Patents Examined by Hong Liu
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Patent number: 6441019Abstract: This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof.Type: GrantFiled: July 17, 2001Date of Patent: August 27, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Arthur A. Santilli, Andrew Q. Viet, Puwen Zhang, Andrew Fensome, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6436923Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: March 17, 2000Date of Patent: August 20, 2002Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Patent number: 6437126Abstract: The invention is directed to a process for the preparation of a substituted phenyluracil of the formula: The process broadly comprises reacting a carbonylphenyluracil of the formula: with an amino compound, an alcohol or a mercaptan. The resultant products are useful as herbicides.Type: GrantFiled: April 24, 2001Date of Patent: August 20, 2002Assignee: Bayer AktiengesellschaftInventors: Mark Wilhelm Drewes, Roland Andree, Markus Dollinger
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Patent number: 6432881Abstract: 2-Benzoylcyclohexane-1,3-diones of formula I : where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3 (n=0, 1, 2), —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen or optionally substituted alkyl, haloalkyl, alkenyl, alkynyl, phenyl or phenylalkyl; Q is optionally substituted cyclohexane-2-yl-1,3-dione; X1 is optionally substituted alkylene, propenylene, alkenylene or alkynylene; R4 is hydrogen or optionally substituted alkyl, alkenyl, alkynyl, phenyl, phenylalkyl; Het is a three- to six-membered, optionally substituted heterocyclic or heteroaromatic group; and agriculturally useful salts thereof, processes and intermediates for preparing compounds of formula I, compositions comprising them, and the use of the compounds of formula I and the compositions comprising them for controlling harmful plants are described.Type: GrantFiled: February 7, 2000Date of Patent: August 13, 2002Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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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: 6432975Abstract: Pharmaceutical compositions include aryl substituted amine compounds, and in particular, carbon-linked aromatic azabicyclo compounds, and in particular, aromatic alkylene azabicyclo compounds and aromatic alkyl azabicyclo compounds.Type: GrantFiled: December 11, 1998Date of Patent: August 13, 2002Assignee: Targacept, Inc.Inventors: Jeffrey Daniel Schmitt, Peter Anthony Crooks, Gary Maurice Dull
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Patent number: 6426350Abstract: The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.Type: GrantFiled: March 30, 2001Date of Patent: July 30, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo Edmond Josephine Kennis, Serge Maria Aloysius Pieters, François Paul Bischoff
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Patent number: 6420400Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis.Type: GrantFiled: April 7, 2000Date of Patent: July 16, 2002Assignee: Kinetek Pharmaceuticals, Inc.Inventors: Zaihui Zhang, Jun Yan, Danny Leung, Shisen Wang, Penelope C. Costello, Jasbinder Sanghera
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Patent number: 6417185Abstract: Novel pyridine and pyrimidine derivatives which selectively inhibit glycogen synthase kinase 3 are provided and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions which may be mediated by glycogen synthase kinase 3.Type: GrantFiled: June 18, 1999Date of Patent: July 9, 2002Assignee: Chiron CorporationInventors: Dane A. Goff, Stephen D. Harrison, John M. Nuss, David B. Ring, Xiaohui A. Zhou
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Patent number: 6413980Abstract: The present application describes nitrogen containing heterobicyclics and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: December 22, 1999Date of Patent: July 2, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: John M. Fevig, Joseph Cacciola, Charles G. Clark, Qi Han, Patrick Yuk Sun Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan, Karen A. Rossi
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3-Substituted tetrahydropyridopyrimidinone derivatives, method for producing the same, and their use
Patent number: 6414157Abstract: 3-substituted tetrahydropyridopyrimidinone derivatives of the formula (I) wherein the radicals have the meanings given in the Description, to a method for producing said derivatives and, to their use for producing active ingredients for drugs.Type: GrantFiled: April 10, 2000Date of Patent: July 2, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Uta Dullweber, Dorothea Starck, Gerd Steiner, Alfred Bach, Franz Emling, Xavier Garcia-Ladona, Hans-Jürgen Teschendorf, Karsten Wicke -
Patent number: 6410530Abstract: New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.Type: GrantFiled: August 31, 2000Date of Patent: June 25, 2002Assignee: AstraZeneca ABInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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Patent number: 6410532Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy—C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptableType: GrantFiled: July 10, 2001Date of Patent: June 25, 2002Assignee: AstraZeneca ABInventors: Stefan Berg, Mats Linderberg, Svante Ross, Seth-Olov Thorberg, Bengt Ulff
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Patent number: 6407116Abstract: A compound represented by the formula: [wherein ring A represents a homocycle optionally having substituents or a nitrogen-containing heterocycle optionally having substituents; D and E are O or S; one of R1 and R2 represents a group represented by the formula: (wherein Ar1 and Ar2 represent an aromatic group optionally having substituents; Ar1 and Ar2 may form a condensed cyclic group optionally having substituents together with an adjacent carbon atom; ring B represents a nitrogen-containing heterocycle optionally having substituents; X and Y are a bond, O, S(O)p (p is an integer of 0 to 2), NR4 (R4 is H or a lower alkyl group) or a bivalent straight-chained lower hydrocarbon group, which may contain 1 to 3 hetero atoms, optionally having substituents; and R3 represents H, a hydroxy group optionally having substituents or an optionally esterified carboxyl group); and the other is a hydrogen atom, a cyano group or a hydrocarbon group optionally having substituents&rsqType: GrantFiled: February 25, 2000Date of Patent: June 18, 2002Assignee: Takeda Chemical Industries, Inc.Inventors: Masahiro Kajino, Shinji Morimoto, Atsuhiro Inaba, Hideaki Nagaya
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Patent number: 6407112Abstract: Optically active tetrahydrobenzindole type compounds having affinity for a 5-HT receptor, useful for prevention and treatment of mental diseases. A species compound is (S)-2a-4-(4-(2-methoxyphenyl)piperazinyl)butyl)-2a,3,4,5,-tetrahydro 1 H-benz[cd]indol-2-one.Type: GrantFiled: October 23, 2000Date of Patent: June 18, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Masao Koyama, Osamu Ushiroda, Chika Kikuchi, Takashi Ando, Eriko Morita, Masayo Okuno, Toyokazu Hiranuma
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Patent number: 6403582Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g.Type: GrantFiled: January 12, 2001Date of Patent: June 11, 2002Assignee: Schering CorporationInventors: Gregory A. Reichard, Neng-Yang Shih, Dasong Wang
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Patent number: 6403600Abstract: The invention relates to novel methoximinophenylacetamides, to a process for their preparation and to their use as fungicides.Type: GrantFiled: April 5, 2001Date of Patent: June 11, 2002Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Herbert Gayer, Peter Gerdes, Ulrich Heinemann, Bernd-Wieland Krüger, Robert Markert, Klaus Stenzel, Gerd Hänssler, Astrid Mauler-Machnik
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Patent number: 6403583Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.Type: GrantFiled: December 22, 1999Date of Patent: June 11, 2002Inventors: Patrick Y. S. Lam, Charles G. Clark, John M. Fevig, Robert A. Galemmo, Qi Han, Irina C. Jacobson, Renhau Li, Donald J. P. Pinto, Ruth R. Wexler
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Patent number: 6399602Abstract: The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.Type: GrantFiled: September 11, 1998Date of Patent: June 4, 2002Assignee: Zeneca LimitedInventors: Andrew John Barker, Craig Johnstone
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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