Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/354)
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Publication number: 20040142878Abstract: This invention relates generally to N-cycloalkylglycines of the Formula (I): 1Type: ApplicationFiled: October 30, 2003Publication date: July 22, 2004Inventor: David J. Carini
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Publication number: 20040132618Abstract: The invention provides compounds of the formula: 1Type: ApplicationFiled: July 3, 2003Publication date: July 8, 2004Inventors: Jerome P. Horwitz, Thomas H. Corbett, Eduardo Palomino, Lisa Polin, Stuart T. Hazeldine
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Publication number: 20040132733Abstract: 2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: ApplicationFiled: July 7, 2003Publication date: July 8, 2004Inventors: Dai-Shi Su, Mark G. Bock
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Patent number: 6759401Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 riType: GrantFiled: October 11, 2002Date of Patent: July 6, 2004Assignee: Biovitrum ABInventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
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Patent number: 6723834Abstract: A reactive dye compound comprising: (a) at least one chromophore moiety; (b) at least one nitrogen-containing heterocycle (c) a linking group to link each chromophore moiety to each nitrogen-containing heterocycle; characterized in that at least one nitrogen-containing heterocycle is substituted with at least one Y group wherein Y is derived from a hydrated aldehyde, a hydrated ketone, a hydrated alpha-hydroxy ketone, or the hydrated form of formic acid and linked via one of its oxygen atoms to the nitrogen-containing heterocycle thereby forming a hemiacetal.Type: GrantFiled: March 27, 2002Date of Patent: April 20, 2004Assignee: North Carolina State UniversityInventors: Peter Jeffrey Broadbent, Dong Wei He, David Malcolm Lewis, Gilles Yves Marie Fernand Ganain, Taher Iqbal Yousaf
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Publication number: 20040067950Abstract: The present invention relates to the method of treating cough with ORL-1 agonists, alone or in combination with additional agents for treating symptoms of cough, allergy or asthma, pharmaceutical compositions comprising the combinations, and to compounds of the formula 1Type: ApplicationFiled: June 17, 2003Publication date: April 8, 2004Applicant: Schering-Plough CorporationInventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 6713613Abstract: A reactive dye compound comprising: (a) at least one chromophore moiety (b) at least one nitrogen-containing heterocycle (c) a linking group to link each chromophore moiety to each nitrogen-containing heterocycle; characterised in that at least one nitrogen-containing heterocycle is substituted with at least one oxy- or thio-carbonyl derivative wherein the oxy- or thio-carbonyl derivative is selected from Y wherein Y is —A(CO)R* wherein A is selected from O or S and wherein R* is an organic residue which comprises at least one nucleophilic group, and salts thereof.Type: GrantFiled: November 8, 2001Date of Patent: March 30, 2004Assignee: North Carolina State UniversityInventors: David Malcolm Lewis, Wei Dong He, Taher Iqbal Yousaf, Gilles Yves Marie Fernand Genain
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Patent number: 6693112Abstract: The present invention provides 2,3-dihydro-1H-pyrrolo[2,3-b]quinolin-4-ylamines, of the formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R7 are as defined herein. Also disclosed are pharmaceutical compositions comprising such compounds, and methods for using the compounds to increase the therapeutic efficacy of drugs.Type: GrantFiled: June 19, 2002Date of Patent: February 17, 2004Assignee: The Pennsylvania State UniversityInventor: Charles D. Smith
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Patent number: 6683101Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof.Type: GrantFiled: December 3, 2002Date of Patent: January 27, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6683184Abstract: The present invention relates to a novel compound of formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity: wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 thioalkoxy; R8 is C1-C4 alkyl; Y is oxygen, sulphur, amino, subsitituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 and X2 are independently CH or nitrogen; and —N═C— and —C═Y— may form a single bond or a double bond provided that if —N═C— forms a single bond, —C═Y&mdType: GrantFiled: March 26, 2002Date of Patent: January 27, 2004Assignee: Samjin Pharmaceutical Co., Ltd.Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Dong-Wook Kang, Jeong-Ho Joo, Young-Hee Lee
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Publication number: 20030236252Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.Type: ApplicationFiled: November 12, 2002Publication date: December 25, 2003Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6667302Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, 0, (C1-C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: June 13, 2001Date of Patent: December 23, 2003Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. La Voie, Jung Sun Kim, Leroy Fong Liu
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Publication number: 20030232810Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.Type: ApplicationFiled: December 3, 2002Publication date: December 18, 2003Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20030220339Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.Type: ApplicationFiled: January 29, 2003Publication date: November 27, 2003Applicant: Tularik Inc.Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Publication number: 20030220196Abstract: The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): 1Type: ApplicationFiled: November 5, 2002Publication date: November 27, 2003Inventors: Reiner Fischer, Jutta Bohmer, Ralf Wischnat, Mark Wilhelm Drewes, Peter Dahmen, Rolf Pontzen, Peter Losel, Christoph Erdelen, Dieter Feucht
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Publication number: 20030215959Abstract: Disclosed is a method of measuring affinity of a test compound for a receptor protein. The method includes the steps of providing a receptor-ligand complex comprising a receptor and a quinoxaline derivative ligand bound thereto; then contacting the receptor-ligand complex with a test compound, thereby yielding a receptor-test compound complex and an amount of free quinoxaline derivative; and then measuring the amount of the free quinoxaline derivative generated as a result of the previous step. In this fashion, the affinity of the test compound for the receptor can be determined.Type: ApplicationFiled: May 14, 2002Publication date: November 20, 2003Inventor: Vasanthi Jayaraman
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Publication number: 20030207887Abstract: This invention comprises the novel compounds of formula (I) 1Type: ApplicationFiled: March 24, 2003Publication date: November 6, 2003Inventors: Patrick Rene Angibaud, Marc Gaston Venet, Laurence Anne Mevellec
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Publication number: 20030203907Abstract: The present invention relates to a compound of the general formula (I): 1Type: ApplicationFiled: January 31, 2003Publication date: October 30, 2003Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
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Publication number: 20030203910Abstract: The present invention provides chemical compounds, pharmaceutical compositions, and methods for increasing the therapeutic efficacy of drugs. Specifically, the invention provides compounds and compositions for inhibiting drug transport proteins that efflux therapeutic agents from cells, and to methods for using these compounds and pharmaceutical compositions to increase the efficacy of the therapeutic agents that are effluxed by these drug transport proteins.Type: ApplicationFiled: March 25, 2003Publication date: October 30, 2003Inventors: Charles D. Smith, David S. Lawrence
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Patent number: 6635641Abstract: Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.Type: GrantFiled: January 19, 2001Date of Patent: October 21, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
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Patent number: 6632813Abstract: The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof as effective ingredients, and processes for the preparation of both. The compounds are 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives represented by the formula (1) where A denotes a single bond or methylene (CH2), Y denotes a nitrogen atom or ═CH—, V denotes a single bond or methylene (CH2), T denotes a hydroxyl group, amino group, lower alkoxycarbonyl group, carboxyl group, aldehyde group or the like, Q denotes a halogen atom, lower alkyl group or lower alkoxy group, and R1 denotes a hydroxyl group, lower alkoxy group or the like, and addition salts thereof.Type: GrantFiled: August 22, 2001Date of Patent: October 14, 2003Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Yasuo Takano, Futoshi Shiga, Tsuyoshi Anraku, Kazunori Fukuchi
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Publication number: 20030162958Abstract: A process for preparing a heteroaromatic compound having a heteroaromatic nucleus substituted with one or more ether groups comprising the step of: condensing at least one hydroxy-group of a compound having said heteroaromatic nucleus, said at least one hydroxy group (—OH) being substituted at &agr;- or &bgr;-positions with respect to a heteroatom of said heteroaromatic nucleus, with an alcohol containing one or more primary or secondary alcohol groups, optionally substituted with nitro, amide, ester, halogen, cyano or (hetero)aromatic groups, using the redox couple of a triaryl- or trialkylphosphine and an azodioxo-compound at a temperature between −40° C. and 160° C.Type: ApplicationFiled: December 20, 2002Publication date: August 28, 2003Applicant: AGFA-GEVAERTInventors: John R. Reynolds, Bert Groenendaal, Kyukwan Zong, Luis Madrigal
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Patent number: 6573264Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: October 23, 2000Date of Patent: June 3, 2003Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Prabha N. Ibrahim, Kevin Shenk, Elfatih Elzein, Venkata Palle
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Publication number: 20030073690Abstract: Novel compounds of the formula 1Type: ApplicationFiled: May 23, 2002Publication date: April 17, 2003Inventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 6537993Abstract: The present invention provides 1H-quinoxalinones, of the formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and n are as defined herein. Also disclosed are pharmaceutical compositions comprising such compounds, and methods for using the compounds to increase the therapeutic efficacy of drugs.Type: GrantFiled: March 30, 2001Date of Patent: March 25, 2003Assignee: Penn State Research FoundationInventors: Charles D. Smith, David S. Lawrence
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Patent number: 6524347Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.Type: GrantFiled: September 29, 2000Date of Patent: February 25, 2003Assignee: Avantis Pharmaceuticals Inc.Inventors: Michael. R. Myers, Alfred P. Spada, Paul E. Persons, Martin P. Maguire
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Patent number: 6525054Abstract: A cyanoiminoquinoxaline derivative of the formula (II) is useful as a preventive or therapeutic agent for diseases due to hyperexcitation of glutamate receptors. (wherein, X and Y each is independently O or NCN, provided that at least one of X and Y is NCN; R1, R2, R3, and R4 each is independently hydrogen, halogen, nitro, optionally substituted heterocyclic group etc.; R5 is hydrogen etc.; R1 and R2, R2 and R3, R3 and R4, and R4 and R5, each taken together with the adjacent atoms may form a carbocycle which may be substituted or may contain a heteroatom(s).Type: GrantFiled: December 1, 2000Date of Patent: February 25, 2003Assignee: Shionogi & Co., Ltd.Inventors: Susumu Takada, Nobuo Chomei, Tsuyoshi Kihara
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Publication number: 20030013714Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.Type: ApplicationFiled: April 2, 2002Publication date: January 16, 2003Applicant: Synaptic Pharmaceutical CorporationInventors: Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
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Patent number: 6492393Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: November 16, 2000Date of Patent: December 10, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Steffen Breitfelder, Pier F. Cirillo, Ming-Hong Hao, Eugene R. Hickey, Rajiv Sharma, Sanxing Sun, Hidenori Takahashi
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Patent number: 6492553Abstract: A method for preparing a N-[(aliphatic or aromatic)carbonyl)]-2-aminoacetamide compound, and for preparing a cyclized compound therefrom, as well as novel resin bound intermediate compounds that are useful for preparing such compounds.Type: GrantFiled: August 4, 1999Date of Patent: December 10, 2002Assignee: Aventis Pharamaceuticals Inc.Inventors: Christopher Hulme, George C. Morton, Joseph M. Salvino, Richard F. Labaudiniere, Helen J. Mason, Matthew M. Morrissette, Liang Ma, Marie-Pierre Cherrier
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Patent number: 6482949Abstract: The present invention provides novel compounds exemplified by pyrrolic nitrogens used as anion and neutral species recognition elements with an aromatic core as a signal group. Described are methods for the synthesis of various pyrrole aryl compounds as well as various applications for these compounds. Methods of use include the binding and detection of specific analytes in a mixture and, in some examples, the separation of the analyte from the mixture. Additional methods of use include the transport of therapeutic agents and the sensing of components, degradants, and impurities in foodstuffs.Type: GrantFiled: May 26, 2000Date of Patent: November 19, 2002Inventors: Jonathan Sessler, Bruno Andrioletti, Andrew Carl Try, Christopher Black
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Patent number: 6455527Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nocicepType: GrantFiled: January 25, 2001Date of Patent: September 24, 2002Assignee: Schering CorporationInventors: Deen Tulshian, Ginny D. Ho, Lisa S. Silverman, Julius J. Matasi, Robbie L. McLeod, John A. Hey, Richard W. Chapman, Ana Bercovici, Francis M. Cuss
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Patent number: 6455698Abstract: A process is disclosed for the preparation of a compound of formula A process is also disclosed for preparing a compound of formulaType: GrantFiled: October 4, 2001Date of Patent: September 24, 2002Assignee: Warner-Lambert CompanyInventors: Brian Edward Kornberg, Sham Shridhar Nikam, Michael Francis Rafferty
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Publication number: 20020115853Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: 1Type: ApplicationFiled: February 12, 2002Publication date: August 22, 2002Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6429207Abstract: The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.Type: GrantFiled: May 19, 2000Date of Patent: August 6, 2002Assignee: NPS Pharmaceuticals, Inc.Inventors: Bradford C. Van Wagenen, Scott T. Moe, Daryl L. Smith, Susan M. Sheehan, Irina Shcherbakova, Richard Travato, Ruth Walton, Robert Barmore, Eric G. Delmar, Thomas M. Stormann
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Patent number: 6423715Abstract: Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.Type: GrantFiled: November 15, 2001Date of Patent: July 23, 2002Assignee: Aventis Pharma S.A.Inventors: Jean-Claude Hardy, Jean Bouquerel, Patrick Nemecek, Jean-Claude Aloup, Serge Mignani, Jean-François Peyronel
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Patent number: 6420130Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.Type: GrantFiled: April 28, 1999Date of Patent: July 16, 2002Assignee: Aurora Biosciences CorporationInventors: Lewis R. Makings, Gregor Zlokarnik
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Patent number: 6410536Abstract: This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: August 3, 2000Date of Patent: June 25, 2002Assignee: Warner-Lambert CompanyInventors: Danette Andrea Dudley, Jeremy John Edmunds
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Patent number: 6407109Abstract: Pyrrolylquinoxalinediones of the formula I and their tautomeric and isomeric forms, and their physiologically tolerated salts, where the variables have the following meanings: R1 hydrogen, cyclohexyl an aliphatic radical which has 1 to 4 carbon atoms and can carry the radical —COOR5, where R5 is hydrogen or C1-C4-alkyl, R2 —COOH, —COO—C1-C4, —COO—(CH2)m—Ph, —CONR6R7 and where m can be an integer from 1 to 6, R6 can be hydrogen, C1-C4-alkyl or OH and R7 can be hydrogen, C1-C4-alkyl, where all the phenyl or pyridyl rings present in R2 can also be substituted by up to 3 of the following radicals: C1-C4-alkyl, halogen, —O—C1-C4-alkyl, —OCF3, —NO2, —CN, —COOR5 or —CONHR5, R3 —CF3, —NO2, —CN, and R4 hydrogen or R3 and R4 can together be a fused-on benzene ring. The compounds are suitable as drugs for human and veterinary medicine.Type: GrantFiled: January 27, 1998Date of Patent: June 18, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Berthold Behl, Hans-Peter Hofmann, Hans-Jürgen Teschendorf
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Publication number: 20020065415Abstract: Described are neuroprotective agents of Formula I 1Type: ApplicationFiled: October 4, 2001Publication date: May 30, 2002Inventors: Brian Edward Kornberg, Sham Shridhar Nikam, Michael Francis Rafferty
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Patent number: 6391878Abstract: This invention involves compounds having the following structure: as described in the Claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzable amides and esters thereof, as well as pharmaceutical compositions comprising such novel compounds. The invention also relates to the use of such compounds for preventing or treating disorders modulated by alpha-2 adrenoceptors.Type: GrantFiled: December 1, 2000Date of Patent: May 21, 2002Assignee: The Procter & Gamble CompanyInventors: Thomas Lee Cupps, Sophie Eva Bogdan, Raymond Todd Henry, Russell James Sheldon, William Lee Seibel, Jeffrey Joseph Ares
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Publication number: 20020058657Abstract: Novel compounds of general formula I: 1Type: ApplicationFiled: February 1, 2001Publication date: May 16, 2002Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020055634Abstract: A method for producing high melting point crystals, which is characterized by heating ethyl=(R)-2-[4-(6-chloro-2-quinoxalyloxy)phenoxy]propionate in the form of low melting point crystals, or low melting point crystals and high melting point crystals, within a range of from 50° C. to lower than the melting point of the low melting point crystals.Type: ApplicationFiled: December 4, 2001Publication date: May 9, 2002Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Masami Yasukawa, Shinji Kuwahara
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Patent number: 6380384Abstract: A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom; or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 10, 2001Date of Patent: April 30, 2002Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
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Patent number: 6380235Abstract: The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5 are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alknyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4 and R5 to from a 5 to 7 membered ring; R1 is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1 to C3 alkyl), —CO(aryl), —CO(C1 to C3 alkoxy), or —CO(C1 to C3 aminoalkyl) groups; R2 is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R3 is selected from a trisubstitutType: GrantFiled: April 19, 2000Date of Patent: April 30, 2002Assignees: American Home Products Corporation, Ligand Pharmaceuticals, Inc.Inventors: Puwen Zhang, Reinhold H. W. Bender, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Publication number: 20020049323Abstract: A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: 1Type: ApplicationFiled: April 10, 2001Publication date: April 25, 2002Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
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Patent number: 6376490Abstract: The invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 5-membered ring heteroaryl group containing 3 or 4 nitrogen heteroatoms which is linked to the quinoxalinedione ring by a ring carbon or nitrogen atom said group being optionally benzo-fused and optionally substituted, including in the benzo-fused portion, by 1 or 2 substituents each independently selected from C1-C4 alkyl, C2-C4 alkenyl, C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, C3-C7 cycloalkyloxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4, —S(O)p(C1-C4 alkyl), —SO2NR3R4, aryl, aryloxy, aryl(C1-C4)alkoxy, and het, said C1-C4alkyl being optionally substituted by C3-C7 cycloalkyl, halo, hydroxy, C1-C4 alkoxy, halo(C1C4)alkoxy, C3-C7 cycloalkyloxy, C3-C7 cycloalkyl (C1-C4) alkoxy, —COOH, C1-C4 alkoxycarbonyl, —CONR3R4, —NR3R4,—S(O)p(C1-C4 alkyl), —SO2(aryl), —SO2NR3R4 morpholino, aryl, aryloxy, aryl(C1-C4)Type: GrantFiled: September 4, 1998Date of Patent: April 23, 2002Assignee: Pfizer IncInventors: David John Bull, Christopher Lee Carr, Michael Jonathan Fray, Elisabeth Colette Louise Gautier, Charles Eric Mowbray, Alan Stobie
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Patent number: 6372750Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing themType: GrantFiled: April 5, 2001Date of Patent: April 16, 2002Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K. S. Pakala
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Patent number: 6369057Abstract: Compounds of the formula I or Ia in which n and the substituents R1, R5 and x have the meaning mentioned have an antiviral activity.Type: GrantFiled: April 7, 1995Date of Patent: April 9, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Uta-Maria Billhardt, Manfred Rösner, Günther Riess, Irvin Winkler, Rudolf Bender
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Patent number: 6353104Abstract: A method for producing &bgr; crystals of ethyl (R)-2-[4-(6-chloro-2-quinoxalin-2-yloxy)phenoxy]propionate, which is characterized by heating &agr; crystals, or &agr; a crystals and &bgr; crystals, within a range of from 50° C. to lower than the melting point of the &agr; crystals.Type: GrantFiled: October 30, 2000Date of Patent: March 5, 2002Assignee: Nissan Chemical Industries, Ltd.Inventors: Masami Yasukawa, Shinji Kuwahara