The Atom Is Carbon Or The Chain Consists Of Carbons Patents (Class 548/524)
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5053504Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.Type: GrantFiled: November 29, 1989Date of Patent: October 1, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
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Patent number: 5037841Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n denotes a number from 1 to 19, andB denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.Type: GrantFiled: April 12, 1989Date of Patent: August 6, 1991Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
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Patent number: 5010090Abstract: 1-Aminobut-3-en derivatives having optionally substituted furanyl, thienyl, pyridyl and/or pyrrolyl in the 4-position and 3-carboxypiperidin-1-yl, 3-carboxytetrahydropyrid-1-yl or 3 carboxymethylpyrrolidin-1-yl in the 1-position potentiate GABA-ergic neurotransmission.Type: GrantFiled: October 7, 1988Date of Patent: April 23, 1991Assignee: Novo Nordisk A/S.Inventors: Frederik C. Gronvald, Claus Braestrup
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Patent number: 5003081Abstract: Pyrrole derivatives of the formula ##STR1## or the tautomers thereof, where R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, hetaryl or amino, it being possible for these radicals to be substituted,R.sup.2 is hydrogen, alkyl, benzyl, alkenyl, cycloalkyl or phenylR.sup.3 is hydrogen, alkyl, benzyl or alkenyl, or R.sup.2 and R.sup.3 together are ##STR2## where T.sup.1, T.sup.2 and T.sup.3 have the meanings mentioned in the description, or R.sup.2 and R.sup.3 together with the nitrogen connecting them are a heterocyclic radical,R.sup.4 is cyano, or carbamoyl or thiocarbamoyl, each of which can be substituted, or --C(NH.sub.2).dbd.N--OH,R.sup.5 is halogen, hydroxyl, alkanoyloxy or benzoyloxy andR.sup.6 is hydrogen, alkyl, phenyl, cyano, halogen, nitro, hydroxysulfonyl, alkanoyl, benzoyl or ##STR3## where T.sup.4 is alkyl or phenyl and T.sup.5 is the radical of an active methylene compound, hydroxyimino or the radical of a primary amine,with the proviso that R.sup.1, R.sup.2 and R.sup.Type: GrantFiled: January 8, 1990Date of Patent: March 26, 1991Assignee: BASF AktiengesellschaftInventors: Juergen Pfister, Matthias Wiesenfeldt, Karl-Heinz Etzbach
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Patent number: 5001142Abstract: Compounds of the formula: ##STR1## pharmaceutical compositions containing the compounds and methods of using the compounds in the treatment of central cholinergic disfunction in a mammal are disclosed.Type: GrantFiled: July 19, 1989Date of Patent: March 19, 1991Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss
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Patent number: 4996215Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.Type: GrantFiled: September 15, 1989Date of Patent: February 26, 1991Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
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Patent number: 4980481Abstract: High performance composites can be made from linear or multidimensional oligomer or blends that include unsaturated hydrocarbon crosslinking functionalities linked to a pyrimidine radical on the terminal ends of the polymeric backbones of the oligomers. The oligomers are made by condensing pyrimidine-based end-cap monomers of the formula: ##STR1## wherein Z=--OH or halogen;Y= ##STR2## wherein R.sub.1 =lower alkyl, lower alkoxy, aryl, aryloxy, substituted alkyl, substituted aryl, halogen, or mixtures thereof;j=0, 1, or 2;G=--CH.sub.2 --, --O--, --S--, --SO--, --CO--, --CHR--, --CR.sub.2 --, or --SO.sub.2 --;T=methallyl or allyl;Me=methyl; andR=hydrogen, lower alkyl, or phenyl,with suitable polymeric precursors.Type: GrantFiled: March 14, 1988Date of Patent: December 25, 1990Assignee: The Boeing CompanyInventors: Hyman R. Lubowitz, Clyde H. Sheppard
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Patent number: 4958021Abstract: Benzopyran derivatives of the formula ##STR1## where X is the radical ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and also the ring A have defined meanings are used in pressure- or heat-sensitive layers.Type: GrantFiled: July 19, 1988Date of Patent: September 18, 1990Assignee: BASF AktiengesellschaftInventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
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Patent number: 4956359Abstract: Novel 3-aryloxy and 3-arylthioazetidinecarboxamides having utility in a method of treating convulsions and epilepsy and compositions therefor are disclosed having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo-substituted-pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, aryl, allyl, substituted allyl, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl, diloweralkylaminoloweralkyl, and R.sup.1 and R.sup.2 when taken with the adjacent nitrogen atom may form a heterocyclic radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof, excepting that when R.sup.3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by trifluoromethyl or aminocarbonyl, then R.sup.1 and R.sup.2 cannot be a combination of hydrogen and loweralkyl, and the further exception that when R.sup.Type: GrantFiled: October 22, 1986Date of Patent: September 11, 1990Assignee: A. H. Robins Company, Inc.Inventors: Chandler R. Taylor, Jr., Albert D. Cale, Jr., Harold F. Stauffer, Jr.
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Patent number: 4937235Abstract: This disclosure describes novel 3 or 4 substituted oxotremorine derivatives having polar substituted oxygen or sulfur groups. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and processes for the production of the compounds.Type: GrantFiled: January 23, 1989Date of Patent: June 26, 1990Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
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Patent number: 4931450Abstract: Compounds of the Formula I ##STR1## wherein R.sup.1 represents phenyl, or phenyl substituted by one, or more substituents selected from the group consisting of halogen, C.sub.1-7 -alkyl, and C.sub.1-7 -alkoxy, R.sup.2 represents furanyl, thienyl, pyridyl or pyrrolyl ortho substituted with C.sub.1-7 -alkyl or halogen and wherein R.sup.3 represents 3-carboxypiperidin-1-yl, 3-carboxy-1,2,5,6-tetrahydropyridin-1-yl or 3-carboxymethyl-pyrrolidin-1-yl, pharmaceutical compositions containing effective amounts of a compound of formula I and treatment of central nervous system ailments by administering a compound of formula I.Type: GrantFiled: October 17, 1988Date of Patent: June 5, 1990Assignee: Novo Industri A/SInventor: Ursula Sonnewald
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Patent number: 4925840Abstract: The invention relates to novel 3-phenyl-4-cyanopyrrole derivatives of the general formula ##STR1## wherein X has the following meanings:A: hydrogen or CO--R.sub.1, wherein R.sub.1 is C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by halogen or C.sub.1 -C.sub.3 alkoxy; or is C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, or C.sub.1 -C.sub.6 alkoxy which is unsubstituted or substituted by halogen or C.sub.1 -C.sub.3 alkoxy; or is C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 cycloalkyl, or tetrahydrofur-2-yl;B: S--R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.3 haloalkyl;C: CH(Y)R.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.8 haloalkyl and Y is hydroxy, halogen or OC(O)R.sub.4, wherein R.sub.4 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxycarbonyl; orD: CH.sub.2 --Z, wherein Z is the group ##STR2## wherein each of R.sub.7 and R.sub.8 independently of the other is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.Type: GrantFiled: August 3, 1988Date of Patent: May 15, 1990Assignee: Ciba-Geigy CorporationInventors: Robert Nyfeler, Josef Ehrenfraund
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Patent number: 4921863Abstract: Cyclic amine derivatives of the formula: ##STR1## or the pharmacologically acceptable salts thereof, wherein the symbols are as defined in the specification, as effective in relieving, curing or preventing mental symptoms due to cerebral vascular disorders.Type: GrantFiled: February 17, 1988Date of Patent: May 1, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizou Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu
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Patent number: 4902334Abstract: A plant metabolism regulating agent comprising as an active ingredient an alpha,beta or beta,gamma-un-saturated carboxylic acid or its derivative. It is useful for controlling the metabolism of a plant, facilitating the growth of a beneficial plant such as cereals by inhibiting the growth of undesirable plants or eradicating them, regulating the growth of a plant and dwarfing a plant.Type: GrantFiled: October 31, 1984Date of Patent: February 20, 1990Assignee: Teijin LimitedInventors: Shizuo Azuma, Toshiyuki Hiramatsu, Teizo Yamaji, Yataro Ichikawa
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Patent number: 4892973Abstract: Disclosed herein is a novel process for producing 1,1-diphenylalkenes, comprising contacting lead peroxide with 1,1-diphenylalkanes having the structure wherein a nitrogen atom of a tertiary amino group is bonded to the para-position of each of the two benzene rings of the 1,1-diphenylalkane, thereby obtaining the corresponding 1,1-diphenylalkenes.Type: GrantFiled: August 31, 1988Date of Patent: January 9, 1990Assignee: Yamada Chemical Co., Ltd.Inventors: Kozo Mizuno, Hideaki Fujisaki, Yoshinori Uda, Tadashi Imai, Katsuhiko Tsunemitsu
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Patent number: 4883655Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing from 1 to 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is a chloride, bromide or iodide anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.Type: GrantFiled: August 28, 1987Date of Patent: November 28, 1989Assignee: GAF CorporationInventors: Robert B. Login, Ratan K. Chaudhuri, David J. Tracy, Michael W. Helioff
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Patent number: 4855425Abstract: The present invention is a process for the selective synthesis of alkanediamines by reacting a secondary amine with an alkanediol. High conversions and high selectivity for the production of alkanediamines is achieved by carrying out the reaction in the presence of a compound or complex of ruthenium in the absence of an organic phosphine co-catalyst.Type: GrantFiled: April 29, 1988Date of Patent: August 8, 1989Assignee: Air Products and Chemicals, Inc.Inventor: John A. Marsella
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Patent number: 4851543Abstract: The invention relates to a novel water soluble aminobenzoic acid in a complexed state which is derived from the reaction between a poly(N-vinyl-2-pyrrolidone)-halogen complex and an aminobenzoic acid and to the process for the preparation of said multicomplex.Type: GrantFiled: February 1, 1988Date of Patent: July 25, 1989Assignee: GAF CorporationInventor: Eugene S. Barabas
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Patent number: 4851544Abstract: A polyimide composition consisting essentially of recurring units having the following structural formula: ##STR1## is produced by the copolymerization of a bismaleimide and bis[4-(3,4-dimethylenepyrrolidyl)phenyl]methane.Type: GrantFiled: July 19, 1988Date of Patent: July 25, 1989Assignee: The United States of America as represented by the Administrator of the National Aeronautics and Space AdministrationInventor: Raphael M. Ottenbrite
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Patent number: 4812452Abstract: Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## or --(CH.sub.2); p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.Type: GrantFiled: March 27, 1986Date of Patent: March 14, 1989Assignee: A. H. Robins Company, IncorporatedInventors: James R. Shanklin, Jr., James M. Wilkinson, II
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Patent number: 4806648Abstract: The one aspect of this invention relates to a process for making cis-vicinal tertiary diamines of general formula: ##STR1## wherein n is from 2-8, and NR.sub.21 is selected from a group including N-piperidino, N-pyrrolidino, dialkylamino containing C.sub.1 -C.sub.12 straight or branched alkyl groups optionally substituted by C.sub.3 -C.sub.7 cycloalkyl groups. The process comprises the formation of a cyclic aminoenamine and the stereospecific catalytic hydrogenation of cyclic aminoenamine to a cis diamine. Another aspect of this invention involves the uses of cis-vicinal tertiary diamines as catalysts of organolithium initiated anionic polymerization of 1,3-dienes, as anti-neoplastic agents and as bacteriacides.Type: GrantFiled: December 18, 1986Date of Patent: February 21, 1989Assignee: Ohio State University Research FoundationInventors: Howard Rosenzweig, Gideon Fraenkel
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Patent number: 4801586Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## wherein X and Y, each, may represent sulfur, oxygen or two hydrogen atoms, A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having 1-4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkylformyl; m is 3-7; q is 2m-2x, wherein x equals the number of double bonds in the lactam ring and may be 1, 2 or 3, and R is CH.sub.3, ##STR2## wherein R" is H or halogen.Type: GrantFiled: October 7, 1986Date of Patent: January 31, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4788187Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: February 26, 1988Date of Patent: November 29, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4783537Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4782086Abstract: Fungicidally active novel E-isomers of N.sup..alpha. -(2-cyano-2-alkoximino-acetyl)-amino acid derivatives and peptides of the general formula (I) ##STR1## in which R represents alkyl, alkenyl, alkinyl, cyanoalkyl, azolylalkyl or optionally substituted phenylalkyl, or represents optionally substituted cycloalkyl;R.sup.1 represents hydrogen, alkyl, optionally substituted phenyl or optionally substituted benzyl, or represents alkoxycarbonylamino;R.sup.2 represents hydrogen or alkyl;R.sup.3 represents hydrogen, alkyl, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aminocarbonylalkyl, azolylalkyl, cyanoalkyl, hydroxyalkyl, alkenyl, alkinyl or optionally substituted cycloalkyl, or represents optionally substituted phenyl or phenylalkyl, or represents the groupingR.sup.4 --SO.sub.n --Z--R.sup.4 n and Z having various meanings, andX is --OH--OR.sup.1 or --NR.sup.2 R.sup.3.Type: GrantFiled: February 20, 1987Date of Patent: November 1, 1988Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Hans Scheinpflug, Wilhelm Brandes
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5-Substituted 1-(4-(1-pyrrolidinyl)-2-butynyl)-2-pyrrolidinones, pharmaceutical compositions and use
Patent number: 4772601Abstract: There are disclosed compounds of the formula ##STR1## where R.sub.1 is loweralkoxycarbonyl, --CH.sub.2 OH or --CONR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl or arylloweralkyl; and R.sub.2 is --CH.sub.2 CH.dbd.CH.sub.2, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group --NR.sub.5 R.sub.6 as a whole being ##STR3## R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; which are useful for enhancing cholinergic activity in mammals and hence for the treatment of various memory dysfunctions characterized by decreased cholinergic function such as Alzheimer's disease.Type: GrantFiled: January 25, 1988Date of Patent: September 20, 1988Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventor: Lawrence L. Martin -
Patent number: 4755527Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S--where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: December 27, 1985Date of Patent: July 5, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier
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Patent number: 4753934Abstract: Compounds of the formula ##STR1## wherein A, B, R.sub.1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.Type: GrantFiled: September 29, 1986Date of Patent: June 28, 1988Assignee: Celamerck GmbH & Co. KGInventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
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Patent number: 4751310Abstract: Compounds having the formula ##STR1## wherein n is 0 or 1, R.sup.2 through R.sup.9 are H or C.sub.1-2 alkyl, and X is pyridyl or mono- or disubstituted phenyl are useful in the preparation of the compounds which inhibit the 5-lipoxygenase pathway.Type: GrantFiled: September 22, 1987Date of Patent: June 14, 1988Assignee: SmithKline Beckman CorporationInventors: Paul E. Bender, Nabil Hanna
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Patent number: 4749698Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.Type: GrantFiled: July 8, 1985Date of Patent: June 7, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, James J. Mencel, Paul Menard
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Patent number: 4748184Abstract: The present invention relates to new compounds of the formula ##STR1## wherein X is ##STR2## wherein R.sub.1 is hydrogen, lower alkyl, phenyl, benzyl, cinnamoyl, thiophene, furan, pyrrole, imidazole, pyrazole oxazole or thiazole; W is hydrogen or hydroxy; (Y).sub.A is positioned ortho to W and is an aminoloweralkyl having the formula --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 are the same or different and may be lower alkyl or R.sub.2 and R.sub.3 may together with N form a pyrrolidine, piperidine or azepine ring, and A is 2; n and m are independently from 0 to 5; and R is straight or branched C.sub.1 -C.sub.10 alkyl, straight or branched C.sub.3 -C.sub.10 cycloalkyl, straight or branched C.sub.2 -C.sub.4 alkenyl or straight or branched C.sub.2 -C.sub.4 alkynyl, or a pharmaceutically acceptable salt thereof.These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: December 27, 1985Date of Patent: May 31, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier, Lawrence A. Black
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Patent number: 4745190Abstract: Selective mono- or di-amination of alkanediols is controllably obtained by catalytic reaction with secondary amines at moderate temperature and autogenous pressure, by selection of the catalyst employed. Ruthenium complexes compounded or admixed with selected organic phosphines, such as triphenylphosphine, favor high yields of alkanolamines, while ruthenium complexes in the absence of organic phosphines favor production of alkylenediamines. Iridium complexes with or without organic phosphines in admixture or chemical combination, also promote production of alkylenediamines.Type: GrantFiled: March 31, 1986Date of Patent: May 17, 1988Assignee: Air Products and Chemicals, Inc.Inventor: John A. Marsella
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Patent number: 4739059Abstract: A novel amine amide of the formula: ##STR1## wherein the various substituents are defined hereinbelow. The compounds are useful as thickening agents, disoxidation catalysts and monomers.Type: GrantFiled: March 27, 1987Date of Patent: April 19, 1988Assignee: Daikin Industries Ltd.Inventors: Yohnosuke Ohsaka, Yoshio Amimoto, Yoshio Negishi
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Patent number: 4734499Abstract: .alpha.,.beta.-Diaminoacrylonitriles of the general formula IR.sup.3 R.sup.2 NC(R.sup.1).dbd.C(NR.sup.2 R.sup.3)CN Iwhere R.sup.1, R.sup.2 and R.sup.3 are identical or different and independently of one another are each hydrogen, alkyl, cycloalkyl, aralkyl, aryl or a heterocyclic radical, and the organic radicals R.sup.2 may furthermore be bonded to one another to form a 6-membered or 7-membered ring, or R.sup.2 and R.sup.3 may be bonded to one another to form a 5-membered or 6-membered ring, are prepared by reacting an .alpha.-dicarbonyl compound R.sup.1 COCHO, or a reactive derivative of this with (a) a salt of sulfurous acid or sulfur dioxide, (b) an amine HNR.sup.2 R.sup.3 or an aliphatic diamine R.sup.3 HN-(CH.sub.2).sub.n NHR.sub.3 where n is 2 or 3 and (c) hydrocyanic acid or a hydrocyanic acid donor in any sequence.Type: GrantFiled: September 19, 1985Date of Patent: March 29, 1988Assignee: BASF AktiengesellschaftInventor: Eckhard Hickmann
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Patent number: 4730057Abstract: A new phthalide derivative useful as a colorless chromogenic material has the following formula: ##STR1## wherein A and n have the same meaning as defined hereinbefore.Type: GrantFiled: January 10, 1986Date of Patent: March 8, 1988Assignee: Kanzaki Paper Manufacturing Co., Ltd.Inventors: Nobuo Kanda, Naoki Yonese, Mitsuru Kondo
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Patent number: 4719218Abstract: A method of inhibiting the production of 5-lipoxygenase products in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a 2(3)-(pyridyl)-3-(2)-substituted phenyl)-6,7-dihydro-[5H]-pyrrolo-[1,2-a]imidazole, a 2(3)-(pyridyl)-3(2)-(substituted phenyl)-5,6,7,8-tetrahydro-imidazo[1,2,-a]pyridine, or a pharmaceutically acceptable salt thereof, to such animal.Type: GrantFiled: April 28, 1986Date of Patent: January 12, 1988Assignee: SmithKline Beckman CorporationInventors: Paul E. Bender, Nabil Hanna
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Patent number: 4677045Abstract: A squarylium dye molecule is synthesized from a phenolic precursor. The resulting hydroxy pyrrolidino squarylium (OHPYRRSQ) dye does not have to be purified in order to provide the dye with a negative response in the Ames test for mutagenicity. A xerographic photoconductor using the molecule shows superior electrophotographic performance.Type: GrantFiled: May 5, 1986Date of Patent: June 30, 1987Assignee: International Business Machines CorporationInventors: Robert B. Champ, Robert L. Vollmer
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Patent number: 4663319Abstract: Novel thioketene derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group, a lower alkenyl group, a phenyl group or a group of the formula: --B--Y;Y is a nitrogen-containing monocyclic heterocyclic group or a substituted or unsubstituted phenyl group;B is a straight or branched lower alkylene group;R.sup.2 and R.sup.3 are both a lower alkyl group or are combined together to form a group of the formula: --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sup.4 is hydrogen atom, a lower alkyl group or a (lower alkoxy)carbonyl group;A is a group of the formula: --(CH.sub.2).sub.n -- or --CH(COOR.sup.5)--;n is an integer of 0, 1 or 2 andR.sup.5 is a lower alkyl group,are disclosed. The compound (I) is useful as an agent for treating and protecting various liver diseases.Type: GrantFiled: January 7, 1985Date of Patent: May 5, 1987Assignee: Tanabe Seiysku Co., Ltd.Inventors: Ikuo Iijima, Koichi Homma, Yutaka Saiga, Yuzo Matsuoka, Mamoru Matsumoto
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Patent number: 4661483Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: May 5, 1986Date of Patent: April 28, 1987Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Clarence S. Rooney, Ta J. Lee
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Patent number: 4620949Abstract: Amino acid derivatives are synthesized by reacting paraformaldehyde, cyclic amides and synthesis gas with a bimetallic catalyst comprising a rhodium-containing compound and a cobalt-containing compound, optionally in the presence of a solvent at a pressure of at least 500 psi and a temperature of at least 50.degree. C. The novel amino acid products may be hydrolyzed to amino dicarboxylic acids or used as monomers to polyamides.Type: GrantFiled: April 5, 1985Date of Patent: November 4, 1986Assignee: Texaco Inc.Inventor: Jiang-Jen Lin
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Patent number: 4610983Abstract: This invention relates to a novel N-acyl acidic amino acid diamide derivative represented by the general formula or a salt thereof: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, represents a hydrogen atom or a substituted or unsubstituted alkyl, cycloalkyl, alkenyl or aralkyl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, when taken together with the respective adjacent nitrogen atoms, form a substituted or unsubstituted heterocyclic group; R.sup.5 represents a substituted or unsubstituted cycloalkyl, acyl or heterocyclic group; A represents a bond or a substituted or unsubstituted alkylene, alkenylene or alkadienylene group; and n is 1, 2 or 3. Said compound has an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such a compound, to a process for the production thereof and to an anti-ulcer agent containing the same.Type: GrantFiled: December 3, 1984Date of Patent: September 9, 1986Assignee: Toyama Chemical Co., Ltd.Inventors: Noboru Takagawa, Shiro Hirai, Takuya Kodama, Hiroshi Hirano, Yasuo Kiba, Mikio Kawabata, Tatsuya Miyaura, Yasuyuki Suzuki
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Patent number: 4608435Abstract: New benzo-1,4-quinones and salts thereof with organic or inorganic acid and bases have the formula I ##STR1## wherein p is 1 or 2 and q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## wherein Q is selected from the residues --CO.sub.2 R.sub.4, --CON(R.sub.4)(R.sub.5), --OR.sub.5, --OCOR.sub.7, --N(R.sub.8)(R.sub.9), --PO(OR.sub.10)([O].sub.x R.sub.11), --SO.sub.2 R.sub.12, --CN, Halogen, --NO.sub.2 or --COR.sub.13, n is an integer from 1 to 20, k is 1 or 2 and x is 0 or 1, and R.sub.1 to R.sub.5 and R.sub.7 to R.sub.13 are as defined in the specification.The compounds of formula I are useful in photographic materials such as bleaching inhibitors in films of photographic silver dye bleach materials.Type: GrantFiled: April 28, 1983Date of Patent: August 26, 1986Assignee: Ciba-Geigy AGInventor: Frederick H. Howell
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Patent number: 4584292Abstract: A series of new 1,5-benzothiazepine analogues are disclosed.These new compounds are represented by the following general formula: ##STR1## wherein : A is >C.dbd.O or >CH.sub.2,n is an integer from 1 to 3,B is ##STR2## wherein R.sup.1 represents H, alkyl or acyl group; R.sup.2 is ##STR3## D represents ##STR4## wherein n' and n" each represents 1 or 2. R, R', R" each represents a lower alkyl, Ph represents phenyl group or a substituted phenyl group.The compounds of the present invention are useful as hypertensive agents.Type: GrantFiled: October 19, 1984Date of Patent: April 22, 1986Assignee: Kotobuki Seiyaku Co., Ltd.Inventor: Tsuyoshi Tomiyama
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Patent number: 4567257Abstract: Disclosed is a novel class of amidinium salts having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 when taken individually are independently selected from lower-alkyl, aralkyl and cycloalkyl, and, when taken together with the respective nitrogen atoms to which they are attached, R.sub.1 together with R.sub.2, and R.sub.3 together with R.sub.4 independently represent heterocyclic groups having 5 to 7 ring atoms, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 are independently selected from hydrogen, lower-alkyl, aryl, aralkyl, and cycloalkyl.The amidinium salts are very active catalysts for converting organic isocyanates to products containing isocyanurate and carbodiimide linkages.Type: GrantFiled: January 16, 1984Date of Patent: January 28, 1986Assignee: The Upjohn CompanyInventor: Dale F. Regelman
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Patent number: 4562201Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: July 26, 1982Date of Patent: December 31, 1985Assignee: American Hospital Supply CorporationInventors: David M. Stout, William L. Matier
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Patent number: 4549015Abstract: New hydroquinone ether compounds of formula I are described: ##STR1## wherein p is 1 or 2 and q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## and R.sub.o, R.sub.oo, R.sub.1, R.sub.2, R.sub.3, Q, n and k are as defined in the specification.The new compounds are useful e.g. as stabilizers in photographic material.Type: GrantFiled: June 14, 1983Date of Patent: October 22, 1985Assignee: Ciba-Geigy AGInventor: Frederick H. Howell
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Patent number: 4546099Abstract: The invention relates to novel N-aminomethyl-3-phenyl-4-cyanopyrrole derivatives of the formula I ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, halogen, methoxy or methylthio,Z is a group ##STR2## wherein R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by cyano, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkoxycarbonyl; or are C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, benzyl or benzyl which is substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl and/or C.sub.1 -C.sub.6 alkoxy, or phenyl or phenyl which is substituted by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl and/or C.sub.1 -C.sub.6 alkoxy, with the proviso that only one of R.sub.3 or R.sub.4 can be hydrogen,R.sub.5 and R.sub.6 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.Type: GrantFiled: July 18, 1984Date of Patent: October 8, 1985Assignee: Ciba-Geigy CorporationInventor: Robert Nyfeler
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Patent number: 4536559Abstract: Resins are prepared from polymers that bear difunctional groups derived from compounds that are condensation products of amino-phenols and acid anhydrides. The polymers are prepared by coreacting aromatic compounds holding two hydroxyl groups, aromatic compounds holding two active halogen groups, and the condensation product of amino-phenol and acid anhydride, the condensation product holding one hydroxyl group. The resulting product has a molecular weight between about 1,000 and 40,000, preferably between about 5,000 and 30,000, and can be cross-linked to form a resin that is thermoplastic and solvent resistant.Type: GrantFiled: June 17, 1983Date of Patent: August 20, 1985Assignee: The Boeing CompanyInventors: Hyman R. Lubowitz, Clyde H. Sheppard
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Patent number: 4499089Abstract: 2-Alkylthio-1-aminoalkyl-2-pyrroline-3-carbonitriles and pharmaceutically acceptable acid addition salts, processes for their preparation and formulation into pharmaceutical compositions as well as their activity as thrombocyte aggregation-inhibitors are described. The compounds are thus useful for the prophylaxis and therapy of thrombotic states.Type: GrantFiled: May 10, 1984Date of Patent: February 12, 1985Assignee: Warner-Lambert CompanyInventors: Hubert Barth, Johannes Hartenstein, Gerhard Satzinger, Edgar Fritschi, Volker Ganser, Horst-Dietmar Tauschel, Gunter Wolf