Benzene Ring Containing Patents (Class 564/237)
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Patent number: 5614630Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 5, 1995Date of Patent: March 25, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew G. Knapp, Lee D. Margolin
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Patent number: 5574054Abstract: Novel quaternary ammonium salts having utility in the medical field for treating gastrointestinal disorders.Type: GrantFiled: January 12, 1995Date of Patent: November 12, 1996Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Osamu Kitagawa, Katsuyuki Ishii, Seiichi Niwa, Sigeru Ueki, Masao Seiki
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Patent number: 5565185Abstract: The present invention provides a no-carrier-added synthesis of radiolabeled meta-halobenzylguanidine by halodestannylation which comprises reacting a meta-trialkylstannylbenzylguanidine with a source of radionuclide of a halogen. The present invention also provides meta-trialkylstannylbenzylguanidine as intermediates in the afore-mentioned process.Type: GrantFiled: July 20, 1994Date of Patent: October 15, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Duncan H. Hunter, Alok Goel, Richard J. Flanagan
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Patent number: 5559154Abstract: 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: August 11, 1993Date of Patent: September 24, 1996Assignees: Oregon State Board of Higher Education, Oregon Health Sciences University, University of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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Patent number: 5494934Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Medicine products.Type: GrantFiled: November 4, 1991Date of Patent: February 27, 1996Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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Patent number: 5489709Abstract: A process for the preparation of a substituted guanidine by reacting a substituted cyanamide with ammonia or a substituted amine in the presence of a Lewis acid catalyst. Also disclosed is a process for the preparation of a tri-substituted guanidine by reacting a mono-substituted cyanamide with a di-substituted amine.Type: GrantFiled: February 8, 1994Date of Patent: February 6, 1996Assignees: Cambridge Neuroscience, Inc., University of ToledoInventors: Graham J. Durant, Sharad S. Magar
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Patent number: 5428065Abstract: Pharmaceutical compounds of the formula: ##STR1## R.sup.1 to R.sup.8 are each hydrogen or C.sub.1-4 alkyl, m, n and p are each 0, 1, or 2, q is 0, 1, 2 or 3, X and Z are each C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, halo, trihalomethyl, carboxy, C.sub.1-4 alkoxy-carbonyl or phenyl, and in addition z, together with the phenyl ring to which it is attached, can be: ##STR2## Y is --O--, --S-- or --CH.sub.2 --, V is --(CH.sub.2).sub.r -- or --(CH.sub.2).sub.r S-- where r is 1 to 15, and W is hydrogen or optionally substituted phenyl; and salts thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 27, 1995Assignee: Lilly Industries LimitedInventors: Barry P. Clark, Graham H. Timms
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Patent number: 5399570Abstract: Aspartic acid derivatives of the formula ##STR1## in which X denotes, for example, ##STR2## and R denotes, for example, cyclohexylamino, have useful pharmacological properties.Type: GrantFiled: March 25, 1993Date of Patent: March 21, 1995Assignee: Cassella AktiengesellschaftInventors: Otmar Klingler, Gerhard Zoller, Melitta Just, Bernd Jablonka
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Patent number: 5395853Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.Type: GrantFiled: November 24, 1993Date of Patent: March 7, 1995Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5373024Abstract: Benzoylguanidines of the formula I ##STR1## are described where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.z --, where R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), and where R(7) is a cycloalkyl or phenyl, where R(5) also has the meaning of H, and R(6) is H or C.sub.1 -C.sub.4 -alkyl, R(2) is hydrogen, halogen, alkyl, O--(CH.sub.2).sub.m C.sub.p F.sub.2p+1, --X--R(10), where X is O, S or NR(11), R(10) is H, (cyclo)alkyl(methyl) or --C.sub.n H.sub.2n --R(12) where R(12) is phenyl, and R(3) is defined, inter alia, as R(1), and their pharmaceutically tolerable salts.The compounds I are obtained by reaction of compounds of the formula II ##STR2## with guanidine, in which L is a leaving group which can be easily nucleophilically substituted.Type: GrantFiled: February 10, 1993Date of Patent: December 13, 1994Assignee: Hoechst AktiengesellschaftInventors: Florian Lang, Hans-Jochen Lang, Dieter Mania, Andreas Weichert, Wolfgang Scholz, Udo Albus, Heinrich Englert
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Patent number: 5364868Abstract: Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing themBenzoylguanidines of the formula I ##STR1## are described in which R(1) or R(2) is an amino group --NR(3)R(4), where R(3) and R(4) are H or (cyclo)alkyl or R(3) is phenyl-(CH.sub.2).sub.p -- where p=0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) can also together be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF.sub.3, C.sub.m F.sub.2m+1 --CH.sub.2 --, benzyl or phenoxy, and their pharmaceutically tolerable salts.The compounds according to the invention have very good antiarrhythmic properties, as occur, for example, in the case of oxygen deficiency symptoms.Type: GrantFiled: February 11, 1993Date of Patent: November 15, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Hans-Jochen Lang, Wolfgang Scholz, Wolfgang Linz, Udo Albus
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Patent number: 5360938Abstract: This invention relates to asymmetric syntheses in which a prochiral or chiral compound is contacted in the presence of an optically active metal-ligand complex catalyst to produce an optically active product.Type: GrantFiled: July 16, 1992Date of Patent: November 1, 1994Assignee: Union Carbide Chemicals & Plastics Technology CorporationInventors: James E. Babin, Gregory T. Whiteker
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Patent number: 5336689Abstract: 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: August 11, 1993Date of Patent: August 9, 1994Assignee: 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: 5296498Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: January 19, 1993Date of Patent: March 22, 1994Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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Patent number: 5292755Abstract: Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylalkyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 --C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(4) are together an alkylene chain,and where n is equal to zero, 1 or 2and their pharmaceutically tolerable salts are outstanding antiarrhythmics.Type: GrantFiled: January 31, 1992Date of Patent: March 8, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich C. Englert, Hans-Jochen Lang, Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz
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Patent number: 5290814Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.Type: GrantFiled: November 5, 1992Date of Patent: March 1, 1994Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5281625Abstract: Guanidines I ##STR1## (A=C.sub.5 -C.sub.12 -cycloalkyl which may bear up to three further substituents; benzyl substituted in the para-position; R.sup.1, R.sup.2, R.sup.3 =H, C.sub.1 -C.sub.4 -alkyl; R.sup.4 =C.sub.5 -C.sub.18 -alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.18 -alkenyl, C.sub.4 -C.sub.18 -alkynyl or phenyl-C.sub.1 -C.sub.6 -alkyl, and these groups may bear up to three further substituents and the phenyl moiety of the phenylalkyl may additionally bear a phenoxy group or up to three C.sub.2 -C.sub.4 -alkenyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkyl or haloalkyl groups, C.sub.5 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.8 -alkyl, where the ring may bear up to three further substituents; A=benzyl and R.sup.4 =C.sub.3 -C.sub.4 -alkyl which may be interrupted by oxygen, or C.sub.4 -alkenyl, both of which may bear up to three further substituents; R.sup.3 +R.sup.4 =C.sub.5 -C.sub.Type: GrantFiled: December 4, 1991Date of Patent: January 25, 1994Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5262568Abstract: 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: March 4, 1991Date of Patent: November 16, 1993Assignee: State of OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 5175365Abstract: There are provided novel nitroguanidine and cyanoguanidine compounds. A method of dessicating and defoliating plants by applying to the foliage thereof certain nitroguanidine or cyanoguanidine compounds and a method for the selective preemergence control of undesirable broadleaf weeds and grasses in the presence of graminaceous crops are disclosed.Type: GrantFiled: June 14, 1991Date of Patent: December 29, 1992Assignee: American Cyanamid CompanyInventors: Robert L. Arotin, Bryant L. Walworth, Michele E. Marini
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Patent number: 5126374Abstract: Guanidines I ##STR1## (A=C.sub.5 -C.sub.12 -cycloalkyl which may bear up to three further substituents; benzyl substituted in the para-position; R.sup.1, R.sup.2, R.sup.3 =H, C.sub.1 -C.sub.4 -alkyl; R.sup.4 -C.sub.5 -C.sub.18 -alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.18 -alkenyl, C.sub.4 -C.sub.18 -alkynyl or phenyl-C.sub.1 -C.sub.6 -alkyl, and these groups may bear up to three further substituents and the phenyl moiety of the phenylalkyl may additionally bear a phenoxy group or up to three C.sub.2 -C.sub.4 -alkenyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkyl or haloalkyl groups, C.sub.5 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.8 -alkyl, where the ring may bear up to three further substituents; A=benzyl and R.sup.4 =C.sub.3 -C.sub.4 -alkyl which may be interrupted by oxygen, or C.sub.4 -alkenyl, both of which may bear up to three further substituents; R.sup.3 +R.sup.4 =C.sub.5 -C.sub.Type: GrantFiled: July 3, 1990Date of Patent: June 30, 1992Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5116838Abstract: There are disclosed novel 1,3-dibenzyl (or diphenethyl)-2-phenylguanidine derivatives. The guanidines possess high control effects on mildew, blight, powdery mildew and rust which are serious diseases of fruit trees, vegetables or cereals, and are useful as agricultural and horticultural fungicides.Type: GrantFiled: November 15, 1990Date of Patent: May 26, 1992Assignee: Hokko Chemical Industry Co., Ltd.Inventors: Hiromichi Ishikawa, Takashi Umeda, Shinji Onoue, Kazuo Kajikawa, Toshihiro Shibata, Hiroshi Ohyama
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Patent number: 5091394Abstract: Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylakyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 -C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(5) are together an alkylene chain,and where n is equal to zero, 1 or 2 and their pharmaceutically tolerable salts are outstanding antiarrhythmics.Type: GrantFiled: September 4, 1990Date of Patent: February 25, 1992Assignee: Hoechst AktiengesellschaftInventors: Heinrich C. Englert, Hans-Jochen Lang, Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz
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Patent number: 5082968Abstract: A method of preparing a hexaalkylguanidinium salt comprising contacting tetraalkylguanidine with an alkylating agent in the presence of at least one alkaline reagent, and optionally, a promoting amount of a phase transfer catalyst.Type: GrantFiled: November 1, 1990Date of Patent: January 21, 1992Assignee: General Electric CompanyInventor: Daniel J. Brunelle
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Patent number: 5059624Abstract: Guanidine derivatives of the following formulas (1) and (2): ##STR1## wherein: R.sup.1 is hydrogen or optionally substituted cinnamoyl,R.sup.2 is hydrogen, alkyl or alkenyl, with the proviso that R.sup.1 and R.sup.2 cannot be both hydrogen,n is an integer from 1 to 8, or: ##STR2## wherein R.sup.3 is truxinoyl or a truxilloyl each optionally substituted, andR.sup.2 and n are as defined above;pharmaceutical compositions containing such compounds and a process for their extraction and purification from plant material, in particular from Verbesina caracasana.Type: GrantFiled: February 24, 1989Date of Patent: October 22, 1991Assignee: Consiglio Nazionale Delle RicercheInventors: Giuliano D. Monache, Franco D. Monache, Marco Carmignani, Stella C. Bonnevaux, Romulo Espinal, Carlo De Luca, Bruno Botta
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Patent number: 5021429Abstract: Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR.sub.1 and R.sub.2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl; or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions --O-- and ##STR3## R.sub.3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents --O--, --S-- or --CH.sub.2 -- or ##STR4## where R.sub.5 is hydrogen or lower alkyl; Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHR.sub.7 ;in which R.sub.6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R.sub.Type: GrantFiled: December 22, 1986Date of Patent: June 4, 1991Assignee: Allen & Hansburys LimitedInventor: Michael Martin-Smith
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Patent number: 4894218Abstract: New radiopharmaceutical compositions for use in nuclear medicine comprise radioastatinated benzylguanidine and radioastatinated carboxamidino phenylpiperazine. These compositions are used for treatment of disease, including neuroendocrine tumors, and specifically neuroblastoma.Type: GrantFiled: May 31, 1988Date of Patent: January 16, 1990Assignee: Regents of the University of CaliforniaInventors: Barry L. Engelstad, David L. White, John P. Huberty
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Patent number: 4851441Abstract: This invention relates to antiviral organic guanidine derivatives compositions; a process of producing the antiviral compositions; and a method for inhibiting viruses utilizing the compositions. More particularly, the compositions are tubastrines derived from marine coral Tubastrea aurea.Type: GrantFiled: January 28, 1988Date of Patent: July 25, 1989Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Tatsuo Higa, Ryuichi Sakai
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Patent number: 4804780Abstract: Novel substituted phenyl and benzyl nitroguanidine and phenyl and benzyl cyanoguanidine compounds. Methods for increasing crop yield, inhibiting lodging of graminaceous crops, and inducing cytokinin-like responses in crop plants with said novel guanidine compounds and derivatives thereof, as well as methods for inhibiting deterioration and/or extending the shelf life of harvested fruit, vegetables, and ornamentals are disclosed.Type: GrantFiled: March 3, 1986Date of Patent: February 14, 1989Assignee: American Cyanamid CompanyInventors: Laurine M. Speltz, Bryant L. Walworth, Alexander D. Pavlista
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Patent number: 4680300Abstract: A compound having the formula ##STR1## where Ar=naphthyl, biphenyl, or quinolinyl;X=oxygen or NH;Y=2 to 8;R.sub.1 =phenyl, substituted phenyl, hydrogen, lower alkyl; andR.sub.2 is the same or different from R.sub.3 and is alkyl, cycloalkyl, phenyl, substituted phenyl, thiazolyl; andthe pharmaceutically acceptable salts thereof.Compounds of this general formula are useful as anti-inflammatories, and as anti-psoriatic agents.Type: GrantFiled: January 10, 1985Date of Patent: July 14, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Peter Nelson, Stefan H. Unger
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Patent number: 4659721Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.Type: GrantFiled: January 22, 1985Date of Patent: April 21, 1987Assignee: Ludwig Heumann & Co. GmbHInventors: Helmut Schickaneder, Stefan Postius, Istvan Szelenyi, Peter Morsdorf, Rolf Herter, Kurt H. Ahrens
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Patent number: 4656180Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.Type: GrantFiled: March 5, 1985Date of Patent: April 7, 1987Assignee: Ludwig Heumann & Co., GmbHInventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
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Patent number: 4622217Abstract: A novel compound, 4-amino-3-iodobenzylguanidine, in radioiodinated form is useful in radiopharmaceutical compositions in nuclear medicine as an imaging agent for the heart, adrenal medulla, and tumors of the adrenal medulla and can be used for treatment of tumors of the adrenal medulla. The radioactive compound can be readily made by reacting 4-aminobenzylguanidine and an N-chloro oxidant in the presence of a radioiodide.Type: GrantFiled: April 27, 1984Date of Patent: November 11, 1986Assignee: The Regents of the University of MichiganInventor: Donald M. Wieland
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Patent number: 4602041Abstract: Compounds of formula (I): ##STR1## or a salt or acyl derivative thereof; whereinY is either --CH.dbd.N or ##STR2## R.sup.1 is hydroxy, halogen, (C.sub.1-4) alkyl, or (C.sub.1-4)alkoxy, R.sup.2 is a nitrogen-containing, basic substituent,R.sup.3 is hydrogen, hydroxy, halogen, (C.sub.1-4) alkyl, (C.sub.1-4) alkoxy or a nitrogen-containing, basic substituent, andR.sup.4 is hydrogen or hydroxy,are useful in treating diarrhoea and scours.Type: GrantFiled: February 8, 1983Date of Patent: July 22, 1986Assignee: Beecham Group P.L.C.Inventors: Peter M. Newsome, Lee J. Beeley, Stephen F. Moss
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Patent number: 4594092Abstract: Novel substituted phenyl and benzyl nitroguanidine and phenyl and benzyl cyanoguanidine compounds. Methods for increasing crop yield, inhibiting lodging of graminaceous crops, and inducing cytokinin-like responses in crop plants with said novel guanidine compounds and derivatives thereof, as well as methods for inhibiting deterioration and/or extending the shelf life of harvested fruit, vegetables, and ornamentals are disclosed.Type: GrantFiled: November 17, 1983Date of Patent: June 10, 1986Assignee: American Cyanamid CompanyInventors: Laurine M. Speltz, Bryant L. Walworth, Alexander D. Pavlista
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Patent number: 4491586Abstract: The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof in which the substituents are defined in the specification.The compounds of formula (I) show pharmacologically activity as selective histamine H.sub.2 -antagonists.Type: GrantFiled: December 16, 1982Date of Patent: January 1, 1985Assignee: Glaxo Group LimitedInventor: Roger Hayes
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Patent number: 4457859Abstract: 2,2-azimidazole derivatives of the formula: ##STR1## wherein R and R.sup.1 are H, a C.sub.1 -C.sub.12 alkyl, a C.sub.1 -C.sub.12 alkoxy; NO.sub.2 ; R.sup.2 is hydrogen, a C.sub.1 -C.sub.3 alkyl; n, m=1 to 3, but where n-m=1, R=R.sup.1 =R.sup.2 =H is excluded, are disclosed as well as a method for preparing these compounds by oxidation of a compound of the formula ##STR2## wherein R, R.sup.1, R.sup.2, n and m are as identified above, except for the compound, wherein R=R.sup.2 =R.sup.2 =H, n=m=1. A liquid-crystal or mesomorphic material containing the 2,2'-azoimidazole compounds and electrooptical device comprised of such mesomorphic material are disclosed. The electrooptical devices are useful for systems of electronic representation and processing of information. The compounds therein have two spectrally spaced absorption bands in the visible part of their spectrum such that their position insures the contrast required for the human eye to be able to readily recognize the difference in color.Type: GrantFiled: March 23, 1982Date of Patent: July 3, 1984Inventors: Alexandr V. Ivaschenko, Valentina T. Lazareva, Elena K. Prudnikova, Vladimir G. Rumyantsev, Tamara S. Pljusnina, Viktor A. Nefedov, Lev M. Blinov, Viktor V. Titov, Vladimir P. Sevostyanov, Vadim M. Shoshin
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Patent number: 4427685Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: a is 1 to 3;b is 0 to 2;c is 2 to 4;d is 1 to 5;X is sulphur, oxygen or --CH.sub.2 --;Y is oxygen, sulphur, NR.sub.4 or CHR.sub.5 wherein R.sub.4 is hydrogen, C.sub.1-4 alkyl, NO.sub.2 or CN, C.sub.1-4 alkylsulphonyl or phenylsulphonyl optionally substituted in the phenyl moiety by one or two substituents selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, fluorine, chlorine or bromine, and R.sub.5 is NO.sub.2, C.sub.1-4 alkylsulphonyl or optionally substituted phenylsulphonyl as defined for R.sub.4 ;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-4 alkyl, or C.sub.3-6 cycloalkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached represent a pyrrolidino or piperidino ring;R.sub.6 and R.sub.7 are independently hydrogen or C.sub.Type: GrantFiled: February 3, 1982Date of Patent: January 24, 1984Assignee: Beecham Group P.L.C.Inventor: Geoffrey Stemp
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Patent number: 4358613Abstract: Guanidines are one of the strongest organic bases and find applications where this property is needed, such as in phase transfer catalysis in the form of their substituted derivatives. Their use, however, has been hampered by their expensive nature due to the only mediocre yields in their preparation. The present invention provides a process for the preparation of substituted guanidines in high yields.Type: GrantFiled: March 16, 1981Date of Patent: November 9, 1982Assignee: General Electric CompanyInventor: Victor Mark
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Patent number: 4317819Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.Type: GrantFiled: December 5, 1980Date of Patent: March 2, 1982Assignee: Glaxo Group LimitedInventors: John W. Clitherow, Barry J. Price, John Bradshaw, Michael Martin-Smith
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Patent number: 4279911Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl; R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.Type: GrantFiled: June 6, 1980Date of Patent: July 21, 1981Assignee: Glaxo Group LimitedInventors: Michael Martin-Smith, Barry J. Price, John Bradshaw, John W. Clitherow
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Patent number: 4269837Abstract: Novel guanylamidines and the pharmaceutically acceptable acid addition salts thereof having activity as hypoglycemic agents are disclosed.Type: GrantFiled: February 19, 1980Date of Patent: May 26, 1981Assignee: Pfizer Inc.Inventors: David S. Watt, Jeffrey L. Ives
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Patent number: 4233302Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in whichY represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl;R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.Type: GrantFiled: December 18, 1978Date of Patent: November 11, 1980Assignee: Glaxo Group LimitedInventors: Michael Martin-Smith, Barry J. Price, John Bradshaw, John W. Clitherow