Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/91)
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Publication number: 20030013707Abstract: The use of a compound comprising formula (I): 1Type: ApplicationFiled: July 6, 2001Publication date: January 16, 2003Inventors: Harold Francis Hodson, Robert Downham, Timothy John Mitchell, Beverley Jane Carr, Christopher Robert Dunk, Richard Michael John Palmer
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Patent number: 6423843Abstract: This invention provides a method for conveniently obtaining a compound of formula (Ia) which is a production intermediate of antimicrobial compounds, in which a salt of optically active acid of formula (IIIa) is obtained by allowing a compound of formula (I), a ketone compound and an optically active acid to react with one another, converted into its free form and then hydrolyzed. In the formula, R1: hydrogen atom or alkyl, aryl or aralkyl group; R2: hydrogen atom or alkyl, aryl, aralkyl, acyl, alkyloxycarbonyl, aralkyloxycarbonyl or substituted sulfonyl; these may further have substituents.Type: GrantFiled: December 15, 2000Date of Patent: July 23, 2002Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Naoki Ohta, Toru Makino, Sadahiro Shimizu
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Patent number: 6413963Abstract: Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.Type: GrantFiled: December 19, 2000Date of Patent: July 2, 2002Assignee: Molecumetics, Ltd.Inventors: Michael Kahn, Masakatsu Eguchi, Hwa-Ok Kim, Marcin Stasiak
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Publication number: 20020040138Abstract: The present invention relates to benzoxazinones of formula I: 1Type: ApplicationFiled: July 31, 2001Publication date: April 4, 2002Inventors: Mona Patel, Joseph Marian Fortunak
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Patent number: 6350745Abstract: Compounds of the invention, useful as thrombin inhibitors and having therapeutic value in for example, preventing coronary artery disease, have the following structure: or a pharmaceutically acceptable salt thereof, wherein A is wherein Y1 and Y2 are independently hydrogen, C1-4 alkyl, C1-4 alkoxy, FuHvC(CH2)0-1 O—, wherein u and v are either 1 or 2, provided that when u is 1, v is 2, and when u is 2, v is 1, C3-7 cycloalkyl, thio C1-4 alkyl, C1-4 sulfinylalkyl, C1-4 sulfonylalkyl, halogen cyano, or trifluoromethyl, and wherein b is 0 or 1.Type: GrantFiled: June 2, 2000Date of Patent: February 26, 2002Assignee: Merck & Co., Inc.Inventors: Craig A. Coburn, Christopher S. Burgey
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Patent number: 6340752Abstract: Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite. Such agents are also employed in the recrystallization and reprocessing of the mercaptoalkanoylamino lactam acids.Type: GrantFiled: December 9, 1998Date of Patent: January 22, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Theodor Denzel, Bang-Chi Chen, James H. Simpson, Rajendra P. Deshpande
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Publication number: 20020006923Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and are selected from the group consisting of: 1Type: ApplicationFiled: March 22, 2001Publication date: January 17, 2002Inventors: James C. Barrow, Bruce D. Dorsey, Harold G. Selnick, Phung L. Ngo
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Patent number: 6306851Abstract: 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: April 19, 2000Date of Patent: October 23, 2001Assignees: American Home Products Corporation, 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: 6303780Abstract: 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 27, 2000Date of Patent: October 16, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Joseph Marian Fortunak, Rodney Lawrence Parsons, Jr., Mona Patel
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Patent number: 6239132Abstract: Compounds of the invention, useful as thrombin inhibitors and having therapeutic value in for example, preventing coronary artery disease, have the following structure: or a pharmaceutically acceptable salt thereof, wherein A isType: GrantFiled: April 18, 2000Date of Patent: May 29, 2001Assignee: Merck & Co., Inc.Inventors: Craig Coburn, Joseph P. Vacca
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Patent number: 6096771Abstract: An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.Type: GrantFiled: February 3, 1999Date of Patent: August 1, 2000Assignee: Sankyo Company, LimitedInventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
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Patent number: 6087358Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic microbes in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial, Clostridium, Cryptosporidium and Helicobacter infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NR.sub.2, where R.sub.2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR.sub.3 or SO.sub.2 R.sub.4 CONR.sub.4 R.sub.5, where R.sub.3, R.sub.4 and R.sub.5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alloxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected from oxygen, CH.sub.2, CO, CR.sub.4 R.sub.5 or NR.sub.4, where R.sub.4 and R.sub.Type: GrantFiled: September 5, 1997Date of Patent: July 11, 2000Assignee: PathoGenesis CorporationInventors: William R. Baker, Cai Shaopei, Eric L. Keeler
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Patent number: 6071860Abstract: Compounds of the formula (I) and salts thereof ##STR1## where R.sup.1 to R.sup.5, A, Z, X, X', n and m are as defined in claim 1 are suitable as herbicides and plant growth regulators.Type: GrantFiled: February 6, 1997Date of Patent: June 6, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Wolfgang Giencke, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6069114Abstract: Compounds of the formula (I) and their salts ##STR1## in which R.sup.1 to R.sup.6, Y.sup.1, to Y.sup.2, Y.sup.3, m and n are as defined in claim 1 are suitable as herbicides and plant growth regulators. They can be prepared analogously to known processes using intermediates of the formula (V) (cf. claim 6).Type: GrantFiled: February 25, 1997Date of Patent: May 30, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Klemens Minn, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6046211Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: May 6, 1998Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5972975Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.Type: GrantFiled: May 22, 1997Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5726126Abstract: There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2, 4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.Type: GrantFiled: November 26, 1996Date of Patent: March 10, 1998Assignee: American Cyanamid CompanyInventors: Alvin Donald Crews, Jr., Philip Mark Harrington, Gary Mitchell Karp, Mark Christopher Manfredi, Michael Anthony Guaciaro
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Patent number: 5714437Abstract: Novel compounds of the formula ?1! are disclosed, wherein X is hydrogen, fluorine or chlorine; Y is fluorine, chlorine or bromine; R.sup.1 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.2 and Q are various groups. Also disclosed are herbicidal compositions containing these compounds as active ingredients and methods for controlling unfavorable weeds by application of these compounds.Type: GrantFiled: August 30, 1995Date of Patent: February 3, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Minoru Takano, Masayuki Enomoto, Kazuo Saito, Satoru Kizawa
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Patent number: 5703075Abstract: This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.Type: GrantFiled: June 7, 1995Date of Patent: December 30, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Ronald B. Gammill, Thomas M. Judge, Joel Morris
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Patent number: 5672599Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.Type: GrantFiled: November 22, 1995Date of Patent: September 30, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5668127Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial and clostridium infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NK.sub.2, where R.sub.2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR.sub.3 or SO.sub.2 R.sub.4 CONR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected CH.sub.2, CO, CR.sub.4 R.sub.5 or NR.sub.4, where R.sub.4 and R.sub.Type: GrantFiled: June 26, 1995Date of Patent: September 16, 1997Assignee: PathoGenesis CorporationInventors: William R. Baker, Cai Shaopei, Eric L. Keeler
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Patent number: 5668278Type: GrantFiled: July 31, 1996Date of Patent: September 16, 1997Assignee: Hoeschst Schering AgrEvo GmbHInventors: Uwe Hartfiel, Gabriele Dorfmeister, Helga Franke, Jens Geisler, Gerhard Johann, Richard Rees
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Patent number: 5665719Abstract: Compounds of the formula ##STR1## X is --O--, --NH-- and --NR.sup.8 --; Y is --CH.sub.2 --, --CHR.sup.8 -- and --C(R.sup.8).sub.2 --; R.sup.1 is camphor-10-yl, C.sub.1-5 alkoxyl, styryl, hydroxystyryl, furyl, unsubstituted or substituted thienyl, naphthyl, indolyl, tetrahydronaphthyl, unsubstituted, mono- or di-substituted pyridyl, pyrazinyl, unsubstituted or substituted cyclohexyl where the substituent is R.sup.4, and unsubstituted or substituted phenyl where the substituents on phenyl are R.sup.5, R.sup.6 and R.sup.7 ; R.sup.2 is hydrogen, C.sub.1-5 alkoxy, C.sub.1-5 alkyl, amino, C.sub.1-5 alkylcarbonylamino, nitro or halogen; R.sup.3 is hydrogen, C.sub.1-5 alkoxycarbonyl, cyano or carbamoyl; R.sup.4 is one to two of hydrogen, oxo, hydroxy, C.sub.1-5 alkoxy, C.sub.1-5 alkoxycarbonylamino-C.sub.1-5 alkyl and amino-C.sub.1-5 alkyl; R.sup.5, R.sup.6 are each independently selected from hydrogen, halogen, C.sub.1-5 alkyl, hydroxyl and C.sub.1-5 alkoxy; R.sup.7 is ##STR2## W is CO or SO.sub.Type: GrantFiled: June 6, 1995Date of Patent: September 9, 1997Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Ben E. Evans, Peter D. Williams, Roger M. Freidinger, Douglas J. Pettibone, Doug W. Hobbs, Paul S. Anderson
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Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5627278Abstract: A process for preparing compounds of the formula ##STR1## wherein X is O or S; n is one or two; m is zero or one; Y is CH.sub.2, O, or S provided that Y is O or S only when m is one; and A is ##STR2## is disclosed. Also disclosed are processes for preparing the corresponding amino intermediates.Type: GrantFiled: January 4, 1996Date of Patent: May 6, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5571773Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: June 2, 1995Date of Patent: November 5, 1996Assignee: American Cyanamid CompanyInventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
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Patent number: 5534483Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: June 2, 1995Date of Patent: July 9, 1996Assignee: American Cyanamid CompanyInventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
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Patent number: 5508272Abstract: Compounds of the formula ##STR1## wherein X is O or S--(O).sub.t ; n is one or two; m is zero or one; Y is CH.sub.2, O, or S--(O).sub.t provided that Y is O or S--(O).sub.t only when m is one; and A is ##STR2## are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors. Also disclosed are methods of preparation and intermediates.Type: GrantFiled: May 5, 1994Date of Patent: April 16, 1996Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 5472960Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl,Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.Type: GrantFiled: August 16, 1994Date of Patent: December 5, 1995Assignee: Nihon Bayer Agrochem K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 5405829Type: GrantFiled: June 13, 1994Date of Patent: April 11, 1995Assignee: Schering AktiengesellschaftInventors: Uwe Hartfiel, Gabriele Dorfmeister, Helga Franke, Jens Geisler, Gerhard Johann, Richard Rees
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Patent number: 5373007Abstract: The invention concerns a bicyclic heterocyclic compound of the formula I ##STR1## wherein Q is an optionally substituted 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's and a further O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which,together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: March 25, 1994Date of Patent: December 13, 1994Assignees: Zeneca Limited, Pharma ZenegaInventors: Pierre A. R. Bruneau, Graham C. Crawley
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Patent number: 5342942Abstract: Pyrazolo[5,1-b]quinazoline compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for treating neurodegenerative disorders, tumors of neuronal origin, inflammation, allergy, and pain, and methods for screening compounds that interact with the neurotrophic receptors using said compositions are disclosed.Type: GrantFiled: March 29, 1993Date of Patent: August 30, 1994Assignee: Warner-Lambert CompanyInventors: Juan C. Jaen, Bradley W. Caprathe
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Patent number: 5294611Abstract: The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R.sup.6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: April 23, 1993Date of Patent: March 15, 1994Assignee: American Cyanamid CompanyInventors: Aranapakam M. Venkatesan, Jeremy I. Levin
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Patent number: 5252734Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 - alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.Type: GrantFiled: February 5, 1992Date of Patent: October 12, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Andreas Krebs, Uwe Petersen, Thomas Schenke, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5141551Abstract: A benzoxazine derivative and a benzothiazine derivative having the formula (I): ##STR1## wherein A is N or a CH group;B is O, S, and SO group or an SO.sub.2 group;W is O, S, a CR.sup.4 R.sup.5 group or an NR.sup.4 group wherein R.sup.4 and R.sup.5 are each independently a hydrogen atom, a CN group or an NO.sub.2 group;X, Y and Z are each independently a hydrogen atom, a halogen atom or a lower haloalkyl group having 1 to 3 carbon atoms;R.sup.1 is a hydrogen atom, a lower alkyl group having 1 to 5 carbon atoms, a lower alkenyl group having 2 to 5 carbon atoms, a lower alkynyl group having 2 to 5 carbon atoms, a lower hydroxyalkyl group having 1 to 5 carbon atoms or a lower haloalkyl group having 1 to 3 carbon atoms; andR.sup.2 and R.sup.3 are each independently a hydrogen atom, a lower alkyl group having 1 to 5 carbon atoms or an aryl group having 6 to 10 carbon atoms and a herbicidal composition containing the compound of the formula (I) as an active ingredient.Type: GrantFiled: December 21, 1990Date of Patent: August 25, 1992Assignee: Suntory LimitedInventors: Naoko Kawaguchi, Harukazu Fukami, Shinjiro Niwata, Ryuichi Sago, Fumio Fujita
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Patent number: 5140033Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.Type: GrantFiled: October 1, 1990Date of Patent: August 18, 1992Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Andreas Krebs, Uwe Petersen, Thomas Schenke, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5017212Abstract: A compound of the general formula: ##STR1## wherein Q is a condensed heterocyclic group having an N atom in the bridgehead which may be substituted, W is O or S, R.sub.1 and R.sub.2 each are an alkyl group, an alkoxy group or halogen and Z is CH or N, and a salt thereof, which is useful as a herbicide.Type: GrantFiled: March 17, 1987Date of Patent: May 21, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuo Ishida, Kazunari Ohta, Tatsuo Nakahama, Harutoshi Yoshikawa
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Patent number: 4990517Abstract: 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1, and addition products thereof.Type: GrantFiled: June 30, 1989Date of Patent: February 5, 1991Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Thomas Schenke, Andreas Krebs, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 4950670Abstract: A pyrimidinedione derivative which is a compound of formula (I): ##STR1## in which: R1 denotes hydrogen, a halogen, a methyl group or a methoxy group,R2 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a benzyl group,n denotes 2, 3 or 4,X denotes a CH group or nitrogen, andR3 denotes hydrogen, a halogen or a methoxy group when X denotes a CH group, with the proviso that R3 denotes hydrogen when X denotes nitrogen,or a pharmacologically acceptable acid addition salt thereof.Type: GrantFiled: May 16, 1989Date of Patent: August 21, 1990Assignee: SynthelaboInventors: Jonathan Frost, Bernard Gaudilliere, Jean Rousseau, Regis Dupont, Philippe Manoury, Daniel Obitz
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Patent number: 4927820Abstract: There are disclosed compounds having the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl or arylloweralkyl;Z is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethyl;Y is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or arylloweralkyl; andX is CR.sub.3, CHR.sub.3, C.dbd.O, C.dbd.S or CHN(CH.sub.3).sub.2, R.sub.3 being hydrogen, loweralkyl or aryl;stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.Type: GrantFiled: November 25, 1988Date of Patent: May 22, 1990Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 4846874Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene- , furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide. 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: December 16, 1987Date of Patent: July 11, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4829066Abstract: This invention relates to substituted pyridooxazinone pyridazinone and pyrazolone compounds, which are useful as cardiotonic agents for the treatment of congestive heart failure. This invention also relates to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including said compound.Type: GrantFiled: May 8, 1987Date of Patent: May 9, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla
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Patent number: 4822794Abstract: This invention relates to substituted pyridooxazinone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.Type: GrantFiled: May 8, 1987Date of Patent: April 18, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Alfred P. Spada, William L. Studt, Henry F. Campbell, Donald E. Kuhla
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Patent number: 4822878Abstract: Novel chromophor derivatives of cyclic anhydrides are provided which have the ability to react with a variety of organic substrates forming adducts which are useful in analytical techniques for the detection and measurement of biological compounds.Type: GrantFiled: May 27, 1988Date of Patent: April 18, 1989Assignee: Viomedics, Inc.Inventor: Spyros Theodoropulos
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Patent number: 4760063Abstract: Novel thienooxazines of the formula ##STR1## in which R.sup.1 and R.sup.2, together with the adjacent C atoms, represent an optionally substituted thiophene ring,R.sup.3 represents hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl or aryl, andR.sup.4 represents optionally substituted alkyl, cycloalkyl, alkenyl or aryl, orR.sup.3 and R.sup.4, together with the adjacent nitrogen atom, form a saturated heterocyclic structure which may optionally contain further hetero atoms,promote the yield of animals, e.g. rate of growth, ratio of meat to fat, etc. They are made from new intermediates of the formulas ##STR2## in which R.sup.5 and R.sup.6 may be hydrogen or various organic radicals, or together form a ring.Type: GrantFiled: November 12, 1986Date of Patent: July 26, 1988Assignee: Bayer AktiengsellschaftInventors: Werner Hallenbach, Hans Lindel, Friedrich Berschauer, Martin Scheer, Anno de Jong
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Patent number: 4737184Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: May 10, 1985Date of Patent: April 12, 1988Assignee: E. I. Du Pont De Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4726837Abstract: 4H-Pyrido[2,3-d][1,3]oxazin-4-one derivatives of the formula ##STR1## where Y is oxygen or sulfur and R is phenyl which is unsubstituted or substituted by halogen, haloalkyl, haloalkoxy, haloalkylmercapto, haloalkylsulfinyl or haloalkylsulfonyl, are used for controlling undesirable plant growth.Type: GrantFiled: July 30, 1985Date of Patent: February 23, 1988Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Juergen Varwig, Bruno Wuerzer, Norbert Meyer