Chalcogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/312)
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Patent number: 6846828Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.Type: GrantFiled: November 6, 2002Date of Patent: January 25, 2005Assignee: Roche Palo Alto LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Publication number: 20040248739Abstract: Compounds of formula (I), wherein the substituents R1, R2, R3, R4 and Z and the suffixes n and m are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomers of those compounds are suitable for use as herbicides.Type: ApplicationFiled: July 14, 2004Publication date: December 9, 2004Inventors: Jurgen Schaetzer, Martin Eberle, Jean Wenger, Sabine Berteina-Raboin, Kurt Nebel, Andre Stoller, Roger Graham Hall, Steven Scott Bondy, Daniel Dennis Comer, Julie Elizabeth Penzotti, Peter Diederik Jan Grootenhuis
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Publication number: 20040235908Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: June 16, 2004Publication date: November 25, 2004Applicant: Schering CorporationInventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jonathan A. Pachter, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
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Patent number: 6818775Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: December 9, 2003Date of Patent: November 16, 2004Assignee: Allergan, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6800650Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: February 11, 2003Date of Patent: October 5, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Markus Boehringer, Bernd Michael Loeffler, Jens-Uwe Peters, Claus Riemer, Peter Weiss
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Patent number: 6790866Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: July 30, 2002Date of Patent: September 14, 2004Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Patent number: 6784294Abstract: A process for making an N1-(2′-pyridyl)-1,2-alkanediamine sulfamic acid of formula II by reacting a compound of formula I with NH2R′ wherein R and R′ are as defined in the specification. The invention also includes the compound of formula II, and optical isomers thereof. The compound of formula II is an intermediate useful for making chiral piperazine derivatives which are active at the 5-HT1A receptor.Type: GrantFiled: March 10, 2003Date of Patent: August 31, 2004Assignee: WyethInventors: Anita Wai-Yin Chan, Gregg Brian Feigelson, Joseph Zeldis, Ivo Jirkovsky
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Patent number: 6747048Abstract: Novel pyridine-based thyroid receptor ligands are provided which have the general formula I wherein: X is oxygen (—O—), sulfur (—S—), sulfoxide (—S(O)—), sulfonyl (—SO2—), CR8R8 or NR8; Y is —NR8, oxygen (—O—), —CH2— or sulfur (—S—); Z is a bond or substituted or unsubstituted C1-4 alkyl; and wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: May 7, 2003Date of Patent: June 8, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Minsheng Zhang, Jon Hangeland, Yolanda Caringal, Todd Friends
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Patent number: 6706920Abstract: An antistatic composition comprises (a) at least one ionic salt consisting of a nonpolymeric nitrogen onium cation and a weakly coordinating fluoroorganic anion, the conjugate acid of the anion being a superacid; and (b) at least one thermoplastic polymer. The composition exhibits good antistatic performance over a wide range of humidity levels.Type: GrantFiled: December 28, 2001Date of Patent: March 16, 2004Assignee: 3M Innovative Properties CompanyInventors: William M. Lamanna, Thomas P. Klun, Kathleen A. Hachey, Alan D. Fanta
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Patent number: 6696456Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, R4, R5, R6, G and Z have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.Type: GrantFiled: October 13, 2000Date of Patent: February 24, 2004Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Norman Eugene Ohler, Kelly Michelle Solinsky, Neil Gregory Almstead, Biswanath De, Michael George Natchus
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6670376Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 12, 2002Date of Patent: December 30, 2003Assignee: Theravance, Inc.Inventors: Edmund J. Moran, John R. Jacobsen, Michael R. Leadbetter, Matthew B. Nodwell, Sean G. Trapp, James Aggen, Timothy J. Church
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Patent number: 6653311Abstract: We have synthesized a series of new derivatives of (2-azinylamino) quinone, that have the general formula shown below. Several compounds of this new series of derivatives have been shown to be inhibitors of 5-lipoxygenase, with minimal or no effect on cycloxygenase-1 and 2-(COX-1 and COX-2) activity. where: A is N, CH, or, CCl; B is N, CH, CCH3, or Cph; X is H, Cl, Br, or I; Y is H, or CH3; R1 is H, CH3, OCH3, or Ph; and R2 is H, CH3, OCH3, or Ph; or R1—R2 is (CH═CH)2; and R3 is H or CH3.Type: GrantFiled: June 25, 2002Date of Patent: November 25, 2003Assignees: Board of Supervisors of Louisiana State University, Agricultural and Mechanical CollegeInventors: Nicholas G. Bazan, Carlos Sunkel, Julio Alvarez Builla-G.
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Patent number: 6645991Abstract: The invention describes novel compounds of the formula I which are biologically active as ligands of integrin &agr;v&bgr;3 X—Y—Z—R1—CH2—R2(R4)—CH2—CO—R5 in which X, Y, Z, R1, R2, R4 and R5 are as defined in claim 1, and their physiologically acceptable salts and solvates.Type: GrantFiled: June 21, 2002Date of Patent: November 11, 2003Assignee: Merck Patent GmbHInventors: Alfred Jonczyk, Oliver Schadt, Simon Goodman
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Patent number: 6632823Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.Type: GrantFiled: December 22, 1997Date of Patent: October 14, 2003Assignee: Merck & Co., Inc.Inventors: Jean-Michel Vernier, Nicholas D. P. Cosford, Ian A. McDonald
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Patent number: 6610701Abstract: Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.Type: GrantFiled: February 8, 2002Date of Patent: August 26, 2003Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Craig Coburn, Harold G. Selnick, Phung L. Ngo
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Publication number: 20030158218Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: 1Type: ApplicationFiled: December 6, 2002Publication date: August 21, 2003Inventors: Philippe G. Nantermet, Harold G. Selnick, James C. Barrow, Craig Coburn, Christopher Burgey, Kyle A. Robinson, Terry Alan Lyle
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Patent number: 6593472Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.Type: GrantFiled: July 12, 2001Date of Patent: July 15, 2003Assignee: Hoffman-La Roche Inc.Inventors: Torsten Hoffmann, Sonia Maria Poli, Patrick Schnider, Andrew Sleight
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Patent number: 6589967Abstract: The present invention relates to novel oxime O-ether compounds represented by a general formula [I]; wherein R1 represents C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, etc., m represents an integer of 1 to 4, R2 represents hydrogen atom, C1-6 alkyl, etc., R3 and R4 each independently represents hydrogen atom or C1-6 alkyl, etc., R5 represents hydrogen atom, C1-6 alkyl, etc., R6 represents C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, Halogen atom, etc. and n represents an integer of 1 to 4, and a fungicide for agricultural and horticultural use comprising the compound as the active ingredient.Type: GrantFiled: May 6, 2002Date of Patent: July 8, 2003Assignee: Nippon Soda Co. Ltd.Inventors: Hiroshi Sano, Tadashi Sugiura, Yuuki Nakagawa, Hiroshi Hamamura, Akira Mitani, Takahiro Ando
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Patent number: 6586433Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-heteroaryl-N-phenyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: July 1, 2003Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20030107027Abstract: A nonlinear optical chromophore having the formula D-&pgr;-A, wherein &pgr; is a &pgr; bridge including a thiophene ring having oxygen atoms bonded directly to the 3 and 4 positions of the thiophene ring, D is a donor, and A is an acceptor.Type: ApplicationFiled: November 22, 2002Publication date: June 12, 2003Inventors: Diyun Huang, Baoquan Chen
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Patent number: 6576643Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 17, 2001Date of Patent: June 10, 2003Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, William H. Miller, Dirk Heerding, James M. Samanen
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Patent number: 6562080Abstract: Primary intermediates useful hair coloring systems comprise 2-arylaminomethyl-4-aminophenols. The invention provides new 2-arylaminomethyl-4-aminophenol compounds of Formula (1): wherein R is a moiety selected from formulae (2), (3) or (4) wherein R1, R2, R3, R4 and R5 are each independently selected from a hydrogen atom, a halogen atom, a hydroxy group, an amino group, a C1-C6 alkyl or haloalkyl group, a C1-C6 alkoxy or haloalkoxy group, and a nitrile group, and R6 is a hydrogen atom, a halogen atom, a C1-C4 alkyl or a C1-C4 alkoxy group.Type: GrantFiled: August 15, 2001Date of Patent: May 13, 2003Assignee: Clairol IncorporatedInventors: Mu-III Lim, Yuh-Guo Pan
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Publication number: 20030078235Abstract: Carbamate compounds of 2-heteroaryl-1,2-ethanediol are described. The compounds are effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.Type: ApplicationFiled: June 21, 2002Publication date: April 24, 2003Inventors: Yong-Moon Choi, Ki-Ho Lee
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Patent number: 6531494Abstract: The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;V&bgr;3 and/or the &agr;V&bgr;5 integrin.Type: GrantFiled: August 29, 2001Date of Patent: March 11, 2003Assignee: Pharmacia CorporationInventors: Ish Kumar Khanna, Yi Yu, Balekudru Devadas, Hwang-Fun Lu, Nizal S Chandrakumar, Renee M. Huff, Bipinchandra N. Desai, Srinivasan Raj Nagarajan, Alan F. Gasiecki, Thomas D. Penning, Mark A. Russell, Mark L. Boys, Lori A. Schretzman, Barbara B. Chen, Thomas Rogers, John Adam Wendt, Albert Khilevich, Yaping Wang
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Patent number: 6492515Abstract: The present invention relates to benzoxazinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.Type: GrantFiled: July 31, 2001Date of Patent: December 10, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Joseph Marian Fortunak, Mona Patel
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Patent number: 6482840Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: May 21, 2001Date of Patent: November 19, 2002Assignee: Merck & Co., Inc.Inventors: William K. Hagmann, George A. Doherty, Shrenik Shah
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Patent number: 6482860Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: GrantFiled: July 18, 1997Date of Patent: November 19, 2002Assignee: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Publication number: 20020143024Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 14, 2000Publication date: October 3, 2002Inventors: Natesan Murugesan, John E. Tellew, Jhon E. Macor, Zhengxiang Gu
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Patent number: 6448290Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: June 18, 1999Date of Patent: September 10, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Publication number: 20020123632Abstract: Substituted anthranilic acids of the formula I 1Type: ApplicationFiled: December 6, 2001Publication date: September 5, 2002Inventors: Andreas Weichert, Hans-Willi Jansen, Heinz-Werner Kleemann, Hans-Jochen Lang, Hartmut Rutten
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Patent number: 6432990Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.Type: GrantFiled: January 30, 2002Date of Patent: August 13, 2002Assignee: Dow AgroSciences LLCInventors: Emily J. Canada, Carl P. Denny, Christopher S. Galka, Neil V. Kirby, Marc McKennon, Mary E. Pieczko, Rebecca L. Rezac, Brent J. Rieder, John K. Swayze, Chrislyn M. Carson, David D. Johnson, Gregory M. Kemmitt
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Patent number: 6432962Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.Type: GrantFiled: May 21, 2001Date of Patent: August 13, 2002Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Anne Marie Horneman
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Patent number: 6420396Abstract: The present invention relates to 2-Mesitylsulfonylamino-3-{3′[(pyridinylamino)methyl][1,1-biphenyl]-4-yl}propanoic acid, pharmaceutical compositions thereof, their preparation, their use in the treatment of cancer, arteriosclerosis, restenosis, osteolytic disorders, ophthalmic disorders, and their use as integrin antagonists.Type: GrantFiled: December 15, 1999Date of Patent: July 16, 2002Assignee: Beiersdorf AGInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6413987Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.Type: GrantFiled: June 6, 2000Date of Patent: July 2, 2002Assignee: Bridge Pharma, Inc.Inventors: A. K. Gunnar Aberg, George E. Wright, Jan L. Chen
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Patent number: 6407247Abstract: A method of using compounds of formula I in which the C═C double bond is present in E and/or Z configuration and the variables have the following meanings: R1 denotes COOR5, COR5, CONR5R6, CN, O═S(—R5)═O, O═S(═OR5)═O, R7O—P(—OR8)═O; R2 denotes COOR6, COR6, CONR5R6, CN, O═S(—R6)═O, O═S(═OR6)═O, R7O—P(—OR8)═O; R3 denotes hydrogen, an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical having in each case up to 18 carbon atoms; R4 denotes an optionally substituted aromatic or heteroaromatic radical containing from 5 to 12 ring atoms; R5 to R8 independently denote hydrogen, an open-chain or branched-chain aliphatic, araliphatic, cycloaliphatic or optionally substituted aromatic radical containing in each case up to 18 carbon atoms, where the variables R3 to R8 may also form, together with the carbon atoms to which they are attached, a 5-membered or 6-memberedType: GrantFiled: January 31, 2000Date of Patent: June 18, 2002Assignee: BASF AktiengesellschaftInventors: Thorsten Habeck, Alexander Aumüller, Volker Schehlmann, Horst Westenfelder, Thomas Wünsch
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Patent number: 6380258Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 24, 1999Date of Patent: April 30, 2002Assignee: G. D. Searle, L.L.C.Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
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Publication number: 20020045642Abstract: Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.Type: ApplicationFiled: July 12, 2001Publication date: April 18, 2002Inventors: Torsten Hoffmann, Sonia M. Poli, Patrick Schnider, Andrew Sleight
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Publication number: 20020045757Abstract: A process is provided for preparing a compound of the formula: 1Type: ApplicationFiled: July 24, 2001Publication date: April 18, 2002Inventor: Robert W. Scott
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Patent number: 6362205Abstract: Described are substituted cyanoenamines of formula I wherein Z, R1, R2 and R3 are defined in the description, compositions thereof and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.Type: GrantFiled: March 16, 2001Date of Patent: March 26, 2002Assignee: Novo Nordisk A/SInventors: John Bondo Hansen, Tina Moller Tagmose, John Patrick Mogensen, Florencio Zaragoza Dorwald, Anker Steen Jorgensen
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Patent number: 6337306Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.Type: GrantFiled: November 5, 1999Date of Patent: January 8, 2002Assignee: Rhone-Poulenc AgroInventors: Norio Sasaki, Atsushi Go, Hideshi Mukaida, Yukiko Oe
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Patent number: 6316632Abstract: A process for preparing 2-phenyl-3-aminopyridine, and substituted phenyl derivatives and salts thereof.Type: GrantFiled: May 11, 2000Date of Patent: November 13, 2001Assignee: Pfizer IncInventors: Tamim F. Braish, Stephane Caron, Michael James Castaldi
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Patent number: 6303787Abstract: This invention relates to an improved process for the preparation of Omeprazole of the formula-I starting from 4-nitro-2,3,5-trimethylpyridine-N-oxide and through novel intermediates 2-hydroxymethyl-3,5-dimethyl-4-nitro pyridine of the formula II and novel 2-chloromethyl-3,5-dimethyl-4-nitro pyridine of the formula III. This invention also relates to processes for the preparation of the above said novel intermediates. Omeprazole is one of the world's widely used drugs for the treatment of ulcer diseases. This compound acts by irreversible inhibition of the H+ K+ ATPase enzyme, which is part of the proton pump located in the parietal cell of the stomach wall.Type: GrantFiled: October 26, 1999Date of Patent: October 16, 2001Assignee: Natco Pharma LimitedInventor: Konakanchi Durga Prasad
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Patent number: 6297197Abstract: 4-Aminopicolinic acids, having halogen, alkoxy, alkylthio, aryloxy, heteroaryloxy or trifluoromethyl substituents in the 3-, 5- and 6-positions, and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.Type: GrantFiled: January 12, 2001Date of Patent: October 2, 2001Assignee: Dow AgroSciences LLCInventors: Stephen Craig Fields, Anita Lenora Alexander, Terry William Balko, Leslie Anne Bjelk, Ann Marie Buysse, Renee Joan Keese, Karl Leopold Krumel, William Chi-Leung Lo, Christian Thomas Lowe, John Sanders Richburg, III, James Melvin Ruiz
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Patent number: 6297249Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.Type: GrantFiled: December 2, 1999Date of Patent: October 2, 2001Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, Michael A. Patane
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Patent number: 6294580Abstract: A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or —NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) —MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or —NR2 wherein R2 represents hydrogen or C1-3alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3alkyl; and (vii) HType: GrantFiled: August 25, 1998Date of Patent: September 25, 2001Assignee: Glaxo Wellcome Inc.Inventors: Timothy Mark Willson, Robert Anthony Mook, Istvan Kaldor, Brad Richard Henke, David Norman Deaton, Jon Loren Collins, Jeffrey Edmond Cobb, Marcus Brackeen, Matthew Jude Sharp, John Mark O'Callaghan, Greg Alan Erickson, Grady Evan Boswell
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Patent number: 6291489Abstract: This invention relates to processes for preparing compounds of the formula (I) and to processes for preparing certain intermediates of the formula wherein R1 is nitro, amino or protected amino; R2 is H, fluoro, chloro CF3, nitro, (C1-C4)alkyl, (C1-C4)alkoxy, amino or protected amino; and X1 is OH or a suitable leaving group, used in that process. The invention also relates novel to compounds of the formulae (II).Type: GrantFiled: May 5, 1999Date of Patent: September 18, 2001Assignee: Pfizer Inc.Inventors: Keith M DeVries, Robert L. Dow, Stephen W. Wright
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Publication number: 20010018523Abstract: The present invention provides compounds having the Formula I 1Type: ApplicationFiled: April 13, 2001Publication date: August 30, 2001Inventors: Helen Tsenwhei Lee, Randy Ranjee Ramharack, Bruce David Roth, Karen Elaine Sexton
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Publication number: 20010007031Abstract: It has been found that one of the enantiomers of 8-aminoquinoline antiparasitic compounds is surprisingly more active than the other enantiomer against parasitic infections including opportunistic parasitic infections. These enantiomers as well as pharmaceutical compositions containing pure enantiomers are disclosed. Also disclosed is a novel class of 8-aminoquinolines which contain a tri-substituted phenoxy substitution.Type: ApplicationFiled: June 15, 1999Publication date: July 5, 2001Inventors: JAMES MCCHESNEY, DHAMMIKA N. NANAYAKKARA, MARILYN BARTLETT, ARBA L. AGER
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Patent number: 6239138Abstract: Compounds of the formula (I): are vitronectin receptor antagonists useful in the treatment of osteoporosis.Type: GrantFiled: December 8, 1999Date of Patent: May 29, 2001Assignee: SmithKline Beecham CorporationInventor: Thomas W. Ku