Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
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Publication number: 20030149041Abstract: Compounds that selectively inhibit inappropriate kinase activities and methods for their preparation are disclosed.Type: ApplicationFiled: June 28, 2002Publication date: August 7, 2003Applicant: Pharmacopeia, Inc.Inventors: Shawn David Erickson, James Inglese, Jeffrey John Letourneau, Christopher Mark Riviello
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Publication number: 20030149057Abstract: The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.Type: ApplicationFiled: December 20, 2002Publication date: August 7, 2003Applicant: Cyclacel LimitedInventors: Shudong Wang, Peter M. Fischer
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Publication number: 20030144246Abstract: This invention is concerned with substituted chromene derivatives of the general formula (I) in which R1 represents alkyl or cycloalkylalkyl, R2 and R3 each independently represent alkyl or cycloalkyl or taken together with the adjacent carbon atom represent a saturated 3- to 6-membered carbocyclic or heterocyclic ring, the alkyl, cycloalkyl, carbocyclic or heterocyclic ring being unsubstituted or substituted, and R4 represents hydrogen, halogen cyano, alkyl, alkylthio, alkenyl, alkynyl, hydroxyalkyl, hydroxyalkynyl, alkoxyalkyl, alkoxyalkynyl, trialkylsilyl, aryl or heteroaryl, and pharmaceutically acceptable acid addition salts of these compounds, their use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable acid addiType: ApplicationFiled: October 28, 2002Publication date: July 31, 2003Inventors: Peter Mohr, Philippe Pflieger
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Patent number: 6599911Abstract: Salts of pyrimidine derivatives are provided having the formula: wherein R represents hydrogen, methyl or ethyl; Z represents a substituted or unsubstituted 1-piperidinyl, a substituted or unsubstituted 4-morpholinyl, or a substituted or unsubstituted 1-pyrrolidinyl; and Ar represents a substituted or unsubstituted phenyl or a substituted or unsubstituted naphthyl. These salts are particularly useful as antiviral agents (e.g., to treat CMV infections).Type: GrantFiled: June 6, 2002Date of Patent: July 29, 2003Assignee: Tularik Inc.Inventor: Jay P. Powers
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Publication number: 20030134838Abstract: The present invention relates to trisubstituted pyrimidines of formula 1Type: ApplicationFiled: October 16, 2002Publication date: July 17, 2003Applicant: Boehringer Ingelheim Pharma KGInventors: Klaus Bornemann, Hans Briem, Cornelia Dorner-Clossek, Katja Fechteler, Klaus Fuchs, Frank Himmelsbach, Klaus Klinder, Markus Kostka
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Publication number: 20030125345Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.Type: ApplicationFiled: October 2, 2002Publication date: July 3, 2003Inventors: William S. Caldwell, Gary M. Dull, Balwinder S. Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared M. Wagner, Peter A. Crooks, Patrick M. Lippiello, Merouane Bencherif
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Publication number: 20030125346Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.Type: ApplicationFiled: August 21, 2002Publication date: July 3, 2003Inventors: John L. Buchanan, Stuart Chaffee, Jean-Christophe Harmange, Perry M. Novak, Xiaotian Zhu
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Publication number: 20030119857Abstract: This invention relates to indole derivatives of the general formula (I) wherein R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfonyl, dialkylsulfamoyl, N-cycloalkyl-N-alkylsulfamoyl, heterocyclylalkyl or phenylalkyl; R2 is hydrogen, halogen, alkyl, alkanoyl, phenyl, phenylalkyl or heterocyclylalkyl; R3 is hydrogen, alkyl; and R4 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfonyl, dialkylsulfamoyl, N-cycloalkyl-N-alkylsulfamoyl, heterocyclylalkyl, or phenylalkyl; and pharmaceutically acceptable acid addition salts of these compounds, there use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptabType: ApplicationFiled: October 25, 2002Publication date: June 26, 2003Inventors: Patrizio Mattei, Philippe Pflieger
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Patent number: 6583148Abstract: The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral systems.Type: GrantFiled: April 8, 1999Date of Patent: June 24, 2003Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
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Publication number: 20030114472Abstract: This invention concerns the use of compounds of formula 1Type: ApplicationFiled: November 1, 1999Publication date: June 19, 2003Inventors: BART DE CORTE, MARC RENE DE JONGE, JAN HEERES, CHIH YUNG HO, PAUL ADRIAAN JAN JANSSEN, ROBERT W. KAVASH, LUCIEN MARIA HENRICUS KOYMANS, MICHAEL JOSEPH KUKLA, DONALD WILLIAM LUDOVICI, KOEN JEANNE ALFONS VAN AKEN
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Patent number: 6579874Abstract: Compounds of formula I wherein the symbols have meaning as defined herein, are p38 MAP kinase inhibitors, and are useful pharmaceutically for treating TNF&agr; and IL-1 mediated diseases, such as rheumatoid arthritis, and diseases of bone metabolism, e.g. osteoporosis.Type: GrantFiled: October 12, 2001Date of Patent: June 17, 2003Assignee: Novartis AGInventors: Lászlo Révész, Achim Schlapbach
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Publication number: 20030105090Abstract: This invention describes novel pyrazole compounds of formula IV: 1Type: ApplicationFiled: December 19, 2001Publication date: June 5, 2003Inventors: David Bebbington, Jean-Damien Charrier
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Publication number: 20030105323Abstract: 1.Type: ApplicationFiled: August 19, 2002Publication date: June 5, 2003Applicant: SUMITOMO PHARMACEUTICALS COMPANY LIMITEDInventors: Hitoshi Fujita, Fujio Antoku, Norio Fujiwara, Kiyotaka Iwai, Hiroshi Tanaka, Hajime Kawakami
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Patent number: 6573377Abstract: This invention provides compounds having antitumor effect, namely a compound represented by the following formula (I) or (Ia) having various substituents in which G and G1 are condensed tricyclic heterocyclic rings or salts thereof, and a compound represented by the following formula (Ib) having various substituents or salts thereof.Type: GrantFiled: January 24, 2001Date of Patent: June 3, 2003Assignee: Daiichi Pharmaceuticals Co., Ltd.Inventors: Akio Ejima, Satoru Ohsuki, Hitoshi Ohki, Hiroyuki Naito, Chie Makino
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Publication number: 20030078265Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: April 24, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6548512Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: January 27, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
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Patent number: 6545008Abstract: The present invention relates to novel pyrimidine derivatives and pharmaceutically acceptable non-toxic salts thereof which possess an excellent inhibitory activity against gastric acid secretion, a pharmaceutical composition containing the same as an active ingredient, and a process for the preparation thereof.Type: GrantFiled: May 17, 2001Date of Patent: April 8, 2003Assignee: Yuhan CorporationInventors: Jong Wook Lee, Bong Yong Lee, Chang Seop Kim, Seung Kyu Lee, Song Jin Lee
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Publication number: 20030065179Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, 1Type: ApplicationFiled: February 28, 2002Publication date: April 3, 2003Inventors: Margaret Y. Chu-Moyer, Jerry A Murry, Banavara L Mylari, William J Zembrowski
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Publication number: 20030045715Abstract: Salts of pyrimidine derivatives are provided having the formula: 1Type: ApplicationFiled: June 6, 2002Publication date: March 6, 2003Applicant: Tularik Inc.Inventor: Jay P. Powers
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Publication number: 20030032647Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): 1Type: ApplicationFiled: August 10, 2001Publication date: February 13, 2003Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Publication number: 20030022885Abstract: This invention describes novel pyrazole compounds of formula II: 1Type: ApplicationFiled: December 20, 2001Publication date: January 30, 2003Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Publication number: 20030004137Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: January 2, 2003Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6500952Abstract: The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)—Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (VIII) of the formula HNR3—Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H.Type: GrantFiled: September 18, 2000Date of Patent: December 31, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Jan Vermehren, Lothar Willms
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Patent number: 6495547Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6—Alk2— (b-1), or —Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen.Type: GrantFiled: August 18, 2000Date of Patent: December 17, 2002Assignee: Janssen Pharmaceutica, N.V.Inventors: Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren, Marc Francis Josephine Schroven, Marcel Frans Leopold De Bruyn
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Patent number: 6492516Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.Type: GrantFiled: May 4, 2000Date of Patent: December 10, 2002Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, David A. Claremon, Cory R. Theberge
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Publication number: 20020183323Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: December 5, 2002Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20020132823Abstract: An assay is provided for the identification and comparison of compounds having activity as modulators of the expression and release of TNFa, IL-1 or IL-6 in humans and animals in which modulation of the catalytic activity of PRAK (p38-regulated/activated protein kinase) is employed for identification and comparison of test compounds.Type: ApplicationFiled: January 17, 2001Publication date: September 19, 2002Inventors: Jiahuai Han, Liguo New, Hermann Gram
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Patent number: 6451738Abstract: The invention relates to novel substituted thienyl(amino)sulphonyl(thio)ureas of the formula (I) in which A represents nitrogen or a CH grouping, E represents a single bond or an NH grouping, Q represents oxygen or sulphur, R1 and R2 independently of one another represent hydrogen, halogen or in each case optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy, aryloxy or heterocyclyloxy, R3 represents hydrogen or optionally substituted alkyl, R4 and R5 independently of one another each represent cyano, halogen or represent in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and R6 represents hydrogen, cyano, halogen or represents in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and to salts of compounds of the formula (I), to processes for preparing the novel compounds and to their use as herbicides.Type: GrantFiled: August 9, 2001Date of Patent: September 17, 2002Assignee: Bayer AktiengesellschaftInventors: Ernst Rudolf F. Gesing, Johannes Rudolf Jansen, Klaus-Helmut Müller, Ulrich Philipp, Markus Dollinger
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Publication number: 20020123629Abstract: The invention provides a compound of formula I 1Type: ApplicationFiled: February 15, 2002Publication date: September 5, 2002Inventor: Bernhard Peter Neumann
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Patent number: 6440975Abstract: The invention relates to amino acid derivatives of the formula I where the radicals have the meanings stated in the description, and to the use thereof as drugs.Type: GrantFiled: March 31, 1998Date of Patent: August 27, 2002Assignee: Abbott LaboratoriesInventors: Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Hartmut Riechers, Liliane Unger, Manfred Raschack
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Patent number: 6432963Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].Type: GrantFiled: June 15, 2000Date of Patent: August 13, 2002Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hiroyuki Hisamichi, Ryo Naito, Souichirou Kawazoe, Akira Toyoshima, Kazuhito Tanabe, Eiichi Nakai, Atsushi Ichikawa, Akiko Orita, Makoto Takeuchi
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Patent number: 6432947Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: August 26, 1999Date of Patent: August 13, 2002Assignees: Berlex Laboratories, Inc., Pharmacopeia, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20020099207Abstract: The invention relates to compounds of the formula 1Type: ApplicationFiled: October 15, 2001Publication date: July 25, 2002Inventor: Heinz Stadler
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Patent number: 6410482Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.Type: GrantFiled: May 13, 1997Date of Patent: June 25, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6410726Abstract: Salts of pyrimidine derivatives are provided having the formula: wherein R represents hydrogen, methyl or ethyl; Z represents a substituted or unsubstituted 1-piperidinyl, a substituted or unsubstituted 4-morpholinyl, or a substituted or unsubstituted 1-pyrrolidinyl; and Ar represents a substituted or unsubstituted phenyl or a substituted or unsubstituted naphthyl. These salts are particularly useful as antiviral agents (e.g., to treat CMV infections).Type: GrantFiled: January 8, 2001Date of Patent: June 25, 2002Assignee: Tularik Inc.Inventor: Jay P. Powers
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Publication number: 20020065279Abstract: Salts of pyrimidine derivatives are provided having the formula: 1Type: ApplicationFiled: January 8, 2001Publication date: May 30, 2002Inventor: Jay P. Powers
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Patent number: 6395742Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl or C3-6alkenediyl; R1 is hydrogen or C1-4alkyl; R2 and R3 each independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; or R2 and R3 may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R4 is hydrogen or halo; Q is aryl, aryloxy, di(aryl)methyl or heteroaryl; aryl is naphthyl or phenyl, said naphthyl and phenyl may optionally be substituted; and heteroaryl is quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4-benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl; said heteroaryls may optionally be substituted; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactivType: GrantFiled: September 22, 2000Date of Patent: May 28, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul René Marie André Bosmans, Christopher John Love, Guy Rosalia Eugène Van Lommen
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Publication number: 20020058664Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: July 20, 2001Publication date: May 16, 2002Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6372740Abstract: 2-Aryl-8-oxodihydropurine derivative of the following formula (I): wherein W is H, lower alkyl, halogen, lower alkoxy, amino, mono- or di-lower alkylamino, or substituted or unsubstituted phenyl; X is H, lower alkyl, cycloalkyl-lower alkyl, substituted or unsubstituted phenyl-lower alkyl, lower alkenyl, carbamoyl, di-lower alkylcarbamoyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); Y is H, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, lower alkenyl, substituted or unsubstituted phenyl-lower alkyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); A is substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; provided that when one of X and Y of the above formula (I) is the group of the formula (Q), then the other is the same groups for X or Y as described above except for the group of the formula (Q), or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: June 1, 2000Date of Patent: April 16, 2002Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Teruya Murata, Kaoru Masumoto, Katsunori Kondo, Kiyoshi Furukawa, Makoto Oka
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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: 6352987Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.Type: GrantFiled: February 26, 2001Date of Patent: March 5, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Hans Jochen Lang, Matthias Gossel, Martin Bickel
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Publication number: 20020016460Abstract: Disclosed are novel compounds of formula (I): 1Type: ApplicationFiled: August 2, 2001Publication date: February 7, 2002Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
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Patent number: 6342503Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer'disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: wherein R1, R3, R4, R5, Z, Y, V, X, X′, J, K, L, and M are as defined herein.Type: GrantFiled: January 7, 1998Date of Patent: January 29, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Paul Edward Aldrich, Argyrios Georgios Arvanitis, Robert Scott Cheeseman, Robert John Chorvat, Thomas Eugene Christos, Paul Joseph Gilligan, Dimitri Emil Grigoriadis, Carl Nicholas Hodge, Paul John Krenitsky, Everett Latham Scholfield, Sang William Tam, Zelda Rakowitz Wasserman
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Patent number: 6342604Abstract: The present invention relates to the use of pyrimidine compounds of the following formula: wherein R1, R2, R3, A, B and Ar have the meanings indicated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.Type: GrantFiled: January 14, 1997Date of Patent: January 29, 2002Assignee: BASF AktiengesellschaftInventors: Beate Hellendahl, Annegret Lansky, Rainer Munschauer, Siegfried Bialojan, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke, Karla Drescher
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Patent number: 6342602Abstract: Compounds of the formula wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: August 4, 2000Date of Patent: January 29, 2002Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6331506Abstract: Disubstituted methylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which R1 to R6, W, X, Y, Z are as defined in claim 1 and the group R2R3C is a carbon atom which is subsituted by at least one electron-withdrawing radical R2 or R3 are suitable as herbicides and plant growth regulators. They can be prepared in accordance with known processes via intermediates, some of which are novel.Type: GrantFiled: September 16, 1998Date of Patent: December 18, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6300357Abstract: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represent a hydrogen atom or an unsubstituted or halo substituted alkyl; n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic group. The compound of the present invention exhibits an excellent antifungal activity.Type: GrantFiled: February 1, 1999Date of Patent: October 9, 2001Assignee: Sankyo Company, LimitedInventors: Sadao Oida, Teruo Tanaka, Yawara Tajima, Toshiyuki Konosu, Atsushi Somada, Takeo Miyaoka, Hiroshi Yasuda
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Publication number: 20010027196Abstract: The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.Type: ApplicationFiled: February 20, 2001Publication date: October 4, 2001Inventors: Edilio Maurizio Borroni, Gerda Huber-Trottmann, Gavin John Kilpatrick, Roger David Norcross
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Patent number: 6274588Abstract: The invention provides compounds of the formula wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may together be —CH═CH—CH═CH—, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4′ are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH2)n-morpholinyl, —(CH2)n-piperidinyl, —(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl or —O&Type: GrantFiled: May 22, 2000Date of Patent: August 14, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler