Nitrogen Or Additional Chalcogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 540/463)
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Patent number: 5703208Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: December 30, 1997Assignee: Corvas International, Inc.Inventors: Joseph Edward Semple, Robert John Ardecky, Ruth Foelsche Nutt, William Charles Ripka, David C. Rowley, Marguerita S. L. Lim-Wilby, Terence Kevin Brunck
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Patent number: 5696256Type: GrantFiled: May 12, 1995Date of Patent: December 9, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasuyuki Kando, Hideki Uneme, Isao Minamida
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Patent number: 5565561Abstract: The invention relates to the natural substance cyclamenol of the formula ##STR1## a process for its preparation from microorganisms of the order of the Actinomycetales, in particular from the Streptomyces strain MHW 846, chemical derivatives thereof, and its use as a medicament, in particular for acute and chronic inflammatory disorders in human and veterinary medicine.Type: GrantFiled: April 27, 1995Date of Patent: October 15, 1996Assignee: Bayer AktiengesellschaftInventors: Hartwig M uller, Erwin Bischoff, Volker-Bernd Fiedler, Karlheinz Weber, Burkhard Fugmann, Bruno Rosen
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Patent number: 5538961Abstract: Macrocylic lactam compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.Type: GrantFiled: August 30, 1993Date of Patent: July 23, 1996Assignee: Abbott LaboratoriesInventors: Leslie A. Freiberg, Carla Edwards, Richard J. Pariza, Hugh N. Nellans
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Patent number: 5523401Abstract: Macrocylic lactam compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein A is selected from ##STR2## also disclosed are synthetic processes and intermediates useful in the preparation of the compounds of the invention, as well as compositions containing the same and methods for their use in stimulating contractile motion of the gastrointestinal tract.Type: GrantFiled: May 4, 1995Date of Patent: June 4, 1996Assignee: Abbott LaboratoriesInventors: Leslie A. Freiberg, Carla Edwards, Richard J. Pariza, Hugh N. Nellans
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Patent number: 5516442Abstract: A rust and corrosion inhibiting marine diesel engine lubricating oil additive is provided which comprises a mixture of:(a) an oligomeric polythiocyclic imide represented by the formula ##STR1## wherein R and R.sup.1 each are a (C.sub.1 -C.sub.50) saturated or unsaturated aliphatic group and n is an integer of 0 to 5; an oligomeric amine represented byR"--NH.sub.2where R" is dodecyl or a (C.sub.12 -C.sub.Type: GrantFiled: August 11, 1995Date of Patent: May 14, 1996Assignee: Texaco Inc.Inventors: Joseph M. Russo, Rodney L. Sung, Benjamin J. Kaufman, Thomas F. Derosa
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Patent number: 5496805Abstract: Diuresis, natriuresis, and the lowering of blood pressure are produced in a host by administering one or more neutral endopeptidase inhibitors. An additional blood pressure lowering agent such as an angiotensin converting enzyme inhibitor can be administered along with the neutral endopeptidase inhibitor.Type: GrantFiled: July 12, 1990Date of Patent: March 5, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Norma G. Delaney, Eric M. Gordon, Jack M. DeForrest, David W. Cushman
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Patent number: 5489583Abstract: 2-Substituted 3-(4-amidinophenyl)propionic acid derivatives of the formula ##STR1## in which A, Ar and B have the meanings stated in the description, and the preparation thereof are described. The compounds are suitable for controlling diseases.Type: GrantFiled: December 28, 1993Date of Patent: February 6, 1996Assignee: BASF AktiengesellschaftInventors: Helmut Mack, Thomas Pfeiffer, Hans W. Hoeffken, Hans-Joachim Boehm, Wilfried Hornberger
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Patent number: 5376529Abstract: This invention relates to novel methods for the release of nucleic acids from cells in complex biological samples or specimens to prepare and make available the nucleic acid material present for a hybridization assay or for extraction. Novel methods for hybridization of nucleic acids are also presented. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with a hybridization medium comprising a lactam which promotes and enables nucleic acid pairing when complementary nucleic acid is introduced. The lactam is preferably about 5 to about 70% of the hybridization medium and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone.Type: GrantFiled: December 13, 1991Date of Patent: December 27, 1994Assignee: MicroProbe CorporationInventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
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Patent number: 5374721Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: October 14, 1992Date of Patent: December 20, 1994Assignee: Merck & Co., Inc.Inventors: William R. Schoen, Matthew J. Wyvratt
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Patent number: 5332807Abstract: A process of producing 8a- and 9a- azalide compounds is disclosed, comprised of reacting an 8a- aza or 9a- aza azalide eastern fragment or a derivative thereof with a compound of the formula:X--A'--Ywherein X and Y are appropriate reactive groups and A' is a fragment or compound which forms the western portion of the azalide, andcyclizing this intermediate to form the target 8a- or 9a-azalide compound. Compounds of formula I, II and III as well as other azalides can be synthesized according to this process.Type: GrantFiled: April 14, 1993Date of Patent: July 26, 1994Assignee: Merck & Co., Inc.Inventors: Sherman T. Waddell, Timothy A. Blizzard
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Patent number: 5281585Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.Type: GrantFiled: November 6, 1992Date of Patent: January 25, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
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Patent number: 5254682Abstract: Compounds of the formula: ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.Type: GrantFiled: June 11, 1991Date of Patent: October 19, 1993Assignee: Merck & Co., Inc.Inventors: Daljit S. Dhanoa, Arthur A. Patchett, William J. Greenlee, William H. Parsons, Thomas A. Halgren, Ann E. Weber, Lihu Yang
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Patent number: 5244888Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.Type: GrantFiled: July 9, 1991Date of Patent: September 14, 1993Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Michael D. Meyer, Kevin B. Sippy
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Patent number: 5190937Abstract: Novel compounds of formula (I), and pharmaceutically acceptable salts thereof; their preparation; compositions containing them; and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R.sub.1 is --OH; alkoxy; aryloxy or aralkyloxy in each of which the aryl group is optionally substituted; --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is independently hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring; or a group:--NH--CH(R.sub.8)--C(O)--R.sub.9where R.sub.8 is hydrogen; alkyl optionally substituted by --OH, alkoxy, --NR.sub.6 R.sub.7 as defined for R.sub.1, guanidine, --CO.sub.2 H, --CONH.sub.2, --SH, or --S--alkyl; or --CH.sub.2 --Ar where Ar is optionally substituted aryl or heteroaryl; and R.sub.Type: GrantFiled: January 11, 1991Date of Patent: March 2, 1993Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Ian Hughes
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Patent number: 5124444Abstract: This invention relates to novel methods for the extraction of nucleic acid. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with an extraction solution comprising a lactam and then the nucleic acid material is isolated from the resulting combined solution. The resulting combined solution is mixed and becomes biphasic and the nucleic acid material is isolated from the aqueous phase by precipitation with ethanol. The lactam is preferably about 5 to about 70% of the extraction solution and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone. Methods for selectively isolating DNA, ribosomal RNA and plasmid DNA are also disclosed.Type: GrantFiled: July 24, 1989Date of Patent: June 23, 1992Assignee: MicroProbe CorporationInventors: Jeffrey Van Ness, Nicolaas Vermuelen, B. Melina Cimler
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Patent number: 5106730Abstract: This invention relates to novel methods for the release of nucleic acids from cells in complex biological samples or specimens to prepare and make available the nucleic acid material present for a hybridization assay or for extraction. Novel methods for hybridization of nucleic acids are also presented. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with a hybridization medium comprising a lactam which promotes and enables nucleic acid pairing when complementary nucleic acid is introduced. The lactam is preferably about 5 to about 70% of the hybridization medium and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone.Type: GrantFiled: July 27, 1990Date of Patent: April 21, 1992Assignee: MicroProbe CorporationInventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
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Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5089471Abstract: Non-peptidyl compounds characterized generally as .beta.-aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: February 18, 1992Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5006651Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.Type: GrantFiled: September 22, 1989Date of Patent: April 9, 1991Assignee: Hoffman-La Roche Inc.Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
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Patent number: 4975441Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a chemical inhibitor of glycosidase activity chosen from lactams having the structure: ##STR1## where A.sup.1 and A.sup.6 are --H, --CH.sub.3, ##STR2## --CH.sub.2 OT or ##STR3## A.sup.1 and A.sup.6 being the same or different, and at least one of which being the group: ##STR4## in a lactam ring; and where Q is --OT', --NHT' or a lactam linkage to A.sup.1 or A.sup.6 ;the Q groups being the same or different, and at least one of which is involved in a lactam linkage;and where T is the same or different and is chosen from --H, --C.sub.p H.sub.2p+1 or a metal ion,T' is --H or --COC.sub.p H.sub.2p+1, andp is an integer of from 1 to 22;provided that:where any of the Q groups is --OT' or --NHT',then that group or groups can be of either stereochemical configuration with respect to the plane of the ring; and(ii) a cosmetically acceptable vehicle for the chemical inhibitor.Type: GrantFiled: March 22, 1989Date of Patent: December 4, 1990Assignee: Unilever Patent Holdings B.V.Inventor: Walter T. Gibson
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Patent number: 4968792Abstract: Disclosed herein are novel benzisothiazole derivatives having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of a variety of central nervous system disorders.Type: GrantFiled: September 25, 1989Date of Patent: November 6, 1990Assignee: American Home Products CorporationInventors: Gary P. Stack, Magid A. Abou-Gharbia, Thomas D. Golobish
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Patent number: 4957911Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: August 17, 1989Date of Patent: September 18, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
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Patent number: 4885283Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.Type: GrantFiled: December 1, 1987Date of Patent: December 5, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
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Patent number: 4876340Abstract: Benzazecinediones of the formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: February 11, 1988Date of Patent: October 24, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
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Patent number: 4873235Abstract: Benzofused lactams of the formula: ##STR1## and their use as angiotensin converting enzyme inhibitors and antihypertensive agents are disclosed.Type: GrantFiled: March 16, 1983Date of Patent: October 10, 1989Assignee: Merck & Co., Inc.Inventors: William H. Parsons, Arthur A. Patchett, Eugene D. Thorsett
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Patent number: 4814001Abstract: Herbicidal and plant growth-regulating novel 5-acylamino-pyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,Ar represents in each case optionally substituted phenyl or pyridyl,X represents oxygen or sulphur,A represents a straight-chain or branched optionally substituted alkylene bridge,n represents the numbers 0 or 1 andY represents cyano or the grouping ##STR2## wherein X.sup.1 represents oxygen or sulphur andR.sup.3 represents hydroxyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, amino, alkylamino, dialkylamino, alkenylamino, dialkenylamino, alkyl-alkenylamino or a --OM radical,whereinM represents one equivalent of the cation of an inorganic or organic base.Intermediates therefor of the formula ##STR3## are also new.Type: GrantFiled: May 5, 1988Date of Patent: March 21, 1989Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Otto Schallner, Reinhold Gehring, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4771044Abstract: Tetraoxo compounds of the Formula (I) ##STR1## wherein R.sup.1 is an alkyl, alkenyl, phenylalkyl or cycloalkylalkyl group,R.sup.2 and R.sup.3 are each independently an alkyl or phenyl group or together denote an alkylene group,W is a (CH.sub.2).sub.n --Q group, in which n is 2 to 10 and Q is(a) a displaceable leaving group X, or(b) Z-R.sup.4, where Z is a 1-piperazinyl group, and R.sup.4 is in position 4, and is hydrogen or a phenyl, substituted phenyl, N-heteroaryl or substituted N-heteroaryl group;and salts and acid addition salts of said compound, and a method for their preparation. Selected compounds of Formula (I) have been found to have central nervous system affecting activity.Type: GrantFiled: August 19, 1986Date of Patent: September 13, 1988Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Wolfgang Kehrbach, Werner Benson, Andreas Fuchs, Michael Ruhland
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Patent number: 4755505Abstract: Disclosed herein are new 4-aryl-benzazocine-2,6-diones of Formula I ##STR1## in which R.sup.1 is phenyl, naphthyl or phenyl or naphthyl substituted by one to three moieties selected from fluoro, chloro, bromo, and alkyl or alkoxy of 1 to 4 carbon atoms;R.sup.2 is --R.sup.3 --NR.sup.4 R.sup.5, wherein R.sup.3, R.sup.4 and R.sup.5 are, independently, straight or branched chain alkyl groups of 1 to 4 carbon atoms or R.sup.4 and R.sup.5 are concatenated to form nitrogen ring having 3 to 8 carbon atoms; andX and Y are, independently, hydrogen, alkyl or alkoxy of 1 to 4 carbon atoms, dialkylamino or dialkyl-carboxamido wherein each alkyl group has 1 to 4 carbon atoms, cyano, alkylacyl of 1 to 4 carbon atoms, fluoro, chloro, nitro, dialkylsulfonamido wherein each alkyl group has 1 to 4 carbon atoms, or alkylsulfonyl of 1 to 4 carbon atoms, or a pharmaceutically acceptable salt thereof.The compounds of Formula I are useful as anti-arrhythmic agents.Type: GrantFiled: August 18, 1987Date of Patent: July 5, 1988Assignee: American Home Products CorporationInventors: Michael W. Winkley, James L. Diebold
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Patent number: 4749791Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen,as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: November 18, 1987Date of Patent: June 7, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
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Patent number: 4734410Abstract: Compounds of formula (I): ##STR1## (wherein R.sup.1 and R.sup.3 are organic groups, A is a direct bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CO--CH.sub.2, --O--CH.sub.2 -- or --S--CH.sub.2 --, B is lower alkylene and n is 1-3) are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group at the 3-position.Type: GrantFiled: October 9, 1986Date of Patent: March 29, 1988Assignee: Sankyo Company LimitedInventors: Hiroaki Yanagisawa, Sadao Ishihara, Akiko Ando, Takuro Kanazaki, Hiroyuki Koike, Yasuteru Iijima
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Patent number: 4732979Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen.as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: January 21, 1987Date of Patent: March 22, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
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Patent number: 4666901Abstract: Substituted lactams and related compounds and methods for their preparation are disclosed. These compounds are useful as angiotensin converting enzyme inhibitors and as antihypertensives.Type: GrantFiled: December 18, 1985Date of Patent: May 19, 1987Assignee: Merck & Co., Inc.Inventor: William H. Parsons