The Carbonyl Is Bonded Directly To Two Non-carbon Atoms, Or To A Non-carbon Atom And An Additional Carbonyl (e.g., Carbamates, Oxamides, Etc.) Patents (Class 558/417)
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Patent number: 9126962Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.Type: GrantFiled: October 15, 2014Date of Patent: September 8, 2015Assignee: Medivation Technologies, Inc.Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
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Publication number: 20140221591Abstract: There is provided a copolymer having the general structure below, wherein a, b, and d are molar ratios varying between about 0.01 and about 0.90 and c is a molar ratio varying between about 0.01 and about 0.90; A1 represents monomer units comprising a cyano-containing pendant group in which the cyano is not directly attached to the backbone of the copolymer; A2 represents monomer units comprising two or more hydrogen bonding sites; A3 represents monomer units that increase solubility in organic solvents; and A4 represents monomer units that increase solubility in aqueous alkaline solutions. There is also provided a near-infrared radiation-sensitive coating composition comprising this copolymer as well as a positive-working thermal lithographic printing plate comprising a near-infrared radiation-sensitive coating comprising this copolymer, a method of producing such a printing plate, and finally a method of printing using such a printing plate. Formula (I).Type: ApplicationFiled: September 14, 2010Publication date: August 7, 2014Applicant: MYLAN GROUPInventors: My T. Nguyen, Akha Phan, Viet-Thu Nguyen-Truong, Marc-André Locas
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Publication number: 20130330582Abstract: A secondary battery includes: a cathode; an anode; and an electrolytic solution including a cyano compound, the cyano compound including a compound represented by R1-O—C(?O)—O—R2 (R1, R2, or both include a cyano-group-containing group), a compound represented by R3-C(?O)—O—R4 (R4 includes the cyano-group-containing group), or both.Type: ApplicationFiled: June 3, 2013Publication date: December 12, 2013Inventors: Masayuki Ihara, Tadahiko Kubota
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Publication number: 20130296551Abstract: A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Tsuyoshi MUTO, Taisaku Tanaka, Hiroshi Maruoka, Seiichi Imajo, Yoshiaki Tomimori
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Publication number: 20130231479Abstract: The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein R1 to R5 each independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof.Type: ApplicationFiled: October 6, 2011Publication date: September 5, 2013Inventors: Hironori Furukawa, Takehiko Nakamura, Tetsuo Tamai, Daisuke Hanai
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Patent number: 8362074Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: October 31, 2007Date of Patent: January 29, 2013Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Publication number: 20130005803Abstract: The use of compounds in the treatment of skin disorders is described. In particular, the use of a compound of formula (I) or one of its pharmaceutically acceptable salts, pharmaceutically acceptable solvates or hydrates in the preparation of a medicament to treat inflammatory skin pathologies is described.Type: ApplicationFiled: December 15, 2010Publication date: January 3, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Jérôme Aubert
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Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
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Publication number: 20120190810Abstract: There is provided a copolymer and polymeric particle comprising the copolymer, a method of producing a polymeric particle, a copolymeric binder, a method of producing a copolymeric binder, a near infrared radiation-sensitive coating composition, a negative working lithographic offset printing plate, a method of producing a negative working lithographic offset printing plate and methods of imaging the plate and printing with the imaged plate.Type: ApplicationFiled: September 14, 2010Publication date: July 26, 2012Applicant: MYLAN GROUPInventors: My T. Nguyen, Marc-Andre Locas
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Publication number: 20120029000Abstract: The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).Type: ApplicationFiled: March 25, 2010Publication date: February 2, 2012Applicant: MAPI PHARMA LIMITEDInventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
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Publication number: 20120010283Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which theyType: ApplicationFiled: August 16, 2011Publication date: January 12, 2012Applicants: The Regents of the University of California, Universita Degli Studi Di Parma, Universita Degli Studi Di UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Publication number: 20110098322Abstract: The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.Type: ApplicationFiled: August 5, 2008Publication date: April 28, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: James R. Sanborn, Bruce D. Hammock, Sung Hee Hwang, Paul D. Jones, Christophe Morisseau
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Publication number: 20100273739Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: February 16, 2010Publication date: October 28, 2010Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
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Patent number: 7795465Abstract: The invention relates to a process for preparing semicarbazone compounds of the formula I, where R1 and R2 are each independently hydrogen, halogen, CN, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy, and R3 is C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy, by reacting a hydrazone compound of the general formula II, where R is C1-C4-alkoxy, amino, C1-C4-alkylamino or di(C1-C4-alkyl)amino, and R1, R2 are each as defined above, with an aniline compound of the general formula III where R3 is as defined above.Type: GrantFiled: March 16, 2005Date of Patent: September 14, 2010Assignee: BASF AktiengesellschaftInventors: Thomas Zierke, Stefan Engel, Peter Otto
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Patent number: 7759520Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: February 23, 2005Date of Patent: July 20, 2010Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
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Patent number: 7705182Abstract: This invention provides androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: February 24, 2003Date of Patent: April 27, 2010Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Dong Jin Hwang, Jiyun Chen
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Patent number: 7659309Abstract: The present invention relates to polymorphic forms of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, processes therein, pharmaceutical compositions thereof, and uses therewith.Type: GrantFiled: March 22, 2005Date of Patent: February 9, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Todd Blythe, Philip Nyce, Yong Cui
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Publication number: 20090082328Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 9, 2008Publication date: March 26, 2009Inventors: Yingfu Li, Joachim Rudolph, Jacques P. Dumas, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther
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Patent number: 7371885Abstract: The present invention relates to the isomerization of the Z-isomer I-Z of semicarbazone compounds of the general formula (I) into its E-isomer I-E, where the variables in formula (I) have meanings given in claim 1Type: GrantFiled: November 12, 2004Date of Patent: May 13, 2008Assignee: BASF AktiengesellschaftInventors: Weiguo Liu, Philip Harrington
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Patent number: 7176201Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which theyType: GrantFiled: October 7, 2003Date of Patent: February 13, 2007Assignees: The Regents of the University of California, Universita Degli Studi di Parma, Universita Degli Studi di UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Patent number: 7087642Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: November 4, 2002Date of Patent: August 8, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Stamos, Martin Trudeau, Scott Bethiel, Steven Ronkin, Michael Badia, Jeffrey Saunders
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Patent number: 7026500Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: February 24, 2003Date of Patent: April 11, 2006Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
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Patent number: 6998500Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.Type: GrantFiled: October 16, 2002Date of Patent: February 14, 2006Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Yali He, Donghua Yin
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Publication number: 20040102518Abstract: The invention relates to N-benzoylureidocinnamic acid derivatives and to their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: June 6, 2003Publication date: May 27, 2004Applicant: Aventis Pharma AGInventors: Karl Schoenafinger, Elisabeth Defossa, Dieter Kadereit, Erich Von Roedern, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt
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Publication number: 20030181442Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: November 27, 2001Publication date: September 25, 2003Applicant: BAYER CORPORATIONInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Publication number: 20030171579Abstract: The invention relates to novel compounds of formula (I), wherein R, R1 and R2 have the meaning as cited claim 1. According to the invention, the compounds are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thrombosis, myocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis post-angioplasty, intermittent claudication, tumours, tumour related illnesses and/or tumour metastases.Type: ApplicationFiled: January 27, 2003Publication date: September 11, 2003Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20030100608Abstract: Disclosed are compounds of the formula (I) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds.Type: ApplicationFiled: May 24, 2002Publication date: May 29, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Eugene R. Hickey
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Patent number: 6528543Abstract: Glucokinase activating compounds of the formula wherein R1 and R2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl; R3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R4 is hydrogen, lower alkyl, lower alkenyl, hydroxy lower alkyl, halo lower alkyl, R5 and R6 are hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereofType: GrantFiled: March 21, 2000Date of Patent: March 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Antonio Focella, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 6515023Abstract: A thrombin receptor antagonist having the formula useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.Type: GrantFiled: January 30, 2001Date of Patent: February 4, 2003Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Philippe G. Nantermet, Harold G. Selnick, John H. Hutchinson, Michael J. Breslin, Kristen L. Glass, Thomas M. Connolly, Andrew Stern
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Patent number: 6498178Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: September 19, 2001Date of Patent: December 24, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Stamos, Martin Trudeau, Scott Bethiel, Steven Ronkin, Michael Badia, Jeffrey Saunders
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Patent number: 6479543Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: March 9, 2000Date of Patent: November 12, 2002Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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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: 6262113Abstract: The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).Type: GrantFiled: August 14, 1998Date of Patent: July 17, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 6252083Abstract: Carbamates of the formula I where the substituents have the following meanings: Z is methoxy, NH2, NHCH3, N(CH3)2, CH3, C2H5, CF3 or CCl3, X and Y are identical or different and each is hydrogen, F, Cl, Br, CF3, CN, NO2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring, R1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O—CO2-alkyl, A is —O—, —S—, —CR2═CR3—, CHR2—O—, —CHR2—S—, —CHR2—O—N═C(R4)—, —CR2═N—O—, —O—N═C(R4)—, —C≡C—, —CHR2—CHR3—, —CHR2—O—CO—, —O—CHR2— or a single bond, B is substituted or unsubstituted and is alkyl, alkeType: GrantFiled: March 16, 2000Date of Patent: June 26, 2001Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 6225345Abstract: The invention relates to compounds of formula (I): wherein R1 and R10 are each independently of the other lower alkoxycarbonyl; either R2, R3 and R4 are each independently of the other C1-C4alkyl and R7, R8 and R9 are each selected from hydrogen and C1-C4alkyl, with not more than 2 of the radicals being hydrogen; or R7, R8 and R9 are each independently of the other C1-C4alkyl and R2, R3 and R4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicals being hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl; or salts thereof; those compounds are inhibitors of retroviral aspartate proteases and are effective, for example, against HIV.Type: GrantFiled: May 21, 1998Date of Patent: May 1, 2001Assignee: Novartis AGInventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang
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Patent number: 6194454Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and X are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.Type: GrantFiled: February 28, 2000Date of Patent: February 27, 2001Assignee: Pfizer Inc.Inventor: Robert L. Dow
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Patent number: 6080860Abstract: Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.Type: GrantFiled: September 29, 1997Date of Patent: June 27, 2000Assignee: Brantford Chemicalss Inc.Inventors: Khashayar Karimian, Keshava Murthy, Darren Hall
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Patent number: 6075148Abstract: Carbamates of the formula I where the substituents have the following meanings:Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.Type: GrantFiled: March 25, 1999Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 6057269Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.Type: GrantFiled: January 5, 1998Date of Patent: May 2, 2000Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
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Patent number: 5981595Abstract: A pharmaceutically useful compound which lowers blood cholesterol levels having the formula ##STR1## wherein X is oxygen or --NH--; Ar is phenyl, substituted phenyl, naphthyl or substituted naphthyl; R.sub.1 is hydrogen, lower alkyl or benzyl; and R.sub.2 is a straight or branched alkyl group having from 5 to 17 carbon atoms which may be substituted on the 1-carbon position with methyl, ethyl, phenyl, or substituted phenyl, or a cycloalkyl group having from 3 to 8 carbon atoms.Type: GrantFiled: July 1, 1993Date of Patent: November 9, 1999Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, William Howard Roark, Bruce David Roth
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Patent number: 5925762Type: GrantFiled: September 15, 1997Date of Patent: July 20, 1999Assignee: Boehringer Ingelheim (Canada) Ltd.Inventor: Bounkham Thavonekham
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Patent number: 5922767Abstract: Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.Type: GrantFiled: October 7, 1997Date of Patent: July 13, 1999Assignee: SS Pharmaceutical Co., Ltd.Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
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Patent number: 5919824Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.Type: GrantFiled: September 12, 1997Date of Patent: July 6, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
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Patent number: 5883282Abstract: There is provided a 3-(3-aryloxyphenyl)-1-(substituted methyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.Type: GrantFiled: May 20, 1997Date of Patent: March 16, 1999Assignee: American Cyanamid CompanyInventors: Alvin Donald Crews, Jr., Philip Mark Harrington, Gary Mitchell Karp, Simon David Gill, Petra Dieterich
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Patent number: 5866609Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.Type: GrantFiled: July 24, 1997Date of Patent: February 2, 1999Assignee: SS Pharmaceutical Co., Ltd.Inventors: Yoshihiko Kanamaru, Hiroyuki Hirota, Akihiro Shibata, Teruo Komoto, Hiroyuki Naito, Koichi Tachibana, Mari Ohtsuka, Fumio Ishii, Susumu Sato
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Patent number: 5856559Abstract: The invention relates to a novel process for preparing substituted aryluracils by reacting aminoalkenoic esters with arylurethanes and then with sulfonamides, and additionally to novel 4-(alkoxycarbonylamino)-2,5-difluorobenzonitriles.Type: GrantFiled: May 28, 1998Date of Patent: January 5, 1999Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Mark Wilhelm Drewes, Bernd Gallenkamp
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Patent number: 5854283Abstract: The optically pure forms of monoocarbamates of halogenated 2-phenyl-1,2-ethanediol and dicarbamates of 2-phenly-1,2-ethaniediol have been found to be effective in the treatment of disorders of the central nervous system, especially as anti-convulsive or anti-epileptic agents.Type: GrantFiled: January 9, 1997Date of Patent: December 29, 1998Assignee: Yukong LimitedInventors: Yong Moon Choi, Min Woo Kim, Jeonghan Park
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Patent number: 5723646Abstract: There are described new amino acid amide derivatives, some of which are known, of the formula (I) ##STR1## in which R.sup.1 to R.sup.8 have the meaning given in the description, and a process for their preparation. The amino acid amide derivatives of the formula (I) are used for the preparation of pesticides.Type: GrantFiled: January 16, 1992Date of Patent: March 3, 1998Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Heinz-Wilhelm Dehne
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Patent number: 5543573Abstract: The present invention relates to a hydrazinecarboxamide derivative of the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, which has a wide insecticidal spectrum at a low dosage, a process for producing said derivative, and utilization of said derivative as an insecticide.Type: GrantFiled: April 14, 1994Date of Patent: August 6, 1996Assignee: Nihon Nohyaku Co., Ltd.Inventors: Kazuhiro Takagi, Takashi Ohtani, Tateki Nishida, Hiroshi Hamaguchi, Tetsuyoshi Nishimatsu, Atsushi Kanaoka
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Patent number: 5412079Abstract: Disclosed is a liquid crystal monomer compound represented by formula (1): ##STR1## wherein n is an integer of from 2 to 18, X is direct bond, --(C.dbd.O)--O--, --(C.dbd.O)--NH-- or --N.dbd.N--, R.sup.1 is hydrogen or a lower alkyl group, and R.sup.2 is hydrogen, a cyano group or a methoxy group, as well as a liquid crystal polymer derived therefrom.Type: GrantFiled: March 25, 1994Date of Patent: May 2, 1995Assignee: Nippon Paint Co., Ltd.Inventors: Junji Furukawa, Hiroshi Okamoto, Yoshio Onouchi, Takushi Andoh, Satoshi Urano