The Cyano Is Bonded Directly To A Benzene Ring Patents (Class 514/522)
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Patent number: 6262113Abstract: The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).Type: GrantFiled: August 14, 1998Date of Patent: July 17, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 6211234Abstract: Compounds of formula (I) are described wherein R1 is hydrogen, -(lower alkyl)q(CO2R6 or OH), —CN, —C(R7)═NOR8, NO2, —O(lower alkyl)R9, —C≡C—R10, —CR11═C(R12)(R13), —C(═O)CH2C(═O)CO2H, —CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4 and R5 are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.Type: GrantFiled: June 27, 1997Date of Patent: April 3, 2001Assignee: Rhone-Poulenc Rorer LimitedInventors: Peter Charles Astles, Mark Francis Harper, Neil Victor Harris, Iain McFarlane McLay, Roger John Aitchison Walsh, Richard Alan Lewis, Christopher Smith, Barry Porter, Clive McCarthy
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Patent number: 6194454Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and X are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.Type: GrantFiled: February 28, 2000Date of Patent: February 27, 2001Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 6187812Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the index have the following meanings: X is oxygen or sulfur; R is hydrogen or alkyl; R1 is hydrogen or alkyl; R2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy; m is 0, 1 or 2, it being possible for the R2 radicals to be different if m is 2; R3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino; R4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, unsubstituted or substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkynyl, alkynyloxy, alkynylthio, alkynylamino, N-alkynyl-N-alkylamino; unsubstituted or substituted cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocyclyType: GrantFiled: February 3, 2000Date of Patent: February 13, 2001Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 6184249Abstract: Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in the therapy of indications associated with the androgen receptor, such as, hirsutism, acne and androgenetic alopecia, and in the therapy and diagnosis of cell hyperplasia dependent on androgens.Type: GrantFiled: December 18, 1998Date of Patent: February 6, 2001Assignee: Biophysica, Inc.Inventors: Milos Sovak, Allen L. Seligson, James Gordon Douglass, III, Brian Campion, Jason W. Brown
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Patent number: 6169103Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: February 24, 1999Date of Patent: January 2, 2001Assignee: Warner-LambertInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6160011Abstract: The present invention relates to a nonsteroidal agonist compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and are a hydrogen, a nitro, a cyano, a carbamoyl, a halogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a .beta.-chloroethylamine; R.sub.4 is a hydrogen, an alkyl, or is joined to R.sub.5 ; R.sub.5 is a hydrogen, a hydroxy, an alkoxy, an acyloxy, an amino, an alkylamino, a halogen, an alkyl, a haloalkyl, or is joined to R.sub.4 ; R.sub.6 is a hydrogen, an alkyl, or a haloalkyl; A.sub.1 and A.sub.2 is the same or different, each is direct link or an alkylene; X.sub.1 is an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or an alkylene; R.sub.Type: GrantFiled: May 29, 1998Date of Patent: December 12, 2000Assignee: The University of Tennessee Research CorporationInventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Patent number: 6153651Abstract: Ortho-substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them.Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.Type: GrantFiled: February 28, 1997Date of Patent: November 28, 2000Assignee: Hoechst AktiengesellschaftInventors: Udo Albus, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Wolfgang Scholz, Jan-Robert Schwark, Andreas Weichert
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Patent number: 6153586Abstract: Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.Type: GrantFiled: July 1, 1998Date of Patent: November 28, 2000Assignee: Praecis Pharmaceuticals, Inc.Inventors: Marc B. Garnick, Christopher J. Molineaux, Malcolm L. Gefter
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Patent number: 6114325Abstract: A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2)n-NR.sup.2 R.sup.3, wherein when A is R.sup.1, B is --(CH.sub.2)n-NR.sup.2 R.sup.3 and when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, B is R.sup.1 ; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.1 is a hydrocarbon group of C.sub.10-30 ; R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, or together represent a heterocyclic ring having 3-7 members; when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.5 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.Type: GrantFiled: October 22, 1998Date of Patent: September 5, 2000Assignee: Shiseido Co., Ltd.Inventors: Hirotada Fukunishi, Kenichi Umishio, Masahiro Tajima, Koji Kobayashi
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Patent number: 6114381Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a .beta.-phenyl-.alpha.-aminopropionic acid N phenyl amide compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.5 is independently selected from hydrido, fluoro, chloro, bromo, methyl and ethyl; wherein R.sup.3 is selected from hydroxy, methoxy, ethoxy, methoxycarbonyloxy, ethoxycarbonyloxy, (2-methylpropoxy)carbonyloxy and (2-propenyloxy) carbonyloxy; wherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrido; wherein each of R.sup.9 and R.sup.10 is independently selected from hydrido, methyl and ethyl; wherein R.sup.Type: GrantFiled: October 13, 1998Date of Patent: September 5, 2000Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Michael Clare
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Patent number: 6103761Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: October 19, 1994Date of Patent: August 15, 2000Assignee: Warner-Lambert CompanyInventors: Bradley Dean Tait, Michael William Wilson
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Patent number: 6090415Abstract: The present invention relates to pesticides which comprise an active ingredient combination composed ofa) sulfur spray granules andb) a pyrethroid, and to processes for the preparation of these pesticides.Type: GrantFiled: March 17, 1998Date of Patent: July 18, 2000Assignee: BASF AktiengesellschaftInventors: Reinhold Stadler, Reiner Kober, Karl-Heinrich Schneider, Volker Harries, Egon Weinmuller, Eberhard Kleinbach, Adolf Parg, Jorn Tidow, Ulrich Brockel, Ulrich Meier, Cleide M. C. Marques Oliveira, Karl-Friedrich Jager, Ulrich Kiessling
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Patent number: 6075049Abstract: Phenylcarbamates of the formula I ##STR1## where the substituents and the index have the following meanings: R is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2;R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and, in the event that X is NR.sup.a, additionally hydrogen;X is a direct bond, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.2 is hydrogen,substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl;R.sup.3 and R.sup.4 independently of one another are hydrogen, cyano, nitro, hydroxyl, amino, halogen, hetaryloxy, hetarylthio, hetarylamino or N-hetaryl-N-alkylamino, andR.sup.5 is one of the groups mentioned under R.sup.3 or a group CR.sup.d .dbd.NOR.sup.e ;processes and intermediates for their preparation, and their use.Type: GrantFiled: April 23, 1998Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Klaus Oberdorf, Franz Rohl, Norbert Gotz, Michael Rack, Ruth Muller, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 6071957Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.Type: GrantFiled: November 25, 1997Date of Patent: June 6, 2000Assignee: The University of Tennessee Research CorporationInventors: Duane D. Miller, Leonid I. Kirkovsky, James T. Dalton, Arnab Mukherjee
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Patent number: 6057362Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease-hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: June 11, 1999Date of Patent: May 2, 2000Assignee: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
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Patent number: 6046235Abstract: A sulfur-containing amino acid compound having a high inhibitory activity on LTA.sub.4 hydrolase which is represented by the following formula: ##STR1## wherein R.sup.1 represents H, alkyl, optionally substituted phenyl alkyl, alkanoyl or optionally substituted benzoyl; R.sup.2 represents ester, amide or carboxyl; R.sup.3 represents hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted phenylthio, halogen atom, alkylsulfonyl, halogenoalkylsulfonyl, nitro or cyano; R.sup.4 represents alkyl; A.sup.1 represents alkylene; and A.sup.2 represents alkylene.Type: GrantFiled: March 1, 1999Date of Patent: April 4, 2000Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Masato Horiuchi, Kenichi Fujimura, Hiroshi Suhara
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Patent number: 6043282Abstract: Azinooxime ethers of the formula I ##STR1## (X=NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ; Y=O, NZ, where Z=H, alkyl; R.sup.1 =H, alkyl; R.sup.2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it being possible for the radicals R.sup.2 to be different if m=2; R.sup.3 =H, cyano, alkyl, haloalkyl, alkoxy, cycloalkyl; R.sup.4, R.sup.5, R.sup.6 =indepedently of one another H, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl), and their salts, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests.Type: GrantFiled: July 29, 1998Date of Patent: March 28, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Muller, Ruth Muller, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6011063Abstract: Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and for infarct treatment and also for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes in the formation of ischemically induced damage, in particular in the illicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: June 3, 1997Date of Patent: January 4, 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: 6001881Abstract: Benzoylguanidines of the formula I ##STR1## in which: R(1) to R(4) have the meanings given in the claims, are antiarrhythmic pharmaceuticals, having a cardioprotective component, which are also valuable for the prevention of ischemically induced damage, in particular in association with the triggering of ischemically induced cardiac arrhythmias. As a consequence of inhibiting the cellular Na.sup.+ /H.sup.+ exchange mechanism, they are used for treating acute or chronic damage triggered by ischemia. In addition to this, they are notable for their strong inhibitory effect on the proliferation of cells. They are suitable for preventing the genesis of high blood pressure.Type: GrantFiled: June 4, 1997Date of Patent: December 14, 1999Assignee: 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: 5994359Abstract: 2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3 (Ia), C(CONHCH.sub.3).dbd.NOCH.sub.3 (Ib), C(CONH.sub.2).dbd.NOCH.sub.3 (Ic), C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3 (Id) or C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3 (Ie);R.sup.2 is cyano, nitro, halogen, alkyl, haloalkyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, hydroxyl, halogen,alkyl, haloalkyl, alkoxyalkyl, alkoxy, haloalkoxy, alkylthio, cyclopropyl, alkenyl,unsubstituted or substituted aryloxyalkyl, benzyl or benzyloxy,R.sup.4 is hydrogen, cyano,unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and hetaryl;unsubstituted or substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, heterocyclyloxy, aryloxy and hetaryloxy;unsubstituted or substituted arylthio and hetarylthio;--Q--C(R.sup.5).dbd.N--Y.sup.1 --R.sup.6 or --Q--O--N.dbd.CR.sup.7 R.sup.8,R.sup.3 and R.sup.Type: GrantFiled: June 25, 1998Date of Patent: November 30, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Hubert Sauter, Reinhard Kirstgen, Herbert Bayer, Ruth Muller, Bernd Muller, Klaus Oberdorf, Wassilios Grammenos, Norbert Gotz, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5994362Abstract: Disclosed is a new treatment for men with prostatic cancer involving combination therapy of a 5.alpha.-reductase inhibitor, i.e., a 17.beta.-substituted 4-azasteroid, a 17.beta.-substituted non-azasteroid, 17.beta.-acyl-3-carboxyandrost-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylamino-phenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an antiandrogen, i.e. flutamide. Pharmaceutical compositions useful for treatment are also disclosed.Type: GrantFiled: June 2, 1995Date of Patent: November 30, 1999Assignee: Merck & Co., Inc.Inventors: Glenn J. Gormley, Elizabeth Stoner
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Patent number: 5981581Abstract: Phenylacetic acid derivatives of the formula I ##STR1##Type: GrantFiled: January 29, 1998Date of Patent: November 9, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5965612Abstract: 4-Cyano-4-deformylsordaricin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: July 28, 1998Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventor: Bruno Tse
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Patent number: 5965741Abstract: The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R.sup.1, and R.sup.3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof, pharmaceutically acceptable salts thereof, and in vivo hydrolizable esters and amides thereof, that are useful to relieve pain. The invention also provides pharmaceutical compositions as well as synthetic and therapeutic methods relating to such compounds.Type: GrantFiled: February 21, 1997Date of Patent: October 12, 1999Assignee: Zeneca LimitedInventors: Gloria Anne Breault, Howard Tucker, John Oldfield, Peter Warner
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5945450Abstract: Naphthalene derivatives represented by formula ?I!: ##STR1## (wherein A is a hydrogen atom, a hydroxy group, a C.sub.7 -C.sub.11 aralkyloxy group, or an alkoxy group composed of an oxy group and a C.sub.1 -C.sub.12 aliphatic or alicyclic, saturated or unsaturated hydrocarbon group where the allyl may be substituted with a C.sub.6 -C.sub.10 allyloxy group; Q represents O, S, CH.sub.2, O--CH.sub.2, S--CH.sub.2, CO, or CHOR.sup.1 ; L represents CO, CR.sup.2 R.sup.3 CO, CH.sub.2 CH.sub.2 CO, or CH.dbd.CHCO; D represents a hydrogen atom, NO.sub.2, NH.sub.2, CO.sub.2 R.sup.4, or a group having the following formula ?II!: ##STR2## (wherein G represents. a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.6, CN, or a tetrazol-5-yl group); E represents a hydrogen atom, OH, SO.sub.2 NH.sub.2, CO.sub.2 R.sup.5, CN, or a tetrazol-5-yl group; M represents a hydrogen atom, a C.sub.1 -C.sub.4 lower alkyl group, a nitro group, or a halogen atom; and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.Type: GrantFiled: November 22, 1996Date of Patent: August 31, 1999Assignee: Teijin LimitedInventors: Kazuya Takenouchi, Katsushi Takahashi, Masaichi Hasegawa, Takahiro Takeuchi, Keiji Komoriya
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Patent number: 5922767Abstract: Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.Type: GrantFiled: October 7, 1997Date of Patent: July 13, 1999Assignee: SS Pharmaceutical Co., Ltd.Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
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Patent number: 5919824Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.Type: GrantFiled: September 12, 1997Date of Patent: July 6, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
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Patent number: 5905090Abstract: Analogues of the active metabolite of leflunomide, and to the use thereof as immunosuppressive and/or antinflammatory agents.Type: GrantFiled: April 29, 1998Date of Patent: May 18, 1999Assignee: Italfarmaco S.p.A.Inventors: Giorgio Bertolini, Mauro Biffi, Flavio Leoni, Maria Letizia Marchetti, Jacques Mizrahi, Flavio Somenzi, Paolo Mascagni
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Patent number: 5900432Abstract: Compounds of formula I: ##STR1## wherein, ring C, A--B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: October 12, 1995Date of Patent: May 4, 1999Assignee: Zeneca LimitedInventors: James Roy Empfield, Cyrus John Ohnmacht, Keith Russell, Diane Amy Trainor, Paul James Warwick, Jr.
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Patent number: 5900436Abstract: Substituted Indanylidineacetylguanidines, process for their preparation, their use as medicaments or diagnostic and medicaments containing them:Indanylidineacetylguanidines I ##STR1## and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and X have the meanings given in the claims, are effective inhibitors of the cellular sodium/proton antiport (Na.sup.+ /H.sup.+ exchanger), which, in numerous diseases (essential hypertension, atherosclerosis, diabetes and the like) is also increased in those cells which are readily accessible for measurements, such as, for example, in erythrocytes, platelets or leukocytes. They are also advantageous for the preparation of a medicament for the treatment or prophylaxis of disorders of lipid metabolism.Type: GrantFiled: July 28, 1997Date of Patent: May 4, 1999Assignee: Hoechst AktiengesellschaftInventors: Nirogi Venkata Satya Ramakrishna, Arun Kumar Jain, Bansi Lal, Rao Venkata Satya Veerabhadra Vadlamudi, Anil Vasantrao Ghate, Ravindra Dattatraya Gupte, Andreas Weichert, Jan-Robert Schwark
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Patent number: 5889059Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is oxygen or sulfur;R is hydrogen or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sub.Type: GrantFiled: August 5, 1996Date of Patent: March 30, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5886033Abstract: The use of isoxazole and crotonamide derivatives for the treatment of carcinomatous disordersThe compound of the formula I or II ##STR1## is suitable for the production of a pharmaceutical for the treatment of carcinomatous disorders, where R.sup.1 is (C.sub.3 -C.sub.5)-cycloalkyl, (C.sub.2 -C.sub.6)-alkenyl or (C.sub.2 -C.sub.6)-alkynyl, R.sup.2 is CF.sub.3, OCF.sub.3, SCF.sub.3, OH, NO.sub.2, halogen, benzyl, phenyl, CN or O-phenyl, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, halogen or a hydrogen atom and X is a --CH group or a nitrogen atom.Type: GrantFiled: October 16, 1996Date of Patent: March 23, 1999Assignee: Hoechst AktiengesellschaftInventors: Wilfried Schwab, Jorg Czech, Klaus Boslett
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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: 5866611Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.Type: GrantFiled: May 19, 1994Date of Patent: February 2, 1999Assignee: Zeneca LimitedInventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5861435Abstract: A method for preventing settlement of aquatic fouling organisms on surface of an aquatic structure without environmental hazard is provided. The method is based upon absolutely novel concept to prevent the settlement by means of thick slime layer, i.e. bio-jelly, deposited on said surface. The present invention also provides a bio-jelly producing agent and a bio-jelly producing paint both useful for the present method. Further, the present invention provides a novel low toxic antifouling agent.Type: GrantFiled: September 15, 1995Date of Patent: January 19, 1999Assignee: Nippon Paint Co., Ltd.Inventors: Junji Yokoi, Isao Nakamura, Ryoji Hamade, Naoki Yamamori, Hiroharu Ohsugi, Akio Harada
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Patent number: 5856311Abstract: Compounds based on derivatives of .beta.-aminopropionic acid having the general formula (I): ##STR1## The compounds having general formula (I) have a high antifungal activity.Type: GrantFiled: October 23, 1995Date of Patent: January 5, 1999Assignee: Isagro Ricerca SrlInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Silvia Mormile, Ernesto Signorini, Carlo Garavaglia
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Patent number: 5849796Abstract: Ortho-substituted benzoic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the given meanings, and Q is guanidyl, and also their physiologically harmless salts, exhibit antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter. In addition, the compounds of the formula I, in which R.sup.1 to R.sup.3 and also Q have the given meanings, are suitable for use as valuable intermediates for the preparation of medicaments, in particular of inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: August 28, 1995Date of Patent: December 15, 1998Assignee: Merck Patent Gelsellschaft mit Beschrankter HaftungInventors: Rolf Gericke, Dieter Dorsch, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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Patent number: 5811456Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.Type: GrantFiled: August 6, 1996Date of Patent: September 22, 1998Assignees: Laboratoires Mayoly Spindler, Michel SemanInventors: Michel Seman, Suzanne Bernard, Rene Milcent, Catherine Paillat
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Patent number: 5780505Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.Type: GrantFiled: July 7, 1997Date of Patent: July 14, 1998Assignee: American Home Products CorporationInventors: Madelene M. Antane, David R. Herbst, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
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Patent number: 5780435Abstract: Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.Type: GrantFiled: December 15, 1995Date of Patent: July 14, 1998Assignee: Praecis Pharmaceuticals IncorporatedInventors: Marc B. Garnick, Christopher J. Molineaux, Malcolm L. Gefter
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Patent number: 5780592Abstract: A composition comprising lipoproteins and a compound of the formula I ##STR1## stereoisomeric form or salt thereof, suitable for the treatment of immunological disorders, cancer or in transplantation.Type: GrantFiled: December 10, 1996Date of Patent: July 14, 1998Assignee: Hoechst AktiengesellschaftInventors: Stefan Mullner, Axel Hofmann, Karin Saar, Hans-Ulrich Schorlemmer, Robert Bartlett
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Patent number: 5776983Abstract: Compounds of the formula ##STR1## or pharmaceutically acceptable salts thereof wherein: A is a bond, --(CH.sub.2).sub.n -- or --CH(B)--, where n is an integer of 1 to 3 and B is --CN, --CON(R.sup.9)R.sup.9' or --CO.sub.2 R.sup.7 ;R.sup.1 is lower alkyl, aryl or arylalkyl;R.sup.2 is hydrogen, hydroxy, alkoxy, --CH.sub.2 OH, cyano, --C(O)OR.sup.7, --CO.sub.2 H, --CONH.sub.2, tetrazole, --CH.sub.2 NH.sub.2 or halogen; ##STR2## R.sup.3 is hydrogen, alkyl, heterocycle or R.sup.4 is hydrogen, alkyl or B;R.sup.5, R.sup.5', R.sup.8, R.sup.8' or R.sup.8" are independently hydrogen, alkoxy, lower alkyl, halogen, --OH, --CN, --(CH.sub.2).sub.n NR.sup.6 COR.sup.7, --CON(R.sup.6)R.sup.6', --CON(R.sup.6)OR.sup.6', --CO.sub.2 R.sup.6, --SR.sup.7, --SOR.sup.7, --SO.sub.2 R.sup.7, --N(R.sup.6)SO.sub.2 R.sup.1, --N(R.sup.6)R.sup.6', --NR.sup.6 COR.sup.7, --OCH.sub.2 CON(R.sup.6)R.sup.6', --OCH.sub.2 CO.sub.2 R.sup.7 or aryl; orR.sup.5 and R.sup.5' or R.sup.8 and R.sup.Type: GrantFiled: December 2, 1994Date of Patent: July 7, 1998Assignee: Bristol-Myers Squibb CompanyInventors: William N. Washburn, Ravindar N. Girotra, Philip M. Sher, Amarendra B. Mikkilineni, Kathleen M. Poss, Arvind Mathur, Gregory S. Bisacchi, Ashvinikumar V. Gavai
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Patent number: 5763474Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 and R.sub.5 are, independently, cyano, nitro, amino, alkyl, perfluoroalkyl, fluoroalkyl, alkoxy, perfluoroalkoxy, fluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl, carboxyl or hydrogen, with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen; or a pharmaceutically acceptable salt thereof, relaxes smooth muscles.Type: GrantFiled: July 7, 1997Date of Patent: June 9, 1998Assignee: American Home Products CorporationInventors: David R. Herbst, Madelene M. Antane, Geraldine R. McFarlane, Eric G. Gundersen, Bradford H. Hirth, Dominick A. Quagliato, Russell F. Graceffa, John A. Butera
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Patent number: 5708034Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.Type: GrantFiled: October 31, 1996Date of Patent: January 13, 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: 5696161Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Br, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.Type: GrantFiled: May 13, 1996Date of Patent: December 9, 1997Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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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: 5679712Abstract: Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.Type: GrantFiled: June 2, 1995Date of Patent: October 21, 1997Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: RE37035Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: October 7, 1997Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim KGInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht