Ureido, Guanido Or Hydrazino In Acid Moiety Patents (Class 560/34)
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Publication number: 20040023806Abstract: The invention relates to novel compounds of the formula I 1Type: ApplicationFiled: September 5, 2002Publication date: February 5, 2004Inventors: Hugo Ziegler, Saleem Farooq, Rene Zurflh
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Patent number: 6683200Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: January 27, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
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Patent number: 6677360Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: April 6, 2001Date of Patent: January 13, 2004Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Publication number: 20030236168Abstract: Processes for preparing &agr;-substituted benzylnitroguanidines include the steps of providing a reaction mixture comprising water, alcohol, an S-alkyl nitroisothiourea, and an &agr;-substituted benzylamine; heating the reaction mixture; steam distilling the alcohol from the reaction mixture; and isolating an &agr;-substituted benzylnitroguanidine from the remaining water layer.Type: ApplicationFiled: June 20, 2002Publication date: December 25, 2003Inventors: David M. Mayes, Vijay C. Desai, Eric Rivadeneira
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Publication number: 20030220497Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.Type: ApplicationFiled: December 27, 2002Publication date: November 27, 2003Applicant: The University of QueenslandInventors: Daniel Yung-Yu Hung, Michael Stephen Roberts
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Patent number: 6638975Abstract: Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which include: 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihydro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07), 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10), 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl ester (3F-11), 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid (3F-15), and 4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) as well as some novel derivatives of these compounds claimed (see Table 2).Type: GrantFiled: December 4, 2002Date of Patent: October 28, 2003Assignee: University of Central FloridaInventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Krasnykh Olga Petrovna, Pimenova Elena Valentinovna, Elena A. Goun
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Publication number: 20030199579Abstract: 1Type: ApplicationFiled: May 21, 2003Publication date: October 23, 2003Inventors: Rikio Yamaguchi, Tetsuyoshi Nishimatsu, Kazuhiro Takagi
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Publication number: 20030187037Abstract: Novel compounds of the formula I, in which R, R1 and R2 are as defined in patent claim 1, are inhibitors of coagulation factor Xa and VIIa and can be employed for the treatment of thromboses, myocardial infarction, arteriosclerosis, inflammation, apoplexis, angina pectoris, restenosis after angioplasty, claudicatio intermittens, tumours, tumour diseases and/or tumour metastases.Type: ApplicationFiled: January 29, 2003Publication date: October 2, 2003Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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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: 20030149083Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to &agr; 4 integrin. They are used as therapeutic agents for various diseases concerning &agr; 4 integrin.Type: ApplicationFiled: May 20, 2002Publication date: August 7, 2003Applicant: AJINOMOTO CO. INCInventors: Yasuhiro Tanaka, Toshihiko Yoshimura, Hiroyuki Izawa, Chieko Ejima, Mitsuhiko Kojima, Yuko Satake, Eiji Nakanishi, Nobuyasu Suzuki, Shingo Makino, Manabu Suzuki, Masahiro Murata
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Publication number: 20030144311Abstract: Novel propanoic acid derivatives are integrin receptor antagonists or inhibitors, in particular of the avb3 integrin receptor. The compounds of the invention are for instance useful for the treatment of solid tumors by inhibition of angiogenic growth of tumor vessel network, thus promoting tumor regression, inhibition of metastatic spread, thus avoiding cancer metastases, inhibition of bone resorption, thus controlling osteoporosis, inhibition of smooth muscle cells migration into neointima, thus blocking restenosis after percutaneous coronary angioplasty and the treatment of other pathological conditions mediated by cell adhesion, cell migration or angiogenesis such e.g. diabetic retinopaty, rheumatoid arthritis and inflammation.Type: ApplicationFiled: November 1, 2002Publication date: July 31, 2003Inventors: Tiziano Bandiera, Paola Vianello, Paolo Cozzi, Arturo Galvani
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Publication number: 20030138712Abstract: An organophotoreceptor that includes:Type: ApplicationFiled: November 6, 2002Publication date: July 24, 2003Applicant: SAMSUNG Electronics Co. Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katrizky, Ritu Jain, Anatoliy Vakulenko
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Patent number: 6593315Abstract: Salicylic acid derivatives of the formula I, where the index and the substituents have the following meanings: X is halogen, NO2, cyano, alkyl or alkoxy; m is 0, 1, 2 or 3, it being possible for the substituents X to be different from each other if n is greater than 1; A is OH, alkoxy, NH2, NHCH3 or N(CH3)2; R1 is phenyl, naphthyl, cycloalkyl, 5-membered or 6-membered hetaryl or 5-membered or 6-membered heterocyclyl, comprising one to three N atoms and/or one O or S atom or one or two O and/or S atoms, the ring systems being unsubstituted or substituted; R2 is hydrogen, cyano, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy or alkylthio, processes for the preparation of these compounds, compositions comprising them, and their use for controlling harmful fungi.Type: GrantFiled: July 2, 2001Date of Patent: July 15, 2003Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Thomas Grote, Joachim Rheinheimer, Ingo Rose, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Müller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20030130515Abstract: Compounds of the formula 1Type: ApplicationFiled: January 2, 2003Publication date: July 10, 2003Inventors: Vidyasagar Vuligonda, Alan T. Johnson, Roshantha A. Chandraratna
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Publication number: 20030125384Abstract: The invention relates to compositions and methods for treating or preventing disease or disorders caused by or associated with certain bacterial infection, especially Escherichia coli (E. coli) or Helicobacter pylori (H. pylori) infection.Type: ApplicationFiled: October 10, 2001Publication date: July 3, 2003Inventors: Dexu Zhu, Mitsumi Muramatsu, Jianshu Xie, Cheng Ni, Ming-Wei Wang
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Publication number: 20030125383Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: ApplicationFiled: September 17, 2002Publication date: July 3, 2003Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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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: 6566554Abstract: The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is anType: GrantFiled: February 22, 2002Date of Patent: May 20, 2003Assignee: Leo Pharmaceutical Products Ltd. a/s (Lovens Kemiske Fabrik Produktionsaktieselskab)Inventor: Erik Rytter Ottosen
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Patent number: 6566547Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.Type: GrantFiled: October 11, 1985Date of Patent: May 20, 2003Assignee: Zeneca LimitedInventors: Michael J Bushell, Kevin Beautement, John M Clough, Vivienne M Anthony, Paul deFraine, Christopher R Godfrey
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Publication number: 20030083504Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: October 4, 2002Publication date: May 1, 2003Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
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Patent number: 6552216Abstract: Pharmacophore models of VLA-4 inhibitors, methods of identifying novel inhibitors and novel inhibitors identified by these methods.Type: GrantFiled: January 25, 1999Date of Patent: April 22, 2003Assignee: Biogen, Inc.Inventors: Juswinder Singh, Zhongli Zheng, Peter Sprague, Herman Van Vlijmen, Alfredo Castro, Steven P. Adams
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Patent number: 6545029Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.Type: GrantFiled: June 12, 2001Date of Patent: April 8, 2003Assignee: Bayer AktiengesellschaftInventor: Andrea Vaupel
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Patent number: 6534283Abstract: Shock is a life threatening complication in situations associated with trauma including burns, surgery, ischemia, sepsis, and other critical care applications. Shock is induced by pancreatic proteases when they are released into the small intestine when the tissue is compromised due to trauma. Administration of protease inhibitors into the small intestine, either orally, intraveneously, or by direct lavage, was demonstrated to prevent shock in rats as determined by both survival time and molecular and histological analysis.Type: GrantFiled: November 22, 2000Date of Patent: March 18, 2003Assignees: The Regents of the University of California, The Scripps InstituteInventors: Geert Schmid-Schoenbein, Tony Hugli, Hiroshi Mitsuoka
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Patent number: 6534546Abstract: Compounds represented by the general formula (1): (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1-6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 6, 1997Date of Patent: March 18, 2003Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Toshio Honda, Toshihiko Makino, Toshiaki Nagafuji, Yasushi Kitoh, Nobuaki Kimura
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Publication number: 20030028047Abstract: Esters derived from fatty acids and juvenoid alcohols of the general formula (I), in which X means the oxygen atom or the NH group, Y means the NH group or the oxygen atom, R means methyl, ethyl, 1-propyl, 2-methylethyl or propargyl and R′ means saturated or unsaturated alkyl with 4 to 22 carbon atoms. Esters derived from fatty acids and juvenoid alcohols are produced by a reaction of a juvenoid alcohol of the general formula (II), in which X means the oxygen atom or the NH group, Y means the NH group or the oxygen atom and R means methyl, ethyl, 1-propyl, 2-methylethyl or propargy] with a fatty acid chloride of the general formula (Ill): R′COC1 in which R′ means saturated or unsaturated alkyl with 4 to 22 carbon atoms, under the continuous stirring, at 0 to 70° C., using a convenient solvent, as toluene, xylene or benzene and under the presence of a base catalyst, as triethylamine, pyridine or quinoline.Type: ApplicationFiled: July 25, 2002Publication date: February 6, 2003Inventors: Zdenek Wimmer, Jelena Kuldova, Ivan Hrdy, Blanka Bennettova
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Publication number: 20030018073Abstract: A caged non-steroidal ecdysome memetic (NSE) compound and a method for producing free NSE by subjecting the charged NSE to UV irradiation.Type: ApplicationFiled: February 21, 2002Publication date: January 23, 2003Inventors: Joseph Pao Yung Kao, David Ari Freilich
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Publication number: 20030013760Abstract: Substituted 1-naphthoylguanidines, process for their preparation, their use as a medicament or diagnostic, and medicament containing them.Type: ApplicationFiled: August 14, 2002Publication date: January 16, 2003Inventors: Joachim Brendel, Heinz-Werner Kleemann, Heinrich Christian Englert, Hans Jochen Lang, Udo Albus, Bansi Lal, Anil Vasantrao Ghate
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Patent number: 6504045Abstract: The invention relates to six new crystal polymorphs, &agr; (alpha), &bgr; (beta), &ggr; (gamma), &dgr; (delta), &zgr; (zeta), and &eegr; (eta), of the disazo colorant of the formula I, having characteristic reflections in the X-ray diffraction spectrum. The novel crystal polymorphs are prepared by treatment in organic solvents.Type: GrantFiled: September 13, 2001Date of Patent: January 7, 2003Assignee: Clariant GmbHInventors: Ruediger Jung, Hans-Joachim Metz, Joachim Weber, Martin U. Schmidt, Olaf Schupp, Andreas Wacker
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Publication number: 20020165275Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.Type: ApplicationFiled: January 25, 2002Publication date: November 7, 2002Inventors: Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
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Publication number: 20020151586Abstract: The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: June 8, 2001Publication date: October 17, 2002Inventors: Elisabeth Defossa, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Heinz Baringhaus
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Patent number: 6465686Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: April 13, 2001Date of Patent: October 15, 2002Assignee: Pharmacia CorporationInventors: Margaret L. Grapperhaus, James A. Sikorski, Alok K. Awasthi, Lijuan J. Wang, Barnett S. Pitzele, Donald W. Hansen, Jr., Pamela T. Manning
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Patent number: 6458986Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-&agr;]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.Type: GrantFiled: February 15, 2002Date of Patent: October 1, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rogelio P. Frutos, Michael Dale Johnson
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Patent number: 6459001Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.Type: GrantFiled: January 25, 2001Date of Patent: October 1, 2002Assignees: Aventis Pharma S.A., GenetechInventors: Serge Bernard, Denis Carniato, Jean-Francois Gourvest, Jean-Georges Teutsch, Jochen Knolle, Hans-Ulrich Stilz, Volkmar Wehner, Sarah C. Bodary, Thomas R. Gadek, Robert S. McDowell, Robert M. Pitti
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Patent number: 6433017Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
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Patent number: 6417393Abstract: The present patent application relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R1, R2 and R3 is a non-cyclic acidic group having a pKa value below 8 or a group which is in vivo convertible to such a group; R4, R5 and the other two of the substituents R1, R2 and R3 are each independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro, amnino, and aryl, aralkyl, arylamino, aryloxy, aryl—CO—, or heteroaryl, wherein the aryl and heteroaryl groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano, nitro and amino; or R3 and R4 or R4 and R5 together form a fused 4- to 7-membered carbocyclic ring which may be unsaturated, or partially or fully saturated, while the other substituents R1, R2, R3, R4 and R5 are asType: GrantFiled: January 22, 1999Date of Patent: July 9, 2002Assignee: Neurosearch A/SInventors: Palle Christophersen, Ove Pedersen
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Publication number: 20020082441Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-a]imidazol-2-one (1): 1Type: ApplicationFiled: February 15, 2002Publication date: June 27, 2002Inventors: Rogelio P. Frutos, Michael Dale Johnson
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Patent number: 6403794Abstract: The invention relates to novel substituted 2-amino-4-alkylamino-1,3,5-triazines of the formula (I) in which R1 represents in each case optionally substituted alkyl having 2 to 6 carbon atoms or cycloalkyl having 3 to 6 carbon atoms, R2 represents hydrogen or represents alkyl having 1 to 4 carbon atoms, A represents oxygen or methylene, Ar represents in each case optionally substituted phenyl, naphthyl or heterocyclyl, and Z represents hydrogen, represents halogen or represents in each case optionally substituted alkyl, alkoxy, alkylcarboxyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenyl or alkinyl, to processes and to novel intermediates for their preparation and to their use as herbicides.Type: GrantFiled: April 5, 2001Date of Patent: June 11, 2002Assignee: Bayer AktiengesellschaftInventors: Hans-Jochem Riebel, Stefan Lehr, Uwe Stelzer, Yukiyoshi Watanabe, Markus Dollinger
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Patent number: 6395763Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs 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 and compositions of this invention.Type: GrantFiled: June 23, 2000Date of Patent: May 28, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean P. Stamos, Randy S. Bethiel
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Publication number: 20020061930Abstract: The invention relates to a process for preparing substituted cyclopentane derivatives represented by the 1Type: ApplicationFiled: November 26, 2001Publication date: May 23, 2002Inventors: Ahmed F. Abdel-Magid, Hans-Ulrich Bichsel, Daniel J. Korey, Gunther G. Laufer, Erja A. Lehto, Sebastiano Mattei, Max Rey, Thomas W. Schultz, Cynthia Maryanoff
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Patent number: 6391917Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: April 19, 2001Date of Patent: May 21, 2002Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Patent number: 6388122Abstract: A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the formula (II), guanidinophenol derivatives of the formula (III), amidinophenol derivatives of the formula (IV), and novel guanidinophenol derivatives of the formula (V) (in the formulae, Gu is guanidino).Type: GrantFiled: October 7, 1998Date of Patent: May 14, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiroshi Kido, Hisao Nakai
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Publication number: 20020052417Abstract: The present invention relates to compounds of the formula I, 1Type: ApplicationFiled: June 6, 2001Publication date: May 2, 2002Inventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Patent number: 6376699Abstract: Hydroazinecarboxylic acid ester of the formula In which R1 is an optionally substituted alkyl group, an aryl group, an arylalkyl group or a cycloalkyl group, and R3 is an optionally substituted alkyl group.Type: GrantFiled: January 26, 2001Date of Patent: April 23, 2002Assignee: Lonza AGInventor: Ulrich Veith
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Patent number: 6365745Abstract: The present invention provides a method for producing a hydrazine derivative of the formula [2]: wherein R1 is alkyl group having 1-12 carbon atoms and the like, R2 is alkyl group having 1-12 carbon atoms and the like, and Ar is phenylene group and the like, from a hydrazone derivative of the formula [1] wherein R1, R2 and Ar are as defined above, in the presence of at least one base selected from the group consisting of an organic base and an inorganic base, and a metal hydrogenating catalyst. By this method, reduction proceeds selectively and a hydrogenolysis reaction (side reaction) can be suppressed.Type: GrantFiled: July 13, 2001Date of Patent: April 2, 2002Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Kozo Matsui, Kiyoshi Sugi, Hiromi Suga, Nobushige Itaya
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Patent number: 6348499Abstract: Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: November 24, 1999Date of Patent: February 19, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
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Patent number: 6344484Abstract: The present invention relates to novel tyrosine alkoxyguanidine compounds that are inhibitors of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins, including conditions such as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, m and n are defined herein.Type: GrantFiled: February 11, 2000Date of Patent: February 5, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Yu Kai Lee
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Patent number: 6337350Abstract: Derivatives of aryl and heterocyclic ureido and aryl and heterocyclic carboxamido phenoxy isobutyric acids have been found to inhibit the nonenzymatic glycation of proteins which often results in formation of advanced glycation endproducts and crosslinks. Many other phenoxyisobutyric acid derivatives as well as certain other compounds as set out in this disclosure also have been found to inhibit the nonenzymatic glycation of proteins. The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become perturbed by these modifications and can result in severe consequences.Type: GrantFiled: April 5, 2000Date of Patent: January 8, 2002Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Patent number: 6310074Abstract: The invention relates to compound of formula (I): A—G1—Cy—G2—Cy′—G3—B (I) wherein: A represents a grouping NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents a grouping NR1C(Q)R2, NR1C(Q)NR2R3, C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy and Cy′, which are different, represent a ring structure or G2 represents a chain and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: May 18, 2000Date of Patent: October 30, 2001Assignee: Adir et CompagnieInventors: Patrick Depreux, Said Yous, Gwenael Cheve, Gérald Guillaumet, Marie-Claude Viaud, Carlos Larraya, Caroline Bennejean, Philippe Delagrange, Pierre Renard, Carole Descamps-Francois
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Patent number: 6291503Abstract: The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4, —COOR4′, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers.Type: GrantFiled: January 15, 1999Date of Patent: September 18, 2001Assignee: Bayer AktiengesellschaftInventors: Andreas Schoop, Gerhard Mueller, Ulf Brueggemeier, Delf Schmidt, Beatrix Stelte-Ludwig, Joerg Keldenich
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Patent number: 6284914Abstract: New compounds of general formulae (III), (IV) and (V).Type: GrantFiled: January 27, 2000Date of Patent: September 4, 2001Assignee: Fuji Yakuhin Kogyo Kabushiki KaishaInventors: Junko Fujisawa, Eiko Suda, Katsuhiro Igeta, Tadanori Morikawa, Tetsunori Fujisawa, Shinjiro Odake, Yasuo Morita, Tomoko Hongo, Hajime Ito