carboxyl-protecting group, and pharmaceutically acceptable salts thereof. The compounds of formula I selectively interact with the retinoic acid subtype RAR.gamma. and have been found to lack the liver toxicity associated with systemic administration of non-selective retinoids.Type: GrantFiled: June 6, 1995Date of Patent: April 29, 1997Assignee: Bristol-Myers Squibb CompanyInventors: R. Thomas Swann, Daniel Smith, Kenneth M. Tramposch, Fred C. Zusi
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Patent number: 5608102Abstract: This invention relates to a method for preparing .beta.-phenylisoserine and analogues thereof having general formula (I) ##STR1## from an aromatic aldehyde and an .alpha.-methylarylamine-S, and through a lactam of general formula (II) as described herein. The acids of general formula (I) (R.dbd.H) may be used to prepare taxane derivatives having remarkable antitumoral and antileukaemic activity.Type: GrantFiled: September 26, 1994Date of Patent: March 4, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Alain Commer.cedilla.on
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Patent number: 5602275Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: February 11, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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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: 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: 5510505Abstract: Provided is a compound of the formula: ##STR1## This compound is an intermediate to and is used for preparing the arthropodicidal oxidiazine Compound II described in the specification.Type: GrantFiled: April 6, 1995Date of Patent: April 23, 1996Assignee: E. I. Du Pont de Nemours and CompanyInventor: Gary D. Annis
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Patent number: 5502061Abstract: The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: September 26, 1994Date of Patent: March 26, 1996Assignee: Eli Lilly and CompanyInventors: Kwan Y. Hui, Charles D. Jones, Louis N. Jungheim, Pamela A. Pennington
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Patent number: 5492917Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 29, 1993Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
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Patent number: 5481020Abstract: Compounds of Formula 1 bind opioid receptors: which binds to the opioid receptor: ##STR1##Type: GrantFiled: December 30, 1994Date of Patent: January 2, 1996Assignee: Chiron CorporationInventors: Simon Ng, Robert L. Warne, Ronald N. Zuckermann, Eric J. Martin, Reyna J. Simon