Ureido, Guanido, Or Hydrazine Patents (Class 562/439)
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Publication number: 20090163592Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: May 29, 2008Publication date: June 25, 2009Applicant: Intrexon CorporationInventors: Robert Eugene Hormann, Bing Li
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Publication number: 20090143592Abstract: 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 glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.Type: ApplicationFiled: December 3, 2007Publication date: June 4, 2009Applicant: Novo Nordisk A/SInventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thoger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thogersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jogensen, Janos Tibor Kodra, Shenghua Shi
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Publication number: 20090111696Abstract: A pyridazinone compound represented by the formula (I) have excellent effect on weed control and are useful as an active ingredient of herbicides.Type: ApplicationFiled: March 13, 2007Publication date: April 30, 2009Inventors: Toshiyuki Kiji, Takafumi Fusaka
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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
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Patent number: 7468360Abstract: Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.Type: GrantFiled: August 8, 2007Date of Patent: December 23, 2008Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20080287536Abstract: This invention relates to certain skin and hair care agents of formula (I), derived from natural amino acids and peptides. These agents provide multi-functional treatment of enzyme-related topical problems, for example, darkened skin including age spots, circles around eyes and stretch marks; skin conditions related to acne including excess facial oil and facial pore size; premature hair aging including hair loss and graying; inflammation including intra-cellular and extra-cellular inflammation; skin aging including wrinkles and fine lines; loss of collagen including thinning skin and loss of skin pliability; malfunction of tyrosinase group of enzymes; malfunction of matrix metalloprotease group of enzymes; and combinations thereof: Wherein, R, R?, and R?=any substituent(s); and M=H, Li, Na, K, Ca, Mg, Zn, Mn, Cu, Fe, Co, Mo, V, Cr, Ammonium, Alkyl ammonium, and Nitrogen Heterocyclic ammonium.Type: ApplicationFiled: July 30, 2008Publication date: November 20, 2008Applicant: BIODERM RESEARCHInventor: SHYAM K. GUPTA
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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
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Publication number: 20080268519Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 26, 2007Publication date: October 30, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
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Publication number: 20080268518Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 26, 2007Publication date: October 30, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
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Publication number: 20080251169Abstract: An ionic liquid is disclosed A precursor composition that comprises at least one ionic liquid and at least one energetic material is also disclosed, as is a method of synthesizing an ionic liquid and a method of desensitizing an explosive composition.Type: ApplicationFiled: April 13, 2007Publication date: October 16, 2008Applicant: ALLIANT TECHSYSTEMS INC.Inventors: Steven M. Nicolich, Alexander J. Paraskos, Daniel W. Doll, Gary K. Lund, Wendy A. Balas
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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
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Publication number: 20080182968Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 17, 2007Publication date: July 31, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
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Patent number: 7405239Abstract: The invention relates to acylhydrazone derivatives of formula (I), which are SGK inhibitors and can be used for the treatment of diseases and afflictions associated with SGK, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systematic and pulmonary hypertension, cardiovascular diseases and kidney diseases and in general for all types of fibroses and inflammatory processes. In said formula: R1 and R5 independently of one another represent H, OH, OA, OAc or methyl; R2, R3, R4, R6, R7, R8, R9 and R10 independently of one another represent H, OH, OA, OAc, OCF3, Hal, NO2, CF3, A, CN, OSO2CH3, SO2CH3, NH2, or COOH; R11 represents H or CH3; A represents an alkyl comprising 1, 2, 3, or 4 C atoms; X represents CH2, CH2CH2, OCH2 or —CH(OH)— and Hal represents F, Cl, Br or I.Type: GrantFiled: September 16, 2004Date of Patent: July 29, 2008Assignee: Merck Patent GmbHInventors: Rolf Gericke, Norbert Beier, Oliver Poeschke, Lars Burgdorf, Helga Drosdat, Florian Lang
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Publication number: 20080132507Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: October 13, 2005Publication date: June 5, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Shinsuke Hirota, Hiroshi Azuma, Kazunobu Kira, Nobuhisa Watanabe, Tadashi Nagakura, Tatsuo Horizoe
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Publication number: 20080125424Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: ApplicationFiled: July 10, 2007Publication date: May 29, 2008Inventors: Pierre DePrez, Sarah E. Lively, Taoues Temal
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Patent number: 7351857Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.Type: GrantFiled: June 3, 2005Date of Patent: April 1, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Xiaoli Chen, Keith T. Demarest, Jung Lee, Jay M. Matthews, Philip Rybczynski
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Publication number: 20080064754Abstract: A free amino ion releasing molecule useful for a wide variety of medical and cosmetic applications. The chemical name of the new molecule in acetate form name is 2-amino 5-triaminoguanidovalericbenzoicdiacetate, sometime referred to herein as Tri-Amino. Its chemical formula is C15H28N6O6. Its chemical structure is described in the drawings. Two methods of preparing the new amino ion releasing molecule are described.Type: ApplicationFiled: September 12, 2006Publication date: March 13, 2008Inventor: Steven R. Schutt
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Patent number: 7312361Abstract: Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.Type: GrantFiled: February 8, 2006Date of Patent: December 25, 2007Assignee: The Scripps Research InstituteInventors: Jeffery W. Kelly, Steven M. Johnson, H. Michael Petrassi
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Patent number: 7265136Abstract: A compound for use in inducing necrosis in vascular tissue of a tumor in an animal. The compound contains a first moiety which is a cis-stilbene moiety and a second moiety which is an inhibitor of the formation or action of nitric acid. Also, a method for inducing necrosis in vasculature of a tumor in an animal by administering to the animal the compound in an amount effective for inducing the necrosis.Type: GrantFiled: February 15, 2000Date of Patent: September 4, 2007Assignee: Angiogene Pharmaceuticals Ltd.Inventor: Peter David Davis
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Patent number: 7223796Abstract: The invention relates to acyl-4-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention particularly relates to compounds of formula I, in which the radicals have the given meanings described herein, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetics.Type: GrantFiled: April 10, 2003Date of Patent: May 29, 2007Assignee: Sanofi-aventis Deutschland GmbHInventors: Elisabeth Defossa, Dieter Kadereit, Karl Schoenafinger, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Alfons Enhsen, Joerg Rieke-Zapp
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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
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Patent number: 7078404Abstract: The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention 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 antidiabetics.Type: GrantFiled: April 10, 2003Date of Patent: July 18, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Elisabeth Defossa, Dieter Kadereit, Karl Schoenafinger, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Alfons Enhsen
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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
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Patent number: 7030133Abstract: 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 disturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.Type: GrantFiled: February 5, 2003Date of Patent: April 18, 2006Assignee: City of HopeInventors: Samuel Rahbar, Iraj Lalezari
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Patent number: 6984661Abstract: The present invention is directed to compounds of the structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof: Formula I (a) R1, R2 and R6 are each independently selected from the group consisting of hydrogen, C1-C8 alkyl substituted C1-C8 alkyl, aryl-C0-4-alkyl, substituted aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, substituted heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and substituted C3-C6 cycloalkylaryl-C0-2-alkyl; (b) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; (c) Y is C, O, S, NH or a single bond; and (d) E is selected from the group consisting of hydrogen, C(R3)(R4)A, A, (CH2)n COOR19 and substituted (CH2)n COOR19.Type: GrantFiled: January 21, 2003Date of Patent: January 10, 2006Assignee: Eli Lilly and CompanyInventors: James Robert Henry, YiHong Li
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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
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Patent number: 6916837Abstract: Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.Type: GrantFiled: November 14, 2002Date of Patent: July 12, 2005Assignee: Eisai Co., Ltd.Inventors: Takashi Satoh, Yasushi Okamoto, Osamu Asano, Nobuhisa Watanabe, Tadashi Nagakura, Takao Saeki, Atsushi Inoue, Masahiro Sakurai
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Patent number: 6875760Abstract: 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 glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.Type: GrantFiled: August 30, 2002Date of Patent: April 5, 2005Assignee: Novo Nordisk A/SInventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Inge Thøger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thøgersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jøgensen, Janos Tibor Kodra, Shenghua Shi
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Patent number: 6844466Abstract: 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 18, 2005Assignee: Syntex (U.S.A.) LLCInventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
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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
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Publication number: 20040248981Abstract: Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: 1Type: ApplicationFiled: November 7, 2003Publication date: December 9, 2004Applicant: SANKYO COMPANY, LIMITEDInventors: Koichi Fujimoto, Fumitoshi Asai, Hayao Matsuhashi
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Patent number: 6821960Abstract: 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 and obesity.Type: GrantFiled: November 16, 2001Date of Patent: November 23, 2004Assignee: Noyo Nordisk Pharmaceuticals, Inc.Inventors: Anker Steen Jørgensen, Peter Madsen
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Publication number: 20040224993Abstract: Compound of formula (I): 1Type: ApplicationFiled: June 7, 2004Publication date: November 11, 2004Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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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
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Publication number: 20040210080Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget s disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: ApplicationFiled: February 3, 2004Publication date: October 21, 2004Inventors: Dongfang Meng, Dann LeRoy Parker, Robert R Wilkening
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Patent number: 6787566Abstract: Advanced glycation endproducts (AGEs) have been implicated in the pathogenesis of a variety of debilitating diseases such as diabetes, atherosclerosis, Alzheimer's and rheumatoid arthritis, as well as in the normal aging process. Seven compounds are here reported to be active in breaking AGE-protein cross-links. These compounds are 1,4-benzene-bis[4-methyleneaminophenoxyisobutyric acid] (LR102); 4-[(3,5-dichlorophenylureidophenoxyisobutyryl]-4-aminobenzoic acid (LR99); L-bis-[4-(4-chlorobenzamidophenoxyisobutyryl)cystine] (LR20); 4-(3,5-dichlorophenylureido)phenoxyisobutyryl-1-amidocyclohexane-1-carboxylic acid (LR23); methylene bis [4,4′-(2-chlorophenylureidophenoxyisobutyric acid)] (LR90); 5-aminosalicylic acid (5-ASA); and metformin. These compounds may be used to reverse the debilitating effects of those diseases in which AGEs are formed.Type: GrantFiled: April 5, 2001Date of Patent: September 7, 2004Assignee: City of HopeInventor: Samuel Rahbar
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Publication number: 20040167211Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.Type: ApplicationFiled: October 17, 2003Publication date: August 26, 2004Inventors: Xiiaoli Chen, Keith T. Demarest, Jung Lee, Jay M. Matthews, Philip Rybczynski
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Publication number: 20040157919Abstract: 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: November 14, 2003Publication date: August 12, 2004Inventors: 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: 20040152132Abstract: The invention provides solid support synthetic methods for producing combinatorial libraries of modulators of LXRs. The combinatorial libraries thus produced are useful both as diagnostic indicators of LXR&agr; function and as pharmacologically active agents. The combinatorial libraries find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: ApplicationFiled: December 30, 2003Publication date: August 5, 2004Applicants: Tularik Inc., Sumitomo Pharmaceuticals Co., Ltd.Inventors: Julio Medina, Naonori Imazaki
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Publication number: 20040152743Abstract: The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: July 11, 2003Publication date: August 5, 2004Applicant: Aventis Pharma Deutschland GmbHInventors: 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: 20040127487Abstract: An agent comprising the benzoic acid of formula (I) 1Type: ApplicationFiled: December 18, 2003Publication date: July 1, 2004Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama
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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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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
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Publication number: 20040087659Abstract: The invention relates to urea- and urethane-substituted acylureas and to their physiologically tolerated salts and physiologically functional derivatives.Type: ApplicationFiled: July 11, 2003Publication date: May 6, 2004Inventors: Elisabeth Defossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger
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Patent number: 6730807Abstract: Compounds containing carbodiimide units and carboxyl or carboxylate groups (compounds V), derived from a) aliphatic or araliphatic C4 to C20 polyisocyanates (component a) b) amino carboxylic acids or amino carboxylic salts (component b) and c) if desired, further compounds which carry groups able to react with isocyanate groups in an addition reaction (component c) d) if desired, other isocyanates (component d), the carbodiimide units deriving essentially exclusively from the isocyanate groups of component (a).Type: GrantFiled: March 29, 2002Date of Patent: May 4, 2004Assignee: BASF AktiengesellschaftInventors: Karl Häberle, Reinhard Treiber, Christian Lach, Ulrike Licht, Bernd Meyer-Roscher, Peter Weyland
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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
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Publication number: 20040072878Abstract: A 2,3-diphenylpropionic acid derivatives or the salts represented by general formula (1) below; and pharmaceutical compositions and cell adhesion inhibitors comprising the derivatives or the salts as the active ingredient. In the formula, A, B and C independently represents a hydrogen atom or a monovalent substituent; and X and X′ independently represents a hydrogen atom or a monovalent substituent.Type: ApplicationFiled: August 19, 2003Publication date: April 15, 2004Inventors: Yoichiro Hoshina, Satoru Ikegami, Akihiko Okuyama, Tatsuhiro Harada, Atsushi Matsuo
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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
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Patent number: 6706744Abstract: Novel 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 and obesity.Type: GrantFiled: November 16, 2001Date of Patent: March 16, 2004Assignee: Novo Nordisk A/SInventors: Peter Madsen, Jesper Lau, Anthony Ling
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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