Ureido, Guanido Or Hydrazino In Acid Moiety Patents (Class 560/34)
-
Publication number: 20110009642Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.Type: ApplicationFiled: February 12, 2009Publication date: January 13, 2011Applicant: Bayer Cropscience AGInventor: Sergii Pazenok
-
Patent number: 7863332Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/or of diseases related to the metabolism of lipids) or, alternatively, in cosmetic compositions.Type: GrantFiled: February 16, 2007Date of Patent: January 4, 2011Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Jean-Guy Boiteau, Corinne Millois Barbuis
-
Patent number: 7825279Abstract: Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to Trypanosoma brucei rhodesiense (T.b.r.) and Plasmodium falciparum. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.Type: GrantFiled: November 18, 2004Date of Patent: November 2, 2010Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Richard R. Tidwell, W. David Wilson, Reto Brun, Reem K. Arafa, Chad E. Stephens
-
Publication number: 20100266945Abstract: A pigment has a compound expressed by Formula (1). The pigment has a number average primary particle size of 30 to 70 nm and has a CuK? characteristic X-ray diffraction spectrum having, when ? represents a Bragg angle, a peak at 2?±0.20° equal to 10.0° and a peak at 2?±0.20° equal to 11.1°, the intensity ratio of the 11.1° peak to the 10.0° peak being 0.1 to 0.6.Type: ApplicationFiled: April 14, 2010Publication date: October 21, 2010Applicant: CANON KABUSHIKI KAISHAInventors: Kei Inoue, Takayuki Toyoda, Yutaka Tani, Taichi Shintou, Yasuaki Murai, Masashi Hirose
-
Publication number: 20100258764Abstract: A polymerizable liquid crystal compound shown by the following formula (I), a polymerizable liquid crystal composition that includes the polymerizable liquid crystal compound and a chiral compound polymerizable with the polymerizable liquid crystal compound, a liquid crystalline polymer obtained by polymerizing the polymerizable liquid crystal compound or the polymerizable liquid crystal composition, and an optical anisotropic article that includes the liquid crystalline polymer. The polymerizable liquid crystal compound shows a liquid crystal phase over a wider temperature range, is chemically stable, can be inexpensively produced, and has a wide selective reflection wavelength band ?? (i.e., a large value ?n).Type: ApplicationFiled: April 24, 2008Publication date: October 14, 2010Applicant: ZEON CORPORATIONInventors: Kei Sakamoto, Naoto Kogoshi, Yoshihide Yachi
-
Publication number: 20100240908Abstract: The invention provides an acetylene compound represented by the following Formula (1), which is useful as a raw material for a polymer achieving high thermal resistance; wherein, in Formula (1), the encircled Ar represents an aryl group or a heteroaryl group; X represents a divalent linking group; R, R? and R1 each independently represent a hydrogen atom, a hydrocarbon group or a heterocyclic group; R2 represents a hydrogen atom or a substituent substitutable on a benzene ring; A represents a hydrocarbon group or a heterocyclic group; Q represents a hydrogen atom, a hydrocarbon group, or a metal element capable of forming a monovalent metal salt; a represents an integer from 0 or more; b, m and n each independently represent an integer of 1 or more; when n, m and b are 1 at the same time, X is not —(C?O)O—; and when n is 2, and both m and b are 1, X is not —O—.Type: ApplicationFiled: September 25, 2008Publication date: September 23, 2010Applicant: FUJIFILM CORPORATIONInventors: Akira Imakuni, Masaya Nakayama, Morio Yagihara
-
Publication number: 20100216881Abstract: The enhydrazone esters for treating asthma, allergy, and inflammation relate to the use of two cyclohexenone derivatives and pharmaceutically acceptable salts thereof in the treatment of asthma, allergies, and inflammation. The esters have the formula: wherein R is ethyl or methyl. Administration of the esters inhibits the degranulation of eosinophils, the degranulation of mast cells, and the release or expression of tumor necrosis factor-?, thereby alleviating the debilitating symptoms of asthma, allergic reactions, and inflammatory responses.Type: ApplicationFiled: May 3, 2010Publication date: August 26, 2010Inventors: Charles I. Ezeamuzie, Ivan O. Edafiogho
-
Patent number: 7777069Abstract: 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: August 7, 2008Date of Patent: August 17, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean P. Stamos, Randy S. Bethiel
-
Patent number: 7659424Abstract: [PROBLEMS] To provide a novel method for the allylation of N-acylhydrazones by which enantioselectively allylated N-acylhydrazines can be efficiently obtained. [MEANS FOR SOLVING PROBLEMS] A method for the production of enantioselectively allylated N-acylhydrazines represented by the general formula [3]: [wherein R0 is an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or —COOR1 (wherein R1 is a hydrocarbon group); R2 is acyl; R3 and R4 are each hydrogen, or one of R3 and R4 is hydrogen and the other is a hydrocarbon group; and R5 and R6 are each independently hydrogen or a hydrocarbon group], characterized by reacting an N-acylhydrazone represented by the general formula [1]: [wherein R0 and R2 are as defined above] with an allylating agent such as allyltrichlorosilane or crotyltrichlorosilane in the presence of a chiral phosphine oxide.Type: GrantFiled: February 24, 2005Date of Patent: February 9, 2010Assignee: Japan Science and Technology AgencyInventors: Shu Kobayashi, Masaharu Sugiura
-
Publication number: 20100015249Abstract: It is an object of the present invention to provide novel antitumor agents which have a high therapeutic index while causing neither serious adverse effects nor drug resistance, both of which are the problems associated with existing antitumor agents. In particular, it is an object of the present invention to provide novel agents and therapies which are effective for pancreas cancer, for which no effective therapies and chemotherapeutic agents exist at this stage, and are also capable of inhibiting cancer metastasis and cancer filtration. The antitumor agents, more specifically the therapeutic agents for pancreas cancer and the cancer metastasis inhibitors, of the present invention contain as an active ingredient 6?-amidino-2?-naphthyl 4-guanidinobenzoate or a salt thereof or more specifically the mesylate thereof known as nafamostat mesilate (generic name; also referred to as “Futhan,” “FUT,” and “FUT175.”).Type: ApplicationFiled: July 28, 2006Publication date: January 21, 2010Inventor: Takashi Uwagawa
-
Publication number: 20090305891Abstract: The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the disclosure relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The disclosure furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.Type: ApplicationFiled: February 8, 2007Publication date: December 10, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Dieter Feucht, Eva-Maria Franken, Olga Malsam, Alfred Angermann, Guido Bojack, Christian Arnold, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger
-
Patent number: 7626054Abstract: Novel biaromatic compounds having the following structural formula (I): are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, in particular in dermatology as well as in the fields of cardiovascular diseases, immune diseases and/or diseases related to the metabolism of lipids, or, alternatively, into cosmetic compositions.Type: GrantFiled: November 3, 2006Date of Patent: December 1, 2009Assignee: Galderma Research & DevelopmentInventors: Jerome Aubert, Laurence Clary, Pascale Mauvais, Michel Rivier, Etienne Thoreau, Jean-Guy Boiteau
-
Patent number: 7608621Abstract: The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: GrantFiled: January 11, 2008Date of Patent: October 27, 2009Assignee: SmithKline Beecham, Corp.Inventors: Antony N. Shaw, Kevin J. Duffy, William Henry Miller, Andrea K. Myers, Michael N. Zimmerman
-
Publication number: 20090239841Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.Type: ApplicationFiled: October 24, 2005Publication date: September 24, 2009Inventors: Alan J. Hutchison, Jun Yuan
-
Publication number: 20090203777Abstract: The invention describes novel pharmaceutically acceptable salt forms of camostat, processes for lyophilisation, taste-masked formulations, nebulised formulations and the use of each of the fore-going in the treatment of respiratory diseases, particularly cystic fibrosis and chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: April 12, 2006Publication date: August 13, 2009Inventors: Henry Luke Danahay, Darren Mark Legrand, David C. Tully, Jennifer Leslie Harris, Silvia Heuerding, Dilraj Singh, Janet Catherine Maas, Juergen Roettele, Jean-Louis Reber, Stephanie Monnier
-
Publication number: 20090105091Abstract: The present invention provides a compound of the general formula (I), wherein X is the connection between the CO-hydrazine and the NR1-oxalic acid or ester group, and uses and synthesis methods. These compounds represent amino acid derivatives, wherein the amine group is turned into an acidic group by the oxalic acid group and the carboxylic acid is turned into an amine functionality by the hydrazine group; as well as peptidomimetics comprising the compound and methods for their synthesis.Type: ApplicationFiled: November 24, 2006Publication date: April 23, 2009Applicant: TECHNISCHE UNIVERSITAT WIENInventors: Ulrich Jordis, Jaywant B. Phopase
-
Publication number: 20090088472Abstract: An object of the present invention is to provide a protective agent for a neuronal cell. The protective agent for a neuronal cell according to the present invention contains a compound represented by the following general formula [I] or a salt thereof as an active ingredient. In the formula, R1, R2 and R3 are the same or different and represent a hydrogen atom or an alkyl group, or R1 and R3 may be joined together to form a ring having one or more double bonds.Type: ApplicationFiled: May 17, 2006Publication date: April 2, 2009Inventors: Kouji Oohashi, Reina Doi, Masaaki Kageyama
-
Publication number: 20090062340Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: ApplicationFiled: November 6, 2008Publication date: March 5, 2009Applicant: Galderma Research & DevelopmentInventors: LAURENCE CLARY, CLAIRE BOUIX-PETER, MICHEL RIVIER, PASCAL COLLETTE, ANDRE JOMARD
-
Publication number: 20090054662Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.Type: ApplicationFiled: July 21, 2006Publication date: February 26, 2009Inventors: Lushi Tan, James Christopher McWilliams, Frederick W. Hartner, Naoki Yoshikawa, Wenji Li
-
Patent number: 7476762Abstract: Methods for preparing substituted phenylsulfonamide compounds of the following structure are provided: or a pharmaceutically acceptable salt thereof, wherein, R1-R7 are defined herein. Also provided are methods for preparing compounds of the following structure: wherein, R9, m, n, p, r, and s are defined herein.Type: GrantFiled: April 19, 2007Date of Patent: January 13, 2009Assignee: WyethInventors: Asaf Ragim Alimardanov, Jean Schmid, Jay Thomas Afragola, Gulnaz Khafizova
-
Publication number: 20080306260Abstract: The invention relates to a method for producing aryl or heteroaryl amines, ethers or thioethers (III) by cross-coupling primary or secondary amities, alcohols or thioalcohols with substituted aryl or heteroaryl compounds (I) in the presence of a Brønsted base and a catalyst or a pre-catalyst containing a) a transition metal, a complex, a salt, or a compound of a transition metal from the group V, Mn, Fe, Co, Ni, Rh, Pd, Ir, Pt, and b) at least one sulfonated phosphane ligand in a solvent or a solvent mixture corresponding to Scheme 1 wherein Hal represents fluorine, chlorine, bromine, iodine, alkoxy, trifluoromethane sulfonate, nonafluorotrimethyl-methane sulfonate, methane sulfonate, 4-nitrobenzene sulfonate, benzene sulfonate, 2-naphthalene sulfonate, 3-nitrobenzene sulfonate, 4-nitrobenzene sulfonate, 4-chlorobenzene sulfonate, 2,4,6-triisopropylbenzene sulfonate or any other sulfonate, and X represents O, S or NR?. The invention also relates to novel phosphane ligands.Type: ApplicationFiled: June 14, 2006Publication date: December 11, 2008Inventors: Andreas Meudt, Sven Nerdinger, Bernd Wilhelm Lehnemann, Joerg Jung, Till Vogel, Victor Snieckus
-
Publication number: 20080300287Abstract: The present invention provides a compound of formula (I), (II), (III) and (IV) as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.Type: ApplicationFiled: September 21, 2005Publication date: December 4, 2008Applicant: UNIVERSITY OF WOLLONGONGInventors: Timothy Patrick Boyle, John Barnard Bremner, Zinka Brkic, Jonathan Alan Victor Coates, Neal Kevin Dalton, John Deadman, Paul Anthony Keller, Jody Morgan, Stephen Geoffrey Pyne, David Ian Rhodes, Mark James Robertson
-
Patent number: 7449446Abstract: There is provided a combination product comprising; (A) melagatran or a pharmaceutically acceptable derivative thereof; and (B) dexamethasone or a pharmaceutically acceptable derivative there of, wherein each of components (A) and (B) is formulated in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, as well as the use of such a combination product in the treatment of conditions including disseminated intravascular coagulation.Type: GrantFiled: October 24, 2002Date of Patent: November 11, 2008Assignee: AstraZeneca ABInventor: Margareta Elg
-
Patent number: 7408079Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.Type: GrantFiled: January 10, 2003Date of Patent: August 5, 2008Assignee: The Johns Hopkins UniversityInventors: Martin Gilbert Pomper, Jiazhong Zhang, Alan P. Kozikowski, John L. Musachio
-
Publication number: 20080177016Abstract: A monomer with a chromophore group represented by Formula (I): wherein AR1 represents a substituted or unsubstituted aromatic group; AR2 represents a substituted or unsubstituted aromatic group or a substituted or unsubstituted alkyl group; and R represents a substituted or unsubstituted alkyl group, with the proviso that one of R, AR1, and AR2 has a substituent with a polymerizable functional group. The monomer can be advantageously used to prepare polymeric dispersants for pigment dispersion, especially inkjet inks.Type: ApplicationFiled: July 4, 2006Publication date: July 24, 2008Applicant: AGFA GRAPHICS NVInventors: Geert Deroover, Wojciech Jaunky, Lambertus Groenendaal, Johan Loccufier
-
Patent number: 7253171Abstract: Novel antagonists of ?4?1 integrin and/or ?4?7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4.Type: GrantFiled: January 15, 2002Date of Patent: August 7, 2007Assignee: Laboratorios Almirall, S.A.Inventors: Juan Miguel Jimenez Mayorga, Jordi Bach Tana, Jesus Maria Ontoria Ontoria, Eloisa Navarro Romero
-
Patent number: 7235672Abstract: A probe, kit comprising the probe, and methods for using the probe are provided where the probe comprises: wherein DM is a detectable marker; and L is a straight or branched chain moiety providing between 1 and 20 atom separation between DM and the ring atom to which DM is attached.Type: GrantFiled: March 11, 2004Date of Patent: June 26, 2007Assignee: Takeda San Diego, Inc.Inventors: Christopher L. Caster, Andrew J. Jennings, Marc E. Navre, Michael B. Wallace, Yiqin Wu
-
Patent number: 7199265Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.Type: GrantFiled: June 15, 2001Date of Patent: April 3, 2007Assignee: Karo Bio ABInventors: Li Yi-Lin, Johan Malm, Chris Litten, Ana Maria Garcia Collazo, Neeraj Garg
-
Patent number: 7144665Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where R1, R2, R3, R4, R5, R6, R7, and R8 are, each independently, an alkyl group, an alkaryl group, an aryl group, or heterocyclic group, X and X? are, each independently, aromatic groups, and Z is a divalent linking group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: December 30, 2003Date of Patent: December 5, 2006Assignee: Samsung Electronics Co., Ltd.Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Ingrida Paulauskaite, Valentas Gaidelis, Edmundas Montrimas
-
Patent number: 7101912Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.Type: GrantFiled: December 8, 2003Date of Patent: September 5, 2006Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Kenneth C. Cundy, Jianhua Li, Feng Xu, Cindy X. Zhou, Laxminarayan Bhat
-
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
-
Patent number: 7049460Abstract: The present invention relates to novel selective inhibitors of the urokinase plasminogene activator (uPA, EC 3.4.21.31) of the aryl guanidine type.Type: GrantFiled: August 23, 2000Date of Patent: May 23, 2006Assignee: Wilex AGInventors: Viktor Magdolen, Luis Moroder, Stefan Sperl, Jörg Stürzebecher, Olaf Wilhelm
-
Patent number: 7049341Abstract: N-Benzoylureidocinnamic acid derivatives, processes for preparing them and their use The invention relates to N-benzoylureidocinnamic acid derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention thus relates to compounds of formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetic agents.Type: GrantFiled: June 6, 2003Date of Patent: May 23, 2006Assignee: Aventis Pharma Deutschland GmbHInventors: Karl Schoenafinger, Elisabeth Defossa, Dieter Kadereit, Erich Von Roedern, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt
-
Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
-
Patent number: 6962905Abstract: A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.Type: GrantFiled: April 19, 2000Date of Patent: November 8, 2005Assignee: AstraZeneca ABInventor: David Gustafsson
-
Patent number: 6960588Abstract: Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors.Type: GrantFiled: September 12, 2000Date of Patent: November 1, 2005Assignee: Altana Pharma AGInventor: Thomas Martin
-
Patent number: 6875884Abstract: Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.Type: GrantFiled: July 28, 2000Date of Patent: April 5, 2005Assignee: Kirin Beer Kabushiki KaishaInventors: Janak Padia, Michael Hocker, Tsuyoshi Nishitoba, Hirohi Ohashi, Eiji Sawa
-
Patent number: 6838472Abstract: 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: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
-
Publication number: 20040220261Abstract: The invention relates to arylcycloalkyl-substituted derivatives and to their physiologically acceptable salts and physiologically functional derivatives.Type: ApplicationFiled: February 27, 2004Publication date: November 4, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Christian Stapper, Heiner Glombik, Eugen Falk, Dirk Gretzke, Jochen Goerlitzer, Stefanie Keil, Hans-Ludwig Schaefer, Wolfgang Wendler
-
Publication number: 20040170910Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising:Type: ApplicationFiled: December 30, 2003Publication date: September 2, 2004Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Ingrida Paulauskaite, Valentas Gaidelis, Edmundas Montrimas
-
Publication number: 20040167216Abstract: Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.Type: ApplicationFiled: December 8, 2003Publication date: August 26, 2004Inventors: Jia-Ning Xiang, Mark A. Gallop, Kenneth C. Cundy, Jianhua Li, Feng Xu, Cindy X. Zhou, Laxminarayan Bhat
-
Publication number: 20040157922Abstract: Carboxyalkoxy-substituted acyl-carboxyphenylurea derivatives and their use as medicamentsType: ApplicationFiled: October 6, 2003Publication date: August 12, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger, Alfons Enhsen
-
Patent number: 6770764Abstract: A compound of the formula (I) wherein R1 is a protecting group for N&agr;, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin substrate such that trypsin cleaves the O—C single bond, which liberates R3—OH; a diagnostic device comprising same; a method for preparing the diagnostic device; and a method of using the diagnostic device to detect levels of urinary trypsin inhibitor in a biological sample; and a diagnostic kit for detecting levels of urinary trypsin inhibitor in a biological sample.Type: GrantFiled: April 30, 2001Date of Patent: August 3, 2004Assignee: Bayer CorporationInventors: Paul F. Corey, Steven W. Felman, Gary E. Rehm, Michael J. Pugia
-
Patent number: 6734212Abstract: 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. One exemplary compound of the present invention has the following formula I: wherein n is 0 or 1, and R is selected from the group consisting of C1-10 alkyl, C6-10 aryl and and wherein when n is 0, R is not C6-10 aryl.Type: GrantFiled: October 10, 2001Date of Patent: May 11, 2004Assignees: Shanghai East Best Biopharmaceutical, Nanjing UniversityInventors: Dexu Zhu, Mitsumi Muramatsu, Jianshu Xie, Cheng Ni, Ming-Wei Wang
-
Publication number: 20040077716Abstract: The invention relates to acyl-4-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: April 10, 2003Publication date: April 22, 2004Inventors: Elisabeth Defossa, Dieter Kadereit, Karl Schoenafinger, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Alfons Enhsen, Joerg Rieke-Zapp
-
Publication number: 20040054190Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.Type: ApplicationFiled: January 10, 2003Publication date: March 18, 2004Applicant: Johns Hopkins UniversityInventors: Martin Gilbert Pomper, Jiazhong Zhang, Alan P. Kozikowski, John L. Musachio
-
Publication number: 20040043952Abstract: The present invention relates, inter alia, to pentaerythritol lipid derivatives that are useful for the intracellular delivery of nucleic acids. Such pentaerythritol lipid derivatives are useful for the preparation of transfection complexes (such as liposomes, lipoplexes, and other lipid vesicles) that can be used to deliver nucleic acids into mammalian cells.Type: ApplicationFiled: May 30, 2003Publication date: March 4, 2004Applicant: Genteric, Inc.Inventors: Edmund J. Niedzinski, Michael Bennett
-
Publication number: 20040034231Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: August 12, 2003Publication date: February 19, 2004Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
-
Publication number: 20040034072Abstract: The invention relates to semicarbazides of the general formula I 1Type: ApplicationFiled: August 4, 2003Publication date: February 19, 2004Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
-
Publication number: 20040024045Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.Type: ApplicationFiled: February 24, 2003Publication date: February 5, 2004Inventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau