Nitrogen In Substituent Q Patents (Class 564/163)
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Patent number: 5621142Abstract: Disclosed are a novel optically active compound represented by formula (1), a racemic modification thereof, and a pharmaceutically acceptable acid addition salt of the optically active compound or racemic modification thereof: ##STR1## wherein R is a straight chain or branched C.sub.1 -C.sub.5 aliphatic group which is saturated or unsaturated, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are each independently selected from the group consisting of a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a nitro group, an amino group, a hydroxyl group and a C.sub.1 -C.sub.4 alkoxy group; and mark * indicates an asymmetric carbon atom.Type: GrantFiled: July 30, 1996Date of Patent: April 15, 1997Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Daisuke Mochizuki, Satoshi Shuto
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Patent number: 5599967Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: February 4, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
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Patent number: 5597825Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: May 16, 1994Date of Patent: January 28, 1997Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5575905Abstract: The invention provides a process for the preparation of a 2,4,6-triiodinated or 2,4,6,2',4',6'-hexaiodinated 3,5-disubstituted-aniline or 3,3'-disubstituted-5,5'-linked bisaniline, which process comprises electrochemically iodinating a 3,5-disubstituted-aniline or a 3,3'-disubstituted-5,5'-linked bisaniline in an acidic solvent which comprises water and optionally at least one water-miscible organic solvent.Type: GrantFiled: May 24, 1995Date of Patent: November 19, 1996Assignee: Nycomed Imaging ASInventors: Lars-G oran Wistrand, Klaes Golman, Finn Radner
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Patent number: 5571845Abstract: The invention provides nitroaniline derivatives represented by general formula (I) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN, COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents.Type: GrantFiled: May 26, 1994Date of Patent: November 5, 1996Assignee: Cancer Research Campaign Technology LimitedInventors: William A. Denny, Brian D. Palmer, William R. Wilson
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Patent number: 5571942Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.Type: GrantFiled: August 22, 1995Date of Patent: November 5, 1996Assignee: Eli Lilly and CompanyInventors: Craig S. Hoechstetter, Diane L. Huser, John M. Schaus, Robert D. Titus
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Patent number: 5567734Abstract: Phenyl-substituted alkylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## are described where R(A) and R(B) are H, Hal, CN, OR(6), alkyl, O.sub.r -perfluoroalkyl or NR(7)R(8); R(6) is hydrogen, (cyclo)alk(en)yl, perfluoroalkyl, phenyl or benzyl; R(7) and R(8) are defined as R(6); X is 1-3; R(1) is H, alkyl or --O.sub.0-1 (CH.sub.2)O.sub.0-1 perfluoroalkyl; R(2), R(3), R(4) and R(5) are defined as R(1), with the condition, however, that R(1), R(2), R(3), R(4) and R(5) are not simultaneously hydrogen and that R(1), R(2), R(3), R(4) and R(5) can only be alkyl when at least one of the substituents R(A) or R(B) contains a O.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+1 group; as are the pharmaceutically acceptable salts thereof. Methods of preparation of compounds of formula I are also described.Type: GrantFiled: January 23, 1995Date of Patent: October 22, 1996Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5543433Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.Type: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
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Patent number: 5527945Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: August 31, 1994Date of Patent: June 18, 1996Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5519055Abstract: The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino; with the provisos that(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.Type: GrantFiled: August 6, 1993Date of Patent: May 21, 1996Assignees: University of Maryland at Baltimore, Pharmacia, S.p.A.Inventors: Robert Schwarcz, Mario Varasi, Arturo Della Torre, Carmela Speciale, Alberto Bianchetti
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Patent number: 5512596Abstract: A composition comprising a compound of the formula: ##STR1## wherein: X is H or OH;Y is a group capable of hydrogen bonding to amino, guanidino, or imidazole function, or a group comprising an acidic hydrogen atom, a protected acidic group, or an anion;E is N or CR.sub.1, wherein R.sub.1 is H, OH, CN, F, Cl, Br, or I;A.sub.4, A.sub.5, and A.sub.6 are each independently N, CH, CR.sub.40 or CZ wherein R.sub.40 is R.sub.43, OR.sub.43, SR.sub.43, S(O)R.sub.43, S(O).sub.2 R.sub.43, or NR.sub.43 R.sub.44 wherein R.sub.43 comprises an alkyl of 1 to 3 carbon atoms, an acyl of 2 to 3 carbon atoms, or an alkyl of 1 to 3 carbon atoms substituted with an acyl of 2 to 3 carbon atoms, and R.sub.44 is H or an alkyl of 1 to 2 carbon atoms, and Z is a group capable of hydrogen bonding to carboxyl, or a group comprising a basic heteroatom, a protected basic heteroatom, or a cation.Type: GrantFiled: September 2, 1994Date of Patent: April 30, 1996Assignee: Gilead Sciences, Inc.Inventors: Choung U. Kim, Matthew A. Williams
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Patent number: 5506356Abstract: An N-acylamino acid derivative of the formula: ##STR1##Type: GrantFiled: January 20, 1995Date of Patent: April 9, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5502053Abstract: Compounds of formula ##STR1## are HIV protease inhibitors, and are synthesized via a novel route. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: August 23, 1994Date of Patent: March 26, 1996Assignee: Merck & Co., Inc.Inventors: Bruce D. Dorsey, Joel R. Huff, Susan F. Britcher
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Patent number: 5502252Abstract: There is disclosed a process of producing an .alpha.-ketamide as an intermediate for use in the production of various alkoxyiminoacetamide compounds which are useful as fungicides. Also disclosed is an intermediate to be used in this process.Type: GrantFiled: November 10, 1994Date of Patent: March 26, 1996Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Moriyasu Masui
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Patent number: 5498792Abstract: There is disclosed a process of producing an N-alkylacetamide of the general formula (III): ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 are the same or different and are independently hydrogen, lower alkyl, lower alkoxy, lower alkenyl, halogen or trifluoromethyl; R.sup.1 and R.sup.2 are the same or different and are independently lower alkyl; and represents a chemical bond of E- or Z-configuration, or a mixture of these configurations, which includes the steps of:(a) reacting an acetonitrile of the general formula (I): ##STR2## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1 and are each as defined above, with an alkylamine of the general formula (IV):R.sup.2 --NH.sub.2 (IV)wherein R.sup.2 is as defined above, to give an N-alkylacetamidine of the general formula (II): ##STR3## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2 and are each as defined above; and(b) reacting the N-alkylacetamidine (II) with a nitrite derivative in the presence of an acid.Type: GrantFiled: September 16, 1994Date of Patent: March 12, 1996Assignees: Shionogi & Co., Ltd., Sumitomo Chemical Co., Ltd.Inventors: Katuhisa Masumoto, Akihiko Nakamura, Yujiro Kiyoshima, Mikio Sasaki, Asako Tanahashi
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Patent number: 5494911Abstract: Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.Type: GrantFiled: November 16, 1992Date of Patent: February 27, 1996Assignee: Hoechst AktiengesellschaftInventors: Robert R. Bartlett, Friedrich-Johannes Kammerer
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Patent number: 5492917Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 29, 1993Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
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Patent number: 5489584Abstract: Compounds of the formula ##STR1## having retinoid like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: February 6, 1996Assignee: Allergan, Inc.Inventors: Vidyasagar Vuligonda, Richard L. Beard, Roshantha A. Chandraratna
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Patent number: 5482975Abstract: The subject invention provides for novel compounds for inactivating viruses. These compounds include 6-nitroso-1,2-benzopyrone, 3-nitrosobenzamide, 5-nitroso-1(2H)-isoquinolinone, 7-nitroso-1(2H)isoquinolinone, 8-nitroso-1(2H)isoquinolinone. The invention also provides for compositions containing one or more of the compounds, and for methods of treating viral infections, cancer, infectious virus concentration with the subject compounds and compositions.Type: GrantFiled: February 24, 1993Date of Patent: January 9, 1996Assignee: Octamer, Inc.Inventors: Ernest Kun, Jerome Mendeleyev
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Patent number: 5482974Abstract: A compound for controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein R.sup.2 is ethyl, iso-propyl, propyl or allyl; A is N(CH.sub.3).sub.1-n H.sub.n R.sup.5 or OR.sup.6 wherein n is 0 or 1, R.sup.5 is (CH.sub.3).sub.m (CH.sub.3 CH.sub.2).sub.3-m C, 1-methylcyclopentyl, 1-methylcyclohexyl or 2,3-dimethyl-2-butyl wherein m is 0, 1, 2 or 3 and R.sup.6 is independently R.sup.5 or 2,3,3-trimethyl-2-butyl;R.sup.3 is H or independently R.sup.4 ; andR.sup.4 is halo or CH.sub.3 ;with the proviso that when A is N(CH.sub.3).sub.1-n H.sub.n R.sup.5, if R.sup.3 is H and R.sup.5 is 1-methyl-1-cyclohexyl or (CH.sub.3).sub.m (CH.sub.2 CH.sub.3).sub.3-m C, where m is 0 or 3, or if R.sup.3 is halo and R.sup.5 is (CH.sub.3).sub.m (CH.sub.3 CH.sub.2).sub.3-m C, where m is 3, then R.sup.2 cannot be ethyl;and with the proviso that when A is OR.sup.6 then m is equal to or less than 2, and if R.sup.3 is H or halo and R.sup.Type: GrantFiled: March 8, 1994Date of Patent: January 9, 1996Assignee: Monsanto CompanyInventors: Dennis P. Phillion, Karey A. Van Sant, Daniel M. Walker
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Patent number: 5481036Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.Type: GrantFiled: January 10, 1994Date of Patent: January 2, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5470977Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: March 14, 1995Date of Patent: November 28, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
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Patent number: 5466268Abstract: Polyalkyl and polyalkenyl aromatic amides having the formula: ##STR1## or a fuel-soluble salt thereof; wherein A is hydroxy, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; R.sub.3 is hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.4 is hydrogen or an acyl group of the formula: ##STR2## wherein A.sub.1 is hydroxy, nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R.sub.6 and R.sub.7 are each independently hydrogen, hydroxy, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; R.sub.Type: GrantFiled: December 30, 1994Date of Patent: November 14, 1995Assignee: Chevron Chemical CompanyInventor: Richard E. Cherpeck
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Patent number: 5451394Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 6; R is an alkyl radical having from 1 to 30 carbon atoms; R.sub.1 and R.sub.2 are each selected from the group of C.sub.1 to C.sub.4 alkyl, hydrogen and, alternatively, R.sub.1 and R.sub.2, together with the attached cationic nitrogen atom can form a 5 to 6-membered heterocyclic ring selected from the group of ##STR2## and X is an anion. These benzamide derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.Type: GrantFiled: August 25, 1993Date of Patent: September 19, 1995Assignee: ISP Van Dyk Inc.Inventors: Ratan K. Chaudhuri, Anatoly Alexander, Anna A. Gripp
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Patent number: 5449692Abstract: The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.Type: GrantFiled: March 22, 1994Date of Patent: September 12, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori
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Patent number: 5449803Abstract: Disclosed are an oxime ether compound represented by the formula (I): ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 6 carbon atoms; R.sup.2 represents OR.sup.5 or NHR.sup.6 where R.sup.5 and R.sup.6 each represent an alkyl group having 1 to 6 carbon atoms; R.sup.3 represents a cycloalkyl group having 3 to 8 carbon atoms; R.sup.4 represents an alkenyloxy group having 3 to 6 carbon atoms, an alkynyloxy group having 3 to 6 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a benzyloxy group, an alkoxycarbonyl group having 2 to 7 carbon atoms, a halogen atom, a cyano group, an alkylthio group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms or an acyl group having 2 to 7 carbon atoms; and n represents an integer of 0 to 5.processes for preparing the same and a fungicide containing the same as an effective ingredient.Type: GrantFiled: March 17, 1994Date of Patent: September 12, 1995Assignee: Ube Industries, Ltd.Inventors: Masanori Watanabe, Toshinobu Tanaka, Shuji Yokoyama, Hideaki Umeyama, Tadashi Murakami
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Patent number: 5446066Abstract: The invention provides new compounds of formula (I) ##STR1## wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxy; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA) ##STR2## wherein R.sub.5 is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.Type: GrantFiled: March 22, 1994Date of Patent: August 29, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori
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Patent number: 5434188Abstract: 1-Ether and 1-thioether-naphthalene-2-carboxamides are described, methods of manufacture therefor and their use as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases, and their utility in inhibiting the activation of human immunodeficiency virus (HIV), latent in infected humans.Type: GrantFiled: March 7, 1994Date of Patent: July 18, 1995Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, Sony S. Khatana, James B. Kramer, Paul C. Unangst
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Patent number: 5427773Abstract: This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary salts of p-dialkylaminobenzamides having the formula ##STR1## wherein R' and R" are each selected from the group of C.sub.1 to C.sub.2 alkyl; n is an integer having a value of from 2 to 3; R is an alkyl radical having from 10 to 18 carbon atoms; R.sub.1 and R.sub.2 are each selected from the group of C.sub.1 to C.sub.2 alkyl, and X is an anion. These benzamide derivatives are active sunscreening agents which are usefully employed at a concentration of from about 0.5 to about 10 wt. % in a formulation requiring protection against the harmful effects of sunlight, such as skin burn, hair damage, color fading, etc.Type: GrantFiled: December 15, 1994Date of Patent: June 27, 1995Assignee: ISP Van Dyk Inc.Inventors: Ratan K. Chaudhuri, Anatoly Alexander, Anna A. Gripp
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Patent number: 5416118Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.Type: GrantFiled: September 28, 1993Date of Patent: May 16, 1995Assignee: Schering CorporationInventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
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Patent number: 5403953Abstract: Compound of formula (I): ##STR1## in which: R.sub.1 represents halogen, or hydroxy, alkyl, alkoxy, cyano, amino, mercapto, alkylthio or phenoxy,R.sub.2 and R'.sub.2 represent two hydrogen when the ring is unsaturated, or alternatively identical or different, represent hydrogen or halogen, or hydroxy, alkyl, alkoxy, cyano, amino or oxo when the ring is saturated,R.sub.3 represents any one of the following groups: ##STR2## in which: m represents 1, 2 or 3,X represents oxygen or sulfur or N-R, R.sub.5 or R.sub.6, which are identical or different, represent hydrogen or alkyl or trifluoromethyl or form (C.sub.3 -C.sub.6) cycloalkyl,n represents 0, 1 or 2,R.sub.7 represents hydroxy, alkoxy, amino, or --O--CH.sub.2 --CO--NRR',R.sub.4 represents hydrogen or halogen or alkyl, alkoxy or trihaloalkyl.Type: GrantFiled: November 23, 1993Date of Patent: April 4, 1995Assignee: Adir et CompagnieInventors: Guillaume de Nanteuil, Michel Vincent, Christine Lila, Jacqueline Bonnet, Armel Fradin
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Patent number: 5395971Abstract: A process for making unsaturated .alpha.-amines from olefins wherein the process includes adding an aminating agent, an olefin and a molybdenum based catalyst to a reaction vessel having a nitrogen atmosphere. The catalyst may be described by the general formula LL'MoO.sub.2, L.sub.2 L'MoO.sub.2, or LL'MoO(X--Y).Type: GrantFiled: March 11, 1994Date of Patent: March 7, 1995Assignee: The Board of Regents of The University of OklahomaInventors: Kenneth M. Nicholas, Anurag S. Srivastava
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Patent number: 5395854Abstract: Ortho-substituted phenyl-acetamides I ##STR1## (R.sup.1 =H, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkynyl, alkoxyalkyl, alkoxycarbonyl, phenyl, phenylalkyl, phenylalkenyl or phenoxyalkyl, 5- or 6-membered heterocycle with 1-3 hetero atoms to which a benzene ring or a 5- or 6-membered heterocycle can be fused; R.sup.2 and R.sup.3 =H, CN, halogen, alkyl, alkoxy; R.sub.4 and R.sup.5 =H, alkyl and R.sup.4 or R.sup.5 =alkoxy; Y=O, S, SO, SO.sub.2, N=N, O--CO, CO--O, CO--O--CH.sub.2, alkylene or haloalkylene, alkenylene, alkynylene, oxy- alkylene, thio-alkylene, alkyleneoxy, carbonylalkylene or alkylenecarbonyl, W=alkoxyimino, alkoxymethylene or alkylthiomethylene), excepting compounds where R.sup.1 is hydrogen, phenyl or 2,2-dimethyl-3-(2,2-dichlorovinyl)cyclopropyl, R.sup.2 to R.sup.5 are each hydrogen, Y is carbonyloxymethylene and W is methoxymethylene or methylthiomethylene, are suitable as fungicides and for controlling pests.Type: GrantFiled: September 22, 1993Date of Patent: March 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
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Patent number: 5393776Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.Type: GrantFiled: May 13, 1994Date of Patent: February 28, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5387714Abstract: There is disclosed a process of producing an .alpha.-ketamide as an intermediate for use in the production of various alkoxyiminoacetamide compounds which are useful as fungicides. Also disclosed is an intermediate to be used in this process.Type: GrantFiled: September 30, 1992Date of Patent: February 7, 1995Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Moriyasu Masui
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Patent number: 5360924Abstract: Process for preparing aromatic olefins of the formula (1) ##STR1## in which R.sup.1 -R.sup.3 are hydrogen, alkyl (C.sub.1 -C.sub.8) , alkoxy-(C.sub.1 -C.sub.5), phenyl, fluorine, chlorine, bromine, --OH, --NO.sub.2, --CN, --CHO, --COalkyl(C.sub.1 -C.sub.4) , --COphenyl, --COOalkyl (C.sub.1 -C.sub.4) , --OCOalkyl(C.sub.1 -C.sub.4), --NHCOalkyl(C.sub.1 -C.sub.4) , --CF.sub.3, --NH.sub.2, --NH--alkyl(C.sub.1 -C.sub.4) or --N(alkyl(C.sub.1 -C.sub.4)).sub.2 and R.sup.4 is hydrogen, alkyl(C.sub.1 -C.sub.8), phenyl, fluorine, chlorine, bromine, --OH, --NO.sub.2, --CN, --CHO or --OCOalkyl (C.sub.1 -C.sub.4) , and X is, inter alia, alkenyl(C.sub.2 -C.sub.12) or cycloalkenyl(C.sub.4 -C.sub.8) or the group ##STR2## in which R.sup.5 and R.sup.6 are, independently of one another, hydrogen or methyl, and Y is --phenyl, --CN, --COOH, --COOalkyl(C.sub.1 -C.sub.12), --COOphenyl, ##STR3## --CON (phenyl).sub.2, --COalkyl(C.sub.1 -C.sub.12), --COphenyl, --Oalkyl(C.sub.1 -C.sub.12) , --Ophenyl or the radical ##STR4## in which R.Type: GrantFiled: January 6, 1994Date of Patent: November 1, 1994Assignee: Hoechst AktiengesellschaftInventors: Matthias Beller, Hartmut Fischer, Heinz Strutz
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Patent number: 5356925Abstract: Novel N-(mercaptoalkyl)urea or carbamates of the formulae I and II ##STR1## wherein A is a monocyclic or bicyclic arylene or heteroarylene;Q is hydrogen or R.sub.9 CO--;Y is --O--,--S-- or --NR.sub.8 --;R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 and R.sub.8 are independently hydrogen; lower alkyl; cyclolower alkyl; substituted lower alkyl; aryl; or heteroaryl;R.sup.3 is --OR.sub.5 or --NR.sub.5 R.sub.6 ;R.sub.4 is --(CH.sub.2).sub.q R.sub.7 ; or R.sub.2 and R.sub.4 and the carbons to which they are attached complete a ring;R.sub.5 and R.sub.6 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl or aryl lower alkyl, or R.sub.5 and R.sub.Type: GrantFiled: February 11, 1993Date of Patent: October 18, 1994Assignee: Schering CorporationInventors: Bernard R. Neustadt, Alan Bronnenkant
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Patent number: 5356935Abstract: A series of dihydrophenanthreneones and tetrahydrophenanthreneones are useful as inhibitors of 5.alpha.-reductase, and a series of hexahydrophenanthreneones are useful as intermediates for preparing such pharmaceuticals.Type: GrantFiled: December 13, 1993Date of Patent: October 18, 1994Assignee: Eli Lilly and CompanyInventors: James E. Audia, Thomas C. Britton, Patrick G. Spinazze
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Patent number: 5349105Abstract: Retinoid like activity is exhibited by compounds of the formula ##STR1## where R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl, cycloalkyl or lower alkenyl, A and B independently are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, SR* or OR* where R* is lower alkyl, cycloalkyl or lower alkenyl; Y is lower alkenyl, lower alkynyl, lower cycloalkyl, lower branched chain alkyl or (CH.sub.2).sub.n where n is 0-6; and Z is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR' or a ketal derivative where R' is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons.Type: GrantFiled: March 17, 1993Date of Patent: September 20, 1994Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5349109Abstract: A process for making unsaturated .alpha.-amines from olefins wherein the process includes adding an aminating agent, an olefin and a molybdenum based catalyst to a reaction vessel having a nitrogen atmosphere. The catalyst may be described by the general formula LL'MoO.sub.2, L.sub.2 L'MoO.sub.2, or LL'MoO(X-Y).Type: GrantFiled: August 26, 1993Date of Patent: September 20, 1994Assignee: The Board of Regents of the University of OklahomaInventors: Kenneth M. Nicholas, Anurag S. Srivastava
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Patent number: 5344959Abstract: Compounds of the formula ##STR1## wherein m is 1-4; R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R.sub.5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I, lower alkoxy or lower thioalkoxy of 1-6 carbons; R.sub.6 is hydrogen, lower alkyl, Cl, Br, I, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 OR NR.sub.11 --COR.sub.11 ; R.sub.20 is independently hydrogen or lower alkyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.Type: GrantFiled: May 18, 1993Date of Patent: September 6, 1994Assignee: Allergan, Inc.Inventor: Roshantha A. Chandraratna
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Patent number: 5342835Abstract: Compounds of formula ##STR1## in which: CYCLE surrounded by a semicircle represents, with the two carbon atoms to which the semicircle is linked, a carbon-containing, optionally heterocyclic, ring containing at least one ethylenic or aromatic bond between the two carbon atoms which carry the --C(Z).dbd.Y group and the phenyl group, Y is oxygen or sulphur, Z is NR.sub.1 R.sub.2, R.sub.1 and R.sub.2, each represents optionally substituted alkyl, alkoxy or cycloalkyl; alkenyl or alkynyl; or --NR.sub.1 R.sub.2 represents saturated or unsaturated heterocyclyl;R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.Type: GrantFiled: January 3, 1992Date of Patent: August 30, 1994Assignee: Rhone-Poulenc AgrochimieInventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat
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Patent number: 5340827Type: GrantFiled: June 14, 1993Date of Patent: August 23, 1994Assignee: Celltech, LimitedInventors: Nigel R. A. Beeley, Thomas A. Millican
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Patent number: 5326755Abstract: The present application discloses pesticidally active compounds of formula I:QQ.sup.1 CR.sup.1 .dbd.CR.sup.2 CR.sup.3 .dbd.CR.sup.4 C(.dbd.X.sup.1)NR.sup.5 R.sup.6or a salt thereof, wherein Q is an monocyclic aromatic ring, or Q is a dihalovinyl group or a group R.sup.7 --C.dbd.C-- where R.sup.7 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X.sup.1 is oxygen or sulphur; R.sup.5 is C.sub.1-8 hydrocarbyl optionally substituted, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy; and R.sup.6 is selected from:(A) --Y.dbd.X.sup.2 --(R.sup.8).sub.a where X.sup.2 is O or S, Y is carbon, R.sup.8 is hydrogen, C.sub.Type: GrantFiled: September 10, 1992Date of Patent: July 5, 1994Assignee: Roussel UCLAFInventors: Robert J. Blade, George S. Cockerill
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Patent number: 5319139Abstract: Compounds of the formula: ##STR1## where R.sup.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a lower alkoxy group;R.sub.3 is a group ##STR2## Z is represented by the formula: ##STR3## where R.sub.2 and R.sub.3 may be the same or different from each other and each stands for a hydrogen atom or a lower alkyl;Y is represented by the formula: --(CH.sub.2).sub.n -- where n is 0 or an integer of 1 to 2 or a group represented by the formula: ##STR4## where R.sup.2 and R.sup.3 may be the same or different from each other and each stands for a lower alkyl group; andR.sup.4 represents a group of the formula: ##STR5## where p is 0 or an integer of 1 to 3 and R.sup.12 is hydrogen, a halogen atom, a lower alkyl or a lower alkoxy group a hydrogen atom, R.sup.2 is a methoxy group, R.sup.3 is a hydroxy group and R.sup.4 is a benzyl group having anti-inflammatory activity.Type: GrantFiled: March 30, 1993Date of Patent: June 7, 1994Assignee: Eisai Co. Ltd.Inventors: Hiroyuki Yoshimura, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Kazuo Okano, Richard S. J. Clark, Takashi Mori, Shuhei Miyazawa, Ryoichi Hashida, Kenzo Muramoto, Koukichi Harada, Takashi Inoue, Hirsohi Shirota, Kenichi Chiba, Kenichi Kusube, Toru Horie, Takeshi Suzuki, Isao Yamatsu
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Patent number: 5310760Abstract: Certain 3,4-disubstituted anilines and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.Type: GrantFiled: July 9, 1993Date of Patent: May 10, 1994Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
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Patent number: 5304532Abstract: Compounds of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 each independently represents hydrogen, halogen or alkyl; n is 0 or 1; Z represents hydrogen or halogen or an amino, alkyl, haloalkyl, alkylthio or alkoxy group or a phenoxy group optionally substituted by haloalkyl; A represents CH or N; Y.sup.1 and ZY.sup.2 each independently represents hydrogen, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy; and W represents hydrogen or, when A is CH and at least one of Y.sup.1 and Y.sup.2 is not hydrogen or when A is N, hydrogen or halogen; with the proviso that when A represents N, then each of Y.sup.1 and Y.sup.2 represents hydrogen, have herbicidal properties. The invention also provides a process for their preparation and their use as herbicides.Type: GrantFiled: May 29, 1991Date of Patent: April 19, 1994Assignee: Shell Research LimitedInventors: David Munro, Bipin Patel
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Patent number: 5298647Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.Type: GrantFiled: December 14, 1987Date of Patent: March 29, 1994Inventors: Dominique Robert, Louis Jung
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Patent number: 5286753Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: April 16, 1993Date of Patent: February 15, 1994Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
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Patent number: 5248823Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: December 4, 1992Date of Patent: September 28, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest