Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/247)
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Publication number: 20020099218Abstract: Compounds and methods of preparing compounds of the formula:Type: ApplicationFiled: October 25, 2001Publication date: July 25, 2002Inventors: Thomas P. Sassi, Ram B. Gupta
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Publication number: 20020088574Abstract: Pulps or papers, especially chemimechanical or thermomechanical pulps or papers, which still contain lignin, have enhanced resistance to yellowing when they contain an effective stabilizing amount of a N,N-dialkylhydroxylamine, an ester, amide or thio substituted N,N-dialkylhydroxylamine or N,N-dibenzylhydroxylamine or an amminium salt thereof. This performance is often further enhanced by the presence of one or more coadditives selected from the group consisting of the UV absorbers, the polymeric inhibitors, the nitrones, the fluorescent whitening agents and metal chelating agents. Combinations of hydroxylamines or their salts, benzotriazole or benzophenone UV absorbers and a metal chelating agent are particularly effective. N,N-Diethylhydroxylamine and N,N-dibenzylhydroxylamine and their acid salts are surprisingly effective for this purpose.Type: ApplicationFiled: January 20, 1999Publication date: July 11, 2002Inventors: RAYMOND SELTZER, DAVID DEVORE, GLEN T. CUNKLE, CYRIL HEITNER, JOHN A. SCHMIDT, PETER F. MCGARRY, JEAN-PIERRE WOLF, RANDALL B. NELSON
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Patent number: 6387512Abstract: A photochromic grey coloring 2H-naphtho[1,2-b]pyran of formula (1) wherein R1 is selected from mono-, di- or poly-substituted aryl groups, mono-, di- or poly-substituted naphthyl groups and mono-, di- or poly-substituted heteroaryl groups, wherein at least one substituent is a nitrogen containing group, including amino, C1-C20 and C6-C20 alkylamino, C1-C20 and C6-C20 dialkylamino, C2-C20 dialkenylamino, C2-C20 or C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, tetra (C1-C10 linear or branched alkyl) guanidino and cyclic-amino groups and at least one of R7 and R9, which may be the same or different, is selected from C1-C20 N alkylamino C1-C20 N-alkylamido, C1-C20 N,N-dialkylamido, amido, nitro, amino, C1-C20 alkylamino, C1-C20 dialkylamino, C2-C20 dialkenylamino, C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, or cyclicamino groups.Type: GrantFiled: March 16, 2001Date of Patent: May 14, 2002Assignee: James Robinson LimitedInventors: David Allan Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Patent number: 6313302Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.Type: GrantFiled: January 26, 2001Date of Patent: November 6, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Publication number: 20010006619Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.Type: ApplicationFiled: January 5, 2001Publication date: July 5, 2001Applicant: RESEARCH CORPORATION TECHNOLOGIES, INC.Inventors: Christy S. John, Jesse Baumgold, John G. McAfee, Terry Moody, Wayne Bowen
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Patent number: 6251918Abstract: The present invention provides compounds that block calcium channels having formula (I). The present invention also provides methods of using the compounds of formula (I) to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of formula (I).Type: GrantFiled: September 29, 1999Date of Patent: June 26, 2001Assignee: Warner-Lambert CompanyInventors: Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
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Patent number: 6225288Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.Type: GrantFiled: March 16, 2000Date of Patent: May 1, 2001Assignee: Merk Frosst Canada & Co.Inventors: Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
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Patent number: 6180759Abstract: This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or psuedopeptides.Type: GrantFiled: April 7, 2000Date of Patent: January 30, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: James J. Mencel, Robert Stammler, Christophe Daubie, Michel Lavigne, Benoit J. Vanasse, Robert C. Liu, Patrick Leon, Geoffrey A. D'Netto, Adam W. Sledeski
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Patent number: 6156899Abstract: Novel N-aryl-2-hydroxyalkylamido compounds having the formula (I): ##STR1## are well suited for inducing/stimulating hair growth and/or retarding hair loss and/or for therapeutically treating hyperseborrhea and/or acne.Type: GrantFiled: November 13, 1998Date of Patent: December 5, 2000Assignee: Societe L'Oreal S.A.Inventors: Jean-Baptiste Galey, Odile Destree, Lionel Breton
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Patent number: 6124332Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6124333Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.Type: GrantFiled: February 3, 1999Date of Patent: September 26, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Andrew Miller, Mark Whittaker, Raymond Paul Beckett
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Patent number: 6066642Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.Type: GrantFiled: December 7, 1998Date of Patent: May 23, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Ji-Long Jiang, Yong-Chul Kim, Yishai Karton, Albert M. Van Rhee
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Patent number: 6015543Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.Type: GrantFiled: June 6, 1995Date of Patent: January 18, 2000Assignee: Research Corporation Technologies, Inc.Inventors: Christy S. John, Jesse Baumgold, John G. McAfee, Terry Moody, Wayne Bowen
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Patent number: 6001905Abstract: A description is given of compounds of formula 1 ##STR1## and of compounds of formula 2 ##STR2## wherein X, Y and Z and the radicals R.sup.1 and also m and n have the meanings claimed in claim 1.The cited compounds are advantageously used e.g. for stabilizing organic material against the damaging effect of light, oxygen and/or heat.Type: GrantFiled: April 20, 1998Date of Patent: December 14, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Alfred Steinmann
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Patent number: 5952316Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.Type: GrantFiled: August 14, 1997Date of Patent: September 14, 1999Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5919934Abstract: Disclosed are bisaminothiol and amino compounds with appended pharmacophores, complexes of these compounds with .sup.99m Tc(V)0, Re(V)0, In.sup.+3, .sup.67 Ga.sup.+3, .sup.90 Y.sup.+3, .sup.109 Pd.sup.+2 or .sup.105 Rh.sup.+3, and pharmaceutical compositions containing the complexes. Also disclosed are methods of diagnosing a mammal for the presence of a mammalian tumor, methods for in vitro detection of a cancer cell in a mammalian tissue sample, and methods of treating a mammal having a tumor.Type: GrantFiled: February 19, 1997Date of Patent: July 6, 1999Assignee: The George Washington UniversityInventors: Christy Seith John, Benjamin Byung-Duk Lim
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Patent number: 5907039Abstract: Amino alcohol derivatives with a primary amino group or a substituted amino group influence the synthesis of glycolipids and have antiviral, antitumor, metastasis inhibiting and neural cell growth enhancing functions. The amino alcohol derivatives are useful in preparing 2-acylamino alcohol derivatives.Type: GrantFiled: December 9, 1996Date of Patent: May 25, 1999Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Masayuki Jinbo, Hidekazu Oyamada, Jinichi Inokuchi
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Patent number: 5877182Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.5, D,E, X, Y, n, x and y are as defined herein. These compounds 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 treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: September 9, 1997Date of Patent: March 2, 1999Assignee: Merck & Co., Inc.Inventors: Ravi Nargund, Arthur A. Patchett, James Tata
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Patent number: 5863903Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.Type: GrantFiled: March 14, 1995Date of Patent: January 26, 1999Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Ole Kirk
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Patent number: 5849732Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: February 14, 1997Date of Patent: December 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
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Patent number: 5830897Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: November 3, 1998Assignees: G. D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5770575Abstract: Nipecotic acid-derived compounds of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.Type: GrantFiled: March 6, 1995Date of Patent: June 23, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Mary Pat Beavers, Patricia Andrade-Gordon, William J. Hoekstra
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Patent number: 5763604Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.Type: GrantFiled: June 4, 1997Date of Patent: June 9, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid
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Patent number: 5728876Abstract: A process for producing optically active primary and secondary amines from the corresponding racemates is characterised in that (a) a racemic amine is enantioselectively acylated in the presence of a hydrolase with an ester whose acid component bears a fluorine, nitrogen, oxygen or sulphur atom at the proximity of the carbonyl carbon atom; (b) the mixture of optically active amine and optically active acylated amine is separated so that an enantiomer of amine is produced; (c) if desired the other enantiomer of the amine is extracted from the acylated amine by amide cleavage.Type: GrantFiled: March 11, 1996Date of Patent: March 17, 1998Assignee: BASF AktiengesellschaftInventors: Friedhelm Balkenhohl, Bernhard Hauer, Wolfgang Ladner, Uwe Pressler, Christoph Nubling
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Patent number: 5672615Abstract: Disclosed are the compounds of formula I ##STR1## wherein R and R.sub.1 together with the chain to which they are attached or R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a ring; pharmaceutically acceptable prodrug derivatives and pharmaceutically salts thereof; methods of preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: March 11, 1996Date of Patent: September 30, 1997Assignee: Novartis CorporationInventors: Lawrence J. MacPherson, David Thomas Parker
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Patent number: 5631376Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5627194Abstract: Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.Type: GrantFiled: October 14, 1994Date of Patent: May 6, 1997Assignee: Allelix Biopharmaceuticals Inc.Inventors: Sumanas Rakhit, Abdelmalik Slassi
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Patent number: 5624941Abstract: The present invention relates to compounds of the formula: ##STR1## These compounds are useful in pharmaceuticals in which cannabis is known to be involved.Type: GrantFiled: November 29, 1994Date of Patent: April 29, 1997Assignee: SanofiInventors: Francis Barth, Pierre Casellas, Christian Congy, Serge Martinez, Murielle Rinaldi, Gilles Anne-Archard
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Patent number: 5622971Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: June 1, 1995Date of Patent: April 22, 1997Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
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Patent number: 5614534Abstract: The present invention concerns .beta.,.beta.-dimethyl-4-piperidineethanamine compounds of the formula: ##STR1## (wherein groups R.sub.1 to R.sub.3 are defined as indicated in the description), and addition salts thereof.It also concerns a process for their preparation and their therapeutic use as inhibitors for the cholesterol biosynthesis, in particular as epoxysqualene cyclase inhibitors, for obtaining an as hypocholesterolemic, hypolipemic, antiatheromatic and/or antifungal drug.Type: GrantFiled: October 30, 1995Date of Patent: March 25, 1997Assignee: Fournier Industrie et SanteInventors: Jean Binet, Soth Samreth, Daniel de Fornel
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Patent number: 5607953Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: November 23, 1994Date of Patent: March 4, 1997Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5604229Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.Type: GrantFiled: June 17, 1994Date of Patent: February 18, 1997Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5585492Abstract: The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.Type: GrantFiled: October 11, 1994Date of Patent: December 17, 1996Assignee: G. D. Searle & Co.Inventors: Nizal S. Chandrakumar, Barbara B. Chen, Michael Clare, Bipinchandra N. Desai, Stevan W. Djuric, Stephen H. Docter, Alan F. Gasiecki, Richard A. Haack, Chi-Dean Liang, Julie M. Miyashiro, Thomas D. Penning, Mark A,. Russell, Stella S. Yu
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Patent number: 5578594Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.Type: GrantFiled: December 21, 1994Date of Patent: November 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, G erard Schmid
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Patent number: 5578731Abstract: An asymmetrical hydrazine derivative of formula V ##STR1## where R.sub.1 is alkoxy of 1 to 18 carbon atoms or cycloalkyl of 5 to 12 carbon atoms;X is --O-- or --NR.sub.2 -- where R.sub.2 is hydrogen, alkyl of 1 to 18 carbon atoms, cycloalkyl of 5 to 12 carbon atoms, phenylalkyl of 7 to 15 carbon atoms, alkyl of 2 to 4 carbon atoms substituted by one alkoxy group of 1 to 12 carbon atoms or a group of formula II ##STR2## in which R.sub.1 is as defined above; and E is a alkyl of 1 to 20 carbon atoms, cycloalkyl of 5 to 12 carbon atoms, aryl of 6 to 14 carbon atoms or phenylalkyl of 7 to 22 carbon atoms, orE is --CONHR.sub.4, --CSNHR.sub.5, --COR.sub.6 COR.sub.7, --COR.sub.8 CONHR.sub.9, --COR.sub.10, --COOR.sub.11 or --SO.sub.2 R.sub.12,in which R.sub.4, R.sub.5, R.sub.7, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are each independently of the other hydrogen, alkyl of 1 to 20 carbon atoms, cycloalkyl of 5 to 12 carbon atoms, aryl of 6 to 14 carbon atoms or phenylalkyl of 7 to 22 carbon atoms; andR.sub.6 and R.sub.Type: GrantFiled: June 5, 1995Date of Patent: November 26, 1996Assignee: Ciba-Geigy CorporationInventors: Ramanathan Ravichandran, Ambelal R. Patel
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Patent number: 5552419Abstract: The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a method of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: November 3, 1994Date of Patent: September 3, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5510386Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: March 11, 1994Date of Patent: April 23, 1996Assignee: Zeneca LimitedInventors: James R. Empfield, Daniel R. Mayhugh, Keith Russell
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Patent number: 5506356Abstract: An N-acylamino acid derivative of the formula: ##STR1##Type: GrantFiled: January 20, 1995Date of Patent: April 9, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5506242Abstract: The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which comprises administering to a mammal in need thereof an effective macrophage metalloelastase inhibiting amount of a compound of formula I ##STR1## wherein Ar, R, R.sub.1 and R.sub.2 have meanings as defined, or of a pharmaceutically acceptable prodrug derivative thereof, or of a pharmaceutically acceptable salt thereof, or of pharmaceutical compositions comprising a said compound.Type: GrantFiled: June 24, 1994Date of Patent: April 9, 1996Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker, Arco Y. Jeng
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Patent number: 5481036Abstract: An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.Type: GrantFiled: January 10, 1994Date of Patent: January 2, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5455258Abstract: Particularly the invention relates to the compounds of formula I ##STR1## (a) wherein Ar is carbocyclic or heterocyclic aryl;R is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, amino, mono- or di-lower alkylamino)-lower alkyl, acylamino-lower alkyl, (N-lower alkyl-piperazino or N-aryl-lower alkylpiperazino)-lower alkyl, or (morpholino, thiomorpholino, piperidino, pyrrolidino, piperidyl or N-lower alkylpiperidyl)-lower alkyl;R.sub.1 is hydrogen, lower alkyl, carbocyclic aryl-lower alkyl, carbocyclic aryl, heterocyclic aryl, biaryl, biaryl-lower alkyl, heterocyclic aryl-lower alkyl, mono- or poly-halo-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.Type: GrantFiled: January 6, 1993Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5434202Abstract: N-(.beta.-carbonyl- and .beta.-cyanovinyl)-2,2,6,6-tetramethylpiperidine derivatives of the formula I ##STR1## where R.sup.1 is COOR.sup.3, COR.sup.4, CONR.sup.4 R.sup.5 or CN,R.sup.2 has the meanings of R.sup.1 or is C.sub.1 -C.sub.12 -alkyl or hydrogen,R.sup.3 is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.5 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.5 -alkenyl or phenyl which can be mono- to trisubstituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, halogen, hydroxyl, phenoxy, phenyl, tolyl or xylyl,R.sup.4 and R.sup.5 are each hydrogen, C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.8 -cycloalkyl or phenyl which can be mono- to trisubstituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkoxycarbonyl, halogen, hydroxyl, phenoxy, phenyl, tolyl or xylyl,n is 1-4,X and A for each individual n have been defined in the specification.Type: GrantFiled: June 3, 1994Date of Patent: July 18, 1995Assignee: BASF AktiengesellschaftInventors: Alfred Krause, Alexander Aumueller, Hubert Trauth
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Patent number: 5423998Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.Type: GrantFiled: April 13, 1993Date of Patent: June 13, 1995Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5405854Abstract: Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.Type: GrantFiled: February 24, 1993Date of Patent: April 11, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Kurt Hilpert, Gerard Schmid
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Patent number: 5399589Abstract: Oxalyl hydrazide-hydroxamic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: R, R.sup.1, R.sup.2 and R.sup.3 independently of one another arehydrogen, substituted or unsubstituted alkyl, alkenyl or alkynyl orsubstituted or unsubstituted cycloalkyl or cycloalkylmethyl,substituted or unsubstituted cycloalkenyl or cycloalkenylmethyl,substituted or unsubstituted phenyl, phenylalkyl, phenylalkenyl, hetaryl- or hetarylalkyl radicals, where R.sup.2 and R.sup.3 may also. together with the nitrogen atom whose substituents they are, form a 5- or 6-membered ring, orR.sup.2 together with R.sup.3 is the group ##STR2## where R.sup.4 and R.sup.5 are one of the radicals R, R.sup.1, R.sup.2 or R.sup.3, or R.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, are monocyclic or polycyclic cycloalkyl, orR.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, form a 5- or 6-membered, saturated heterocycle containing O, S or --N(R.sup.Type: GrantFiled: November 29, 1993Date of Patent: March 21, 1995Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5290796Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl;R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl;n is zero or one;R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl;R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.Type: GrantFiled: November 20, 1992Date of Patent: March 1, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5278311Abstract: Novel nonionic contrast agents of the formula ##STR1## or dimers of the formula ##STR2## are disclosed where X, Z and R.sub.1 -R.sub.5 are as defined herein.Type: GrantFiled: June 5, 1992Date of Patent: January 11, 1994Assignee: E. R. Squibb & Sons, Inc.Inventors: Thangavel Arunachalam, Ramachandran Ranganathan
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Patent number: 5270310Abstract: The present invention provides methods for inhibiting protein kinase C which comprise contacting protein kinase C with an inhibitory amount of a compound having the formula ##STR1## wherein R.sub.1 is C.sub.8 through C.sub.15 alkyl; R.sub.2 is H, C.sub.1 through C.sub.10 alkyl, or benzyl; R.sub.3 is N-heterocyclic, N-alkylheterocyclic, quaternized N-heterocyclic, NR.sub.4 R.sub.5 or N.sup.+ R.sub.4 R.sub.5 R.sub.6 X.sup.- ; R.sub.4, R.sub.5 and R.sub.6 are independently C.sub.1 through C.sub.10 alkyl; n is 2, 3, 4, or 5; and X is an anion. The invention also provides novel compounds having the formula ##STR2## wherein R.sub.1 is C.sub.8 through C.sub.15 alkyl; R.sub.2 is H, C.sub.1 through C.sub.10 alkyl, or benzyl; R.sub.3 is N-heterocyclic, N-alkylheterocyclic or quaternized N-heterocyclic; and n is 2, 3, 4, or 5.Type: GrantFiled: December 13, 1991Date of Patent: December 14, 1993Assignees: Sphinx Pharmaceuticals Corporation, Duke UniversityInventors: Robert M. Bell, Robert J. Fogelsong, Jeffrey B. Nichols
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Patent number: 5266572Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.Type: GrantFiled: June 18, 1992Date of Patent: November 30, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Paul J. Gilligan, Sang W. Tam