At 2-position Patents (Class 544/315)
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Patent number: 6479435Abstract: Diaryl ether compounds useful in the control of weeds are described. An exemplary compound is represented by the general formula (I): In this formula Q is represented by Q1 X and Y represent a hydrogen atom, halogen atom, cyano group, nitro group or (C1-6)haloalkyl group; R1 is halogen; R2 and R3 represent a hydrogen atom, a (C1-6)alkyl group or a (C1-6)haloalkyl group . Methods of making the compounds are also described.Type: GrantFiled: February 9, 2001Date of Patent: November 12, 2002Assignee: ISK Americas IncorporatedInventors: David A. Pulman, Bai-Ping Ying, Shao-Yong Wu, Sandeep Gupta, Hiroshi Shimoharada, Masamitsu Tsukamoto
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Patent number: 6469018Abstract: Novel pyridin-4-yl or pyrimidin-4-yl substituted pyridine compounds and compositions for use in therapy.Type: GrantFiled: July 5, 2001Date of Patent: October 22, 2002Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Jeffrey C. Boehm
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Publication number: 20020151555Abstract: Selective MMP-13 inhibitors are pyrimidine derivatives of the formula 1Type: ApplicationFiled: February 13, 2002Publication date: October 17, 2002Inventors: Nicole Chantel Barvian, William Chester Patt
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Patent number: 6465484Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.Type: GrantFiled: February 28, 2001Date of Patent: October 15, 2002Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
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Publication number: 20020143023Abstract: Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.Type: ApplicationFiled: December 26, 2001Publication date: October 3, 2002Applicant: AJINOMOTO CO. INCInventors: Seiji Ohno, Akiko Okajima, Seiji Niwa, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Yuki Kajigaya, Tomoko Takeda, Hajime Koganei
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Publication number: 20020137747Abstract: N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed.Type: ApplicationFiled: June 26, 2001Publication date: September 26, 2002Inventors: Kevin Joseph Moriarty, Yvonne Shimshock, Gulzar Ahmed, Junjun Wu, James Wen, Wei Li, Shawn David Erickson, Jeffrey John Letourneau, Edward McDonald, Katerina Leftheris, Stephen T. Wrobleski, Zahid Hussain, Ian Henderson, Axel Metzger, John J. Baldwin, Alaric J. Dyckman
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Publication number: 20020123491Abstract: Compound represented by the structural formula 1Type: ApplicationFiled: December 14, 2000Publication date: September 5, 2002Inventors: Neng-Yang Shih, Ho-Jane Shue, Gregory A. Reichard, Sunil Paliwal, David J. Blythin, John J. Piwinski, Dong Xiao, Xiao Chen
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Patent number: 6441169Abstract: Novel pyrimidin-4-one and pyrimidin-4-thione derivatives of formula (I) wherein A is phenyl, thienyl (including all 3 isomers), thiazolyl or pyridyl; X is oxygen or sulfur; R1 is hydrogen, halogen or trimethylsilyl; R2 is hydrogen, halogen or trimethysilyl; and at least one of R1 and R2 is not hydrogen; R3 is C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6haloalkenyl, C2-C6alkynyl, C2-C6haloalkynyl, —(CH2)n—C3-C8cycloalkyl which are unsubstitituted or substituted by halogen, C1-C6alkyl or C1-C6haloalkyl, C1-C4alkoxy-C1-C6alkyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkythio-C1-C6alkyl; C1-C4alkylthio-C2-C6alkenyl; C1-C4alkythio-C2-C6alkynyl; mono-C1-C4alkylamin-C1-C6alkyl; mono-C1-C4alkylamin-C1-C6alkenyl; mono-C1-C4alkylamin-C2-C6alkynyl; —(CH2)n—C1-C4alkoxy-C3-C6cycloalkyl; —(CH2)n—C1-C4alkylthio-C3-C6cycloalkyl; —(CH2)2-mono-C1-C4alkylamin-C3-C6cycloalkyl; or N═CR9R10; n is 1, 2, 3, or 4; R4, R5, R6, R7, and R8 are each independently of theType: GrantFiled: March 3, 2000Date of Patent: August 27, 2002Assignee: Syngenta Crop Protection, Inc.Inventor: Harald Walter
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Publication number: 20020115864Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 18, 2002Publication date: August 22, 2002Inventors: MacKlin Brian Arnold, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6399620Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: June 29, 2000Date of Patent: June 4, 2002Assignee: Aventis Pharma S.A.Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
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Patent number: 6387915Abstract: Isoxazole-sulfonamide endothelin antagonists of formula (I) below having good affinity for endothelin receptors and selectivity for ETA over ETB are described herein. Such compounds are useful in the treatment of conditions mediated by endothelin, in particular, conditions mediated by endothelin ETA.Type: GrantFiled: May 30, 2001Date of Patent: May 14, 2002Assignee: Pfizer Inc.Inventors: Bernard Joseph Banks, Nathan Anthony Logan Chubb, James John Eshelby, Michael Stephen Pacey, Darren John Schulz
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Patent number: 6387893Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.Type: GrantFiled: September 27, 2000Date of Patent: May 14, 2002Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
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Publication number: 20020052497Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.Type: ApplicationFiled: October 9, 2001Publication date: May 2, 2002Applicant: Targacept, Inc.Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
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Publication number: 20020049220Abstract: 1Type: ApplicationFiled: October 12, 2001Publication date: April 25, 2002Inventors: Laszlo Revesz, Achim Schlapbach
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Publication number: 20020040026Abstract: The present invention provides novel 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 palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems.Type: ApplicationFiled: October 2, 2001Publication date: April 4, 2002Inventors: Robert John Chorvat, Parthasarathi Rajagopalan
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Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP-1B)
Patent number: 6365592Abstract: The invention encompasses compounds represented by formula I: as well as compositions and methods of treatment. The compounds are inhibitors of the PTP-1B enzyme.Type: GrantFiled: May 12, 2000Date of Patent: April 2, 2002Assignee: Merck Frosst Canada & Co.Inventors: Yves Leblanc, Claude Dufresne, Patrick Roy, Zhaoyin Wang -
Patent number: 6365738Abstract: Described are preferred processes for preparing heterocycles having one or more nitrogen and/or oxygen heteroatoms, utilizing a 1,3-dihalopropene as an effective 3-carbon fragment. Preferred processes yield pyridines, quinolines, oxazoles, pyrimidines and pyrazoles, depending upon the other reactant or reactants utilized with the 1,3-dihalopropene.Type: GrantFiled: June 29, 1999Date of Patent: April 2, 2002Assignee: Reilly Industries, Inc.Inventors: Ramiah Murugan, Eric F. V. Scriven
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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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Publication number: 20020010183Abstract: The invention relates to novel pyrrolopyridinone derivatives of the formula (I) or (II): 1Type: ApplicationFiled: May 2, 2001Publication date: January 24, 2002Inventors: Zhihua Sui, Mark J. Macielag, Jihua Guan, Weiqin Jiang, James C. Lanter
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Publication number: 20020010186Abstract: This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: May 15, 2001Publication date: January 24, 2002Applicant: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Bharat Lagu, Dhanapalan Nagarathnam, Mohammad R. Marzabadi, Charles Gluchowski
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Patent number: 6340687Abstract: Antiatherosclerotic agents are provided having the following structure: wherein: R1 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenylalkyl of 7-10 carbon atoms; and R2, R3, R4, R5, and R6 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy of 6-12 carbon atoms, aralkyloxy of 7-12 carbon atoms, fluoroalkoxy of 1-6 carbon atoms, trifluoromethyl, alkylthio of 1-3 carbon atoms, alkylsulfonyl of 1-3 carbon atoms, —SCF3, nitro, alkylamino in which the alkylamino moiety has 1-6 carbon atoms, or dialkylamino in which each alkyl group has 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 2, 1998Date of Patent: January 22, 2002Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Jay S. Shumsky, Kevin A. Memoli, Donald P. Strike
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Publication number: 20010044440Abstract: Compounds of formula I are effective modulators of p38 MAP kinase.Type: ApplicationFiled: February 23, 2001Publication date: November 22, 2001Inventors: David J. Morgans, Silke Thode, Dongxu Sun
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Publication number: 20010039343Abstract: This invention relates to a process for the manufacture of compounds which are useful to make either pesticides that can be used as fungicides, herbicides, insecticides, rodenticides or biocides, or pharmaceutical compounds for both human and veterinary application.Type: ApplicationFiled: March 13, 2001Publication date: November 8, 2001Inventors: Mark Joseph Mulvihill, James Joseph Gallagher, Brian Scott MacDougall, Damian Gerard Weaver
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Patent number: 6313296Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: February 23, 2000Date of Patent: November 6, 2001Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6313072Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.Type: GrantFiled: February 18, 1999Date of Patent: November 6, 2001Assignee: American Cyanamid CompanyInventors: Stephen Scheiblich, Thomas Maier, Axel Kleemann, Helmut Siegfried Baltruschat
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Patent number: 6310204Abstract: Calculated performance improvements are expected from a particularly new class of compounds, geminal-bis(difluoramino)-substituted heterocyclic nitramines, when formulated into explosives and propellants. This invention involves novel and nonintuitive methods for the preparation of certain derivatives of 2,2-bis(difluoramino)-N-nitro-1,3-propanediamine which are suitable precursors leading to 5,5-bis(difluoramino)hexahydro-1,3-dinitropyrimidine (RNFX). The invention also involves novel and nonintuitive methods for the preparation of RNFX, a specific member of a general class of compounds with the substructure 2,2-bis(difluoramino)-N-nitro-1,3-propanediamine. RNFX is produced by the use of key intermediates, including tetrahydropyrimidin-5(4H)-ones, which allow formation of the target structural subcomponent, 2,2-bis(difluoramino)-N-nitro-1,3-propanediamine, and a more specific substructure of 2,2-bis(difluoramino)-N,N′-dinitro-1,3-propanediamine.Type: GrantFiled: February 16, 2000Date of Patent: October 30, 2001Assignee: The United States of America as represented by the Secretary of the NavyInventors: Robert Dale Chapman, Ba Van Nguyen
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Patent number: 6306855Abstract: The invention relates to novel fluoromethoximino compounds, to a process for their preparation and to their use as pesticides, and also to novel intermediates and to a plurality of processes for their preparation.Type: GrantFiled: December 2, 1999Date of Patent: October 23, 2001Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Albrecht Marhold, Uwe Stelzer, Reinhard Lantzsch, Ralf Tiemann, Klaus Stenzel, Astrid Mauler-Machnik, Stefan Dutzmann, Martin Kugler, Hans-Ulrich Buschhaus
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Patent number: 6306866Abstract: There are provided compositions and methods comprising compounds of formula I: wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.Type: GrantFiled: March 6, 1998Date of Patent: October 23, 2001Assignee: American Cyanamid CompanyInventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
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Publication number: 20010031759Abstract: 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 them.Type: ApplicationFiled: April 5, 2001Publication date: October 18, 2001Applicant: DR. REDDY'S RESEARCH FOUNDATION & REDDY- CHEMINOR, INC.Inventors: Dya Bhushan Lohray, Raj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K.S. Pakala
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Patent number: 6303783Abstract: There are provided 1-(3-heterocyclyphenyl)isothio-urea, -isourea, -guanidine and -amidine compounds of formula I Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.Type: GrantFiled: August 4, 1999Date of Patent: October 16, 2001Assignee: American Cyanamid Co.Inventor: Gary Mitchell Karp
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Publication number: 20010029239Abstract: The invention relates to aryl vinyl ether compounds of formula (I): 1Type: ApplicationFiled: December 20, 2000Publication date: October 11, 2001Inventors: Michael Colin Cramp, Stephen Robert Mack, Michael Gingell
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz HĂĽter
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Patent number: 6288068Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.Type: GrantFiled: January 12, 2000Date of Patent: September 11, 2001Assignee: Schering CorporationInventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Javaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
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Patent number: 6281219Abstract: The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.Type: GrantFiled: July 12, 1999Date of Patent: August 28, 2001Assignee: American Cyanamid Co.Inventors: Salvatore John Cuccia, William Wakefield Wood, Brian Lee Buckwalter, John Francis Chiarello, Linda Barbara Fleming
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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
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Patent number: 6262051Abstract: The invention relates to novel methoximinomethyldioxazines, to a plurality of processes for their preparation and to their use as fungicides, and also to novel intermediates and to a process for their preparation.Type: GrantFiled: September 28, 1999Date of Patent: July 17, 2001Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Bernd-Wieland Krüger, Robert Markert, Thomas Seitz, Bernd Gallenkamp, Uwe Stelzer, Ralf Tiemann, Astrid Mauler-Machnik, Stefan Dutzmann, Klaus Stenzel, Gerd Hänssler
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Patent number: 6248747Abstract: This invention is directed to the use of dihydropyrimidine compounds, which are selective antagonists for cloned human &agr;1C receptors, for the treatment of benign prostatic hyperplasia and other diseases where antagonism of the human &agr;1C receptor is useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-identified compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: April 14, 1999Date of Patent: June 19, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski
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Patent number: 6248770Abstract: The present invention relates to new benzimidazoles of general formula wherein Ra to Rc, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain a group which is negatively charged under physiological conditions, instead of a carboxy group, and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein Rc denotes one of the amidino groups mentioned in claim 1 which have valuable pharmacological properties, particularly an antithrombotic activity.Type: GrantFiled: June 24, 1999Date of Patent: June 19, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Iris Kauffmann, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6245773Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 16, 1997Date of Patent: June 12, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Bharat Lagu, Dhanapalan Nagarathnam, Mohammad R. Marzabadi, Charles Gluchowski
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Patent number: 6211184Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are &agr;v&bgr;3 antagonists, &agr;v&bgr;5 antagonists or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: June 14, 1999Date of Patent: April 3, 2001Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Robert S. Meissner, James J. Perkins, Ben C. Askew, Paul J. Coleman, John J. Hutchinson, Adel M. Naylor-Olsen
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Patent number: 6194575Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with urea.Type: GrantFiled: September 21, 1999Date of Patent: February 27, 2001Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Wolfgang Krämer, Eric Rivadeneira
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Patent number: 6172226Abstract: A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.Type: GrantFiled: July 16, 1998Date of Patent: January 9, 2001Assignee: PerSeptive Biosystems, Inc.Inventors: James M. Coull, Michael Egholm, Richard P. Hodge, Mohamed Ismail, S. B. Rajur
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Patent number: 6166041Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen;Q is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --, a single or a double bond, or --NR.sub.1 --;R.sub.1 is a C.sub.Type: GrantFiled: November 3, 1997Date of Patent: December 26, 2000Assignee: Euro-Celtique, S.A.Inventors: David J. Cavalla, Mark Chasin, John W F Whitehead, Lesley Walton, Andrew C. Mansfield
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Patent number: 6162804Abstract: The present invention relates to benzinidazole compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.Type: GrantFiled: March 11, 1999Date of Patent: December 19, 2000Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, April M. Cunningham, Randall W. Hungate, Timothy J. Koester
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Patent number: 6133277Abstract: 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 Alk.sup.1 is C.sub.1-6 alkanediyl optionally substituted with hydroxy, C.sub.1-4 alkyloxy or C.sub.1-4 alkylcarbonyloxy; --Z.sup.1 --Z.sup.2 -- is a bivalent radical; R.sup.1, R.sup.2 and R.sup.3 are each independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, halo and the like; or when R.sup.1 and R.sup.2 are on adjacent carbon atoms, R.sup.1 and R.sup.2 taken together may form a bivalent radical; R.sup.4 is hydrogen or C.sub.1-6 alkyl; A is a bivalent radical of formula --NR.sup.6 --Alk.sup.2 -- (b-1), or --Npiperidinyl--(CH.sub.2).sub.m (b-2) wherein m is 0 or 1; R.sup.5 is a radical of formula ##STR1## wherein n is 1 or 2; p.sup.1 is 0, and p.sup.2 is 1 or 2; or p.sup.1 is 1 or 2, and p.sup.2 is 0; X is oxygen, sulfur or .dbd.NR.sup.9 ; Y is oxygen or sulfur; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.Type: GrantFiled: November 16, 1998Date of Patent: October 17, 2000Assignee: 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: 6124306Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula I ##STR1## and pyrimidine-thioalkyl and alkylethers of Formula I, where R.sub.4 is selected from the group consisting of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, --NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; andR.sub.6 is --S--C.sub.1-6 alkyl (preferably --SCH.sub.3);The compounds of Formula I are useful in the treatment of individuals who are HIV positive.Type: GrantFiled: September 21, 1998Date of Patent: September 26, 2000Assignee: Pharmacia & Upjohn CompanyInventors: Joel Morris, Wade J. Adams, Janice M. Friis, Donn G. Wishka
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Patent number: 6114524Abstract: The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group.Type: GrantFiled: June 8, 1999Date of Patent: September 5, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Shigemitsu Okada, Ryosuke Ushijima, Kiyofumi Ishikawa
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Patent number: 6103898Abstract: Cyclic urea derivatives of the formula I ##STR1## in which X, X', Y, Y' and Z can have various meanings, are prepared by a) reacting a urea derivative of the formula II ##STR2## with a diketone of the formula III ##STR3## and b) hydrogenating the product from step a) in the presence of a metal-containing catalyst.Type: GrantFiled: September 28, 1998Date of Patent: August 15, 2000Assignee: BASF AktiengesellschaftInventors: Andreas Kramer, Wolfgang Siegel
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Patent number: 6066734Abstract: Chloropyrimidine compounds, such as 4,6-dichloro-2-ethoxypyrimidine, were prepared in good yield and good purity from the corresponding hydroxypyrimidine compounds in the absence of organic solvents and with a reduced amount of phosphorus oxychloride by carrying out the reaction in the presence of a trialkylamine compound and phosphorus trichloride. The additions of hydroxypyrimidine compound and trialkylamine compound could be made in segments. The chloropyrimidine compounds produced were recovered in an improved manner by adding chlorine to convert the chlorophosphoric acid by-products and phosphorus trichloride to phosphorus oxychloride, diluting the mixture with additional chloropyrimidine compound and removing the phosphorus oxychloride by distillation, combining the residue with water and a base, distilling the trialkylamine compound from the resulting mixture, and removing the aqueous phase.Type: GrantFiled: December 18, 1998Date of Patent: May 23, 2000Assignee: Dow AgroSciences LLCInventors: Ronald B. Leng, Julie L. Maurer, James W. Ringer
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Patent number: 6051580Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: March 2, 1999Date of Patent: April 18, 2000Assignee: Zeneca LimitedInventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi