The Additional Hetero Ring Consists Of One Oxygen And Four Carbons Patents (Class 546/214)
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Patent number: 4987132Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.Type: GrantFiled: August 16, 1988Date of Patent: January 22, 1991Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
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Patent number: 4975445Abstract: Substituted cyclohexenes 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: December 4, 1990Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
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Patent number: 4942170Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.Type: GrantFiled: May 27, 1988Date of Patent: July 17, 1990Assignee: The Rockefeller UniversityInventors: Graeme B. Henderson, Peter C. Ulrich, Anthony Cerami
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N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannonojirimycin and pharmaceutical use
Patent number: 4940705Abstract: N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannojirimycin of the formula ##STR1## in which one of R and R' are hydroxyl and the other is hydrogenn is a number from 1 to 6R.sup.1 is hydrogen, alkyl or benzyl andR.sup.2 is alkyl which is optionally substituted by an optionally substituted aryl or by pyridyl, thienyl, furyl, pyrimidyl, pyrazinyl or quinolyl or R.sub.1 is cycloalkyl or R.sup.2 is optionally substituted by aryl or R.sup.2 is a saturated bridged heterocycle or R.sup.1 and R.sup.2 together can form a heterocyclic ring which is optionally substituted. These compounds are useful in the treatment of and prophylaxis of viral infections.Type: GrantFiled: October 26, 1988Date of Patent: July 10, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Bodo Junge, Arnold Paessens, Matthias Schuller -
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: 4918187Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sub.c is carboxy, esterified carboxy or amidated carboxy; R.sub.2 is hydrogen or lower alkyl or joins with R.sub.a and R.sub.b and the atoms therebetween to form a fused ring ##STR2## and either R.sub.a is methyl and R.sub.b is ##STR3## or R.sub.2 and R.sub.b and the atoms therebetween form a group ##STR4## wherein R.sub.3 and R.sub.4 are either both hydrogen, or together are propylene, butylene, or with the two atoms to which they are attached form a benzene ring. Methods of manufacture and use thereof in the production of angiotensin converting enzyme inhibitors are disclosed.Type: GrantFiled: September 27, 1988Date of Patent: April 17, 1990Assignee: Ciba-Geigy CorporationInventor: Stephen K. Boyer
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Patent number: 4910312Abstract: Selected analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: June 16, 1988Date of Patent: March 20, 1990Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4904656Abstract: Fungicidally active 2-aminomethyltetrahydrofurans of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted aryl, heteroaryl, cycloalkyl, tetrahydronaphthyl or decahydronaphthyl;R.sup.2 represents hydrogen or methyl; andR.sup.3 and R.sup.4, independently of one another, in each case represent hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroxyalkyl, hydroxyalkoxyalkyl, dioxolanylalkyl, oxolanylalkyl, dioxanylalkyl, or in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bound, represent an optionally substituted saturated heterocyclic ring which may optionally contain further heteroatoms,or acid-addition salts thereof.Type: GrantFiled: January 25, 1988Date of Patent: February 27, 1990Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Dieter Berg, Stefan Dutzmann, Gerd Hanssler
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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: 4888337Abstract: This invention relates to:(a) new tetrahydrofuran derivatives having the general formula I: ##STR1## wherein either each of R and R' independently represents a hydrogen atom or various hydrocarbon substituents and A represents either a nitrogen containing ring or an alkylammonium salt or an alkylaminoacid rest;(b) a process for the preparation of said compounds and(c) therapeutic compositions containing said compounds as an active ingredient.Type: GrantFiled: January 15, 1988Date of Patent: December 19, 1989Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Jean-Jacques Godfroid, Francoise Heymans, Pierre Braquet
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Patent number: 4876262Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R1 is a lower alkyl or a tolyl, R2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH2-- 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, --CH2COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## 1 being 1 or 2, --A--B, A being --(CH2)n--, n being an integer of 1 to 5, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalentType: GrantFiled: February 18, 1987Date of Patent: October 24, 1989Assignee: 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: 4861892Abstract: A method is disclosed for the chemical synthesis of 1,5-dideoxy-1,5-imino-D-mannitol or 1,5-dideoxy-1,5-imino-L-mannitol from, respectively, 2,3-O-isopropylidene-L-gulono-.gamma.-lactone or 2,3-O-isopropylidene-D-gulono-.gamma.-lactone which comprises carrying out interconversion between the L-gulono and D-mannono forms or between the D-gulono and L-mannono forms, respectively, and connecting of C-1 to C-5 by nitrogen.Type: GrantFiled: September 26, 1988Date of Patent: August 29, 1989Assignee: G. D. Searle & Co.Inventor: George W. J. Fleet
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Patent number: 4859673Abstract: Novel amide derivatives are disclosed. As examples of said amide derivatives are mentioned 1-[2-(5-(3-methoxy-4-benzyloxyphenyl)-2,4-pentadienoyl)aminoethyl]-4-diphe nylmethoxypiperidine, 1-[2-(5-(3-methoxy-4-pentadienoyl)aminoethyl]-4-diphenylmethoxypiperidine and 1-[2-(5-(3-methoxy-4-ethoxymethoxyphenyl)-2,4-pentadienoyl)aminoethyl]-4-d iphenylmethoxypiperidine. These amide derivatives are useful as antiallergic agents.Type: GrantFiled: April 23, 1987Date of Patent: August 22, 1989Assignee: Terumo Kabushiki KaishaInventors: Makoto Takai, Kazuhiro Omori, Takahiro Kumonaka, Shinji Ozawa, Toshio Wakabayashi
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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: 4806552Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --NM.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: November 12, 1986Date of Patent: February 21, 1989Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4798892Abstract: The present invention relates to compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1, wherein R.sub.1, R.sub.2 and R.sub.3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: April 14, 1986Date of Patent: January 17, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
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Patent number: 4791133Abstract: This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.Type: GrantFiled: June 26, 1987Date of Patent: December 13, 1988Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
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Patent number: 4774334Abstract: Compounds possessing antiallergy activity have the formula: ##STR1## wherein R and R.sup.1 are independently hydrogen or alkyl, or R and R.sup.1 together with the attached nitrogen form a heterocyclic ring system selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl and 1, 2, 3, 4-tetrohydroquinolinyl, and R.sup.2 is phenyl or phenyl monosubstituted with a lower alkyl, a nitro, a halogenated methyl, a halogen or a lower alkoxy group.Type: GrantFiled: November 9, 1987Date of Patent: September 27, 1988Assignee: Pennwalt CorporationInventors: Vassil S. Georgiev, Thomas R. DeCory
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Patent number: 4772618Abstract: Substituted benzamides of the general formula I ##STR1## in which: R represents an alkoxy, alkenyloxy or alkynyloxy group containing up to 7 carbon atoms in the group,R.sub.1 is hydrogen or a NR.sub.4 R.sub.5, or NR.sub.6 COR.sub.7 group, where R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, is each hydrogen or an alkyl group and R.sub.7 is an alkyl or trifluoromethyl group,R.sub.2 is hydrogen, halogen, or a nitro, or sulphamoyl group,R.sub.3 represents hydrogen or a methyl or methoxy group,X represents a hydrocarbon chain containing 1 to 4 carbon atoms, one of which may optionally be replaced by an oxygen atom,Y represents a non-aromatic cyclic ether or a non-aromatic cyclic thioether group and pharmaceutically acceptable salts thereof are useful in the treatment of gastro-intestinal disorders. Various methods of synthesis are described including synthesis via novel amines of the formula ##STR2## which are themselves obtained by reduction of the corresponding oximes.Type: GrantFiled: July 31, 1986Date of Patent: September 20, 1988Assignee: Fordonal, S.A.Inventors: Armando Vega-Noverola, Jose M. Prieto-Soto, Fernando Pujol-Noguera, Jacinto Moragues-Mauri, Robert G. W. Spickett
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Method for controlling emesis caused by chemotherapeutic agents and antiemetic agents useful therein
Patent number: 4772459Abstract: A method for alleviating emesis caused by chemotherapy which comprises administering an antiemetic agent or a pharmaceutically acceptable salt thereof to a patient in conjunction with the administration of a chemotherapeutic agent, said antiemetic agent being represented by the formula (I) ##STR1## wherein Z represents a substituent such as a lower alkyl group, a methoxyethoxymethyl group, or a benzoylmethyl group; or Z in conjunction with the adjacent position represents the atoms necessary to complete a 5 to 7 membered saturated or unsaturated oxygen-containing ring; R represents a hydrogen atom, a halogen atom, a lower alkyl group, a cycloalkyl group, a lower alkoxy group, an amino group, an alkylsulfonyl group, a lower alkyl-substituted amino group, an acylamido group, a sulfamoyl group, a sulfonamido group or a nitro group; n is an integer of 1 to 3; W is a straight chain or branched chain alkylene group of 1 to 4 carbon atoms; and X represents the atoms necessary to complete a 5 or 6 membered ring; saidType: GrantFiled: September 9, 1986Date of Patent: September 20, 1988Assignee: Erbamont, Inc.Inventors: Jung-Hui Sun, Chih-Yun J. Tu -
Patent number: 4736055Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.Type: GrantFiled: April 11, 1986Date of Patent: April 5, 1988Assignee: Ciba-Geigy CorporationInventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
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Patent number: 4727072Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.Type: GrantFiled: February 12, 1986Date of Patent: February 23, 1988Assignee: McNeilab, Inc.Inventors: Philip P. Grous, Richard J. Mohrbacher
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Patent number: 4722930Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: September 30, 1985Date of Patent: February 2, 1988Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4703072Abstract: Novel tetrahydrofurancarboxylic acid derivatives of the general formula I ##STR1## or polymers of these containing units of the formula II ##STR2## where the radicals R independently of one another are each C.sub.1 -C.sub.4 -alkyl, cyclohexyl or phenyl, m is from 0 to 3, n is 1 or 2, and R' is a radical of the formula ##STR3## suitable terminal groups in the polymers being chlorine or hydroxyl in the case of the CO group and hydrogen in the case of the --NR.sup.2 group, A is a bridge member, R.sup.1 is hydrogen, C.sub.2 -C.sub.6 -alkenyl, C.sub.1 -C.sub.12 -alkyl which may be interrupted by up to 3 oxygen atoms, unsubstituted or substituted phenylalkyl or C.sub.5 -C.sub.7 -cycloalkyl and R.sup.2 is radical of the formula ##STR4## where R.sup.3 is hydrogen or methyl, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are each methyl or ethyl and R.sup.8 is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.8 -alkenyl, C.sub.2 -C.sub.Type: GrantFiled: June 16, 1986Date of Patent: October 27, 1987Assignee: BASF AktiengesellschaftInventors: Reinhard Helwig, Peter Neumann, Alexander Aumueller, Hubert Trauth
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Patent number: 4659721Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.Type: GrantFiled: January 22, 1985Date of Patent: April 21, 1987Assignee: Ludwig Heumann & Co. GmbHInventors: Helmut Schickaneder, Stefan Postius, Istvan Szelenyi, Peter Morsdorf, Rolf Herter, Kurt H. Ahrens
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Patent number: 4647560Abstract: The present invention relates to novel benzodiazepines, acid addition salts thereof, processes for their preparation and their use in combating diseases, in particular for the treatment of cerebral disorders caused by old age and for the treatment of disorders in learning and memory and amnesia.Type: GrantFiled: August 8, 1985Date of Patent: March 3, 1987Assignee: Troponwerke GMBH & Co. KGInventors: Karl-Heinz Boltze, Eugen Etschenberg, Jorg Traber, Herbert Busgen
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Patent number: 4642315Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.Type: GrantFiled: October 22, 1984Date of Patent: February 10, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Harold N. Weller, III
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Patent number: 4639436Abstract: The invention includes certain 3,4,5-trihydroxypiperidine compounds, methods for their preparation, compositions containing said 3,4,5-trihydroxypiperidine compounds and methods for the use of said compounds and compositions.The subject matter of the invention is useful against diabetes, hyperlipaemia and adiposity as well as in animal nutrition.Type: GrantFiled: August 23, 1978Date of Patent: January 27, 1987Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Hans P. Krause, Lutz Muller, Walter Puls
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Patent number: 4634701Abstract: Compounds of formula (I): ##STR1## wherein: A represents a CH-NO.sub.2 group or a N-CN group;B represents CH.sub.2, O, S or a direct bond;R represents a bicyclic or polycyclic residue, variously substituted and functionalized;R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl groups; andn and m, which may be the same or different, are 0, 1, 2, 3 or 4;are valuable pharmacological agents.Type: GrantFiled: May 28, 1985Date of Patent: January 6, 1987Assignee: Ausonia Farmaceutici s.r.l.Inventor: Leonardo De Vincentiis
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Patent number: 4615725Abstract: Tetrahydrofuran-2-ylmethylamines of the formula ##STR1## in which R.sup.1 represents optionally substituted naphthyl, optionally substituted cycloalkyl or cycloalkenyl, optionally substituted phenyl, or alkyl which is substituted by in each case optionally substituted phenyl, phenoxy or phenylthio,R.sup.2 represents hydrogen or methyl,R.sup.3 represents alkyl andR.sup.4 represents alkyl, alkenyl, alkinyl or optionally substituted aralkyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical, which can contain further hetero-atoms,excluding the compounds in which R.sup.3 and R.sup.4 both represent methyl, R.sup.1 represents unsubstituted phenyl and R.sup.2 at the same time represents hydrogen, or plant-tolerated addition products thereof with acids or metal salts, which possess fungicidal and plant growth regulating activities.Type: GrantFiled: April 8, 1985Date of Patent: October 7, 1986Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Wolfgang Kramer, Dieter Berg, Paul Reinecke, Wilhelm Brandes, Gerd Hanssler, Klaus Lurssen
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Patent number: 4616017Abstract: Novel tertiary aminohydroxypropoxy substituted aryl compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.Type: GrantFiled: June 4, 1984Date of Patent: October 7, 1986Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 4613596Abstract: New compounds active in the treatment of ulcers and alergic skin symptoms are prepared by reacting 2-[[5-[(dimethylamino)methyl]furfuryl]thio]ethylmethylsulphide with a suitable compound of formula RH. Said compounds are particularly useful as active principles in pharmaceutical compositions for use in the treatment of affections which require the administration of antagonists for histamine H.sub.2 receptors.Type: GrantFiled: December 16, 1985Date of Patent: September 23, 1986Assignee: Magis Farmaceutrici s.r.l.Inventor: Adolfo Moroni
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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: 4603205Abstract: Novel furancarboxylic acid derivatives of the general formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3 independently of one another are each hydrogen, C.sub.1 -C.sub.8 -alkyl, cyclohexyl or phenyl, but not more than two of these radicals are simultaneously hydrogen, and R.sup.4 is a radical of the formula --NR.sup.5 R.sup.6, ##STR2## or OR.sup.6, where A is a bridge member, R.sup.5 is hydrogen, C.sub.2 -C.sub.6 -alkenyl, C.sub.5 -C.sub.7 -cycloalkyl or C.sub.1 -C.sub.12 -alkyl which may or may not be interrupted by 1, 2 or 3 oxygen atoms, and R.sup.6 is a radical of the formula ##STR3## where R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are each C.sub.1 -C.sub.4 -alkyl, or R.sup.7 and R.sup.8 or R.sup.9 and R.sup.10 together form a tetramethylene or pentamethylene bridge, and R.sup.11 is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.8 -alkenyl, C.sub.2 -C.sub.4 -hydroxyalkyl or aralkyl, and their salts are useful as light stabilizers for organic polymers, in particular olefin polymers.Type: GrantFiled: December 13, 1984Date of Patent: July 29, 1986Assignee: BASF AktiengesellschaftInventors: Peter Neumann, Reinhard Helwig, Stefan Weiss, Hubert Trauth
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Patent number: 4594351Abstract: Compounds of the following formula (I): ##STR1## wherein Alk is a straight or branched chain alkylene of about 1 to 12 carbons and R.sup.1 is a heterocyclic ring system, have been found to possess potent antisecretory activity and are thus useful in the treatment of hyperacidity.Type: GrantFiled: April 25, 1985Date of Patent: June 10, 1986Assignee: McNeilab, Inc.Inventor: Malcolm K. Scott
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Patent number: 4588826Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: December 3, 1984Date of Patent: May 13, 1986Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4585779Abstract: cis-4a-Aryl-1,2,3,4,4a,9b-hexahydro-benzofuro[3,2-c]pyridines and methods of preparing same are described. On the nitrogen atom there may be a substituent including loweralkyl, loweralkenyl, phenylloweralkyl, hydrogen cyanoloweralkyl, phenylcarbonylloweralkyl, phenoxyloweralkyl and cycloalkylloweralkyl. The 4a-aryl group may be a phenyl, mono-halogen substituted phenyl, tolyl, methoxyphenyl, hydroxyphenyl, or furyl. These compounds are useful as analgesic and anticonvulsant agents.3-o-Fluorophenyl-1-methyl-4-aryl-4-piperidinols which are useful as intermediates for preparing the aforementioned compounds and methods for preparing same are also described.Type: GrantFiled: December 21, 1984Date of Patent: April 29, 1986Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Solomon S. Klioze
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Patent number: 4585791Abstract: The present invention relates to new furyl derivatives of 16-substituted prostaglandins, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.The new compounds of the invention are optically active or racemic prostaglandins of the following formula (I) ##STR1## wherein R is(1) --OH or --OR' wherein R' is C.sub.1 -C.sub.6 alkyl optionally substituted by phenyl or by a monocycloalkyl group or by a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N;(2) ##STR2## wherein each of R" and R"', is independently, hydrogen; C.sub.1 -C.sub.6 alkyl; phenyl; or a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N; or R" and R"', together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic heteromonocyclic ring optionally containing a further heteroatom chosen from O, S and N;(3) --W--(CH.sub.2).sub.Type: GrantFiled: November 1, 1984Date of Patent: April 29, 1986Assignee: Farmitalia Carlo Erba, S.p.A.Inventors: Franco Faustini, Achille Panzeri, Fabrizio Orzi, Enrico di Salle, Roberto Ceserani
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Patent number: 4579951Abstract: This invention relates to novel substituted (azacycloalk-2-yl)iminophenols that are useful in the treatment of diarrhea.Type: GrantFiled: March 19, 1984Date of Patent: April 1, 1986Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Stella S. T. Yu, Robert W. Hamilton
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Patent number: 4568376Abstract: 5-Amino-3-oxo-4-(substituted-phenyl)-2,3-dihydrofuran and derivatives thereof. The compounds generally exhibit both pre-emergence and post-emergence phytotoxicity and are useful as herbicides and also at low dosages as plant growth regulating agents.Type: GrantFiled: April 16, 1985Date of Patent: February 4, 1986Assignee: Chevron Research CompanyInventor: Carl E. Ward
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Patent number: 4568377Abstract: 5-Amino-2-aryl-3-oxo-4-(substituted-phenyl)-2,3-dihydrofuran and derivatives thereof. The compounds generally exhibit both pre-emergence and post-emergence phytotoxicity with respect to grassy and broadleaf weeds and have improved crop safety.Type: GrantFiled: April 26, 1985Date of Patent: February 4, 1986Assignee: Chevron Research CompanyInventor: Carl E. Ward
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Patent number: 4568375Abstract: 2-Halo and 2-alkoxy-5-amino-3-oxo-4-(substituted-phenyl)-2,3-dihydrofuran and derivatives thereof. The 2-alkoxy and 2-fluoro compounds generally exhibit both pre-emergence and post-emergence phytotoxicity and are useful as herbicides and also at low dosages as plant growth regulating agents. The 2-bromo, chloro and iodo compounds are primarily useful as intermediates for the 2-alkoxy and 2-fluoro analogs.Type: GrantFiled: October 26, 1984Date of Patent: February 4, 1986Assignee: Chevron Research CompanyInventor: Carl E. Ward
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Patent number: 4563466Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammoniun salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 26, 1983Date of Patent: January 7, 1986Inventors: John L. Archibald, Terence J. Ward
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Patent number: 4556649Abstract: Insecticidally active novel substituted malonic acid diamide insecticides of the formula ##STR1## wherein R.sup.1 represents aryl or heteroaryl, each of which can optionally be substituted,R.sup.2 represents hydrogen or trialkylsilyl, and represents alkyl, cycloalkyl, alkenyl, alkinyl, aralkyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphenyl, arylsulphenyl, alkylsulphonyl, arylsulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl, arylaminosulphonyl or arylalkylaminosulphonyl, each of which can optionally be substituted, and represents radicals of the formula--CO--NR.sup.5 R.sup.6whereinR.sup.5 and R.sup.6 independently of one another represent hydrogen, alkyl, cycloalkyl, aryl, alkylaminocarbonyl, arylaminocarbonyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphonyl or arylsulphonyl, it being possible for these radicals to be optionally substituted,R.sup.3 represents hydrogen or the radical R.sup.4,R.sup.7 and R.sup.Type: GrantFiled: December 21, 1984Date of Patent: December 3, 1985Assignee: Bayer AktiengesellschaftInventors: Herbert Salzburg, Rudolf Fauss, Kurt Findeisen, Bernhard Homeyer
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Patent number: 4539416Abstract: A process for making N-furfurylthioalkyl carboxamide by reacting an oxaz(ol)ine with furfurylmercaptan in the absence of a transition metal catalyst. The carboxamide may then be hydrolyzed to form the 2-furfurylthioalkylamine.Type: GrantFiled: June 10, 1983Date of Patent: September 3, 1985Assignee: The Dow Chemical CompanyInventors: Harold G. Fravel, Jr., Michael J. Fazio
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Patent number: 4537963Abstract: Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3,2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl]-7-oxa-2-azabicyclo[3.3.1]octane in which L is a leaving group selected from the group consisting of --Cl, --Br, --I, p--MeC.sub.6 H.sub.4 SO.sub.3 -- and MeSO.sub.3 --.Type: GrantFiled: August 11, 1983Date of Patent: August 27, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Ashokkumar B. Shenvi
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Patent number: 4532327Abstract: A novel alkaloid compound named "sesbanimide" has been isolated from the tissue of a leguminous plant known as Sesbania drummondii. Sesbanimide is characterized by the structural formula ##STR1## and is effective as an antineoplastic agent in animals.Type: GrantFiled: December 28, 1983Date of Patent: July 30, 1985Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Richard G. Powell, Cecil R. Smith, Jr.
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Patent number: 4513139Abstract: Novel substituted lactones of amino acids in all their possible stereoisomeric forms or mixtures thereof of the formula ##STR1## wherein A is a hydrocarbon chain of 1 to 10 chain members containing one or more heteroatoms and one or more unsaturations and the chain members being a mono- or polycyclic system or comprises a system of spiro or endo type and may contain one or more chiral atoms or the lactone copula can present a supplementary chirality due to the asymetric spatial configuration of the molecule make up and R is selected from the group consisting of ##STR2## wherein Z is the organic remainder of an amino acid of the formula ##STR3## Y is derived from a primary, secondary or tertiary alcohol of the formula Y--OH and B is the remainder of a heterocyclic amino acid of 3 to 6 carbon atoms of the formula ##STR4## and their preparation and their use for the resolution of amino acids.Type: GrantFiled: June 30, 1982Date of Patent: April 23, 1985Assignee: Roussel UclafInventors: Jacques Martel, Jean Tessier, Andre Teche
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Patent number: 4503051Abstract: 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: June 13, 1983Date of Patent: March 5, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas