Nitrogen Bonded Directly To The Hetero Ring Patents (Class 540/527)
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Patent number: 5654294Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.Type: GrantFiled: June 19, 1996Date of Patent: August 5, 1997Assignee: Bristol-Myers SquibbInventor: Jeffrey A. Robl
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Patent number: 5646276Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.Type: GrantFiled: June 19, 1996Date of Patent: July 8, 1997Assignee: Bristol-Myers Squibb Co.Inventor: Jeffrey A. Robl
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Patent number: 5643904Abstract: The present invention relates to novel substituted hexahydroazepinones and tetrahydrobenzazepinones of the formulae ##STR1## wherein R.sup.1, Z.sup.1, Z.sup.2, W.sup.1, W.sup.2, Y.sup.1 and Y.sup.2 are as defined below, and to novel intermediates used in the synthesis of such compounds.Such compounds are useful in the treatment and prevention of gastrointestinal disorders, pain and anxiety disorders.Type: GrantFiled: June 27, 1995Date of Patent: July 1, 1997Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Patent number: 5618811Abstract: This invention relates to compounds of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are as defined in the application. These compounds are CCK-B receptor antagonists and are useful in the treatment and prevention of central nervous system and gastrointestinal disorders.Type: GrantFiled: January 18, 1996Date of Patent: April 8, 1997Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Patent number: 5587375Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.Type: GrantFiled: February 17, 1995Date of Patent: December 24, 1996Assignee: Bristol-Myers Squibb CompanyInventor: Jeffrey A. Robl
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Patent number: 5552397Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibitory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.Type: GrantFiled: December 1, 1993Date of Patent: September 3, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Donald S. Karanewsky, Jeffrey A. Robl
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Patent number: 5529995Abstract: The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.Type: GrantFiled: March 1, 1995Date of Patent: June 25, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Robert J. Cregge, Thomas L. Fevig, Shyam Sunder, Patrick W. Shum
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Patent number: 5527926Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.Type: GrantFiled: June 6, 1995Date of Patent: June 18, 1996Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Radhakrishna K. Pillai
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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: 5484917Abstract: The present invention relates to novel substituted hexahydroazepinones and tetrahydrobenzazepinones of the formulae ##STR1## wherein R.sup.1, Z.sup.1, Z.sup.2, W.sup.1, W.sup.2, Y.sup.1 and Y.sup.2 are as defined below, and to novel intermediates used in the synthesis of such compounds.Such compounds are useful in the treatment and prevention of gastrointestinal disorders, pain and anxiety disorders.Type: GrantFiled: June 16, 1903Date of Patent: January 16, 1996Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Patent number: 5399557Abstract: This invention provides a pyrroloazepine compound represented by the following formula (I) or (II): ##STR1## wherein Z.sub.1, Z.sub.2, R, A and Y are defined in the claims. The pyrroloazepine compounds according to the present invention are drugs having excellent anti-serotonin action. Coupled with their high safety, they can therefore be used as novel therapeutics for ischemic heart diseases. In addition, the compounds of the present invention include those having anti-.alpha..sub.1 action. Such compounds are effective as hypotensive drugs. Pyrroloazepine compounds according to the present invention are therefore extremely useful as therapeutics for a wide variety of circulatory diseases.Type: GrantFiled: April 7, 1993Date of Patent: March 21, 1995Assignee: Suntory LimitedInventors: Akira Mizuno, Mikiko Miya, Norio Inomata, Toshio Tatsuoka, Takafumi Ishihara
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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: 5317017Abstract: There are disclosed certain compounds identified as N-biphenyl-3-amido substituted benzolactams 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 benzolactams as the active ingredient thereof are also disclosed.Type: GrantFiled: September 30, 1992Date of Patent: May 31, 1994Assignee: Merck & Co., Inc.Inventors: Hyun O. Ok, William R. Schoen, Matthew Wyvratt
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Patent number: 5308520Abstract: Various heterocyclic compounds have been discovered that impart improved fuel economy and friction modification to lubricant and fuel compositions. These heterocyclic compounds of the invention preferably contain nitrogen and may be further reacted with hydrocarbyl carboxylic acid acylating reactants or hydrocarbyl phenolic reactants to give higher molecular materials. These higher molecular weight materials have higher oil-solubility and impart dispersancy properties to lubricant and fuel compositions.Type: GrantFiled: July 31, 1989Date of Patent: May 3, 1994Assignee: The Lubrizol CorporationInventors: Joseph W. Pialet, Paul E. Adams
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Patent number: 5300639Abstract: New thiazolo[5,4-b]azepine compounds represented by ##STR1## wherein R.sup.1 is a hydrogen atom, an aliphatic group which may be substituted, a carboxylic acyl group which may be substituted or a sulfonic acyl group which may be substituted; R.sup.2 is a hydrogen atom, an aromatic group which may be substituted or an aliphatic group which may be substituted, which are capable of e.g., inhibiting lipoperoxide formation.Type: GrantFiled: March 17, 1992Date of Patent: April 5, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Masahiro Suno, Go Kito
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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: 5149805Abstract: Monoblocked diisocyanates which contain little free and diblocked diisocyanate are obtained by a process which involves adding 1 mole of a blocking agent to a diisocyanate which is present in excess and subsequently removing the excess diisocyanate by thin film evaporation. The compounds produced are useful for the production of cataphoresis resins.Type: GrantFiled: September 13, 1988Date of Patent: September 22, 1992Assignee: Huels AktiengesellschaftInventors: Rainer Gras, Elmar Wolf, Josef Disteldorf, Werner Huebel, Horst Schnurbusch
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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: 5075302Abstract: Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.Type: GrantFiled: March 9, 1990Date of Patent: December 24, 1991Assignee: Schering CorporationInventor: Bernard R. Neustadt
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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: 4908445Abstract: A new class of novel, biologically active sesquiterpene compounds, pharmaceutical compositions containing them, methods of producing the compounds and compositions and methods of using them are disclosed. This new class of compounds have the generic formulae: ##STR1## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 =H or lower alkyl.Type: GrantFiled: January 9, 1989Date of Patent: March 13, 1990Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Kenneth L. Rinehart, Ashok D. Patil
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Patent number: 4831135Abstract: Novel .delta.-caprolactam derivatives of formula I have anti-tumor, antibiotic and anthelmintic activity: ##STR1## wherein: R is H, lower alkyl, or lower acyl;R.sub.1, R.sub.2, and R.sub.3 are each independently H or lower acyl;R.sub.4 is H or acyl of 1 to 22 carbon atoms;R.sub.5 is H or lower acyl;R.sub.6 and R.sub.7 are each H or OH, or R.sub.6 and R.sub.7 together form an epoxide or a double bond;and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 18, 1986Date of Patent: May 16, 1989Assignees: The Regents of the University of California, Syntex (U.S.A.), Inc.Inventors: Philip Crews, Thomas R. Matthews, Emilio Quinoa, Madeline Adamczeski
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Patent number: 4784782Abstract: Various heterocyclic compounds have been discovered that impart improved fuel economy and friction modification to lubricant and fuel compositions. These hetrocyclic compounds of the invention preferably contain nitrogen and may be further reacted with hydrocarbyl carboxylic acid acylating reactants or hydrocarbyl phenolic reactants to give higher molecular materials. These higher molecular weight materials have higher oil-solubility and impart dispersancy properties to lubricant and fuel compositions.Type: GrantFiled: March 27, 1986Date of Patent: November 15, 1988Assignee: The Lubrizol CorporationInventors: Joseph W. Pialet, Paul E. Adams
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Patent number: 4778790Abstract: Compounds of formula (I): ##STR1## (wherein A is an alkylene group substituted by an optionally substituted amino or heterocyclic group and optionally interrupted by an oxygen or sulfur atom, R.sup.2 is various organic groups, B is C.sub.1 -C.sub.2 alkylene and Y is sulfur or methylene) and pharmaceutically acceptable salts and esters thereof are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group in place of the group A--CH(COOH)--NH--.Type: GrantFiled: April 3, 1987Date of Patent: October 18, 1988Assignee: Sankyo Company LimitedInventors: Hiroaki Yanagisawa, Sadao Ishihara, Akiko Ando, Hiroyuki Koike, Yasuteru Iijima
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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: 4680392Abstract: The invention in its broad aspects relates to caprolactam derivatives which are useful as angiotensin converting enxyme inhibitors and as antihypertensives.Type: GrantFiled: May 19, 1986Date of Patent: July 14, 1987Assignee: Merck & Co., Inc.Inventors: Elbert E. Harris, Arthur A. Patchett, Eugene D. Thorsett
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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
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Patent number: 4629787Abstract: The invention in its broad aspects relates to caprolactam derivatives which are useful as angiotensin converting enxyme inhibitors and as antihypertensives.Type: GrantFiled: July 2, 1982Date of Patent: December 16, 1986Assignee: Merck & Co., Inc.Inventors: Elbert E. Harris, Arthur A. Patchett, Eugene D. Thorsett