Benzene Ring Containing Patents (Class 564/237)
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Publication number: 20020137968Abstract: Benzoic acid derivatives of the formula I 1Type: ApplicationFiled: October 10, 2001Publication date: September 26, 2002Inventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss
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Patent number: 6436999Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 18, 1997Date of Patent: August 20, 2002Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Patent number: 6420556Abstract: The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetranikylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.Type: GrantFiled: June 12, 2001Date of Patent: July 16, 2002Assignee: The Procter & Gamble CompanyInventor: Lawrence Joseph Wilson
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Patent number: 6369110Abstract: A compound represented by the general formula (1): wherein each of R1, R2, R3, R4 and R5 is a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, an aromatic group, an acyl group or the like; each of Y1, Y2, Y3 and Y4 is a single bond, —CH2—, —O—, —CO— or the like, provided that at least two of Y1 through Y4 are independently a group other than a single bond; and Z may be absent, or one or more Zs may be present and are independently an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a saturated heterocyclic group, a halogen atom, a carboxyl group, an alkoxycarbonyl group, an aromatic group, an acyl group or the like, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton exchange transport system.Type: GrantFiled: November 27, 2000Date of Patent: April 9, 2002Assignee: Sumitomo Pharmaceuticals CompanyInventors: Masahumi Kitano, Naohito Ohashi
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Patent number: 6346527Abstract: A compound of the formula: wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)amino, sulfamoylamino, (dimethylsulfamoyl)amino, N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, lower alkoxyimino(lower)alkyl, acyl, lower alkoxycarbonyl, carbamoyl, di(lower)alkylcarbamoyl, (amino(lower)alkyl)carbamoyl, N,N-di(lower)alkylamino(lower)alkylcarbamoyl, guanidinocarbonyl, morpholinylsulfonyl, sulfamoyl, lower alkylsulfamoyl, (lower alkylsulfonyl)(lower)alkyl, guanidinocarbonyl(lower)alkenyl, lower alkylthio, cyano, acyl(lower)alkyl, acyl(lower)alkenyl, aryl which has one or more substituent(s) or a heterocyclic group which has one or more substituent(s), and X is —O—, or a salt thereof.Type: GrantFiled: October 24, 2000Date of Patent: February 12, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kohei Takenaka, Yoshikazu Inoue, Masatoshi Minagawa, Atsushi Akahane
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Patent number: 6288123Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: September 11, 2001Assignee: Cambridge NeuroSciences, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Publication number: 20010014699Abstract: The invention relates to a compound of formula (1), 1Type: ApplicationFiled: December 22, 2000Publication date: August 16, 2001Inventors: Thomas Allmendinger, Walther Helmut Wernsdorfer
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Patent number: 6251948Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.Type: GrantFiled: June 6, 1995Date of Patent: June 26, 2001Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 6235934Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.Type: GrantFiled: December 17, 1998Date of Patent: May 22, 2001Assignee: General Electric CompanyInventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
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Patent number: 6218426Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.Type: GrantFiled: March 1, 1999Date of Patent: April 17, 2001Assignee: Agouron Pharmaceuticals, Inc.Inventors: Mark Brian Anderson, Alexander Polinsky, Yufeng Hong, Vlad Edward Gregor
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Patent number: 6204384Abstract: The present invention provides peptide aldehydes having an 3-amino-2-hydro yenyl acetamide group as part of the peptide backbone d an arginine group or analog at P1. These compounds e potent and specific or inhibitors of thrombin. Ther pharmaceutically acceptable salts, pharmaceutic ly acceptable compositions thereof, and methods of using t as therapeutic agents for disease states in mammals charachterized by abnormal thrombosis are also described. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having in history activity towards proteases of the trypsin/chymotrypsin class.Type: GrantFiled: November 26, 1997Date of Patent: March 20, 2001Assignee: Corvas International, Inc.Inventors: Joseph Edward Semple, Marguerita S. Lim-Wilby, Terence K. Brunck
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Patent number: 6187955Abstract: A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof wherein each of A and B is a C2-C8 alkylene, D is a single bond, —CO— or a C1-C6 alkylene, E is H, a lower alkyl or the like, m is 1 to 6, n is 0 to 6 and R1 is H, a lower alkyl or the like, 1 is 1 to 10 and G is H, —OH or the like and a skin cosmetic containing the same. It can exert excellent keratin layer softening effect continuously for a long period of time.Type: GrantFiled: November 6, 1997Date of Patent: February 13, 2001Assignee: Kao CorporationInventors: Minoru Nagai, Hiromitsu Kawada, Mayumi Tsuchiya, Seiji Yamasaki, Akira Yamamuro, Toshiya Ono
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Patent number: 6174924Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: January 16, 2001Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6166239Abstract: Compounds of the invention having general formula ##STR1## are useful reagents for protecting amine, guanidine, amidine or hydroxyl groups during organic synthesis. In particular, compounds are useful during oligonucleotide synthesis to protect nucleobase amines as well as tethered amines used for attaching functional moieties to oligonucleotides.Type: GrantFiled: September 4, 1998Date of Patent: December 26, 2000Assignee: Isis Pharmaceuticals, Inc.Inventor: Muthiah Manoharan
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Patent number: 6166088Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: September 9, 1999Date of Patent: December 26, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica Kochanny, Raju Mohan, Michael M. Morrissey, Howard P. Ng, Weiya Yun
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Patent number: 6156800Abstract: There are described benzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m, R(5)R(6)N--SO.sub.2 --; O.sub.p --(CH.sub.2).sub.q --(CF.sub.2).sub.r --CF.sub.3 ; --SR(10), --OR(10) or --CR(10)R(11)R(12); R(2) is --(CH.sub.2).sub.u --(CF.sub.2).sub.t --CF.sub.3 ; R(3) is hydrogen or independently defined as R(1); and their pharmaceutically tolerable salts. They are obtained by reaction of a compound of the formula II ##STR2## with guanidine. They are compounds of outstanding activity on the cardiovascular system.Type: GrantFiled: June 22, 1998Date of Patent: December 5, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Wolfgang Scholz, Udo Albus
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Patent number: 6143932Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.Type: GrantFiled: July 1, 1999Date of Patent: November 7, 2000Assignee: Trega Biosciences, Inc.Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
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Patent number: 6121489Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.Type: GrantFiled: March 5, 1997Date of Patent: September 19, 2000Assignee: Trega Biosciences, Inc.Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
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Patent number: 6118007Abstract: A process, as a substitute for hydrolysis, for preparing a nitroguanidine derivative represented by the following formula (2): ##STR1## wherein A represents a substituted or unsubstituted aromatic or non-aromatic hydrocarbon ring, a substituted or unsubstituted aromatic or non-aromatic heterocycle, a hydrogen atom or a substituted or unsubstituted alkyl, alkenyl or alkynyl group; and R.sub.2 represents a hydrogen atom, a substituted or unsubstituted C.sub.1-6 alkyl, alkenyl or alkynyl group, which comprises reacting a compound represented by the following formula (1): ##STR2## wherein R.sub.1 represents a substituted or unsubstituted, linear or cyclic C.sub.1-10 alkyl group and A and R.sub.2 have the same meanings as defined above, with ammonia, a primary amine or a secondary amine, or a salt thereof.Type: GrantFiled: March 24, 1998Date of Patent: September 12, 2000Assignee: Mitsui Chemicals, Inc.Inventors: Koichi Ebihara, Tatsuo Kaiho, Michihiko Miyamoto, Daisuke Ura
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Patent number: 6114392Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.Type: GrantFiled: April 16, 1996Date of Patent: September 5, 2000Inventors: Gad M. Gilad, Varda H. Gilad
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Patent number: 6075054Abstract: Benzoylguanidines of formula I ##STR1## with R(1) to R(4) as defined in the specification, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and infarct treatment as well as for the treatment of angina pectoris.They inhibit, in a preventive manner, the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: February 24, 1998Date of Patent: June 13, 2000Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 6013675Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: January 11, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 6011059Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R.sup.5 wherein R.sup.5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and where X is N, R.sup.1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above acyl guanidines.Type: GrantFiled: November 23, 1998Date of Patent: January 4, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Karnail S. Atwal, Sundeep Dugar
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Patent number: 5998481Abstract: There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system.Type: GrantFiled: February 24, 1998Date of Patent: December 7, 1999Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5955507Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: September 21, 1999Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 5922772Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: July 13, 1999Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 5883133Abstract: Compounds of the formula I ##STR1## are described in which at least one of the substituents R(1), R(2), R(3), R(4) and R(5) is a nitrogen-containing heterocyclic radical. They are outstanding cardiovascular therapeutic agents. They are obtained by reaction of a compound II ##STR2## with guanidine.Type: GrantFiled: July 24, 1996Date of Patent: March 16, 1999Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Andreas Weichert, Udo Albus, Wolfgang Scholz
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Patent number: 5856344Abstract: Benzoylguanidines of the formula I ##STR1## in which R(1) to R(6) have the meanings stated in the claims, are antiarrhythmic pharmaceuticals which have excellent activity and a cardioprotective component and are highly suitable for the prophylaxis of infarcts and the treatment of infarcts, and for the treatment of angina pectoris, in which case they also preventively inhibit or greatly reduce the pathophysiological processes in the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.Type: GrantFiled: October 31, 1996Date of Patent: January 5, 1999Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
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Patent number: 5847006Abstract: The present invention provides N,N'-diaryl substituted guanidines having therapeutic utility. The compounds of the present invention are represented by the formula: ##STR1## wherein R and R.sup.1 represent hydrogen or other group and Ar and Ar.sup.1 represent selected aryl groups, and at least one being acenaphthyl.Type: GrantFiled: May 31, 1995Date of Patent: December 8, 1998Assignee: Cambridge NeuroScience, Inc.Inventors: Sharad Magar, Graham J. Durant, Lain-Yen Hu, Stanley M. Goldin, N. Laxma Reddy, James B. Fischer, Subbarao Katragadda, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 5830917Abstract: There is disclosed a novel amino alcohol amine derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.Type: GrantFiled: September 11, 1995Date of Patent: November 3, 1998Assignee: G. D. Searle & Co.Inventors: William M. Moore, E. Ann Hallinan
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Patent number: 5807896Abstract: Arylbenzoylguanidines of the formula I ##STR1## in which R.sup.1 R.sup.2, R.sup.3 and Ph have the given meanings herein, and also the physiologically harmless salts thereof, exhibit antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: August 25, 1995Date of Patent: September 15, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftingInventors: Rolf Gericke, Dieter Dorsch, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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Patent number: 5798390Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.Type: GrantFiled: May 22, 1995Date of Patent: August 25, 1998Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 5792769Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 --R.sup.4, R.sup.7 --R.sup.8, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: August 15, 1996Date of Patent: August 11, 1998Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Carl R. Illig, Bruce E. Tomczuk, Richard M. Soll, Nalin L. Subasinghe, Roger F. Bone
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Patent number: 5773469Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.Type: GrantFiled: June 18, 1996Date of Patent: June 30, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
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Patent number: 5767162Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.Type: GrantFiled: June 6, 1995Date of Patent: June 16, 1998Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 5753710Abstract: Substituted benzyloxycarbonylguanidines, a process for their preparation, their use as a medicament or diagnostic, and a medicament containing them. There are described compounds of the formula I ##STR1## in which the substituents R(1) to R(7) and X have the meanings shown in the claims, and their pharmaceutically tolerable salts. These are effective inhibitors of the cellular sodium proton antiporter (Na.sup.+ /H.sup.+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases which can be attributed to increased Na.sup.+ /H.sup.+ exchange.Type: GrantFiled: May 15, 1996Date of Patent: May 19, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans-Jochen Lang, Udo Albus, Wolfgang Scholz
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Patent number: 5753715Abstract: The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.Type: GrantFiled: June 2, 1995Date of Patent: May 19, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Robert H. Chen, Maud Urbanski, Min Xiang, John Francis Barrett
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Patent number: 5739142Abstract: 4-Aminobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: January 26, 1996Date of Patent: April 14, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rolf Gericke, Manfred Haumgarth, Norbert Beier, Klaus-Otto Minck
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Patent number: 5733934Abstract: Indenoylguanidines of formula I and formula II, the process for their preparation, their use as medicaments, medicaments containing them, their use as diagnostic agents and medicaments containing them are described. Compounds I are useful for treating cardiac arrhythmias. Further they are useful as cardioprotective agents in mammals, which comprises administering the compound of formula-I or II with the above properties in combination with pharmaceutically accepted carrier to said mammal.Type: GrantFiled: April 16, 1996Date of Patent: March 31, 1998Assignee: Hoechst AktiengesellschaftInventors: Nigrogi Venkata Satya Ramakrishna, Tulsidas Sitaram More, Anagha Suhas Kulkarni, Bansi Lal, Rao Venkata Satya Veerabhadra Vadlamudi, Anil Vasantrao Ghate, Ravindra Dattatraya Gupte, Wolfgang Scholz, Hans Jochen Lang
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Patent number: 5723133Abstract: A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof ##STR1## wherein each of A and B is a C.sub.2 -C.sub.8 alkylene, D is a single bond, --CO-- or a C.sub.1 -C.sub.5 alkylene, E is H, a lower alkyl or the like, m is 1 to 6, n is 0 to 6 and R.sup.1 is H, a lower alkyl or the like, l is 1 to 10 and G is H, --OH or the like and a skin cosmetic containing the same. It can exert excellent keratin layer softening effect continuously for a long period of time.Type: GrantFiled: July 26, 1995Date of Patent: March 3, 1998Assignee: Kao CorporationInventors: Minoru Nagai, Hiromitsu Kawada, Mayumi Tsuchiya, Seiji Yamasaki, Akira Yamamuro, Toshiya Ono
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Patent number: 5719187Abstract: Guanidine derivatives are provided useful for promoting growth, repair and regeneration of a neuronal axon and for treating neuropathies and myopathies. The compounds have the formula: ##STR1## wherein R.sub.1 is an isopropyl radical, a benzyl radical which is optionally substituted by one or more (C.sub.1 -C.sub.6)alkoxy radicals or a radical: ##STR2## R.sub.2, R.sub.3 and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: February 17, 1998Assignee: Centre National De La Recherche Scientifique(CNRS)Inventors: Claude Thal, Catherine Quirosa-Guillou, Pierre Potier, Dolor Renko, Jean-Pierre Zanetta, Marie-Madeleine Portier, Monique Sensenbrenner, Janine Koenig, Herbert Koenig
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Patent number: 5696290Abstract: The present invention is the novel synthesis of sterically hindered penta-substituted guanidines by a process in which (1a) an isocyanate is reacted first with a di-substituted amine or (1b) a urea is reacted with two moles of a mono-substituted amine to form a tri-substituted urea followed by (2) treatment of the tri-substituted urea with an activating agent before reacting with a second di-substituted amine in the presence of a base.Type: GrantFiled: September 12, 1994Date of Patent: December 9, 1997Assignee: Monsanto CompanyInventors: Kenneth W. Ruettimann, William D. McGhee, A. John Solodar
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Patent number: 5696138Abstract: A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinX, Z, Y, A, D, E, F, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12 have the meanings set forth in the specification, pharmaceutical compositions comprising the same, and a method of treating therewith.The compounds are useful as potassium channel openers.Type: GrantFiled: December 27, 1995Date of Patent: December 9, 1997Assignee: NeuroSearch A/SInventors: S.o slashed.ren-Peter Olesen, Peter Moldt, Ove Pedersen
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Patent number: 5693672Abstract: 3,4,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themBenzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where R(4) and R(5) are alk(en)yl, --C.sub.n H.sub.2n --R(7), and where R(7) is cycloalkyl or phenyl, where R(5) is also H, R(6) is H or C.sub.1 --C.sub.4 --alkyl,R(2) is hydrogen, (cyclo)-alk(en)(yn)yl, aryl and hetaryl,R(3) is defined as R(2)and their pharmaceutically tolerable salts are described.Type: GrantFiled: May 26, 1995Date of Patent: December 2, 1997Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Hans-Jochen Lang, Wolfgang Scholz, Udo Albus, Florian Lang
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Patent number: 5670544Abstract: There are described benzoylguanidines of the formula I ##STR1## where R(1) is hydrogen, Hal, --NO.sub.2, --CN, --CF.sub.3, R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where m is zero to 2, R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), n is zero to 4, where R(5) also has the meaning of H,R(6) is H or (C.sub.1 -C.sub.4)-alkyl, where R(5) and R(6) together can be 4 or 5 methylene groups,R(2) is --SR(10), --OR(10), --NRH(10), --NR(10)R(11), --CHR(10)R(12), ##STR2## where R(10) and R(11) are identical or different and are--?CHR(16)!.sub.s --(CH.sub.2).sub.p --(CHOH).sub.q --(CH.sub.2).sub.r --(CH.sub.2 OH).sub.t --R(21) or --(CH.sub.2).sub.p --O--(CH.sub.2 --CH.sub.2 O).sub.q --R(21)R(12) and R(13) are hydrogen or alkyl or, together with the carbon atom carrying them, form a cycloalkyl,R(14) is H, (cyclo)alkyl or --C.sub.n H.sub.2n --R(15),R(3) is defined as R(1), or is alkyl, hydrogen or --X--R(22) where X is oxygen, S or NR(16),and their pharmaceutically tolerable salts.Type: GrantFiled: May 26, 1995Date of Patent: September 23, 1997Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Hans-Jochen Lang, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
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Patent number: 5646188Abstract: A compound of general formula I ##STR1## wherein n is 1 or 2; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy or halogeno;R.sub.5 is hydrogen, substituted or unsubstituted C.sub.1-4 alkyl, amino or NR.sub.6 R.sub.7 ;R.sub.3, R.sub.4, R.sub.6 and R.sub.7 are each independently hydrogen or (CH.sub.2).sub.m --[NH(CH.sub.2).sub.x ].sub.y --NHR.sub.11 wherein m is from 0-5, y is from 0-5 and each x is independently from 1-5 and R.sub.11 is hydrogen or C(NH)NH.sub.2 ;provided that when R.sub.3 and R.sub.4 are both hydrogen, R.sub.5 is amino or NR.sub.6 R.sub.7 ; pharmaceutically acceptable salts and optically active isomers thereof.Type: GrantFiled: July 5, 1995Date of Patent: July 8, 1997Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Gad Gilad, Varda Gilad, Jeffrey Sterling, Yaacov Herzig, David Lerner, Alex Veinberg, Isaac Milman, Nina Finkelstein
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Patent number: 5643950Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: June 2, 1995Date of Patent: July 1, 1997Assignee: Ortho Pharmaceutical CorporationInventors: James P. Demers, Sigmond Johnson, Michele Ann Weidner-Wells, Ramesh M. Kanojia, Stephanie A. Fraga, Dieter Klaubert
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Patent number: 5637622Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.Type: GrantFiled: May 22, 1995Date of Patent: June 10, 1997Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 5637621Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.Type: GrantFiled: November 14, 1994Date of Patent: June 10, 1997Assignee: NZYM, Inc.Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu
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Patent number: 5629348Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.Type: GrantFiled: November 14, 1994Date of Patent: May 13, 1997Assignee: NZYM, Inc.Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu