Quinolinyl Or Isoquinolinyl (including Hydrogenated) Patents (Class 514/82)
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Publication number: 20040204347Abstract: This invention is directed to pharmaceutical compositions and methods for treating demyelinating disorders based upon inhibitors of the interaction of glutamate with the AMPA and of the interaction of glutamate with the kainate receptor complex.Type: ApplicationFiled: December 22, 2000Publication date: October 14, 2004Inventors: Lechoslaw Turski, Terence Smith
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Patent number: 6713462Abstract: The invention relates to compounds of the general formula (and pharmaceutically acceptable derivatives thereof): in which RA, RB, RC, RD, R5, R7, R9, R9a, AK, p, q, r and X are as defined herein, and to their preparation and use.Type: GrantFiled: June 21, 2002Date of Patent: March 30, 2004Assignee: Ariad Pharmaceuticals, Inc.Inventors: Chester A. Metcalf, III, William C. Shakespeare, Tomi K. Sawyer, Yihan Wang, Regine Bohacek, Rajeswari Sundaramoorthi
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Patent number: 6706699Abstract: This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use.Type: GrantFiled: June 21, 2002Date of Patent: March 16, 2004Assignee: Ariad Pharmaceuticals, Inc.Inventors: Yihan Wang, Chester A. Metcalf, III, William C. Shakespeare, Tomi K. Sawyer, Regine Bohacek, Rajeswari Sundaramoorthi
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Publication number: 20030220298Abstract: The present invention relates to the syntheses and structural elucidation of Combretastatin A1-Phosphate Prodrugs and Combretastatin B1-Phosphate Prodrugs and the utilization of those prodrugs in the treatment of neoplastic diseases. The prodrugs described herein have the structure: Combretastin A-1 Phosphate Prodrug (I) and Combretastin B-1 Phosphate Prodrug (II).Type: ApplicationFiled: October 25, 2002Publication date: November 27, 2003Inventors: George R. Pettit, John W. Lippert
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Patent number: 6649605Abstract: NMDA receptor antagonists, especially mirtazapine, can be used to treat tension-type headaches.Type: GrantFiled: August 30, 2001Date of Patent: November 18, 2003Assignee: Head Explorer A/SInventors: Jes Olesen, Lars Bendtsen, Rigmor Jensen, Ulf Madsen
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Patent number: 6630135Abstract: An improved method of sterilizing the field of surgery prior to an ophthalmic surgical procedure is described. The invention eliminates the need for painful and potentially traumatic injections of antibiotics by utilizing sustained release compositions which allow the antibiotics contained therein to penetrate deeply into the eye, thereby ensuring a sterile field of surgery during intraocular surgical procedures. The compositions may also be utilized to prevent post-surgical infections.Type: GrantFiled: November 12, 1999Date of Patent: October 7, 2003Assignee: Alcon Laboratories, Inc.Inventors: Gerald D. Cagle, Tai-Lee Ke, Barry A. Schlech, Ole J. Lorenzetti
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Patent number: 6596709Abstract: The invention relates to a compound of formula (I): wherein: X represents chlorine or fluorine or CF3, R represents hydrogen or a group and methods for using the same.Type: GrantFiled: December 9, 2002Date of Patent: July 22, 2003Assignee: Les Laboratoires ServierInventors: Alex Cordi, Patrice Desos, Pierre Lestage
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Publication number: 20030105065Abstract: This invention relates to compounds of the general formula: 1Type: ApplicationFiled: June 21, 2002Publication date: June 5, 2003Inventors: Yihan Wang, Chester A. Metcalf, William C. Shakespeare, Tomi K. Sawyer, Regine Bohacek
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Publication number: 20030064997Abstract: Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.Type: ApplicationFiled: March 27, 2001Publication date: April 3, 2003Applicant: SmithKline Beecham CorporationInventors: Jerry Leroy Adams, Timothy Francis Gallagher, John C. Lee, John Richard White
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Patent number: 6498151Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.Type: GrantFiled: March 21, 2001Date of Patent: December 24, 2002Assignee: Merck Frosst Canada & Co.Inventors: Chun Sing Li, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Cheuk Kun Lau, Patrick Roy, Michel Therien, Zhaoyin Wang, Claude Dufresne, Rejean Fortin
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Patent number: 6486143Abstract: The invention relates to a compound of formula (I): wherein: R1 represents halogen or a group CF3, R2 represents hydrogen or alkyl or cycloalkyl, R3 is as defined in the description, R4 and R5 represent hydrogen or alkyl, cycloalkyl, aryl or arylalkyl a group Medicaments.Type: GrantFiled: February 15, 2001Date of Patent: November 26, 2002Assignee: Les Laboratoires ServierInventors: Alex Cordi, Patrice Desos, Pierre Lestage
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Patent number: 6468990Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.Type: GrantFiled: May 2, 2000Date of Patent: October 22, 2002Assignee: Queen's University at KingstonInventors: Gregory M. Ross, Igor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
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Patent number: 6465444Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.Type: GrantFiled: March 21, 2001Date of Patent: October 15, 2002Assignees: Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd.Inventors: Christopher Bayly, Mitsuru Ohkubo
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Publication number: 20020107207Abstract: The present invention provides an antiproliferative compound having a structural formula 1Type: ApplicationFiled: November 5, 2001Publication date: August 8, 2002Inventors: Bob G. Sanders, Kimberly Kline, Weiping Yu
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Patent number: 6417177Abstract: This invention provides compositions and methods for increasing cellular respiration of melanized catecholamine neurons, and methods for alleviating symptoms or stopping appearance and/or progression of symptoms of Parkinson's Disease, and methods for preventing symptoms of on-off syndrome associated with treatment with dopamine or a dopamine agonist of a patient suffering symptoms of a disease selected from the group consisting of idiopathic and atypical Parkinson's disease, conditions characterized by nigrostriatal degeneration and multiple system atrophy, said methods comprising administering to said patient an effective amount of a neuromelanin-binding composition having a quinoline ring in a suitable pharmaceutical carrier. Preferably the composition comprises (−)-chloroquine.Type: GrantFiled: July 13, 2000Date of Patent: July 9, 2002Assignee: Alpha Research Group, LLCInventor: Jodi Nelson
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Patent number: 6410592Abstract: The present invention relates to aminomethylcarboxylic acid derivatives general formula (I), wherein Z is (CH2)n, O, S, SO, SO2 or N—R5; n is 0, 1 or 2; X represents 1-3 substituents independently selected from hydrogen, halogen, (C1-6)alkyloxy, (C3-6)cycloalkyloxy, (C6-12)aryloxy, (C6-12)aryl, thienyl, SR6, SOR6, SO2R6, NR6R6, NHR6, NH2, NHCOR6, NSO2R6, CN, COOR6 and (C1-4)alkyl, optionally substituted with halogen, (C6-12)aryl, (C1-6)alkyloxy or (C6-12)aryloxy; or 2 substituents at adjacent positions together represent a fused (C5-6)aryl group, a fused (C5-6)cycloalkyl ring or O—(CH2)m—O; m is 1 or 2; Y represents 1-3 substituents independently selected from hydrogen, halogen, (C1-4)alkyloxy, SR6, NR6R6 and (C1-4)alkyl, optionally substituted with halogen; R1 is COOR7 or CONR8R9; R2 and R6 are (C1-4)alkyl; R3, R4 and R5 are independently hydrogen or (C1-4)alkyl; R7, R8 and R9 are independently hydrogen, (C1-4)alkyl, (C6-12)aryl or arylalkyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 25, 2001Date of Patent: June 25, 2002Assignee: Akzo Nobel N.V.Inventors: S. G. Gibson, D. R. Jaap, S. N. Thorn, R. R. Gilfillan
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Patent number: 6395749Abstract: The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.Type: GrantFiled: September 1, 1998Date of Patent: May 28, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Patent number: 6337324Abstract: The invention relates to pharmaceutical compositions for topical administration comprising a topically acceptable antiviral substance and an antiinflammatory glucocorticoid in a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the prophylactic and curative treatment of herpesvirus infections in mammals including man. The invention also relates to the use of a combination of a topically acceptable antiviral substance and an antiinflammatory glucocorticoid for the manufacture of a medicament for said prophylactic and curative treatment.Type: GrantFiled: March 8, 1996Date of Patent: January 8, 2002Assignee: Medivir, ABInventors: Johan Georg Harmenberg, Ann Harriet Margareta Kristofferson
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Patent number: 6322821Abstract: A composition for preventing and treating milk fever in freshening cows, and a method of administering the composition. The basic composition is a mixture of water, calcium chloride, propylene glycol, B vitamins and minerals. The calcium content is lower than conventional calcium treatments used for this purpose. The propylene glycol gives the cow an energy boost and sweetens the taste so the cow does not object to it as it does to conventional gels and liquids. The B vitamins stimulate the cow's appetite. The minerals replace minerals lost in the milk and also help the cow absorb calcium. The composition of the present invention is in a liquid form and is preferably administered using a 200-300 cc drench gun. The end of the dispensing tube of the drench gun is placed between the teeth and cheek of the cow near the receptors that stimulate the esophageal groove reflex.Type: GrantFiled: September 27, 1999Date of Patent: November 27, 2001Inventor: Jack W. Register
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Publication number: 20010031746Abstract: The invention relates to a compound of formula (I): 1Type: ApplicationFiled: February 15, 2001Publication date: October 18, 2001Inventors: Alex Cordi, Patrice Desos, Pierre Lestage
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Patent number: 6228393Abstract: The present invention is directed to a vehicle for effecting drug delivery from a solid substrate. Hydrogels loaded with liposomal therapeutic agents such as antibiotics are covalently bonded to the surface of substrates such as in-dwelling medical devices, such as implants, catheters, and the like. The present invention is particularly useful in the treatment and prevention of biofilm mediated infection often associated with the use of in-dwelling medical devices.Type: GrantFiled: October 5, 1999Date of Patent: May 8, 2001Assignee: Uroteq, Inc.Inventors: Frank DiCosmo, Valerio DiTizio
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Patent number: 6200961Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.Type: GrantFiled: December 16, 1998Date of Patent: March 13, 2001Assignee: Aquatrols Corporation of America, Inc.Inventors: Stanley J. Kostka, Rennan Pan
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Patent number: 6130231Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: November 26, 1997Date of Patent: October 10, 2000Assignee: DuPont PharmaceuticalsInventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6117885Abstract: Compounds of the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, A, B, D and E are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.Type: GrantFiled: February 24, 1994Date of Patent: September 12, 2000Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis Evan Ryono, John Lloyd
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Patent number: 6071895Abstract: The present invention discloses the compounds of general formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effective in treating conditions characterized by unwanted activity of these enzymes, such as acquired immume deficiency syndrome.Type: GrantFiled: February 22, 1999Date of Patent: June 6, 2000Assignee: Narhex LimitedInventor: Damian Wojciech Grobelny
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Patent number: 6040299Abstract: There is disclosed a cold storage stabilized organophosphorus insecticide formulation. The formulation comprises a solid carrier and between approximately 2% and 40% by weight of the ultimate formulation of a nominally solid organophosphorus insecticide and between approximately 0.5% and 10% by weight of the ultimate formulation of a stabilizer compound selected from cyclohexanone and N-methylpyrrolidone. A method of making the cold storage stabilized organophosphorus insecticide formulation is also disclosed.Type: GrantFiled: October 23, 1998Date of Patent: March 21, 2000Assignee: Griffin LLCInventor: Hamid Ullah
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Patent number: 6010711Abstract: A class of active agents, and articles and compositions containing them and methods for treating human patients with them, which inhibit bone resorption of all types. This class of active agents comprises phosphodiester inhibiting compositions which inhibit any of interleukin 1 (IL1), interleukin 6 (IL6) and tumor necrosis factor alpha (TNF), which are cytokines that mediate bone resorption. Exemplary compositions in this class include: pentoxifylline; isobutylmethyl xanthine; ciprofloxacin; rolipram; terferol; and the quinolones generally. Each of these IL1/IL6/TNF inhibitors may be administered alone or in combination by a variety of delivery routes and dosage forms, and they may optionally be administered in conjunction with additional active agents including but not limited to metal chelators.Type: GrantFiled: January 26, 1996Date of Patent: January 4, 2000Assignee: University of RochesterInventors: Regis James O'Keefe, Randy Nathan Rosier
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Patent number: 5990150Abstract: Heterocyclic derivatives of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.Type: GrantFiled: March 19, 1997Date of Patent: November 23, 1999Assignee: Sankyo Company, Ltd.Inventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura, Katsuo Wada
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Patent number: 5985259Abstract: An improved method of sterilizing the field of surgery prior to an ophthalmic surgical procedure is described. The invention eliminates the need for painfull and potentially traumatic injections of antibiotics by utilizing sustained release compositions which allow the antibiotics contained therein to penetrate deeply into the eye, thereby ensuring a sterile field of surgery during intraocular surgical procedures. The compositions may also be utilized to prevent post-surgical infections.Type: GrantFiled: April 30, 1997Date of Patent: November 16, 1999Assignee: Alcon Laboratories, Inc.Inventors: Gerald D. Cagle, Tai-Lee Ke, Barry A. Schlech, Ole J. Lorenzetti
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Patent number: 5958905Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.Type: GrantFiled: March 26, 1996Date of Patent: September 28, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Erik Joel Verner
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Patent number: 5958464Abstract: A composition for preventing and treating milk fever in freshening cows, and a method of administering the composition. The basic composition is a mixture of water, calcium chloride, propylene glycol, B vitamins and minerals. The calcium content is lower than conventional calcium treatments used for this purpose. The propylene glycol gives the cow an energy boost and sweetens the taste so the cow does not object to it as it does to conventional gels and liquids. The B vitamins stimulate the cow's appetite. The minerals replace minerals lost in the milk and also help the cow absorb calcium. The composition of the present invention is in a liquid form and is preferably administered using a 200-300 cc drench gun. The end of the dispensing tube of the drench gun is placed between the teeth and cheek of the cow near the receptors that stimulate the esophageal groove reflex.Type: GrantFiled: November 12, 1997Date of Patent: September 28, 1999Inventor: Jack W. Register
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Patent number: 5900410Abstract: The present invention is directed to compositions, methods and kits for treating areas of H. pylori infection in the GI tract. The active ingredient is an antibiotic-bisphosphonate adduct wherein the antibiotic is selected for its ability to eradicate H. pylori. Other components include a salt of a divalent cation that is insolubilized in vivo at alkaline pH, and optionally a substrate from which the enzyme urease liberates NH.sub.3.Type: GrantFiled: August 12, 1997Date of Patent: May 4, 1999Inventor: John F. Hartmann
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Patent number: 5888992Abstract: The invention relates to retroviral protease inhibitors of the general formula (I): W--(A).sub.n --B--(A*).sub.m --V where W, A, B, A*, V, n and m are as defined herein, including related prodrugs of general formula (I) comprising a solubilizing group which is labile in vivo.Type: GrantFiled: April 29, 1996Date of Patent: March 30, 1999Assignee: Narhex LimitedInventor: Damian Wojciech Grobelny
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Patent number: 5880111Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
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Patent number: 5750701Abstract: A compound of the formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, X represents a moiety of formula (a), in which A.sup.1 represents --CH.dbd.CH.dbd., NH, S or O; A.sup.2 represents an oxo or a thioxo group; A.sup.3 represents H or an alkylcarbonyl group; and A.sup.4 represents hydroxy or NR.sup.s R.sup.t wherein R.sup.s and R.sup.t each independently represents H or alkyl; R.sup.0 and R.sup.1 each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b), wherein R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl or R.sup.4 together with R.sup.5 represents (CH.sub.2).sub.n wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.Type: GrantFiled: September 16, 1996Date of Patent: May 12, 1998Assignee: SmithKline Beecham plcInventors: Lee James Beeley, David Kenneth Dean
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Patent number: 5741784Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; ....... represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## ,or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: August 30, 1996Date of Patent: April 21, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5691322Abstract: Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have a quinoline or a pyridine anchor attached by means of a linker to a binding domain sidechain, which compounds inhibit the enzyme 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: E.R. Squibb & Sons, Inc.Inventor: Jeffrey Adam Robl
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Patent number: 5646132Abstract: Compound of formula (I): ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, represent hydrogen or halogen or alkyl, nitro, cyano or aminosulfonyl, or alternatively, when two of them are located on adjacent carbons, form, with the carbon atoms to which they are attached, (C.sub.3 -C.sub.7) cycloalkyl ring or substituted or unsubstituted benzene ring,R.sub.4 represents hydrogen, linear or branched (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl or a group ##STR2## in which R.sub.6 and R.sub.7, which are identical or different, represent hydrogen or substituted or unsubstituted, linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.5 represents hydrogen, hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy, phenoxy, mercapto, linear or branched (C.sub.1 -C.sub.6) alkylthio, substituted or unsubstituted, linear or branched (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl or substituted or unsubstituted amino, or a group ##STR3## in which R.sub.6 and R.sub.Type: GrantFiled: July 10, 1995Date of Patent: July 8, 1997Assignee: Adir et CompagnieInventors: Alex Cordi, Patrice Desos, Jean Lepagnol
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Patent number: 5631004Abstract: An improved method of sterilizing the field of surgery prior to an ophthalmic surgical procedure is described. The invention eliminates the need for painful and potentially traumatic injections of antibiotics by utilizing sustained release compositions which allow the antibiotics contained therein to penetrate deeply into the eye, thereby ensuring a sterile field of surgery during intraocular surgical procedures. The compositions may also be utilized to prevent post-surgical infections.Type: GrantFiled: September 30, 1993Date of Patent: May 20, 1997Assignee: Alcon Laboratories, Inc.Inventors: Gerald D. Cagle, Tai-Lee Ke, Barry A. Schlech, Ole J. Lorenzetti
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Patent number: 5614509Abstract: The use of NMDA receptor antagonists or their physiologically compatible salts for preventing the development of tolerance during the long-term treatment with benzodiazepine-receptor-binding active ingredients as well as the combination of new pharmaceutical agents with benzodiazepine-receptor-binding active ingredients is described.Type: GrantFiled: March 2, 1995Date of Patent: March 25, 1997Assignee: Schering AktiengesellschaftInventors: Lechoslaw Turski, Karin G. Steppuhn, Herbert Schneider, David N. Stephens
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Patent number: 5583123Abstract: The present invention relates to the phosphono-alkylamino-substituted tetrazole derivatives of formula I ##STR1## and tautomers thereof wherein R.sub.1 is (carbocyclic or heterocyclic) aryl-C.sub.1 -C.sub.4 -alkyl; X is phenylene, phenylene substituted by lower alkoxy, lower-alkyl, halogen or trifluoromethyl or X.sub.1 is ethynylene; R.sub.2 is carbocyclic or heterocyclic aryl; pharmaceutically acceptable mono- or di-ester derivatives thereof in which one or both of the acidic hydroxy groups of the phosphono functional group are esterified in form of a pharmaceutically acceptable mono- or di-ester, and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of endothelin-converting enzyme by administration of said compounds to mammals in need of such treatment.Type: GrantFiled: December 22, 1994Date of Patent: December 10, 1996Assignee: Ciba-Geigy CorporationInventor: St ephane De Lombaert
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Patent number: 5580863Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: May 13, 1994Date of Patent: December 3, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5571506Abstract: This invention relates to aromatic oligomeric compounds useful in the treatment of cardiovascular, bone metabolic, hypolipidaemic, neuronal, gastrointestinal and elastase-mediated connective tissue degradation disorders and disorders which may be treated by agents effective in binding DNA, to processes for preparation of such oligomeric compounds, to pharmaceutical compositions including such oligomeric compounds, and to their use in the treatment of such disorders.Type: GrantFiled: September 10, 1993Date of Patent: November 5, 1996Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Daniel G. McGarry, Michael N. Chang, Jeffrey N. Barton, Jack Newman, Schmuel Ben-Sasson
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Patent number: 5569456Abstract: A rupununine, either in purified form or a derivative in which one or both of the hydroxyl groups is substituted, the rupununine having the formula: ##STR1## where R.dbd.--H or --CH.sub.3.Type: GrantFiled: February 1, 1994Date of Patent: October 29, 1996Inventor: Conrad Gorinsky
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Patent number: 5563128Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.Type: GrantFiled: May 4, 1995Date of Patent: October 8, 1996Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Henry W. Pauls, Yong-Mi Choi, Dilip V. Amin
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Patent number: 5536709Abstract: Compound of formula (I): ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, which are identical or different, represent hydrogen or halogen or alkyl, nitro, cyano or aminosulfonyl, or alternatively, when two of them are located on adjacent carbons, form, with the carbon atoms to which they are attached, (C.sub.3 -C.sub.7) cycloalkyl ring or substituted or unsubstituted benzene ring,R.sub.4 represents hydrogen, linear or branched (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl or a group ##STR2## in which R.sub.6 and R.sub.7, which are identical or different, represent hydrogen or substituted or unsubstituted, linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.5 represents hydrogen, hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy, phenoxy, mercapto, linear or branched (C.sub.1 -C.sub.6) alkylthio, substituted or unsubstituted, linear or branched (C.sub.1 -.sub.6) alkyl, substituted or unsubstituted phenyl or substituted or unsubstituted amino; or a group ##STR3## in which R.sub.6 and R.sub.Type: GrantFiled: August 30, 1994Date of Patent: July 16, 1996Assignee: Adir et CompagnieInventors: Alex Cordi, Patrice Desos, Jean Lepagnol
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Patent number: 5510338Abstract: The present invention pertains to antagonists of excitatory amino acid receptors, their method of preparation as well as compositions pertaining to them, which have the general formula: ##STR1## wherein n is 0, 1, 2, or 3; R1 and R.sub.2 are selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl and C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 14, 1994Date of Patent: April 23, 1996Assignee: Guilford Pharmaceuticals Inc.Inventor: Gregory S. Hamilton
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Patent number: 5500418Abstract: Compounds of formula I ##STR1## wherein R is diethoxymethyl, R.sub.1 is hydrogen, R.sub.2 is pyrid-3-ylmethyl and R.sub.3 is hydrogen, or R is cyclohexylmethyl, R.sub.1 is hydrogen and R.sub.2 is quinolin-4-ylmethyl, or R.sub.1 is hydroxy and R.sub.2 is 3,4-methylenedioxybenzyl, 1-(3,4-methylenedioxyphenyl)ethyl, and R.sub.3 is hydrogen, or R is benzyl, R.sub.1 is hydroxy, R.sub.2 is 1-(3,4-methylenedioxyphenyl)ethyl, and R.sub.3 is hydrogen, and salts thereof have GABA.sub.B -antagonistic properties and can be used for the treatment of diseases responsive to GABA.sub.B -antagonists.Type: GrantFiled: September 16, 1994Date of Patent: March 19, 1996Assignee: Ciba-Geigy CorporationInventor: Stuart J. Mickel
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Patent number: 5476846Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.Type: GrantFiled: November 17, 1994Date of Patent: December 19, 1995Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Claude Lardy, Daniel Guerrier, Gilles Chavernac, Francois Collonges
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Patent number: 5449785Abstract: Compounds of the formula ##STR1## which have antifungal activity.Type: GrantFiled: July 10, 1992Date of Patent: September 12, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Yuhko Aoki, Hiromichi Kotaki, Kazunao Masubuchi, Toru Okuda, Nobuo Shimma, Takuo Tsukuda, Isao Umeda