Plural Chalcogens Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/425)
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Publication number: 20010049371Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.Type: ApplicationFiled: February 9, 2001Publication date: December 6, 2001Inventors: George Muller, Hon-Wah Man
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Patent number: 6323180Abstract: A racemate, diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a satuType: GrantFiled: August 5, 1999Date of Patent: November 27, 2001Assignee: Boehringer Ingelheim (Canada) LtdInventors: Montse Llinas-Brunet, Murray D. Bailey, Dale Cameron, Elise Ghiro, Nathalie Goudreau, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic, Bruno Simoneau
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Patent number: 6316489Abstract: This invention relates to (2R,3R,4R)-3,4-dihydroxy-2-hydroxymethylpyrrolidine D-tartrate, preparation thereof and use as therapeutic agent.Type: GrantFiled: March 10, 2000Date of Patent: November 13, 2001Assignee: Novo Nordisk A/SInventors: Claus Ulrich Jessen, Petra Christine Lugstein
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Patent number: 6316486Abstract: The present invention relates to new compounds of the formula (I) in which X represents halogen, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that always one of the radicals Y and Z represents halogen while the other represents alkyl, and Het represents one of the groups in which A, B, D and G have the meanings given in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: October 31, 1997Date of Patent: November 13, 2001Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Hans-Joachim Santel, Alan Graff, Wolfram Andersch, Norbert Mencke, Andreas Turberg
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Patent number: 6294573Abstract: Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.Type: GrantFiled: January 27, 2000Date of Patent: September 25, 2001Assignee: Abbott LaboratoriesInventors: Michael L. Curtin, Yujia Dai, Steven K. Davidsen, Joseph F. Dellaria, Jr., Alan S. Florjancic, Jianchun Gong, Yan Guo, Howard R. Heyman, James H. Holms, Michael R. Michaelides, Jamie R. Stacey, Douglas H. Steinman, Carol K. Wada, Lianhong Xu
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Patent number: 6288058Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3Type: GrantFiled: December 21, 2000Date of Patent: September 11, 2001Assignee: Janssen Pharmceutica N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernández-Gadea, Theo Frans Meert
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Publication number: 20010018441Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: March 12, 2001Publication date: August 30, 2001Applicant: Ajinomoto Co., Inc.Inventors: Yukio Iino, Kohichi Fujita, Takashi Tsuji, Ariko Kodaira, Kenji Takehana, Tsuyoshi Kobayashi, Takashi Yamamoto
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Publication number: 20010004629Abstract: The present invention relates to novel compounds of the formula (I) 1Type: ApplicationFiled: April 14, 2000Publication date: June 21, 2001Inventors: Volker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Alan Graff, Udo Schneider
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Patent number: 6248743Abstract: A novel butadiene derivative of the formula: wherein Ring A is heterocycle, or benzene being optionally substituted by lower alkyl, alkoxy, nitro, hydroxy, substituted or unsubstituted amino or halogen, Ring B is heterocycle, or benzene being optionally substituted by lower alkoxy, lower alkylenedioxy or di-lower alkylamino, R1 and R2 are each H or lower alkyl, one of —COR32 and —COR42 is carboxyl, and the other is carboxyl being optionally esterified, or the corresponding amide or pyrrolidine derivatives, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 28, 1998Date of Patent: June 19, 2001Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Hiroshi Ohmizu, Akio Ohtani, Tsuyoshi Ohgiku, Hiroshi Sai, Jun Murakami
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Patent number: 6239163Abstract: A new salt of (2R,3R,4R)-3,4-dihydroxy-2-hyroxymethylpyrrolidine is disclosed. Specifically, (2R,3R,4R-3,4-dihydroxy-2-hydroxymethylpyrrolidine, 2-naphthalenesulfonate is disclosed, as well as its preparation and use for treating and preventing diabetes and obesity and for regulating appetite. This salt is characterized as having a high melting point and low hygroscopicity.Type: GrantFiled: March 10, 2000Date of Patent: May 29, 2001Assignee: Novo Nordisk A/SInventors: Claus Ulrich Jessen, Petra Christine Lugstein
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Patent number: 6235791Abstract: The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of pharmaceutical compositions intended to combat cell proliferation.Type: GrantFiled: April 12, 1999Date of Patent: May 22, 2001Assignee: Sanofi-SynthelaboInventors: Jean Claude Breliere, Pascual Ferrara, Christine Lebouteiller, Raymond Paul, Jorge Rosenfeld, Didier Van Broeck
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Patent number: 6214857Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.Type: GrantFiled: July 30, 1998Date of Patent: April 10, 2001Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Patent number: 6194405Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3Type: GrantFiled: March 22, 2000Date of Patent: February 27, 2001Assignee: Janssen Pharmaceutica N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernández-Gadea, Theo Frans Meert
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Patent number: 6180095Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.Type: GrantFiled: October 30, 1998Date of Patent: January 30, 2001Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Annapurna Pendri, Yun H. Choe
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Patent number: 6172060Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: February 10, 1999Date of Patent: January 9, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6162927Abstract: 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: August 4, 1997Date of Patent: December 19, 2000Assignee: 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, Bruce G. Szczepankiewicz, Kenneth J. Henry, Gang Liu, Steven J. Wittenberger, Steven A. King
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Patent number: 6162815Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.Type: GrantFiled: September 10, 1998Date of Patent: December 19, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6153586Abstract: Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.Type: GrantFiled: July 1, 1998Date of Patent: November 28, 2000Assignee: Praecis Pharmaceuticals, Inc.Inventors: Marc B. Garnick, Christopher J. Molineaux, Malcolm L. Gefter
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Patent number: 6143776Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.Type: GrantFiled: February 2, 2000Date of Patent: November 7, 2000Assignee: Sunesis Pharmaceuticals, Inc.Inventor: Daniel A. Erlanson
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Patent number: 6140358Abstract: The present invention relates to novel compounds of the formula (I) ##STR1## in which Het represents one of the groups ##STR2## in which A, B, D, G, V, W, X, Y and Z are as defined in the description,processes and intermediates for their preparation, and to their use as pesticides and herbicides.Type: GrantFiled: September 29, 1998Date of Patent: October 31, 2000Assignee: Bayer AktiengesellschaftInventors: Volker Lieb, Hermann Hagemann, Arno Widdig, Michael Ruther, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Alan Graff, Udo Schneider
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Patent number: 6121296Abstract: This invention is directed to transition-state analog compounds and to the use of said compounds as inhibitors of nucleoside hydrolase and transferase enzyme activity of parasites. This invention is further directed to the use of said compounds to treat infections and diseases caused by certain bacterial and plant toxins.Type: GrantFiled: February 2, 1998Date of Patent: September 19, 2000Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Benjamin Horenstein
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Patent number: 6110948Abstract: A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula: ##STR1## wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula --CO--, --CH(OH)--, or --NR.sup.3 -- (R.sup.3 represents an alkyl group that may be substituted); m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R.sup.1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R.sup.1 ; L and M respectively represent hydrogen or may be combined with each other to form a bond, provided that when m and n are 0, X represents CH, A represents a bond, Q represents sulfur, R.sup.Type: GrantFiled: September 30, 1998Date of Patent: August 29, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Yu Momose, Etsuya Matsutani, Takashi Sohda
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Patent number: 6075023Abstract: Fish mycoses and single-cell ectoparasites on fish are controlled using an active compound suitable for inhibiting the mitochondrial respiratory chain at the stage of the b/c.sub.1 complex.Type: GrantFiled: February 17, 1998Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Gerhard Peter Dohmen, Christoph Kunast, Reinhart Munk, Gerhard Rothhaas
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Patent number: 6066662Abstract: The invention provides hydroxylamine derivatives of formula (I) wherein A, R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, which are matrix metalloproteinase inhibitors and which also prevent TNF release. They are therefore useful for the control or prevention of degenerative joints diseases such as rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis. They can be manufactured according to generally known methods.Type: GrantFiled: November 20, 1996Date of Patent: May 23, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 6051573Abstract: Compositions of non-steroidal glucocorticoid antagonists for treating GLC1A glaucoma and methods for their use are disclosed.Type: GrantFiled: December 19, 1997Date of Patent: April 18, 2000Assignee: Alcon Laboratories, Inc.Inventor: Abbot F. Clark
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Patent number: 6015569Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: November 17, 1997Date of Patent: January 18, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5994274Abstract: The present invention relates to new compounds of the formula (I) ##STR1## in which X represents alkyl,Y represents halogen or alkyl andZ represents halogen or alkyl,with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl,Het represents one of the groups ##STR2## in which A, B, D and G have the meanings given in the description,a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: December 23, 1997Date of Patent: November 30, 1999Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 5985926Abstract: There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an effective amount of a compound that inhibits cellular signaling through a specific phospholipid-based cellular signaling and signal amplification pathway. The invention further provides a method for preventing or delaying clinical symptoms of a group of viral diseases wherein the viral disease is mediated by host cell viral replication. The invention provides an advantage by attacking host cellular signaling mechanisms to prevent the development of drug resistance from rapidly mutating viruses.Type: GrantFiled: February 10, 1997Date of Patent: November 16, 1999Assignee: Cell Therapeutics, Inc.Inventors: David W. Leung, Gail E. Underiner, Jack W. Singer
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Patent number: 5952363Abstract: The present invention relates to novel pyrrolidine compounds having the general formula I ##STR1## and pharmaceutically acceptable acid addition salts or hydrates or prodrugs thereof, wherein R.sup.1 is straight or branched C.sub.1-14 -alkyl optionally substituted with C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkoxy, phenoxy, perhalomethyl, halogen, optionally substituted phenyl;CR.sup.2 is optionally C.dbd.R.sup.2 or C--R.sup.2R.sup.2 is oxygen, hydroxy, halogen, amino or mercapto,R.sup.3 and R.sup.4 independently are hydroxy, halogen, amino or mercapto, the use of these compounds as medicament, the use of these medicaments in the treatment of diabetes, pharmaceutical compositions containing these compounds and methods of preparing the compounds.Type: GrantFiled: March 5, 1998Date of Patent: September 14, 1999Assignee: Novo Nordisk A/SInventors: Marit Kristiansen, Palle Jakobsen, Jane Marie Lundbeck
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Patent number: 5942537Abstract: A method of inhibiting the transport of a neurotransmitter away from the synapse comprising contacting a neurotransmitter transporter with a compound having the structure ##STR1## wherein ##STR2## or CONHR.sup.3 in any combination and and wherein R.sup.2 =OR.sup.3, NR.sup.3.sub.2, alkyl, or substituted alkyl and R.sup.3 =alkyl or substituted alkyl.Type: GrantFiled: August 9, 1993Date of Patent: August 24, 1999Assignee: The Regents of the University of CaliforniaInventors: A. Richard Chamberlin, Richard J. Bridges, Carl W. Cotman, Mark S. Stanley
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Patent number: 5932520Abstract: There is provided a method for controlling or combatting the attachment of a fouling organism to an underwater surface which comprises contacting said organism with an antifouling-effective amount of a 2-arylpyrrole compound. A method for protecting aquatic structures against fouling by a marine or freshwater fouling organism and antifoulant compositions therefor are also provided.Type: GrantFiled: May 23, 1995Date of Patent: August 3, 1999Assignee: American Cyanamid CompanyInventors: Mark Arthur Josepha Van der Flass, Lantz Stephen Crawley
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Patent number: 5919790Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.Type: GrantFiled: October 2, 1997Date of Patent: July 6, 1999Assignees: Warner-Lambert Company, BASF AktiengesellsschaftInventors: Hamish John Allen, Kenneth Dale Brady, Bradley William Caprathe, Paul Galatsis, John Lodge Gilmore, Sheryl Jeanne Hays, Robert Vincent Talanian, Nigel Walker, Joseph Scott Warmus
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Patent number: 5877204Abstract: The present invention relates to compounds which are useful as sunscreens. The compounds persist on the skin for much longer than conventional sunscreens because they comprise a Michael acceptor linked directly or indirectly to a chromophore. The Michael acceptor is capable of undergoing a conjugate addition reaction with thiol groups present in cysteine residues of keratin and thus the compound is chemically bound to the skin and will not be removed by immersion in water.Type: GrantFiled: November 5, 1996Date of Patent: March 2, 1999Assignee: Vanguard Medica LimitedInventors: Bruce Everett Davison, Bryan Colin Nicholas Morgan Jones, Charon Robin Ganellin, Paul Beaumont Bishop, David Jack
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Patent number: 5874459Abstract: Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method and novel compounds can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, for example cancer chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.Type: GrantFiled: November 12, 1997Date of Patent: February 23, 1999Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Sonyan Lin, William Adam Hill
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Patent number: 5854272Abstract: The present invention relates to (2R,3R,4R)-3,4-dihydroxy-2-hydroxymethylpyrrolidine and other substituted 2-methylpyrrolidines and their use for the treatment of diabetes.Type: GrantFiled: July 14, 1997Date of Patent: December 29, 1998Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Palle Jakobsen, Marit Kristiansen, Leif N.o slashed.rskov-Lauritsen, Lars Naerum
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Patent number: 5849783Abstract: Physically and chemically latentiated autobiotics are described. The latentiated autobiotics are useful for the treatment or prevention of any disease or condition, which results from the presence of nonself cells in a vertebrate host. Latentiated autobiotics are furthermore useful in suppressing immune rejection processes, as radiosensitizers and as anticoagulants.Type: GrantFiled: September 28, 1995Date of Patent: December 15, 1998Assignee: Cell Research CorporationInventor: Laszlo G. Egyud
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Patent number: 5843983Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 represents a saturated heterocyclic group attached to the bond or group represented by A through a ring carbon atom; R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a, R.sup.3b, R.sup.3c and R.sup.3d are hydrogen or various other groups or atoms; and A represents a single bond or an alkylene group having from 1 to 6 carbon atoms are serotonin 2 receptor antagonists and have the ability to inhibit the activity of squalene synthase. They can not only prevent and inhibit the development and progression of arteriosclerosis but can also inhibit thrombosis in arteriosclerotic lesions and can improve hemodynamics.Type: GrantFiled: February 10, 1997Date of Patent: December 1, 1998Assignee: Sankyo Company, LimitedInventors: Koichi Fujimoto, Naoki Tanaka, Fumitoshi Asai, Taketoshi Ogawa, Teiichiro Koga, Tatsuo Tanimoto, Yoshio Tsujita, Hiroyuki Koike
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Patent number: 5837703Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH.sub.2).sub.m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.Type: GrantFiled: November 12, 1993Date of Patent: November 17, 1998Assignee: Cell Therapeutics, Inc.Inventors: Anil M. Kumar, John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
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Patent number: 5830826Abstract: The present invention relates to novel 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, G, X, Y and Z have the meaning given in the description, to processes for their preparation and to intermediates for this purpose. The compounds of the formula (I) are used as pesticides and herbicides.Type: GrantFiled: September 27, 1996Date of Patent: November 3, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kruger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5824677Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: October 20, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5801181Abstract: Therapeutic compounds have the formula:(X)j--(core moiety),J being an integer from one to three, the core moiety having at least one, five- to seven-membered ring and X being a racemic mixture, R or S enantiomer, slovate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: September 1, 1998Assignee: Cell Therapeutics, Inc.Inventors: John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
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Patent number: 5798377Abstract: A compound which inhibits human thrombin and where has the structure ##STR1## such as ##STR2##Type: GrantFiled: October 21, 1996Date of Patent: August 25, 1998Assignee: Merck & Co., Inc.Inventors: William C. Lumma, Thomas J. Tucker, Keith M. Witherup, Stephen F. Brady, Willie L. Whitter, Joseph P. Vacca, Craig Coburn, Jules A. Shafer
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Patent number: 5783591Abstract: Pharmaceutical preparations for the local treatment of inflammations are claimed herein, characterized in that they contain as the active ingredient one or two compounds of general Formula I ##STR1## wherein X is an oxygen atom or a methylene group,R.sub.1 and R.sub.2 represent a hydrogen atom or a hydrocarbon residue of maximally eight carbon atoms, optionally interrupted by an oxygen atom,R.sub.3 is a hydrogen atom or a hydrocarbon residue of maximally eight carbon atoms, optionally substituted by an oxo group, andR.sub.4 is a hydrogen atom or an alkyl group of maximally four carbon atoms.Type: GrantFiled: November 17, 1994Date of Patent: July 21, 1998Assignee: Schering AktiengesellschaftInventors: Walter Klose, Gerald Kirsch, Andreas Huth, Wolfgang Froehlich, Henry Laurent
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Patent number: 5780435Abstract: Methods for treating prostate cancer are disclosed. The methods of the invention generally feature administration to a subject of an LHRH-R antagonist, in combination with a second therapy. In one embodiment, this second therapy is performance of a procedure that removes or destroys prostatic tumor tissue, such as a radical prostatectomy, cryosurgery or X-ray therapy (external or interstitial). In another embodiment, the second therapy is treatment with an LHRH-R agonist, either simultaneous with or subsequent to LHRH-R antagonist therapy. The methods of the invention can further involve administering an antiandrogen and/or an inhibitor of sex steroid biosynthesis to the subject in combination with the LHRH-R antagonist.Type: GrantFiled: December 15, 1995Date of Patent: July 14, 1998Assignee: Praecis Pharmaceuticals IncorporatedInventors: Marc B. Garnick, Christopher J. Molineaux, Malcolm L. Gefter
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Patent number: 5767144Abstract: 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: May 30, 1995Date of Patent: June 16, 1998Assignee: 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: 5739155Abstract: Haloalkylthio, -sulfinyl and -sulfonyl arylpyrrole compounds which are effective for the control of insects and acarids are described. A method for the insecticidal and acaricidal use of said compounds and methods for the preparation of said compounds are presented.Type: GrantFiled: November 7, 1995Date of Patent: April 14, 1998Assignee: American Cyanamid Co.Inventors: Keith Douglas Barnes, Victor Marc Kamhi, Robert Eugene Diehl
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Patent number: 5714499Abstract: 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 17, 1994Date of Patent: February 3, 1998Assignee: Corvas International, Inc.Inventors: Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
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Patent number: 5710140Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: August 16, 1996Date of Patent: January 20, 1998Assignee: Merck Frosst Canada, Inc.Inventors: Yves Ducharme, Jacques Yves Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
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Patent number: 5705522Abstract: A new family of compounds having anti-inflammatory, anti-viral, and brocho-dilating activity having the following linear and cyclic formulas: ##STR1## and compositions of these, which alone, and in combination with reverse transcriptase inhibitors thereby resulting in an additive or synergistic effect, are useful in inhibiting or suppressing viruses including those exhibiting retroviral replication, or in treating viruses including a retrovirus such as HIV in a human cell population and methods of using these compositions, compounds, and salts thereof.Type: GrantFiled: February 13, 1996Date of Patent: January 6, 1998Assignee: Compagnie de Developpement Aguettant S.A.Inventors: Farid Hamedi-Sangsari, Fabienne Nugier, Thierry Vallet, Jacques Grange, Jorge Vila