Acyclic Nitrogen Bonded Directly To The Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 548/495)
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Patent number: 5002943Abstract: Novel condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, A.sup.1, A.sup.2 and R.sup.1 -R.sup.10 are as defined herein. The condensed diazepinones are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia and they have spasmolytic effects on peripheral organs, particularly the colon, bladder and bronchi.Type: GrantFiled: June 15, 1989Date of Patent: March 26, 1991Inventors: Gerhard Mihm, Wolfgang Eberlein, Wolfhard Engel, Gunter Trummlitz, Norbert Mayer, Adrian de Jonge, Henri Doods
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Patent number: 4987130Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.Type: GrantFiled: December 22, 1989Date of Patent: January 22, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Tsushima, Muneo Takatani, Minoru Hirata
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Patent number: 4977272Abstract: This invention relates to new compounds of the formula: ##STR1## where each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 has zero to 10 C atoms, and no acetylenic unsaturation; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from H and hydrocarbyl; with the proviso that R.sup.6 is C.sub.1 -C.sub.10 hydrocarbyl; each of R.sup.5 and R.sup.Type: GrantFiled: June 29, 1989Date of Patent: December 11, 1990Assignee: The Standard Oil CompanyInventors: Mark C. Cesa, James E. Rinz, Gilles Klopman, Teodora T. Kopp
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Patent number: 4975444Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.Type: GrantFiled: August 25, 1989Date of Patent: December 4, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
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Patent number: 4975298Abstract: The invention provides a compound of the formula: ##STR1## and which is: 3-(1-amino-1,3-dicarboxy-3-hydroxy-but-4-yl)-indole, including the isomers, salts and specified internal condensation derivatives thereof, and in particular those which have enhanced sweetening powers relative to sucrose and which are useful as sweeteners for foods and beverages.Type: GrantFiled: June 15, 1988Date of Patent: December 4, 1990Assignee: South African Inventions Development CorporationInventors: Pieter J. Van Wyk, Louis G. Ackerman
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Patent number: 4943587Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 19, 1988Date of Patent: July 24, 1990Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 4918196Abstract: A process for optically isomerizing an optically active alpha-amino acid amide comprising heating a D-alpha-amino acid amide or an L-alpha-amino acid amide in the presence of a strongly basic compound; and a process for producing an L-alpha-amino acid, which comprises(1) subjecting a D,L-alpha-amino acid amide or a mixture of a major amount of a D-alpha-amino acid amide and a minor amount of an L-alpha-amino acid amide to the action of a microorganism having the ability to hydrolyze the L-alpha-amino acid to obtain a hydrolyzate containing the L-alpha-amino acid and D-alpha-amino acid,(2) separating the L-alpha-amino acid from the hydrolyzate and recovering the remaining D-alpha-amino acid amide.Type: GrantFiled: February 21, 1986Date of Patent: April 17, 1990Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Masaharu Doya, Toshio Kondo, Hideo Igarashi, Takako Uchiyama
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Patent number: 4908451Abstract: A process is disclosed for the preparation of .alpha.-substituted carbonyl compounds, wherein .alpha.-substituted ketone is prepared by the following reaction: ##STR1## .alpha.-azo ester is prepared by the following reaction: ##STR2## and .alpha.-hydrozono ester is prepared by the following reaction: ##STR3## wherein the .alpha.-azo ester and .alpha.-hydrazono ester obtained by the above reactions include novel compounds, which are also disclosed.Type: GrantFiled: March 23, 1988Date of Patent: March 13, 1990Assignee: Agency of Industrial Science and TechnologyInventors: Masato Tanaka, Toshiyasu Sakakura
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Patent number: 4902708Abstract: In general, the invention features compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein each R.sup.1 is, independently, an alkyl group having 1-5, inclusive, carbon atoms, an alkoxy group having 1-5, inclusive, carbon atoms, a halogen, amino, hydroxy, nitro, cyano, carboxyl, trifluoreomethyl, ethyl carboxylate, or a hydrogen; m is an integer between 0 and 2, inclusive; and A is either ##STR2## where n is an integer between 1 and 5, inclusive, and R.sup.Type: GrantFiled: April 12, 1988Date of Patent: February 20, 1990Assignee: Biomeasure, Inc.Inventor: Sun H. Kim
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Patent number: 4898977Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.Type: GrantFiled: August 13, 1987Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Herold, Christof Angst
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Patent number: 4873259Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;wherein X is oxygen, sulfur, SO.sub.2, or NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl, (4) aroyl, or (5) alkylsulfonyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 1-5;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.Type: GrantFiled: January 11, 1988Date of Patent: October 10, 1989Assignee: Abbott LaboratoriesInventors: James B. Summers, Jr., Bruce P. Gunn, Dee W. Brooks
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Patent number: 4870097Abstract: N-acylated derivatives of L-tryptophan of general formula (I), ##STR1## in which R is selected from the group consisting of: (a) a phenyl group, mono-substituted or di-substituted in the meta and para positions with halogens, linear or branched alkyl groups containing from 1 to 9 carbon atoms, the cyano group or the trifluoromethyl group, (b) a benzyloxy group, mono-substituted or di-substituted in the meta and para position with substituents selected from those indicated at (a), and (c) a benzydryloxy group. The derivatives are used in therapy, particularly for human pain relief, in the treatment of pathological conditions of the central nervous system and of pathological intestinal conditions.Type: GrantFiled: July 11, 1988Date of Patent: September 26, 1989Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Rolando Chiste, Angelo L. Rovati
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Patent number: 4855286Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1 is absent or denotes hydrogen, alkyl or acyl, A denotes an acyl radical or an amino acid residue, B denotes an amino acid residue, and R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification, and to their salts, to a process for their preparation, to pharmaceutical products containing them, and to their use as medicaments, and intermediates for the preparation of these compounds.Type: GrantFiled: July 28, 1987Date of Patent: August 8, 1989Assignee: Hoechst AktiengesellschaftInventors: Adalbert Wagner, Heinz-Werner Kleemann, Dieter Ruppert, Bernward Scholkens
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Patent number: 4814463Abstract: In general, the invention features CCK antagonist compounds having the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein each R.sup.1 is, independently, an alkyl group having 1 to 5, inclusive, carbon atoms, an alkoxy group having 1 to 5, inclusive, carbon atoms, a halogen, amino, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, ethyl carboxylate, or a hydrogen; m is an integer between 0 and 2, inclusive; and A is either ##STR2## where n is an integer between 1 and 5, inclusive, and R.sup.2 is hydroxy, an alkoxy group having 1 to 5, inclusive, carbon atoms, aralkoxy (e.g., benzyloxy), aralkyl (e.g., benzyl), amino, an alkyl group having 1 to 5, inclusive, carbon atoms, an alkylamino group having 1 to 5, inclusive, carbon atoms, a dialkylamino group with each alkyl group, independently having 1 to 5, inclusive, carbon atoms, a cycloalkylamino group wherein the ring has 4 to 6, inclusive, carbon atoms (e.g.Type: GrantFiled: December 31, 1985Date of Patent: March 21, 1989Assignee: Biomeasure, Inc.Inventor: Sun H. Kim
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Patent number: 4803284Abstract: The compound characterized by the structural Formula I: ##STR1## is therapeutically useful as an anti-hypertensive agent. A process for the preparation of the compound having Formula I and their synthetic intermediates is described. One of the synthetic intermediates is the compound characterized by the structural Formula: ##STR2## which is also therapeutically useful as an anti-hypertensive agent.Type: GrantFiled: August 19, 1987Date of Patent: February 7, 1989Assignee: Centro de Investigacion y de Estudios Avanzados Del Instituto Politecnico NacionalInventors: Pedro Joseph-Nathan, Martha S. Morales-Rios
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Patent number: 4748252Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1 and 4. The nucleus may be optionally substituted at position 8. The derivatives are useful anti-inflammatory and analgesic agents and methods and chemical intermediates for their preparation are also disclosed.Type: GrantFiled: January 28, 1987Date of Patent: May 31, 1988Assignee: American Home Products CorporationInventors: Eckhardt S. Ferdinandi, Dominick Mobilio, Joseph P. Sabatucci, Leslie G. Humber
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Patent number: 4748160Abstract: There are described compounds of formula I,ZCHRCON(--N.dbd.CR.sub.4 R.sub.5)CHR.sub.6 (CH.sub.2).sub.n COY Iwhere the substituents are defined in the disclosure.There are also described methods for making the compounds, formulations containing them and their use, e.g. as antihypertensives.Type: GrantFiled: November 14, 1985Date of Patent: May 31, 1988Assignee: Fisons plcInventors: Colin Bennion, David P. Marriott, Anthony R. Cook, David H. Robinson
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Patent number: 4743614Abstract: Novel compounds of the following formula have restorative pharmacological activities in immuno-deficient hosts, ##STR1## wherein R.sup.1 is amino or a protected amino group,R.sup.2 is hydrogen, carboxy or a protected carboxy group,R.sup.3 is hydrogen, carboxy or a protected carboxy group,R.sup.4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carbamoyl(lower)alkyl or protected carbamoyl(lower)alkyl,R.sup.5 is hydrogen or lower alkyl, andR.sup.6 is hydrogen, hydroxyphenyl(lower)alkyl, imidazolyl(lower)alkyl or indolyl(lower)alkyl.Type: GrantFiled: March 4, 1986Date of Patent: May 10, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroshi Terano, Yasuhisa Tsurumi, Hiroyuki Setoi, Masashi Hashimoto, Masanobu Kohsaka
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Patent number: 4742067Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: July 30, 1986Date of Patent: May 3, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Sesha I. Natarajan, Eric M. Gordon
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Patent number: 4738803Abstract: Derivatives having the general formula: ##STR1## in which the various radicals, A,B,X,R.sub.1, R.sub.2, R.sub.3 and n have indicated definitions. These compounds have in particular enkephalinase-inhibiting, antalgic, antidepressive, antidiarrhea and hypotensive activities.Type: GrantFiled: August 22, 1986Date of Patent: April 19, 1988Inventors: Bernard Roques, Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Patent number: 4719288Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.Type: GrantFiled: June 2, 1986Date of Patent: January 12, 1988Assignee: Ciba-Geigy CorporationInventors: Walter Fuhrer, Peter Buhlmayer, Vittorio Rasetti, Bernhard Riniker
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Patent number: 4705857Abstract: Indole derivatives of formula I ##STR1## R is hydrogen, one or two halogen atoms or one or two organic radicals in the 4-, 5-, 6- or 7-position(s),R.sup.1 and R.sup.4 are the same or different and each is hydrogen, alkyl of 1 to 3 carbon atoms or alkoxyalkyl of 1 to 3 carbon atoms in each of the alkoxy and alkyl portions,R.sup.3 is phenyl, --COOalkyl, --PO.sub.3 (alkyl).sub.2, --SO.sub.2 aryl, --SO.sub.2 alkyl, ##STR2## each of 1 to 3 carbon atoms in each alkyl group, and A and B each independently is alkyl of 1 to 3 carbon atoms or together with the connecting N-atom form a pyrrolidono, piperidino, morpholino or piperazino group,are valuable intermediates for preparing valuable tryptophans and .beta.-carbolines.Type: GrantFiled: October 28, 1983Date of Patent: November 10, 1987Assignee: Schering AktiengesellschaftInventor: Helmut Biere
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Patent number: 4681973Abstract: Acylated amino acids having the general formula ##STR1## are prepared by reacting a compound of formula II ##STR2## with a compound of formula IIIROCOClwherein R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein.Type: GrantFiled: February 27, 1986Date of Patent: July 21, 1987Assignee: USV Pharmaceutical CorporationInventor: Martin L. Kantor
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Patent number: 4665193Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.Type: GrantFiled: June 27, 1986Date of Patent: May 12, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
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Patent number: 4661628Abstract: A new process for the optical resolution of racemic mixtures of .alpha.-naphthyl-propionic acids of formula ##STR1## This process comprises reacting a racemic mixture of a compound of formula ##STR2## with an optically active substance of formula R.sub.4 --NH.sub.2 (III), said substance being a .beta.-aminoalcohol, thus forming a pair of diastereoisomeric amides which are resolved into the single diastereoisomers by fractional crystallization. The obtained single diastereoisomeric amide is then hydrolyzed to give the desired optically active .alpha.-naphthyl-propionic acid of formula ##STR3## In the above compound I.fwdarw.III and VI, R.sub.1 is (C.sub.1-6)alkyl, R.sub.2 stands for hydrogen, halogen, mercapto, (C.sub.1-6)alkylthio, phenylthio, benzylthio, (C.sub.1-6)alkylsulfonyl, benzenesulfonyl, benzenesulfonyl substituted by halogen or (C.sub.1-4)alkyl, R.sub.3 is a reactive group and R.sub.4 is the residue of a primary or secondary alcohol.Type: GrantFiled: November 5, 1984Date of Patent: April 28, 1987Assignee: Alfa Chemicals Italiana S.p.A.Inventors: Vincenzo Cannata, Giancarlo Tamerlani
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Patent number: 4661510Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.Type: GrantFiled: October 21, 1985Date of Patent: April 28, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Arlindo L. Castelhano
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Patent number: 4658038Abstract: Analgesia-effecting 5-hydroxytryptophan derivatives are disclosed of the formulae: ##STR1## wherein R is selected from the group consisting of C.sub.2 -C.sub.16 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.16 alkenyl, C.sub.2 -C.sub.16 alkynyl, aryl containing up to 14 carbon atoms, and arylalkyl containing up to 20 carbon atoms;R.sup.2 and R.sup.2a are each H or R, as defined above;R.sup.3 and R.sup.3a are each H or alkyl containing from 1 to 4 carbons;R.sup.4 and R.sup.4a are each H or alkyl containing from 1 to 4 carbons;and their non-toxic, pharmacologically acceptable acid addition salts.Type: GrantFiled: November 13, 1984Date of Patent: April 14, 1987Assignees: Research Foundation for Mental Hygiene, Inc., Yeda Research and Development Co. Ltd.Inventors: Hadassah Tamir, Stephen E. Karpiak, Meir Wilchek
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Patent number: 4634775Abstract: There are described new optically active 3,4-bis-(diphenylphosphino)-pyrrolidines of the formula ##STR1## wherein Ph is a phenyl group and R is hydrogen, an alkyl group, an arylalkyl group or an acyl group, rhodium complexes containing a compound of formula (I) as its chiral ligands, said rhodium complexes having the formula[RH(en).sub.2 A].sup.+ X.sup.- (II),where (en).sub.2 is two molecules of a monoolefin or one molecule of a diolefin, A is an optically active compound of formula (I) and X.sup.- is a tetrafluoroborate, hexafluorophosphate or a perchlorate ion, and use of the rhodium complexes as catalysts for the homogeneous asymmetric hydrogenation of unsubstituted or .beta.-substituted .alpha.-acylamino-acrylic acids.Type: GrantFiled: January 2, 1985Date of Patent: January 6, 1987Assignee: Degussa AktiengesellschaftInventors: Wolfgang Beck, Ulrich Nagel
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Patent number: 4624962Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.Type: GrantFiled: February 1, 1985Date of Patent: November 25, 1986Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
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Patent number: 4616088Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.Type: GrantFiled: December 14, 1984Date of Patent: October 7, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
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Patent number: 4570002Abstract: The invention relates to new carbazic acid derivatives, a process for the preparation thereof and compositions--particularly feed additives and animal feeds--containing the same.The new compounds according to the invention correspond to the formula (I)R.sup.1 .dbd.N--NH--COOR.sup.3 (I)whereinR.sup.1 stands for a C.sub.7-12 cycloalkylidene group, an indanylidene group or a group of the formula (IX) ##STR1## wherein A represents a phenyl group optionally carrying one or more identical or different substituents selected from the group consisting of halo nitro, hydroxy, C.sub.1-14 alkoxy, C.sub.1-4 alkyl, amino or C.sub.1-4 alkoxycarbonylhydrazino; phenyl-(C.sub.1-4 alkyl), C.sub.1-16 alkyl, C.sub.3-7 cycloalkyl or indolyl or a C.sub.3 -C.sub.6 cycloalkyl group substituted by a C.sub.3 -C.sub.6 cycloalkyl group;R.sup.2 denotes a hydrogen atom, a C.sub.1-16 alkyl or a C.sub.3-7 cycloalkyl group; andR.sup.3 represents a C.sub.1-4 alkyl group.Type: GrantFiled: January 24, 1984Date of Patent: February 11, 1986Assignee: Egyt Gyogyszervegyeszeti GyarInventors: Zoltan Budai, Pal Benko, Ildiko Ratz nee Simonek, Eva Rakoczy nee Pinter, Karoly Magyar, Jozsef Kelemen, Attila Mandi
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Patent number: 4540791Abstract: A process for producing a compound of the formula ##STR1## wherein A is aryl or alkyl, R.sub.1 is an aromatic radical and R.sub.2 is hydrogen, alkyl, aryl, cyano, --COOalkyl or --COOaryl, which process comprises reacting 1 mol of an aromatic nitrile of the formula R.sub.1 --CN (II) with 1 mol of an acetic ester of the formula (X)(R.sub.2)CH--COOA (III) in which X is halogen, in the presence of zinc, in an inert organic solvent and at a temperature of less than 80.degree. C.; hydrolyzing in an alkaline medium the formed reaction product; and then isolating the compound of the formula I.The compounds of the formula I are valuable intermediates for producing heterocyclic compounds.Type: GrantFiled: July 8, 1983Date of Patent: September 10, 1985Assignee: Ciba-Geigy CorporationInventors: Luigi Cassar, Abul Iqbal, Alain C. Rochat
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Patent number: 4515803Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.Type: GrantFiled: September 1, 1982Date of Patent: May 7, 1985Assignee: Hoechst AktiengesellschafatInventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
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Patent number: 4515982Abstract: Organic materials which contain from 0.001 to 10% by weight of an aminoreductone I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H, methyl or ethyl and R.sup.4 is the radical of a naturally occurring .alpha.- or .beta.-aminoacid or of a C.sub.1 -C.sub.10 -alkyl ester thereof or, in the case of an .alpha.-aminoacid, a lactone having a 2--OH group in the cyclohexenone ring, or R.sup.4 is C.sub.1 -C.sub.20 -alkyl which is unsubstituted or substituted by --OH, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -acyloxy, or is --(CH.sub.2 --CH.sub.2 --O).sub.n H, which may be etherified with a C.sub.1 -C.sub.4 -alkanol or esterified with a C.sub.1 -C.sub.4 -fatty acid, and where n is from 2 to 10, or a mineral salt thereof.Novel compounds Ia differ from I in having the radical R.sup.4a, where R.sup.4a is R.sup.4 with the exception of methyl. Compounds I are prepared by reacting the corresponding 2,3-dihydroxycyclohex-2-en-1-one with an amine HN(R.sup.3)R.sup.4 or a mineral acid salt thereof.Type: GrantFiled: December 15, 1982Date of Patent: May 7, 1985Assignee: BASF AktiengesellschaftInventors: Peter Lechtken, Gerhard Mueller, Klaus Schmieder
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Patent number: 4503232Abstract: The invention provides a novel method for the preparation of an .alpha.-ketoamide imine having a characteristic structure expressed by the formula ##STR1## in which R is a group such as an alkyl, aryl or the like group, in a one-step reaction in which a halogen-containing organic compound reacts with a primary amine and carbon monoxide in the presence of a carbonylation catalyst. The product compound is useful as an intermediate for the synthesis of various kinds of organic compounds including medicines and agricultural chemicals.Type: GrantFiled: September 24, 1982Date of Patent: March 5, 1985Assignee: Agency of Industrial Science & TechnologyInventors: Toshiaki Kobayashi, Masato Tanaka
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Patent number: 4499079Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.Type: GrantFiled: November 18, 1982Date of Patent: February 12, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Harold N. Weller, III
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Patent number: 4497964Abstract: A process for the production of an N-acyl-.alpha.-amino acid represented by the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, independently from each other, represent a hydrogen atom, an alkyl or cycloalkyl group which may be substituted, or an aryl or heteroaromatic group selected from the group consisting of furyl, pyrrolyl, pyridinyl, thienyl and indolyl which may be substituted, which comprises reacting an oxirane represented by the general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, an amide compound represented by the general formulaR.sup.3 CONHR.sup.4 (III)wherein R.sup.3 and R.sup.4 are as defined above, and carbon monoxide in the presence of hydrogen, a cobalt-containing catalyst, and a promoter composed of a compound containing a metal selected from Groups I, II, III and IV of the periodic table.Type: GrantFiled: November 15, 1982Date of Patent: February 5, 1985Assignee: Sagami Chemical Research CenterInventors: Iwao Ojima, Kenji Hirai
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Patent number: 4491590Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: May 26, 1983Date of Patent: January 1, 1985Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4491664Abstract: A process for the production of an ergot alkaloid comprising intramolecularly cyclizing a 3-iminoethyl-4-trans-buta-1',3'-dienylindole to produce an 8-ergolene and as necessary converting the resultant ergolene into the desired ergot alkaloid.Type: GrantFiled: March 12, 1982Date of Patent: January 1, 1985Assignee: Sandoz Ltd.Inventor: Wolfgang Oppolzer
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Patent number: 4482725Abstract: The S-acylation of a mercaptoacyl amino acid having ACE inhibitory action with a diuretic containing a carboxyl group yields a product having both ACE inhibitory action and diuretic activity in vivo.Type: GrantFiled: April 3, 1980Date of Patent: November 13, 1984Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, Denis E. Ryono
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Patent number: 4468520Abstract: The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.Type: GrantFiled: July 29, 1981Date of Patent: August 28, 1984Assignee: Boehringer Mannheim GmbHInventors: Helmut Michel, Wolfgang Kampe, Roland Ofenloch, Karl Dietmann, Gisbert Sponer
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Patent number: 4456611Abstract: Derivatives of 2-[3-(3-indolyl 2-amino propionyloxy] acetic acid corresponding to the following general formula I: ##STR1## in which R represents a hydrogen atom, a linear or branched alkyl radical including 1 to 12 carbon atoms, or a mono-alicyclic or polycyclic radical containing 5 to 16 carbon atoms, possibly linked by a methylene radical, and their pharmaceutically acceptable addition salts, are useful as medicaments for palliating deficiency of the serotoninergic system.Type: GrantFiled: January 26, 1982Date of Patent: June 26, 1984Assignee: Laboratoires PanmedicaInventors: Claude Laruelle, Marcel Lepant
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Patent number: 4442295Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom, an aralkyl radical or a radical of the general formula: ##STR2## in which B is a reactive group or, together with R.sub.5, represents a valency bond, and R.sub.5 is a hydrogen atom or an aliphatic or aromatic acyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen atom, a methyl radical or a --CH.sub.2 --O--R.sub.5 radical, R.sub.5 having the same meaning as above, and R.sub.4 is an aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, with the proviso that R.sub.1 is not an aralkyl radical when R.sub.4 is a formyl radical. The present invention also provides processes for the preparation of these compounds. Furthermore, the present invention is concerned with the use of these compounds for the preparation of compounds with a heart and circulatory activity.Type: GrantFiled: July 29, 1981Date of Patent: April 10, 1984Assignee: Boehringer Mannheim GmbHInventors: Helmut Michel, Wolfgang Kampe, Roland Ofenloch
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Patent number: 4415560Abstract: Silicon-containing amides, e.g., N-[1'-phenyl-2'-(4"-methylphenyl)ethyl]-2,2,6,6-tetramethyl-1-oxa-2,6-disi lacyclohexane-4-carboxamide, are useful as anti-atherosclerotic agents. The amides are obtainable by acylation of a primary amine (the substituents on the amine being of the aralkyl phenyl, tryptophanyl, benzocycloalkyl-type) with a corresponding silicon-containing carboxylic acid (or active form thereof).Type: GrantFiled: October 12, 1982Date of Patent: November 15, 1983Assignee: Sandoz, Inc.Inventor: Sandor Barcza
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Patent number: 4393081Abstract: Disclosed is the novel compound methyl 3-acetamido-2-(5-methoxyindol-3-yl) propanoate which is useful as an anti-hypertensive agent.Type: GrantFiled: October 28, 1981Date of Patent: July 12, 1983Assignee: Miles Laboratories, Inc.Inventors: Robert N. Schut, Max E. Safdy, Enrique Hong
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Patent number: 4384124Abstract: Cyclopropanyl-group-bearing-amides, eg N-[1-(benzyl)-2-(phenyl)ethyl]-cis-2-octyl-cyclopropanoctanamide and N-(.alpha.-methyl-benzyl)-(cis)-2-octyl-cyclopropanoctanamide, are useful as pharmaceutical agents and are obtainable, eg by reacting a mixed anhydride of a cyclopropanyl-group bearing-long chain carboxylic acid with an appropriate amino compound.Type: GrantFiled: July 10, 1980Date of Patent: May 17, 1983Assignee: Sandoz, Inc.Inventors: Faizulla G. Kathawala, John G. Heider
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Patent number: 4378363Abstract: This invention relates to new aminopropanol compounds having beta-adrenergic activity. In addition, the invention is directed to pharmaceutical compositions containing such compounds for the treatment of cardiac and circulatory infirmities and to methods for treating such infirmities.More particularly, the invention relates to new aminopropanol compound of the formula ##STR1## wherein R.sub.1 is a low alkyl moiety, which can be substituted, if desired, by a group Z-R.sub.5 ;R.sub.2 is hydrogen or a low alkanoyl group;R.sub.3 is a mono- or bicyclic heterocyclic compound having 1 to 2 hetero atoms, which can be mono- or polysubstituted, if desired, by halogen, amino, hydroxyl, low alkoxyl, low alkyl;R.sub.4 is hydrogen, a low alkanoyl group or an aroyl group;R.sub.Type: GrantFiled: November 17, 1980Date of Patent: March 29, 1983Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Wolfgang Kampe, Wolfgang Bartsch, Gisbert Sponer, Karl Dietmann
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Patent number: 4362738Abstract: Compounds of the formula ##STR1## wherein each X, which may be identical or different from the other X, is oxygen or imino;R.sub.1 is hydrogen, fluorine, chlorine or bromine;R.sub.2 and R.sub.3, which may be identical or different from each other, are each hydrogen; unsubstituted or mono-substituted alkyl of 1 to 6 carbon atoms, where the substituent is phenyl or dialkylamino with 1 to 3 carbon atoms in each alkyl moiety; pyridyl; or cycloalkyl of 5 to 7 carbon atoms;R.sub.2 and R.sub.Type: GrantFiled: June 11, 1980Date of Patent: December 7, 1982Assignee: Dr. Karl Thomae GmbHInventors: Johannes Keck, Gerd Kruger, Helmut Pieper, Klaus Noll, Gunther Engelhardt, Norbert Promberger, Rainer Zimmermann