Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Bonded Directly To Each Other Patents (Class 514/353)
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Patent number: 6180654Abstract: Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. These novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes.8 The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.Type: GrantFiled: December 4, 1998Date of Patent: January 30, 2001Assignee: Wayne Hughes InstituteInventors: Rakesh Vig, Chen Mao, Fatih A. Uckun
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Patent number: 6156741Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: December 5, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6153604Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 28, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6147063Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 14, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6136335Abstract: Novel phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity as well as anti-viral activity. These novel compounds can be incorporated within contraceptive compositions to provide for spermicidal or sperm-immobilizing activity.Type: GrantFiled: December 31, 1998Date of Patent: October 24, 2000Assignee: Hughes InstituteInventors: Fatih M. Uckun, Osmond D'Cruz
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Patent number: 6133299Abstract: The instant invention is novel uses of known N-(2,6-disubstituted phenyl)-N'-3- and 4-pyridinyl ureas and pharmaceutically acceptable acid addition salts thereof. Such compounds as N-(2-chloro-6-methylphenyl)-N'-4-pyridinyl urea monohydrochloride or N-(2,3-dichlorophenyl)-N'-4-pyridinyl urea are used for treating neurodegenerative disorders, perinatal asphyxia, Alzheimer's disease, Huntington's disease, Parkinson's disease, and Amyotrophic Lateral Sclerosis. The instant invention is similar novel uses of known anticonvulsant compounds as ralitoline, phenytoin, lamotrigine, tetrodotoxin, lidocaine, and carbamazepine.Type: GrantFiled: February 25, 1993Date of Patent: October 17, 2000Assignee: Warner-Lambert CompanyInventors: Charles Price Taylor, Jr., Mark Lawrence Weber
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Patent number: 6046221Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.Type: GrantFiled: August 25, 1998Date of Patent: April 4, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Patent number: 6034117Abstract: This invention relates to a method for treating snoring, sleep apnea and other form of sleep-disordered breathing, which comprises administration of a therapeutically effective dose of an acetyl choline esterase inhibitor (CEI) such as pyridostigmine or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 21, 1998Date of Patent: March 7, 2000Inventors: Jan Hedner, Holger Kraiczi
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Patent number: 6034111Abstract: The invention relates to the use of flupirtine or its salts as drugs in the prophylaxis and therapy of diseases associated with an impairment of the haematopoetic cell system, for example lymphocytes. Especially important in this respect is the treatment of HIV infected patients/AIDS patients.Type: GrantFiled: November 7, 1996Date of Patent: March 7, 2000Assignee: ASTA Medica AktiengesellschaftInventors: Gabriela Pergande, Werner E. G. Muller
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Patent number: 6034112Abstract: The invention relates to the use of flupirtine or its salts as drugs in the prophylaxis and therapy of diseases associated with an impairment of the haematopoetic cell system, for example lymphocytes.Especially important in this respect is the treatment of HIV infected patients/AIDS patients.Type: GrantFiled: April 16, 1998Date of Patent: March 7, 2000Assignee: ASTA Medica AktiengesellschaftInventors: Gabriela Pergande, Werner E. G. Muller
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Patent number: 6017937Abstract: A pyridine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein W represents a group expressed by the following formula 2 or formula 3; ##STR2## wherein R.sub.1 represents an alkenyloxy group; n represents 1 or 2;Ra represents a lower alkyl group; andRb represents a halogen atom; and whereineach of R.sub.2 and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, or halogenated alkyl group;Y represents a group expressed by --S--, --NH-- or --CONH--;m represents an integer of 0 to 2; andp represents 0 or 1.The pyridine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulcers.Type: GrantFiled: April 7, 1998Date of Patent: January 25, 2000Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima
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Patent number: 6001860Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.17, R.sup.18 and R.sup.1 are as defined below. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.Type: GrantFiled: January 17, 1995Date of Patent: December 14, 1999Assignee: Pfizer Inc.Inventor: Ernest S. Hamanaka
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Patent number: 5929082Abstract: The invention provides novel sulphonylurea, sulphonylthiourea and sulphonylguanidine compounds which have the ability to block potassium ion channels regulated by intracellular concentrations of ATP. Methods of synthesis, pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes, cardiac arrhythmias, ischaemic and hypoxic cardiovascular incidents, and cancers are also claimed.Type: GrantFiled: January 23, 1998Date of Patent: July 27, 1999Assignees: Polychip Pharmaceuticals Pty Ltd, The University of SydneyInventors: Noel John Chambers, Graham Allen Ross Johnston
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Patent number: 5916906Abstract: This invention relates to compositions comprising nicotinylalanine (NAL) and/or related analogues, and an inhibitor of glycine conjugation, either synthetic or naturally occurring. Vitamin B6 may also be present in the compositions of this invention in place of, or in addition to, the inhibitor of glycine conjugation. The compositions may be pharmaceutical in nature. The compositions are useful for inhibiting cellular poly(ADP-ribose) polymerase (PARP, PARS, poly(ADP-ribose) synthetase), an enzyme which causes cellular toxicity and which is activated in a variety of toxic and pathological conditions. PARP is inhibited by some metabolites of the tryptophan oxidative pathway, including nicotinamide, kynurenic acid and xanthurenic acid, which are induced by interferon-gamma. The NAL-containing compositions of the invention enhance the intracellular levels of these metabolites, and thereby augment the natural defense of interferon-induced inhibition of PARP.Type: GrantFiled: September 12, 1997Date of Patent: June 29, 1999Inventor: Edward G. Shaskan
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Patent number: 5908842Abstract: Substituted 2-acylaminopyridine compounds and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.Type: GrantFiled: May 20, 1997Date of Patent: June 1, 1999Assignee: Merck & Co., Inc.Inventors: Ravindra Guthikonda, William Hagmann, Malcolm Maccoss, Shrenik Shah, Philippe Durette
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Patent number: 5840724Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: June 24, 1997Date of Patent: November 24, 1998Assignee: Rhone-Poulenc Rorer LimitedInventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Keith Alfred James Stuttle, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher
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Patent number: 5821239Abstract: There are disclosed various substituted 4-amino-3-pyridinol compounds of the formula below, ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Type: GrantFiled: February 16, 1996Date of Patent: October 13, 1998Assignee: Frommer Lawrence & Huag LLPInventors: Gregory Micahel Shutske, Kevin James Kapples, John Dick Tomer, Nicholas Joseph Hrib, John Gerard Jurcak
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Patent number: 5767134Abstract: The present invention relates to novel prodrug forms of ribonucleoside diphosphate reductase inhibitors 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) which have increased water solubility, bioavailablity and resistance to in vivo acetylation of their amino functions. Novel compounds according to the present invention relate to those of the formula: ##STR1## where R.sup.4 is H or CH.sub.3 andR.sup.5 is CHR, benzyl or ortho or para substituted benzyl;R is H, CH.sub.3, CH.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 CH.sub.3 or ##STR2## R' is a free acid phosphate, phosphate salt or an --S--S--R" group; R" is CH.sub.2 CH.sub.2 NHR.sup.6, CH.sub.2 CH.sub.2 OH, CH.sub.2 COOR.sup.7, an ortho or para substituted alkylphenyl and ortho or para substituted nitro-phenyl;R.sup.6 is H, C.sub.1 -C.sub.4 acyl group, trifluoroacetyl, benzoyl or substituted benzoyl group, andR.sup.7 is H, C.sub.1 -C.sub.4 alkyl or a benzyl or substituted benzyl.Type: GrantFiled: May 15, 1997Date of Patent: June 16, 1998Assignee: Vion Pharmaceuticals, Inc.Inventors: Jun Li, Chuan-Sheng Niu, Xiuyan Li, Terrence W. Doyle, Shu-Hui Chen
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Patent number: 5721259Abstract: A method of treatment of tumors is provided based upon a compound of the formula ##STR1## wherein one of R.sup.1 is NHR.sup.4 or NR.sup.4 R.sup.5 or R.sup.3 is NHR.sup.4, NR.sub.4 R.sup.5 or OH, and the other is hydrogen;R.sup.2 is hydrogen or C.sub.1-4 lower alkyl;R.sup.4 is hydrogen, hydroxyl or C.sub.1-4 lower alkyl; andR.sup.5 is C.sub.1-4 lower alkyl; ora pharmaceutically acceptable salt or hydrate thereof.In a further aspect there is provided a method for the treatment of a tumor in a mammal which comprises administration of a compound which is 3- or 5-hydroxy-4-methyl-2-formylpyridine thiosemicarbazone to said mammal.Type: GrantFiled: August 22, 1996Date of Patent: February 24, 1998Assignee: Yale UniversityInventors: Alan C. Sartorelli, Tai-Shun Lin
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Patent number: 5696140Abstract: The present invention relates to hitherto unknown compounds of formula or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which R', R" are the same or different and stand for hydrogen, halogen, or trifluoromethyl, hydroxy, C.sub.1 -C.sub.4 alkyl or alkoxy, nitro, or cyano groups. Alkylene stands for a straight or branched C.sub.1 -C.sub.8 carbon chain, which may be substituted by hydroxy or halogen, nitro or cyano groups. X stands for oxygen, for --S(O).sub.n -- where n stands for an integer from 0 to 2, or for ##STR1## where R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl. R stands for hydrogen or for one or more C.sub.1 -C.sub.4 alkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl or nitro radicals. The present compounds are of value in the human and veterinary practice for treating asthma, allergy, CNS disorders, or cancer.Type: GrantFiled: October 3, 1996Date of Patent: December 9, 1997Assignee: Leo Pharmaceutical Products Ltd.Inventors: Erik Bramm, Hans J.o slashed.rgen Petersen
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Patent number: 5668157Abstract: Cyanoguanidine compounds of formula (I) and its pharmaceutically acceptable acid addition salts wherein R.sub.1 is hydrogen or methyl; R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5 cycloalkenyl hydroxy methyl, methoxy-C.sub.1 -C.sub.5 alkyl, or R.sub.1 and R.sub.2 are combined to form a C.sub.3 -C.sub.6 carbocyclic ring; R.sub.3 and R.sub.4 are each independently selected to be hydrogen, C.sub.1 -C.sub.4 alkyl, F, Cl, Br, I or CF.sub.3 ; R.sub.5 is hydrogen, F or Cl; R.sub.6 is hydrogen, --NH.sub.2, --NHCH.sub.3, --NHC.sub.2 H.sub.5, --NHCH(CH.sub.3).sub.2, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2, NH(CH.sub.2).sub.m, --OC.sub.1 -C.sub.3 alkyl (where m is 2 or 3), --NHC(O)C.sub.1 -C.sub.3 alkyl, Cl or Br; and n is 0 or 1. The compounds of formula (I) are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension and as a diuretic.Type: GrantFiled: June 25, 1996Date of Patent: September 16, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Stephen J. Humphrey, Kaushik D. Meisheri, James H. Ludens, Jackson B. Hester, Jr.
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Patent number: 5661139Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a bis-(2-aryl)hydrazone capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Alteon Inc.Inventors: Michael E. Lankin, David H. Shih, Dilip R. Wagle, San-Bao Hwang
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Patent number: 5652251Abstract: The present invention relates to the new use of 6-amino-5-nitro- and -5-cyano-1,4-dihydropyridines of the general formula (I) ##STR1## in which A, D and R.sup.1 -R.sup.4 have the meaning given in the description, new 6-acylamino-dihydropyridines, processes for their preparation and their use as medicaments as selective potassium channel modulators, in particular for treatment of the central nervous system.Type: GrantFiled: August 18, 1995Date of Patent: July 29, 1997Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Siegfried Goldmann, Hans-Georg Heine, Bodo Junge, Rudolf Schohe-Loop, Henning Sommermeyer, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry
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Patent number: 5639768Abstract: The invention relates to the compounds of formula (I) wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); and X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical.Type: GrantFiled: July 25, 1995Date of Patent: June 17, 1997Assignee: Ciba-Geigy CorporationInventors: Michael M. Morrissey, Hongsuk Suh
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Patent number: 5585389Abstract: There are provided substituted acid amide, arylhydrazone compounds (amidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.Type: GrantFiled: April 28, 1995Date of Patent: December 17, 1996Assignee: American Cyanamid CompanyInventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
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Patent number: 5576334Abstract: The invention concerns chemical compounds of formula IR.sup.1 --CON(R.sup.2)--CON(R.sup.3)--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention concerns processes for the preparation of the chemical compounds of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: November 19, 1996Assignee: Zeneca LimitedInventors: George R. Brown, Richard E. Shute
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Patent number: 5576335Abstract: Urea derivatives of formula (1) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: September 29, 1994Date of Patent: November 19, 1996Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Noriyoshi Sueda, Kazuhiko Yamada, Makoto Yanai, Katsutoshi Miura, Masato Horigome, Norio Oshida, Shigeru Hiramoto, Koichi Katasuyama, Fumihisa Nakata, Nobuhiro Kinoshita, Yoko Tsukada
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Patent number: 5571843Abstract: Therapeutic compounds having the formula: ##STR1## in which R.sub.2 and R.sub.3 independently denote H, C.sub.1 -C.sub.4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R.sub.1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHNHCONHR.sub.4 or R and R.sub.1 together denote .dbd.N--NH--CX--NHR.sub.5, .dbd.N--NH--CX--N(phenyl).sub.2, .dbd.N--NH--CX--NH--NH--R.sub.5, .dbd.N--NH--C(SCH.sub.3).dbd.N--R.sub.6 or .dbd.N--N.dbd.C(SCH.sub.3)--NH--R.sub.6 ; or (A, B)=(N--OH, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2 ; or (A, B)=(N--NH--CX--NHR.sub.5, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 ; or (A, B)=(N--OH, N--OH) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2.Type: GrantFiled: March 24, 1994Date of Patent: November 5, 1996Assignee: InnotheraInventors: Michel P. Cugnon de Sevricourt, Catherine G. Dacquet, Michel A. Finet, Florence J. Le Marquer, Max F. Robba, Norbert O. Tembo, Sylvie J. Yannic-Arnoult, Jean-Luc Torregrosa
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Patent number: 5567721Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: October 22, 1996Assignee: Centre International de Recherches DermatologiquesInventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5567722Abstract: Cyanoguanidine compounds of Formula I and its pharmaceutically acceptable acid addition salts ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5 cycloalkenyl hydroxy methyl, methoxy-C.sub.1 -C.sub.5 alkyl, or R.sub.1 and R.sub.2 are combined to form a C.sub.3 -C.sub.6 carbocyclic ring;R.sub.3 and R.sub.4 are each independently selected to be hydrogen, C.sub.1 -C.sub.4 alkyl, F, Cl, Br, I or CF.sub.3 ;R.sub.5 is hydrogen, F or Cl;R.sub.6 is hydrogen, --NH.sub.2, --NHCH.sub.3, --NHC.sub.2 H.sub.5, --NHCH(CH.sub.3).sub.2, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2, NH(CH.sub.2).sub.m -- OC.sub.1 -C.sub.3 alkyl (where m is 2 or 3), --NHC(O)C.sub.1 -C.sub.3 alkyl, Cl or Br; and n is 0 or 1.The compounds of Formula I are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension and as a diuretic.Type: GrantFiled: February 6, 1995Date of Patent: October 22, 1996Assignee: The Upjohn CompanyInventors: Stephen J. Humphrey, Kaushik D. Meisheri, James H. Ludens, Jackson B. Hester, Jr.
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Patent number: 5563160Abstract: The present invention relates to hitherto unknown compounds of formula or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which R', R" are the same or different and stand for hydrogen, halogen, or trifluoromethyl, hydroxy, C.sub.1 -C.sub.4 alkyl or alkoxy, nitro, or cyano groups. Alkylene stands for a straight or branched C.sub.1 -C.sub.8 carbon chain, which may be substituted by hydroxy or halogen, nitro or cyano groups. X stands for oxygen, for --S(O).sub.n -- where n stands for an integer from 0 to 2, or for .dbd.N--R.sub.1 where R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl. R stands for hydrogen or for one or more C.sub.1 -C.sub.4 alkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl or nitro radicals. The present compounds are of value in the human and veterinary practice as selective serotonin receptor antagonists.Type: GrantFiled: March 15, 1995Date of Patent: October 8, 1996Assignee: Leo Pharmaceutical Products Ltd. A/S (L.o slashed.vens Kemiske Fabrik Produktionsaktieselskab)Inventors: Erik Bramm, Hans J.o slashed.rgen Petersen
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Patent number: 5547966Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is a single bond, O, CO, S, NH or N(lower alkyl); Y is O, S or NCN; and R.sup.1 to R.sup.5' are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: October 7, 1993Date of Patent: August 20, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Karnail S. Atwal, Francis N. Ferrara, Charles Z. Ding
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Patent number: 5519037Abstract: Antiinfluenza A activity was found in compounds of the formula: ##STR1## wherein X is ##STR2## where one of R.sup.1 and R.sup.2 is H and the other is phenylamino and Z is --SCH.sub.3 or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 22, 1995Date of Patent: May 21, 1996Assignee: American Home Products CorporationInventors: Kuo-Hom L. Hsu, Daniel M. Teller, Alan R. Davis, Michael D. Lubeck, Harry R. Munson, Jr., Gunnar E. Jagdmann, Ibrahim M. Uwaydah
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Patent number: 5439925Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.Type: GrantFiled: December 16, 1993Date of Patent: August 8, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
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Patent number: 5438065Abstract: Diaminoethylene derivatives of the formula: ##STR1## wherein R.sup.1 is a heterocyclic group which may be substituted, R.sup.2, R.sup.3 and R.sup.4 are a hydrogen atom or a hydrocarbon group which may be substituted or R.sup.3 and R.sup.4 are combined to form a cyclic amino group together with the adjacent nitrogen atom; R.sup.5 is hydrogen atom or a hydrocarbon group or heterocyclic group which may be substituted; X is an electron attractive group; Y is a hydroxyl or substituted hydroxyl group, amino or substituted amino group or mercapto or substituted mercapto group; n is 0 or 1; or their salts, which are useful as insecticides.Type: GrantFiled: April 12, 1990Date of Patent: August 1, 1995Assignee: Takeda Chemical IndustriesInventors: Hideki Uneme, Isao Minamida, Tetsuo Okauchi
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Patent number: 5428039Abstract: While performing cardiopulmonary bypass, the aorta is cross-clamped and the beating heart is stopped by introducing of an ATP-dependent potassium channel opening agent. The infusion into the coronary circulation shortens the cardiac action potential thereby arresting the heart muscle at a hyperpolarized membrane potential. This maintains the heart in a state of minimal metabolic requirement, thereby preserving transmembrane ionic gradients, intercellular energy stores and cellular integrity. Cardiac arrest is reversed simply by flushing the heart by the coronary circulation upon removal of the aortic cross-clamp. This use is also germane to organ preservation during transport for transplantation. For example, the donor heart is arrested using an ATP-dependent potassium channel opening agent, it is then removed and transported to the recipient and transplanted. Cardiac arrest is reversed by reperfusing the orthotropic graft.Type: GrantFiled: February 20, 1994Date of Patent: June 27, 1995Assignee: The Center for Innovative TechnologyInventor: Neri Cohen
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Patent number: 5424333Abstract: This invention relates to the anthelmintic use of compositions containing N'-substituted-N,N'-disubstitutedhydrazines. Specifically, the invention relates to methods of controlling helminths by contacting the helminths with a compound having a nucleus of the formula ##STR1## wherein X and X' are the same or different O, S, or NR and A', B', R.sup.1 and R.sup.2 are a variety of substituents.Type: GrantFiled: July 5, 1991Date of Patent: June 13, 1995Assignee: Rohm and Haas CompanyInventor: Keith D. Wing
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Patent number: 5420164Abstract: A cycloalkylurea compound of the formula (I): ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and antiatherosclerotic medicine.Type: GrantFiled: May 3, 1993Date of Patent: May 30, 1995Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tadashi Mishina, Kanou Harada, Joji Yasuoka, Hidenobu Kushuhara, Noriyoshi Izumi
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Patent number: 5405856Abstract: There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl;m is 1 or 2;eachR.sub.4 is independently hydrogen or loweralkyl; andY is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.Type: GrantFiled: April 2, 1993Date of Patent: April 11, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis, Russell R. L. Hamer, Brian S. Freed
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Patent number: 5401758Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 to R.sup.4 and n are as defined herein and X is O, S or NCN. These compounds have potassium channel opening activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: October 7, 1993Date of Patent: March 28, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Karnail S. Atwal, Francis N. Ferrara
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Patent number: 5376655Abstract: A derivative of p-guanidinobenzoic acid of the general formula (IA): ##STR1## wherein Y represents an oxygen atom or a sulfur atom and (a) when Y is an oxygen atom, (R.sup.1).sub.m is selected from the group consisting of:5-(4-guanidinobenzoyloxy)-3-methoxymethyl, 3,5-dicarboxy, 3,5-bis(isopropoxycarbonyl), 3,5-bistrifluoromethyl, 3-acetyl, 3,5-bis(N-ethylcarbamoyl), and 3,5-bis(N-propylcarbamoyl);(b) when Y is a sulfur atom, (R.sup.1).sub.m is selected from the group consisting of:2-methyl, 3-methyl, 4-fluoro, 2-chloro, 3-chloro, 2,5-dichloro 2,6-dichloro, 3,4-dichloro, 2-bromo, 2-methoxycarbonyl, and 4-(N,N-diethylaminosulfonyl);or an acid addition salt of said derivative. A method for the treatment or prevention of diseases induced by abnormal enhancing of degradation of proteins by the action of elastase in mammals subject to or suffering therefrom, including the step of administering an effective amount of a p-guanidinobenzoic acid as described herein, is also disclosed.Type: GrantFiled: June 2, 1993Date of Patent: December 27, 1994Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Yoshinobu Arai, Hiroyuki Ohno
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Patent number: 5364843Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are piperazinyl benzyl compounds such as 1-[.alpha.-(4-Chlorophenyl)-3-methoxybenzyl]-4-allylpiperazine dihydrochloride.Type: GrantFiled: June 10, 1992Date of Patent: November 15, 1994Assignee: Burroughs Wellcome Co.Inventor: Ann C. King
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Patent number: 5354764Abstract: A method is provided for inhibiting myocardial cell necrosis and improving myocardial function during myocardial ischemia and/or reperfusion by locally administering to the heart a potent potassium channel activator such as pinacidil or cromakalim.Type: GrantFiled: November 2, 1992Date of Patent: October 11, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Gary J. Grover, Karnail Atwal
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Patent number: 5354762Abstract: This invention relates to insecticidal compositions containing six-membered heterocyclic derivatives of N'-substituted-N,N'-diacylhydrazines, methods of using such compositions and novel six-membered heterocyclic derivatives of N'-substituted-N,N'-diacylhydrazines.Type: GrantFiled: February 19, 1987Date of Patent: October 11, 1994Assignee: Rohm and Haas CompanyInventors: Adam C. Hsu, Dat P. Le
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Patent number: 5326759Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.Type: GrantFiled: November 1, 1993Date of Patent: July 5, 1994Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
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Patent number: 5288758Abstract: New urea derivatives corresponding to the general formula 1 ##STR1## in which: R.sup.1 represents a C.sub.1 -C.sub.4 alkyl group;R.sup.2 represents:a C.sub.5 -C.sub.7 cycloalkyl groupa cycloalkylmethyl group in which the cycloalkyl radical contains from 5 to 7 carbon atomsa benzyl groupa benzyl group in which the aromatic ring bears a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a halogen atom or a nitro group;A represents an oxygen atom or a methylene radical;n represents 1 or 2;X represents an oxygen or sulfur atom;B represents a direct bond, a methylene radical or a carbonyl radical;as well as the therapeutically acceptable salts of these molecules.The invention also relates to the application of the compounds of general formula 1 in therapy, and to the preparation processes.Type: GrantFiled: July 22, 1992Date of Patent: February 22, 1994Assignee: Pierre Fabre MedicamentInventors: Jean-Louis Vidaluc, Dennis Bigg
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Patent number: 5264445Abstract: This compound provides the compound (-)-N"-cyano-N-3-pyridyl-N'-1,2,2-trimethylpropylguanidine, its salts and pharmaceutical formulations, and its method of use for opening potassium channels in mammals.Type: GrantFiled: October 29, 1992Date of Patent: November 23, 1993Assignee: Eli Lilly and CompanyInventors: David W. Robertson, Mitchell I. Steinberg
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Patent number: 5262419Abstract: Ulcerative conditions of the gastro-intestinal tract, e.g., antiinflammatory-drug-induced ulcers, are treated or prevented by the administration of a potassium channel activator. Methods and combination products are also disclosed for the treatment of inflammatory conditions without causing ulceration of the gastrointestinal tract.Type: GrantFiled: June 11, 1992Date of Patent: November 16, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: A. K. Gunnar Aberg, Martin L. Ogletree, Eugene H. O'Keefe
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Patent number: 5240950Abstract: There are provided carbazate derivatives of the formula:R.sup.1 --N.dbd.CH--NHNH--R.sup.2wherein R.sup.1 is a heterocyclic group; and R.sup.2 is an esterified carboxyl group, and their salts, which are useful as AGE-formation inhibitory agents.The derivatives or the salts can be produced by reacting compounds of the formula: R.sup.1 --N.dbd.CH--OR.sup.3 wherein R.sup.1 is a heterocyclic group; and R.sup.3 is a lower alkyl group, with a carbazic acid ester or its salt.Type: GrantFiled: September 7, 1989Date of Patent: August 31, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hitoshi Ikeda, Yu Momose
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles