Additional Hetero Ring Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 540/596)
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Patent number: 4994450Abstract: A compound, or a solvate or salt thereof, of formula (I) ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;p is 1, 2, 3 or 4, andR is a group of formula (II) ##STR2## in which the group --(CHR.sub.4).sub.n --X-- is in the meta- or para-position with respect to YR.sub.5 or R.sub.6, R.sub.4 is hydrogen or C.sub.1-6 alkyl, preferably hydrogen;n is 0, 1 or 2, preferably 1;X is a direct bond, or O, S or NR.sub.a in which R.sub.a is hydrogen or C.sub.1-6 alkyl, and is preferably a direct bond;Y is >C.dbd.O, >CHOH, --S.dbd.O or --SO.Type: GrantFiled: February 10, 1989Date of Patent: February 19, 1991Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Antonio Giordani
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Patent number: 4992465Abstract: R represents hydrogen or lower alkyl; R.sub.1 represents hydrogen, lower alkyl or aryl-lower alkyl; R.sub.2 represents hydrogen, lower alkyl or aryl-lower alkyl; or R.sub.1 and R.sub.2 together represent alkylene of 4 to 6 carbon atoms; R.sub.3 represents hydrogen, hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy in compounds wherein Z represents S; or R.sub.3 represents hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy, and is attached only at the 5- or 8- position in compounds wherein Z represents O; R.sub.4 and R.sub.5 represent independently hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts thereof; and mono or di- S-oxides of compounds of formula I wherein Z represents S and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof; and use thereof as central nervous system active agents for the treatment of central nervous system disorders.Type: GrantFiled: February 16, 1990Date of Patent: February 12, 1991Assignee: Ciba-Geigy CorporationInventor: Alan J. Hutchison
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Patent number: 4992435Abstract: Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.Type: GrantFiled: September 23, 1988Date of Patent: February 12, 1991Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Pauline Sanfilippo, James J. McNally, Robert Falotico
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Patent number: 4968676Abstract: Cyclohexylamines of the formula ##STR1## where X is a single bond or an alkylene chain, Y is hydrogen or an aryl, cyclohexyl, 4-cyclohexylcyclohexyl, perhydro-1- or 2-naphthyl or piperidyl radical, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, cycloalkyl, cycloalkenyl or arylalkyl, or R.sup.1 and R.sup.2 together form an alkylene group and, together with the N atom, form a ring, and acid addition salts thereof, with the exception of compounds in which X is a single bond, Y is cyclohexyl, R.sup.1 and R.sup.2 are hydrogen or methyl, and the compounds in which X is C.sub.6 -, C.sub.7 - and C.sub.8 -alkyl, Y is hydrogen and R.sup.1 and R.sup.2 together with the N atom whose substituents they are form a 2,6-dimethylmorpholine radical, and fungicides containing such cyclohexylamines.Type: GrantFiled: September 20, 1989Date of Patent: November 6, 1990Assignee: BASF AktiengesellschaftInventors: Bernhard Zipperer, Ernst Buschmannm, Norbert Goetz, Ulrich Schirmer, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 4966973Abstract: The present invention relates to a compound of the formula ##STR1## wherein R.sup.1 stands for hydrogen or a lower alkyl; n denotes an integer of 1 to 6; X stands for an optionally oxidized sulphur atom, oxygen atom or an optionally substituted imino; R.sup.2 stands for methyl or an organic residual group bonded through methylene, methine a quaternary carbon; R.sup.3 stands for a lower alkyl; R.sup.4 stands for hydrogen or acyl; R.sup.5 and R.sup.6 each stand for a lower alkoxy or a lower alkyl, or R.sup.5 and R.sup.6 combinedly stand for butadienylene, and salts thereof.The compound (I) of the present invention has a strong 5-lipoxygenase inhibiting action, is of high safety and is useful as, among others, an agent for ameliorating dysfunction of circulatory system, an anti-allergic agent and a pharmaceutical agent for central nervous system.Type: GrantFiled: June 9, 1989Date of Patent: October 30, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Shigenori Ohkawa, Naohisa Fukuda
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Patent number: 4960768Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.Type: GrantFiled: May 8, 1989Date of Patent: October 2, 1990Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4957921Abstract: Substituted cyclohexanols are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: December 6, 1989Date of Patent: September 18, 1990Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
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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: 4950766Abstract: A method for preparing a benzamide by reacting an aromatic acid with an amine having a primary amino group and a secondary amino group wherein the reaction is directed to the primary amino group by first reacting the acid with N,N'-carbonyldiimidazole.Type: GrantFiled: September 21, 1989Date of Patent: August 21, 1990Assignee: Erbamont, Inc.Inventor: Jung-Hui Sun
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Patent number: 4925839Abstract: Disclosed herein are novel benzopyrans having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of hypertension.Type: GrantFiled: June 24, 1988Date of Patent: May 15, 1990Assignee: American Home Products CorporationInventors: Dominick A. Quagliato, Leslie G. Humber
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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: 4902818Abstract: The manufacture of optically active bifunctional compounds of the general formula ##STR1## wherein R represents protected hydroxymethyl, protected formyl or alkoxycarbonyl and R.sup.1 represents a group of the formula ##STR2## in which R.sup.2 and R.sup.3 represents lower alkyl or cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom represent a heterocyclic ring, by isomerizing compounds of the general formula ##STR3## wherein R, R.sup.2 and R.sup.3 have the above significance and R.sup.3 can additionally signify hydrogen, is described.The compounds of formula I are potential intermediates in the manufacture of, interalia, natural vitamin E and natural vitamin K.sub.1.Type: GrantFiled: October 5, 1988Date of Patent: February 20, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Hans-Jurgen Hansen, Rudolf Schmid, Max Schmid
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Patent number: 4900727Abstract: The present invention relates to novel 4H-1-benzopyran-4-one derivatives, to processes for the preparation thereof and to their use as anti-inflammatory, analgesic, immuno-suppressive and anti-allergic agents. In particular, the present invention relates to novel compounds of the formula I, ##STR1## in which R.sub.1 is hydrogen, alkyl having 1 to 6 carbon atoms, arly-C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, aryl or carboxyl or an aldehyde or COO--C.sub.1 -C.sub.4 -alkyl group, R.sub.2 is hydrogen, alkyl having 1 to 6 carbon atoms, nitro, amino, di-C.sub.1 -C.sub.4 -alkylamino or a halogen, R.sub.3 is C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.4 -alkyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, aryl-C.sub.1 -C.sub.4 -alkyl, nitro, amino, a C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino group or halogen, R.sub.Type: GrantFiled: January 26, 1989Date of Patent: February 13, 1990Assignee: Hoechst AktiengesellschaftInventors: Samba L. Kattige, Ramchandra G. Naik, Aftab D. Lakdawalla, Alihussein N. Dohadwalla, Richard H. Rupp, Noel J. de Souza
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Patent number: 4898941Abstract: A process for preparing a diphenylalkene derivative of the formula [II] ##STR1## which comprises oxidizing a diphenylalkanoic acid derivative of the formula [I] ##STR2## wherein R.sub.1 and R.sub.2 are each substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or substituted or unsubstituted aryl, R.sub.1 and R.sub.2 may form a heteroring together theirwith or with an adjacent benzene ring, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are each hydrogen atom, halogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyl or substituted or unsubstituted amino, R.sub.12 and R.sub.13 are each hydrogen atom or substituted or unsubstituted alkyl, X is carboxyl, amide, ester or halide thereof.Type: GrantFiled: August 11, 1987Date of Patent: February 6, 1990Assignee: Kanzaki Paper Manufacturing Co., Ltd.Inventors: Nobuo Kanda, Haruo Omura, Yukihiro Abe, Mitsuru Kondo
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Patent number: 4895840Abstract: Novel N-(Aryl-,aryloxy-,arylthio-,arylsulfinyl-and arylsulfonyl-)alkyl-N,N'-(or N',N')alkylaminoalkyl ureas, thioureas and cyanoguanidines represented by the following formula: ##STR1## wherein Ar is aryl selected from the group consisting of 1- and 2-naphthyl, 2,3-dihydro-1H-inden-4(or 5)-yl,2-furanylmethyl,2-pyridinyl, phenyl and phenyl substituted by 1-3 radicals commonly used in the pharmaceutical art; (X).sub.d is oxygen, thio, sulfinyl, sulfonyl or d is zero; Z and W are each R or-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 wtih the proviso that when Z is R, W is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 and when Z is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2, W is R; B is carbonyl, thioxomethyl, or cyanoiminomethyl; R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl wherein phenyl may be substituted by 1-3 radicals commonly used in the pharmaceutical art; R.sup.1 and R.sup.2, and R.sup.3 and R.sup.Type: GrantFiled: June 10, 1987Date of Patent: January 23, 1990Assignee: A. H. Robins Company, IncorporatedInventor: James R. Shanklin, Jr.
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Patent number: 4895841Abstract: A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22)r--, R22 being H or methyl, --CO--(CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.Type: GrantFiled: June 20, 1988Date of Patent: January 23, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Yutaka Tsuchiya, Kunizou Higurashi, Norio Karibe, Youichi Iimura, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Takashi Kosasa, Atsuhiko Kubota, Michiko Kosasa, Kiyomi Yamatsu
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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: 4889864Abstract: Compounds of the formula (I) ##STR1## in which n denotes a number from 2 to 6, m denotes 1 or 2,R denotes ##STR2## R.sup.1 denotes (substituted) alkyl, (substituted) alkenyl, C.sub.3 -alkynyl, cycloalkyl, cycloalkenyl or an aromatic or heteroaromatic radical, R.sup.2 denotes H or alkyl and Y denotes H, alkyl, phenyl or halophenyl, and the metal-salt complexes thereof have advantageous fungicidal actions and are highly suitable for use in plant protection or in the industrial sector.Type: GrantFiled: December 1, 1987Date of Patent: December 26, 1989Assignee: Hoechst AktiengesellschaftInventors: Heinz Ehrhardt, Hilmar Mildenberger, Thomas Maier, Rainer Schaller, Burkhard Sachse, Peter Braun
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Patent number: 4880800Abstract: Compounds are described of the formula ##STR1## where: R.sup.1 is --H or --CH.sub.3,n is 1, m is 2-4 and X is --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --;Y is a saturated heterocyclic amino group,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thineylalkyl or naphthylalkyl or (ii) cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formualted for use as antithrombotic or antiasthmatic agents.Type: GrantFiled: September 15, 1987Date of Patent: November 14, 1989Assignee: Glaxo Group LimitedInventors: Christopher J. Wallis, Harry Finch, Peter Hallett
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Patent number: 4879293Abstract: The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S-- is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychoromatic disease and anxiety neurosis.Type: GrantFiled: September 8, 1988Date of Patent: November 7, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Kentaro Hiraga, Yoshiaki Saji
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Patent number: 4877901Abstract: The present invention relates to a process for synthesizing N,N'-dithiobis(sulfonamides) by reacting a sulfonamide of the formula: ##STR1## with sulfur monochloride and caustic in a mixed organic-aqueous mediua, wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkyl radicals having from about 1 to about 20 carbon atoms, cycloalkyl radicals having from about 5 to about 20 carbon atoms, phenyl radicals, alkaryl radicals having from about 7 to 20 carbon atoms, and haloaryl radicals having about 6 to about 10 carbon atoms and where R.sup.1 is also selected from radicals having the formula: ##STR2## wherein R.sup.3 and R.sup.4 are individually selected from said alkyl, cycloalkyl, phenyl, alkaryl and haloaryl radicals and wherein R.sup.3 and R.sup.4 can be joined together to represent radicals selected from --CH.sub.2 --.sub.n, where n is an integer of 4 to 7 and --CH.sub.2).sub.2 O--CH.sub.2 --.sub.2.Type: GrantFiled: October 28, 1988Date of Patent: October 31, 1989Assignee: The Goodyear Tire & Rubber CompanyInventors: Roger J. Hopper, Niranjan V. Shah, Steven M. Ryba
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Patent number: 4861776Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.Type: GrantFiled: February 25, 1988Date of Patent: August 29, 1989Assignee: Syntex (U.S.A) Inc.Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
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Patent number: 4857522Abstract: Derivatives of pravastatin are provided which are useful in inhibiting cholesterol biosynthesis and in preparing radiolabeled compounds useful in the radioimmunoassay (RIA) of pravastatin and derivatives thereof. The pravastatin derivatives have the structure ##STR1## wherein R is hydroxy, lower alkylamine, arylamine, arylalkylamine or heterocyclic alkylamine such as histamine, tyramine, O-benzyltyramine, methyl tyrosinate as well as iodinated derivatives thereof.Type: GrantFiled: March 21, 1988Date of Patent: August 15, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Richard A. DiPietro, Jan-I Tu, Noor Z. Turabi
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Patent number: 4855316Abstract: Certain 1,2-diamino-4,5-dimethoxycyclohexane amide derivatives have analgesic activity, and bind selectively to the kappa opioid receptor site. Pharmaceutical compositions containing these compounds, and a method of alleviating pain in mammals are also disclosed.Type: GrantFiled: February 18, 1988Date of Patent: August 8, 1989Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Stephen J. Johnson
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Patent number: 4851406Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.Type: GrantFiled: September 4, 1986Date of Patent: July 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
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Patent number: 4849422Abstract: New alkylol derivatives are described, which belong to the class having the structure formula ##STR1## where R represents a 5 or 6 membered heterocyclic ring selected among pyridine, pyrimidine, pyrazine, pyridazine, thiophene, furan, thiazole which optionally may be substituted with one or more groups selected among alkyl, alkoxy, halogen, amide, hydroxy, methylthio, trifluoromethyl, cyano, carboxy and the corresponding alkyl esters and salts with alkali metalsn is 2X and X' represent each a hydrogen atom or hydroxy group with the exception of both being hydrogen atom, and X' may be hydroxyethoxy moietym is 0 or 1and the corresponding non-toxic pharmaceutically acceptable acid addition salts. The compounds of the formula I are endowed with an interesting antitussive activity and, at their active dose, practically they are free of undesired side effects.Type: GrantFiled: January 16, 1987Date of Patent: July 18, 1989Assignee: Dompe' Farmaceutici S.p.A.Inventors: Roberto P. Giani, Salvatore Malandrino, Giancarlo Tonon
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Patent number: 4837316Abstract: Alkylamide derivatives having the formula, These compounds have a strong antiulcer action depend on histamine H.sub.2 -receptor antagonistic action and a cytoprotective action upon gastric mucous membrance.Type: GrantFiled: August 27, 1986Date of Patent: June 6, 1989Assignee: Fujirebio Kabushiki KaishaInventors: Yasuo Sekine, Nobuhiro Hirakawa, Noriaki Kashiwaba, Tetsuaki Yamaura, Hisako Harada, Teruo Kutsuma, Hajime Matsumoto, Akihiro Sekine, Yoshikazu Isowa
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Patent number: 4835164Abstract: Novel heterocyclicmethanols are disclosed having the formula: ##STR1## wherein Z is pyrrolidinyl, piperidinyl, homopiperidinyl or pyridinyl; R.sup.1 is hydrogen, loweralkyl or carbethoxymethyl;R.sup.2 is hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl;R.sup.3 is 1 or 2-naphthalenyl, 2,3-dihydroinden-4 or 5-yl, phenyl or phenyl substituted by loweralkyl, loweralkoxy, halogen, trifluoromethyl, phenyl, methylenedioxy, nitro, amino, loweralkylamino, diloweralkylamino, loweracylamino;the 1-position of 2-pyrrolidinyl, 2-piperidinyl or 2-homopiperidinyl may be substituted by an R.sup.4 loweralkyl group, or R.sup.1 may form methylene or --CH.sub.2 -C(O)-bridges with R.sup.4 ;the pharmaceutically acceptable salts and diastereomers thereof, which compounds have antiarrhythmic and/or hypotensive activity in animals.Type: GrantFiled: February 20, 1987Date of Patent: May 30, 1989Assignee: A. H. Robins Company, IncorporatedInventors: James R. Shanklin, Jr., Christopher P. Johnson, III
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Patent number: 4835271Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is C.sub.1-7 alkyl substituted by NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen or C.sub.1-4 alkyl or together are C.sub.3-7 polymethylene optionally containing a further hetereoatom which is oxygen, sulphur or nitrogen substituted by R.sub.10 where R.sub.10 is hydrogen, C.sub.1-4 alkyl or benzyl, and optionally substituted by one or two C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups or by a benzyl group, cyano, phenyl or benzyl and wherein any phenyl or benzyl group is optionally substituted in the phenyl ring by one or two halo, CF.sub.3, C.sub.1-4 alkyl, C.sub.Type: GrantFiled: June 26, 1986Date of Patent: May 30, 1989Assignee: Beecham-Wuelfing GmbH & Co., KGInventors: Dagmar Hoeltje, Dietrich Thielke
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Patent number: 4826836Abstract: Fungicidally active novel saccharine salts of aminomethyl heterocyclic compounds of the formula ##STR1## in which R represents optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted thienyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents alkyl, alkenyl or alkinyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms,X represents oxygen or sulphur,Y represents oxygen, sulphur or the methylene group,m represents 0 or 1 andn represents 0 or 1.Type: GrantFiled: November 5, 1987Date of Patent: May 2, 1989Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Wolfgang Kramer, Paul Reinecke, Gerd Hanssler
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Patent number: 4822803Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: February 4, 1988Date of Patent: April 18, 1989Assignee: Merck Frosst Canada, Inc.Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
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Patent number: 4816474Abstract: Disclosed are compounds of the formula ##STR1## wherein A represents the divalent radical --S--CR.sub.4 .dbd.CR.sub.5 -- in which R.sub.4 and R.sub.5 independently represent hydrogen or lower alkyl; R.sub.1 represents hydrogen, lower alkyl or aryl-lower alkyl; R.sub.2 represents hydrogen, lower alkyl or aryl-lower alkyl; or R.sub.1 and R.sub.2 combined represent alkylene of 4 to 6 carbon atoms; R.sub.3 represents hydrogen or lower alkyl; an S-oxide thereof; or a pharmaceutically acceptable salt thereof; which are useful as presynaptic dopamine receptor agonists for the treatment of central nervous system disorders; processes for preparing same; and pharmaceutical compositions comprising said compounds.Type: GrantFiled: February 27, 1987Date of Patent: March 28, 1989Assignee: Ciba-Geigy CorporationInventor: Alan J. Hutchison
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Patent number: 4806604Abstract: The present invention discloses a new class of calcium chelating compounds which have a decreased affinity for calcium following illumination. These new compounds contain a photolabile nitrobenzyl derivative coupled to a tetracarboxylate Ca.sup.2+ chelating parent compound having the octacoordinate chelating groups characteristic of EGTA or BAPTA. However unlike EGTA or BAPTA-like compounds, in which the two halves of the chelator are linked by a simple 1,2-ethanediyl moiety, the compounds of the present invention modify the stereochemical conformation of this linkage by adding bulky substituents or incorporating the linkage into a carbocyclic or heterocyclic ring. In a first form, the new compounds are comprised of a BAPTA-like chelator coupled to a single 2-nitrobenzyl derivative, which in turn is a photochemical precursor of a 2-nitrosobenzophenone.Type: GrantFiled: May 13, 1987Date of Patent: February 21, 1989Assignee: Regents of the University of CaliforniaInventors: Roger Yonchien Tsien, Stephen R. Adams
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Patent number: 4801585Abstract: A compound of formula (I): ##STR1## or a salt or solvate thereof in which R. CO is an acyl group containing a substituted or unsubstituted carbocyclic or heterocyclic aromatic ring, R.sub.1 and R.sub.2 are independently C.sub.1-6 alkyl or together form a C.sub.3-6 polymethylene or alkylene group, and p is 1, 2, 3 or 4, is useful for treating pain.Type: GrantFiled: December 22, 1986Date of Patent: January 31, 1989Assignee: Dr.Lo.Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Massimo Signorini, Antonio Giordani
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Patent number: 4801605Type: GrantFiled: February 27, 1987Date of Patent: January 31, 1989Assignee: Ciba-Geigy CorporationInventor: Alan J. Hutchison
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Patent number: 4788184Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.Type: GrantFiled: November 13, 1987Date of Patent: November 29, 1988Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4767757Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1##Type: GrantFiled: March 19, 1987Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4764617Abstract: A novel quinaldinamide derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents a lower alkyl group or R.sup.1 and R.sup.2 are combined together with the adjacent nitrogen atom to form a 5-7 membered ring; and X represents the hydrogen atom, a lower alkyl group or a lower alkoxy group, and its acid-addition salt, which show prominent central muscle relaxant effect, namely rigidity relieving effect on anemic decerebrated rigidity.Type: GrantFiled: August 13, 1986Date of Patent: August 16, 1988Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Haruhiko Shinozaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro
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Patent number: 4760061Abstract: Mono- or bis-complex esters or ethers of a phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; whereinA is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, whereinR.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, whereinR.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; whereinR.sup.12 is hydrogen or alkyl, and whereinR.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: July 26, 1988Assignee: Imperial Chemical Industries PLCInventors: Philip N. Edwards, Brian S. Tait
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Patent number: 4752607Abstract: Alkoxycarbonyl-substituted hydroxythiophenecarboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl or alkinyl or represents cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.3 represents alkyl, alkoxyalkyl, alkylthioalkyl, cyanoalkyl, fluoroalkyl, alkenyl, alkinyl, cycloalkyl or alkoxy andR.sup.4 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl, orR.sup.3 and R.sup.4, together with the nitrogen atom, represent a heterocyclic radical which is optionally substituted by alkyl and can be further substituted in the alkylene chain by oxygen, sulphur or nitrogen,are useful as fungicides and intermediates.Type: GrantFiled: June 17, 1986Date of Patent: June 21, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4751316Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is >C.dbd.O or >CH--OR.sub.5 (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.Type: GrantFiled: April 15, 1987Date of Patent: June 14, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4749786Abstract: Disclosed is the hydrocarboxylation of defined enamides with CO and a compound ROH to make amido acids or amido esters, either of which can be hydrolyzed to .alpha.-amino acids.Type: GrantFiled: April 6, 1987Date of Patent: June 7, 1988Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, James D. Burrington
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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: 4748173Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.Type: GrantFiled: September 23, 1987Date of Patent: May 31, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
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Patent number: 4745121Abstract: This invention relates to pyrazolo[3,4-b]pyridine amides useful as anxiolytic agents.Type: GrantFiled: September 11, 1985Date of Patent: May 17, 1988Assignee: ICI Americas Inc.Inventor: Thomas M. Bare
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Patent number: 4745127Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.Type: GrantFiled: January 7, 1987Date of Patent: May 17, 1988Assignee: Merck Frosst Canada, Inc.Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
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Patent number: 4737518Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.Type: GrantFiled: September 12, 1986Date of Patent: April 12, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima, Yoshio Kozai
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Patent number: 4737494Abstract: A 1,3-dithiole derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 is a substituted or unsubstituted alkyl, cycloalkyl, lower alkenyl, lower alkynyl, aryl or aralkyl group or R.sup.1 and R.sup.2 together form a substituted or unsubstituted alkylene or alkenylene group having from 3 to 6 carbon atoms, which may contain a cycloalkylene group, an o-phenylene group or a hetero atom selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom which may have a substituent, and Q is an acid residue useful for the treatment of liver diseases.Type: GrantFiled: December 26, 1985Date of Patent: April 12, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Mitsuo Yano, Yoshimi Tsuchiya, Yukio Hirayama, Kyoko Nakamichi, Junji Yoshizawa
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Patent number: 4737493Abstract: Substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzofuranyl-, and benzo[b]thiofuranylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes are useful as analgesic agents.A method of making the compounds, pharmaceutical compositions employing the compounds, and a method of alleviating pain in warm-blooded animals are also disclosed.Type: GrantFiled: June 9, 1986Date of Patent: April 12, 1988Assignee: Warner-Lambert CompanyInventor: David C. Horwell
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Patent number: 4736031Abstract: Novel condensed seven-membered heterocyclic compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy,R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom,X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated,Y is >C.dbd.O or >CH--OR.sub.5 in which R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl,A is oxygen atom or sulfur atom, E is oxygen atom or methylene, andG is lower alkylene, provided that when A is sulfur atom, E is methylene,and salts thereof exhibit serotonin S.sub.Type: GrantFiled: April 15, 1986Date of Patent: April 5, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata