Acyclic Carbon Bonded Directly To The -c(=x)- (e.g., N-oleoylpyrrolidine, Etc.) Patents (Class 548/540)
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Patent number: 6756378Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are pharmaceutical compositions, methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion, which involve compounds of Formula I.Type: GrantFiled: December 28, 2001Date of Patent: June 29, 2004Assignees: Pharmacopeia Drug Discovery, Inc., Daiichi Pharmaceutical Co., Ltd.Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Shin Iimura, Yoshiyuki Yoneda
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Patent number: 6727275Abstract: The present invention provides pharmaceutical compositions and novel compounds useful in the treatment of conditions mediated by CCR2, MCP-1 or the interaction thereof. The compounds of the present invention are pyrrolidinones and pyrrolidine-thiones.Type: GrantFiled: September 26, 2002Date of Patent: April 27, 2004Assignee: UCB, S.A./N.V.Inventors: Dong Zou, Olivier Dasse, Janelle Evans, Paul Higgins, Jeremy Kintigh, Rama Kondru, Eric Schwartz, Laurent Knerr, Hai-Xiao Zhai
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Patent number: 6723856Abstract: The present invention provides a process for preparing of 2-acetyl-1-pyrroline, the principle aroma component of basmati and other varieties of scented rice, and also of processed cereal and grain products, said flavor chemical is of great value, in the art of application of flavor to foodstuffs like rice and bakery products.Type: GrantFiled: March 28, 2003Date of Patent: April 20, 2004Assignee: Council of Scientific and Industrial ResearchInventors: Pullabhatia Srinivas, Kambadoor Nagarajarao Gurudutt
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Patent number: 6716843Abstract: Compound of formula (I): wherein: represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or phenylalanylprolyl, Ak represents an alkylene or heteroalkylene chain, X represents a single bond or optionally substituted phenylene, R2 represents optionally substituted alkyl, (C3-C10)cycloalkyl, or —NR2aR2b wherein R2a and R2b, which may be the same or different, each represent hydrogen or alkyl or, together with the nitrogen atom carrying them, form a nitrogen-containing heterocycle, Y represents R3 represents hydrogen or a group selected from alkyl, (C3-C7) cycloalkyl and aryl, R4, R5 and R6, which may be the same or different, each represent hydrogen or alkyl, or R4 and R6, or R5 and R6, together with the atoms carrying them, form an imidazolidine or dihydrobenzimidazole ring, its optical isomers and addition salts thereof with a pharmaceuticallyType: GrantFiled: March 28, 2002Date of Patent: April 6, 2004Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Bernard Portevin, Alain Benoist, Nigel Levens, Olivier Nosjean, Bernadette Husson-Robert
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Patent number: 6710040Abstract: The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for treating diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, hyperglycemia, impaired glucose tolerance, metabolic syndrome (Syndrome X or insulin resistance syndrome), glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inType: GrantFiled: June 3, 2003Date of Patent: March 23, 2004Assignee: Pfizer Inc.Inventors: Bernard Hulin, Janice C. Parker
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Patent number: 6706742Abstract: Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single bond or phenylene, R1 and R2, which may be identical or different, each represent hydrogen or alkyl, R3 represents alkyl, nitro or cyano, Y represents NR4 or CHNO2, R4 represents hydrogen or alkyl, its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, with the exclusion of compounds wherein, simultaneously, represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents —(CH2)3—, X represents a single bond, Y represents NH and R3 represents nitro. Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.Type: GrantFiled: May 15, 2002Date of Patent: March 16, 2004Assignee: Les Laboratories ServierInventors: Guillaume De Nanteuil, Bernard Portevin, Alain Benoist, Nigel Levens, Olivier Nosjean, Bernadette Husson-Robert, Michelle Boulanger
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Patent number: 6699990Abstract: The present patent application relates to 3-(2,5-diaminophenyl)acrylamide derivatives of general formula (I) or to physiologically tolerated, water-soluble-salts thereof and to agents containing said compounds and used for oxidative dyeing of fibers.Type: GrantFiled: October 21, 2002Date of Patent: March 2, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6660741Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: where R1 is an optionally substituted or halogenated alkyl, aryl, heteroalkyl or heteroaryl amine, said R1 further comprising a cyclic or bicyclic structure; R2 is methyl, CH2CH3, (CH2)2CH3, C(CH3)3, phenyl, 3,4-dichiorophenyl, biphenyl, benzyl, 4-hydroxybenzyl, piperidine, N-Boc-4-piperidine, CH2-(N-Boc-4-piperidine), 4-tetrahydropyran, CH2-4-tetrahydropyran, 3-methyl indolyl, 2-naphthyl, 3-pyridyl, 4-pyridyl, 3-thienyl; R3 is R2 or C3-8alkyl, R4 is C1-3alkyl; and R5 is NH2, OH, NHOH, NHOCH3, N(CH3)OH, N(CH3)OCH3, NHCH2CH3, NH(CH2CH3), NHCH2(2,4-(OCH3)2Ph, NHCH2(4-NO2)Ph, NHN(CH3)2, proline, or 2-hydroxymethyl pyrrolidine.Type: GrantFiled: March 19, 2002Date of Patent: December 9, 2003Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: William G. Bornmann, Francis Sirotnak, Howard Scher, Ephraim Vidal, Christopher Borella, David Scheinberg
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Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
Patent number: 6645995Abstract: Described are compounds of formula I wherein at least one of the bonds in the five-membered ring is a double bond; B is any alpha or beta amino acid connected to the ring with an amide or peptide bond; or a salt thereof with a pharmaceutically acceptable acid or base. Pharmaceutical compositions containing these compounds are also described. These compounds are useful for treating type II diabetes.Type: GrantFiled: February 8, 2002Date of Patent: November 11, 2003Assignee: Novo Nordisk A/SInventors: Anders Kanstrup, Jane Marie Lundbeck, Lise Brown Christiansen -
Patent number: 6642391Abstract: A compound named Amycomycin of the formula: is described, as well as its pharmaceutically acceptable salts and derivatives, in all their stereoisomeric and tautomeric forms. The compound is obtained by growing the microorganism Amycolatopsis species ST101170 (DSM 12216) and is useful as a pharmaceutical, particularly as an antibiotic.Type: GrantFiled: December 7, 2000Date of Patent: November 4, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Cordula Hopmann, Michael Kurz, Heinrich Decker, Dominique Le Beller, Jozsef Aszodi
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Patent number: 6630504Abstract: The invention provides compounds of general formula (I) wherein R1 is H or C1-C6 alkyl; R2 and R3, together with the interconnecting atoms form a 4 to 8-membered saturated ring containing one or two heteroatoms (including the nitrogen to which R2 is attached) wherein a second heteroatom, if present, is selected from oxygen, nitrogen and sulfur, with the proviso that said ring cannot contain two adjacent heteroatoms; Z is CF3, OCF3, C1-C6alkylthio or C1-C6alkoxy; Y is hydrogen, halogen, —ORa, Ra or C1-C6alkylthio, and wherein Ra is C1-C4 alkyl optionally substituted with fluorine atoms; or when Z and Y are attached para and meta to the ether linkage linking rings A and B, Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected froType: GrantFiled: August 24, 2001Date of Patent: October 7, 2003Assignee: Pfizer Inc.Inventors: Mark David Andrews, David Hepworth, Donald Stuart Middleton, Alan Stobie
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Patent number: 6627769Abstract: Novel molecules without intramolecular peptidic bonds, able to mimic the RGD peptide, containing ARG-GLY-ASP motif “arginine-glycine-aspartic acid” (that is a potent inhibitor, in vivo and in vitro, of cellular adhesion) In vitro experimentation demonstrated that said molecules are efficient inhibitors of RASMC adhesion, proliferation and migration.Type: GrantFiled: February 20, 2002Date of Patent: September 30, 2003Assignee: Provincia Italiana Della Congregzaione dei Figli Dell'Immacolata Concezione - Istituto Dermopatico Dell'ImmacolataInventors: Antonio Facchiano, Francesco Facchiano, Ivan Rossi, Rita Casadio
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Patent number: 6610729Abstract: The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition containing the derivative or a salt thereof, and to pharmaceutical use thereof. The hydroxamic acid derivative and a pharmacologically acceptable salt thereof of the present invention have an inhibitory activity of TNF &agr; production, and are useful for, for example, the prophylaxis and treatment of the diseases such as autoimmune diseases and inflammatory diseases (e.g., sepsis, MOF, rheumatoid arthritis, Crohn's disease, cachexia, myasthenia gravis, systemic lupus erythematosus, asthma, I type diabetes, psoriasis and the like), and the like.Type: GrantFiled: November 22, 2000Date of Patent: August 26, 2003Assignee: Mitsubishi Pharma CorporationInventors: Tomokazu Gotou, Shinji Takeda, Kazuhiro Maeda, Tomohiro Yoshida, Naoki Sugiyama, Tadahiro Takemoto
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Patent number: 6593312Abstract: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.Type: GrantFiled: June 18, 2002Date of Patent: July 15, 2003Assignee: Les Laboratoires ServierInventors: Michel Wierzbicki, Jean-Marie Fourquez, Nigel Levens, Bernadette Husson-Robert, Olivier Nosjean, Michelle Boulanger
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Patent number: 6573385Abstract: The present invention provides intermediates of formula IIb and IIc useful for the preparation of Simvastatin: wherein R1 and R2 are each independently an alkyl, heteroalkyl, aryl or heteroaryl moiety, or R1 and R2, taken together, form a heterocyclic moiety containing 5-8 atoms; wherein each of the foregoing alkyl and heteroalkyl moieties may be linear or branched, substituted or unsubstituted, cyclic or acyclic or saturated or unsaturated, and each of the foregoing heterocyclic, aryl and heteroaryl moieties may be substituted or unsubstituted.Type: GrantFiled: July 12, 2002Date of Patent: June 3, 2003Assignee: Biocon India LimitedInventors: Ganesh Sambasivam, Madhavan Sridharan, Poornaprajna Acharya, Joy Mathew
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Patent number: 6566553Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.Type: GrantFiled: August 10, 2001Date of Patent: May 20, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: François Soucy, Louis Plamondon, Mark Behnke, William Roush
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Patent number: 6531511Abstract: The use of a compound of formula (1), as disclosed in the specification, wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl and aryl, or pharmaceutically acceptable salts thereof, with the proviso that wherein R1 to R4 and R6 are hydrogen, R5 is not selected from CH2CH2NHSO2CH3, CH2CH2NHSO2CF3 and methyl substituted by SO2NH2, SO3H, PO3H2, CONHOH or a heterocyclic group selected from formulae (a), (b), (c), (d) and (e) in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission.Type: GrantFiled: October 16, 2001Date of Patent: March 11, 2003Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Nathaniel Julius Thomas Monck, Andrew James Bird, Simon Edward Ward
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Patent number: 6521760Abstract: A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: a) reaction of S(−)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L-proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a potassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of a zofenopril potassium salt aqueous solution to a CaCl2 aqueous solution at a temperature of 70-90° C. with simultaneous seeding to promote the precipitation of polymorph A.Type: GrantFiled: June 4, 2001Date of Patent: February 18, 2003Assignee: Menarini Richerche S.p.A.Inventors: Raffaello Giorgi, Antonio Giachetti, Carlo Mannucci, Anita Falezza
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Publication number: 20020198255Abstract: This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: ApplicationFiled: December 19, 2001Publication date: December 26, 2002Inventors: Denis John Kertesz, Michael Garret Roepel
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Patent number: 6498273Abstract: The present invention provides basic ionic contrast agents that have anticoagulant activity. The contrast media incorporate a lysine or arginine group or derivative, and have a free amino or guanidino group. Methods of using the contrast media are also disclosed.Type: GrantFiled: May 25, 2001Date of Patent: December 24, 2002Assignee: The University of North CarolinaInventors: Don A. Gabriel, Laura J. Melton
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Patent number: 6458787Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: May 2, 2001Date of Patent: October 1, 2002Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlacter
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6433185Abstract: The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in claim 1. These compounds are pharmacologically active.Type: GrantFiled: September 6, 2001Date of Patent: August 13, 2002Assignee: Sanofi-SynthelaboInventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
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Patent number: 6432969Abstract: The present invention relates to certain N-(substituted glycyl)-2-cyanopyrrolidines of formula I wherein Y is as defined herein, in free form or in acid addition salt form. Compounds of formula I inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.Type: GrantFiled: June 12, 2001Date of Patent: August 13, 2002Assignee: Novartis AGInventor: Edwin Bernard Villhauer
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Patent number: 6399628Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 12, 1999Date of Patent: June 4, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Jon K. Reel, Eugene D. Thorsett, Celia A. Whitesitt
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Patent number: 6395737Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.Type: GrantFiled: December 28, 1999Date of Patent: May 28, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Hans Matter, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose
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Patent number: 6388122Abstract: A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the formula (II), guanidinophenol derivatives of the formula (III), amidinophenol derivatives of the formula (IV), and novel guanidinophenol derivatives of the formula (V) (in the formulae, Gu is guanidino).Type: GrantFiled: October 7, 1998Date of Patent: May 14, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiroshi Kido, Hisao Nakai
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Publication number: 20020052510Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.Type: ApplicationFiled: December 3, 1998Publication date: May 2, 2002Inventors: GREGORY S. HAMILTON, MARK H. NORMAN, YONG-QIAN WU
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Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV
Patent number: 6380398Abstract: Described are compounds of formula I wherein at least one of the bonds in the five-membered ring is a double bond; B is any alpha or beta amino acid connected to the ring with an amide or peptide bond; or a salt thereof with a pharmaceutically acceptable acid or base. Pharmaceutical compositions containing these compounds are also described. These compounds are useful for treating type II diabetes.Type: GrantFiled: January 23, 2001Date of Patent: April 30, 2002Assignee: Novo Nordisk A/SInventors: Anders Kanstrup, Jane Marie Lundbeck, Lise Brown Christiansen -
Patent number: 6380254Abstract: The present invention provides a method and composition for treating or preventing pathogenic effects in a mammal caused by intracellular calcium overload, comprising administering to a mammal a mixture of sodium co-transport dependent amino carboxylic acids or their physiologically acceptable salts in an amount sufficient to substantially saturate sodium-dependent amino carboxylic acid transport mechanisms of a cell's plasma membranes. Administration of these amino carboxylic acids can advantageously treat or prevent cell lysis and irreversible cell damage caused by intracellular calcium overload, especially in mammals suffering from a disease condition associated with or resulting from insufficient tissue oxygenation.Type: GrantFiled: March 12, 2001Date of Patent: April 30, 2002Assignee: Leigh Biotechnology, Inc.Inventors: Robert D. Pearlstein, Richard S. Kramer
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Patent number: 6362174Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.Type: GrantFiled: August 9, 2001Date of Patent: March 26, 2002Assignee: Warner-Lambert CompanyInventors: Michael Francis Rafferty, Yuntao Song
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Patent number: 6348628Abstract: Novel hydrazones of formula [2] having the following structural formula are provided, which are useful intermediates to form active ingredients of herbicides, wherein R3 is hydrogen, alkyl, haloalkyl, or alkoxy alkyl; and Q is [Q-1], [Q-2], [Q-3], [Q-4] or [Q-5] as defined herein.Type: GrantFiled: March 7, 2000Date of Patent: February 19, 2002Assignee: Sumitomo Chemical Company, LimitedInventors: Tadashi Katayama, Shinichi Kawamura, Yuzuru Sanemitsu, Yoko Mine
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Patent number: 6331537Abstract: This invention relates to novel N-heteorocyclic carboxylic acids and carboxylic acid isosteres, their preparation and use for treating neurological disorders including physically damaged nerves and neurodengenerative diseases, for treating alopecia and promoting hair growth, for treating vision disorders and/or improving vision, and for treating memory impairment and/or enhancing memory performance by administering such compounds.Type: GrantFiled: December 2, 1999Date of Patent: December 18, 2001Assignee: GPI Nil Holdings, Inc.Inventors: Gregory S. Hamilton, Mark H. Norman, Yong-Qian Wu
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Patent number: 6316440Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.Type: GrantFiled: December 27, 1999Date of Patent: November 13, 2001Assignee: Warner-Lambert CompanyInventors: Michael Francis Rafferty, Yuntao Song
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Patent number: 6313120Abstract: The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in Claim 1. These compounds are pharmacologically active.Type: GrantFiled: June 13, 2000Date of Patent: November 6, 2001Assignee: Sanofi-SynthelaboInventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
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Patent number: 6306891Abstract: Nitrogen-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: June 1, 1999Date of Patent: October 23, 2001Assignees: Merck & Co., Inc., Tularik Inc.Inventors: Harold G. Selnick, Melissa Egbertson, Daria Jean Hazuda, James P. Guare, Jr., John S. Wai, Steven D. Young, David L. Clark, Julio C. Medina
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang -
Publication number: 20010018450Abstract: A compound named Amycomycin of the formula: 1Type: ApplicationFiled: December 7, 2000Publication date: August 30, 2001Inventors: Cordula Hopmann, Michael Kurz, Heinrich Decker, Dominique Le Beller, Jozsef Aszodi
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Patent number: 6274741Abstract: The present invention relates to a process for the preparation of the acyl heteroaromatic compounds useful as important intermediates for drugs, pharmaceuticals and flavouring agents, said process comprising reacting an heteroaromatic compound selected from furan, thiophene and pyrrole with a C2-C5 acid anhydride as an acylating agent employing metal ion exchanged clays as catalysts at temperatures in the range of 0-130° C. for a period of 1-24 h, and separating the acyl heteroaromatic compound by a conventional method to obtain a product of high purity.Type: GrantFiled: March 29, 2000Date of Patent: August 14, 2001Assignee: Council of Scientific and Industrial ResearchInventors: Boyapati Manoranjan Choudary, Mutyala Sateesh, Mannepalli Lakshmi Kantam, Kondapuram Vijaya Raghaven
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Patent number: 6265610Abstract: The present invention provides basic ionic contrast agents that have anticoagulant activity. The contrast media incorporate a lysine or arginine group or derivative, and have a free amino or guanidino group. Methods of using the contrast media are also disclosed.Type: GrantFiled: January 11, 2000Date of Patent: July 24, 2001Assignee: The University of North Carolina at Chapel HillInventors: Don A. Gabriel, Laura J. Melton
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Patent number: 6265614Abstract: Intermediates having the formula wherein BI is —CH2OH or —CH2ORP, and RP is an alcohol protecting group; a is 1, 2, or 3; TI is —OH or QI is phenyl, naphthyl ohr heteroaryl having 1-3 substituents; Ra and Rc are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl cycloalkyl, aryl, or —OH; or Ra and Rc together with the C—N—C chain to which they are bound, form a 5-7 membered ring; Rb and Rd are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl, cycloalkyl, aryl, or —OH; and D is a directing group capable of directing lithiation alpha to a nitrogen atom of a nitrogen compound having D as a substituent bound to the nitrogen atom when the nitrogen compound is reacted with s-butyl lithium, are disclosedType: GrantFiled: October 13, 2000Date of Patent: July 24, 2001Assignee: Schering CorporationInventors: Anantha R. Sudhakar, Suhan Tang
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Patent number: 6258833Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: December 23, 1999Date of Patent: July 10, 2001Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlacter
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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: 6222043Abstract: The present invention provides synthetic methodology to produce novel dipeptide compounds and pharmaceutically acceptable salts thereof which exhibit excellent HIV protease inhibitory activity and excellent bioavailability from digestive tracts. Methods of using the dipeptide compounds and pharmaceutically acceptable salts thereof also are provided.Type: GrantFiled: January 8, 1999Date of Patent: April 24, 2001Assignee: Japan Energy CorporationInventors: Ryohei Kato, Tsutomu Mimoto, Tominaga Fukazawa, Naoko Morohashi, Yoshiaki Kiso
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Patent number: 6218424Abstract: This invention relates to neurotrophic, low molecular weight, small molecule heterocyclic ketone and thioester compounds, compositions containing the same, and the use of such compounds for treating neurological disorders, including physically damaged nerves and neurodegenerative diseases.Type: GrantFiled: November 22, 1999Date of Patent: April 17, 2001Assignee: GPI NIL Holdings, Inc.Inventors: Gregory S. Hamilton, Jia-He Li
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Patent number: 6207672Abstract: Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.Type: GrantFiled: March 9, 1999Date of Patent: March 27, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Eckart Bartnik, Klaus-Ulrich Weithmann
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Patent number: 6197770Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: March 1, 2000Date of Patent: March 6, 2001Assignee: The Procter & Gamble Co.Inventors: Michael George Natchus, Roger Gunnard Bookland, Neil Gregory Almstead, Stanislaw Pikul, Biswanath De, Menyan Cheng
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Patent number: 6153609Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: February 16, 1999Date of Patent: November 28, 2000Assignee: Pfizer IncInventors: Ralph P. Robinson, Todd A. Blumenkopf
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Patent number: 6133266Abstract: The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: ##STR1## (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia and are useful as an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and stone removal in urolithiasis.Type: GrantFiled: February 10, 1999Date of Patent: October 17, 2000Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Makio Kitazawa, Kosuke Okazaki, Tetsuro Tamai, Masaru Saito, Nobuyuki Tanaka, Hiroaki Kobayashi, Ken Kikuchi, Hideyuki Muranaka
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Patent number: 6117897Abstract: A 1/2 sulfate of a [(S)-1-[(S)-2-[(trans-4-aminocyclohexylmethyl) carbamoyl]pyrrolidine-1-carbonyl]-2-isopropylthio-2-methylpropyl]carbamic acid propyl ester represented by the following formula (I): a hydrate or solvate thereof.Type: GrantFiled: November 18, 1998Date of Patent: September 12, 2000Assignee: Mitsubishi Chemical CorporationInventors: Norimichi Iwase, Naoto Inakoshi, Koichi Sugawara, Jun Anabuki