Nitrogen Patents (Class 562/430)
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Patent number: 7638556Abstract: A method for the preparation of a freeze-dried product of N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate dissolved in a mixed solvent of water and ethanol, and the freeze-dried product obtained by the method. According to the present invention, N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate is dissolved in a small amount of a mixed solvent of water and ethanol, and therefore it is possible to manufacture high-dosage product by freeze-drying.Type: GrantFiled: April 26, 2007Date of Patent: December 29, 2009Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Takada, Masao Sudo
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Publication number: 20090312328Abstract: [Object] A compound that can be used as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom. [Means for Solution] It was confirmed that a sulfonamide compound having an amide structure and characterized by a chemical structure in which a carbon atom in the amide bonds to the N atom in sulfonamide through lower alkylene, or a salt thereof, has a potent EP1 receptor antagonistic activity, accomplishing the present invention. Since the sulfonamide compound of the present invention or a pharmaceutically acceptable salt thereof has a potent EP1 receptor antagonistic activity, it is useful as an agent for treating a disease associated with an EP1 receptor, in particular, a lower urinary tract symptom.Type: ApplicationFiled: August 9, 2007Publication date: December 17, 2009Applicant: Astellas Pharma Inc.Inventors: Hideki Kubota, Susumu Toda, Issei Tsukamoto, Yuta Fukuda, Ryutaro Wakayama, Kazuki Ono, Toru Watanabe, Hidenori Azami
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Publication number: 20090275659Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: ApplicationFiled: December 18, 2008Publication date: November 5, 2009Applicant: Amgen Inc.Inventors: Mark Grillo, An-Rong Li, Jiwen Liu, Julio C. Medina, Yongli Su, Yingcai Wang, Janan Jona, Alan Allgeier, Jacqueline Milne, Jerry Murry, Joseph F. Payack, Thomas Storz
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Patent number: 7601729Abstract: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH?CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1? each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl;Type: GrantFiled: September 10, 2004Date of Patent: October 13, 2009Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Patent number: 7541383Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: GrantFiled: November 26, 2007Date of Patent: June 2, 2009Assignee: Amgen Inc.Inventors: Zice Fu, Xi Alan Huang, Jiwen Liu, Julio C. Medina, Michael J. Schmitt, H. Lucy Tang, Yingcai Wang, Qingge Xu
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Publication number: 20090124828Abstract: ?,?-Unsaturated sulfides, sulfones, sulfoxides and sulfonamides according to Formula I: wherein Ar1, Ar2, X, n, * and R are as defined herein, are prepared by dehydration of ?-hydroxy sulfides, sulfones, sulfoxides or sulfonamides.Type: ApplicationFiled: February 24, 2006Publication date: May 14, 2009Applicants: TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION, ONCONOVA THERAPEUTICS INC.Inventors: M.V. Ramana Reddy, E. Premkumer Reddy, Stanley C. Bell
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Publication number: 20090069428Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substrates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.Type: ApplicationFiled: August 4, 2008Publication date: March 12, 2009Inventors: Herbert Weissbach, Nathan Brot
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Patent number: 7488844Abstract: The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.Type: GrantFiled: December 30, 2004Date of Patent: February 10, 2009Assignee: AstraZeneca ABInventors: Eva-Lotte Lindstedt Alstermark, Anna Christina Olsson, Lanna Li
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Publication number: 20090029903Abstract: The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.Type: ApplicationFiled: March 29, 2005Publication date: January 29, 2009Inventors: Dominique Swinnen, Catherine Jorand-Lebrun, Patrick Gerber, Jerome Gonzalez, Agnes Bombrun
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Patent number: 7482484Abstract: Disclosed are Compounds of formula I And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.Type: GrantFiled: December 16, 2003Date of Patent: January 27, 2009Assignee: Merck Patent GmbHInventors: Nathalie Adje, Michel Brunet, Didier Roche, Jean-Jacques Zeiller, Stéphane Yvon, Valérie Guyard-Dangremont, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
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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: 20080275114Abstract: Compounds of formula (I), in which R1 and R2 are independently a substituted phenyl group, where the substituents are as defined in the claims and with the proviso that at least one of the substituents is a cyano, carboxy or (C1-4)alkoxycarbonyl group, are inhibitors of CCR9 activity useful for therapeutic treatment, particularly of irritable bowel disease.Type: ApplicationFiled: December 22, 2006Publication date: November 6, 2008Inventors: Jose M. Carballido Herrera, Herbert Jaksche, Philipp Lehr, Gudrun Werner, Anthony Winiski
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Publication number: 20080262086Abstract: Disclosed herein are substituted anthranilic acids, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of hypertension, edema associated with congestive heart failure, hepatic disease, renal disease including nephrotic syndrome, or clearance of toxic substances from the body.Type: ApplicationFiled: April 18, 2008Publication date: October 23, 2008Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20080261981Abstract: Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treating related disorders such as body weight gain, elevated free fatty acid, cholesterol and triglyceride levels and other disorder exacerbated by obesity.Type: ApplicationFiled: June 3, 2008Publication date: October 23, 2008Inventors: DEBENDRANATH DEY, Abjiheet Nag, Bindu Pandey, Preeti Balse, Partha Neogi, Bishwajit Nag
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Patent number: 7429677Abstract: The present invention concerns a compound having the formula (I) a N-oxide form, a stereochemical isomer, racemic mixture, salt, prodrug, ester or metabolite thereof. It further relates to processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.Type: GrantFiled: March 11, 2003Date of Patent: September 30, 2008Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Marie-Pierre T. M. M. G De Bethune, Sandra De Meyer, Kurt Hertogs, Rong Jian Lu, Lieve Emma Jan Michiels, Abdellah Tahri, Dong Xie, Michael Eissenstat
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Publication number: 20080227858Abstract: Compounds of formula (I): wherein R1 represents optionally substituted C4-12 alkyl, optionally substituted C2-6alkylaryl, or optionally substituted 5- or 6-membered aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR4, OCR4R5, CR4R5O, or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents COR3 or N(OR8)COR9; R2 represents SO2R10 or SO2NR10R11; R3 represents OR6NR6R7 or NR6OH; R4 and R5 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R6 and R7 each independently represents H, C1-6 alkyl, or C1-6 alkyl substituted with one or more heteroaryl groups, or R6 and R7 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; R8 and R9 each independently represents H or C1-6 alkyl; R10 and R11 each independently represents H or C1-6 alkyl; and and physiologicType: ApplicationFiled: May 19, 2008Publication date: September 18, 2008Inventors: Ian Holmes, Stephen Paul Watson
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Publication number: 20080227684Abstract: The present invention relates to compositions for use in the modulation of PDZ domain interactions with cognate ligands. Methods of assessing and characterizing PDZ domain interactions from various polypeptides also are provided.Type: ApplicationFiled: December 29, 2006Publication date: September 18, 2008Inventors: MICHAEL P. BELMARES, Peter S. Lu, Kenneth A. Mendoza
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Patent number: 7417164Abstract: A novel class of compounds that includes HPTS-Cys-MA, and methods of making them are disclosed herein. The class of compounds including HPTS-Cys-MA are useful as fluorescent dyes for analyte detection.Type: GrantFiled: July 24, 2007Date of Patent: August 26, 2008Assignee: Glumetrics Inc.Inventor: Jeff T. Suri
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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: 7388008Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: August 2, 2004Date of Patent: June 17, 2008Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valérie Perron
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Patent number: 7375248Abstract: Compounds of formula (I): wherein R1 represents optionally substituted C4-12 alkyl, optionally substituted C2-6alkylaryl, or optionally substituted 5- or 6-membered aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR4, OCR4R5, CR4R5O, or Z, R1 and Q together form an optionally substituted fused tricyclic group; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents COR3 or N(OR8)COR9; R2 represents SO2R10 or SO2NR10R11; R3 represents OR6, NR6R7 or NR6OH; R4 and R5 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R6 and R7 each independently represents H, C1-6 alkyl, or C1-6 alkyl substituted with one or more heteroaryl groups, or R6 and R7 together with the nitrogen atom to which they are attached form a 5- or 6-membered ring which may optionally include 1 or more further heteroatoms selected from O, S and N; R8 and R9 each independently represents H or C1-6 alkyl; R10 and R11 each independently represents H or C1-6 alkyl; and and physioloType: GrantFiled: June 16, 2004Date of Patent: May 20, 2008Assignee: Glaxo Group LimitedInventors: Ian Holmes, Stephen Paul Watson
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Patent number: 7371888Abstract: Compounds having a formula: or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders.Type: GrantFiled: February 17, 2005Date of Patent: May 13, 2008Assignee: Metabolex, Inc.Inventors: Zuchun Zhao, Xin Chen, Jianchao Wang, Hongbin Sun, Jack Shih-Chieh Liang
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Publication number: 20080096922Abstract: A compound of the formula (1): wherein m, n and p is independently an integer of 0 to 4 with the proviso that 3?m+n?8; X is the formula: NR4, etc.; R1, R3 and R4 are a substituted or unsubstituted aryl group, etc.; R2 is a hydrogen atom, etc.; a, b, c, d, e and f are a hydrogen atom or a substituted or unsubstituted alkyl group, etc.; Y is the formula: —SO2—, etc.; and Z is an oxygen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt of the same has an activity of potentiating an expression of a low density lipoprotein receptor and thus is useful as an agent for treating hyperlipidemia or arteriosclerosis.Type: ApplicationFiled: April 4, 2005Publication date: April 24, 2008Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Hitoshi Ban, Shigehiro Asano
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Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
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Patent number: 7342127Abstract: Novel thyroid receptor ligands are provided having the general formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: January 23, 2004Date of Patent: March 11, 2008Assignees: Bristol-Myers Squibb Company, Karo Bio ABInventors: William N. Washburn, Wei Meng, Denis E. Ryono, Bruce A. Ellsworth, Thomas Ericsson, Mahmoud Rahimi-Ghadim, Neeraj Garg, Johan Malm
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Patent number: 7321001Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: GrantFiled: December 19, 2003Date of Patent: January 22, 2008Assignee: Amgen Inc.Inventors: Zice Fu, Xi Alan Huang, Jiwen Liu, Julio C. Medina, Michael J. Schmitt, H. Lucy Tang, Yingcai Wang, Qingge Xu
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Patent number: 7297817Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: April 12, 2005Date of Patent: November 20, 2007Assignees: Cephalon France, Cephalon, Inc.Inventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
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Patent number: 7268135Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: December 1, 2004Date of Patent: September 11, 2007Assignee: WyethInventors: Jason Shaoyun Xiang, Steve Yikkai Tam, Yonghan Hu, Phaik-Eng Sum, David Brian How, Darrin William Hopper, Matthew Douglas Vera, Joshua James Sabatini, Thomas Saltmarsh Rush, III
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Patent number: 7262317Abstract: A method for the preparation of a freeze-dried product of N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate dissolved in a mixed solvent of water and ethanol, and the freeze-dried product obtained by the method. According to the present invention, N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate is dissolved in a small amount of a mixed solvent of water and ethanol, and therefore it is possible to manufacture high-dosage product by freeze-drying.Type: GrantFiled: July 23, 2001Date of Patent: August 28, 2007Assignee: Ono Pharmaceuticals Co., Ltd.Inventors: Akira Takada, Masao Sudo
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Patent number: 7250439Abstract: Compounds of formula (I): wherein: Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, NR5 or CR6 R7; Y represents CHOH, CHSH, NOR8, CNR8 or CNOR8; Z represents a bond, CR10R11, O, S, SO, SO2, NR10, OCR10R11, CR10R11 O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R1, R1?, R3 and R3? each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R2 represents CO2R8, CONR5OR9 or NR5COR9; R4 represents optionally substituted 5- or 6-membered aryl or heteroaryl; R5 represents H or C1-3 alkyl; R6 and R7 each independently represents H, C1-3 alkyl or halo; R8 represents H or C1-2 alkyl; R9 represents H or C1-3 alkyl; R10 and R11 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metalloproteinase enzymes (MMPs) are described.Type: GrantFiled: June 1, 2004Date of Patent: July 31, 2007Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Paul Watson
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Patent number: 7199158Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7?, R8, R30–R34, X?, Y, Y?, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 18, 2005Date of Patent: April 3, 2007Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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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: 7193108Abstract: Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning ? 4 integrin, such as inflammatory diseases in which ? 4 integrin-depending adhesion process participates in the pathology, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.Type: GrantFiled: January 26, 2004Date of Patent: March 20, 2007Assignee: Ajinomoto Co., Inc.Inventors: Akira Chiba, Kazuyuki Sagi, Toshihiko Yoshimura, Tatsuya Okuzumi, Hiroyuki Izawa, Masahiro Murata
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7153869Abstract: This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 12, 2004Date of Patent: December 26, 2006Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 7071358Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: July 4, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7064229Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseasesType: GrantFiled: June 24, 2002Date of Patent: June 20, 2006Assignee: Bayer Healthcare AGInventors: Thomas Rolle, Thomas Lehmann, Markus Albers, Gerhard Muller, Gerhard Hessler, Rudiger Fischer, Masaomi Tajimi, Karl Ziegelbauer, Kevin Bacon, Haruki Hasegawa, Hiromi Okigami
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Patent number: 7056903Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.Type: GrantFiled: May 9, 2003Date of Patent: June 6, 2006Assignee: Syntex (U.S.A.) LLCInventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
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Patent number: 7022851Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein R1, R2, R3, R4, R5 is independently H, halogen, C1–C4 alkyl, nitro, nitrile, C1–C4 alkoxy, halogenated C1–C4 alkyl, or halogenated C1–C4 alkoxy, wherein at least one of R1, R3, and R5 is nitro; R6 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases.Type: GrantFiled: January 24, 2003Date of Patent: April 4, 2006Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee
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Patent number: 6974828Abstract: 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: GrantFiled: April 19, 2001Date of Patent: December 13, 2005Assignee: Pharmacia Italia S.p.A.Inventors: Tiziano Bandiera, Paola Vianello, Paolo Cozzi, Arturo Galvani
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Patent number: 6951886Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors and in particular as inhibitors of HIV protease.Type: GrantFiled: December 10, 2002Date of Patent: October 4, 2005Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6919375Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: July 22, 1998Date of Patent: July 19, 2005Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Wantanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6919369Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: August 19, 2002Date of Patent: July 19, 2005Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
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Patent number: 6890942Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.Type: GrantFiled: May 5, 2004Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
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Patent number: 6887877Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.Type: GrantFiled: June 11, 2002Date of Patent: May 3, 2005Assignee: ViroChem Pharma Inc.Inventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Stephen Joseph Shuttleworth, Mohammad Arshad Siddiqui, Wuyi Wang
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Patent number: 6887903Abstract: The compounds of formula 1 wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.Type: GrantFiled: October 14, 1999Date of Patent: May 3, 2005Assignee: Dompe S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Gianfranco Caselli, Marcello Allegretti, Maria Candida Cesta, Carmelo Gandolfi, Marco Mantovanini, Francesco Colotta, Stefano Porzio
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Patent number: 6884907Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: May 10, 2002Date of Patent: April 26, 2005Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
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Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6881727Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: July 3, 2002Date of Patent: April 19, 2005Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6875765Abstract: The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1? converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized structure: and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis, using a compound of the invention or a pharmaceutical composition thereof, are described.Type: GrantFiled: May 10, 2002Date of Patent: April 5, 2005Assignee: Warner-Lambert CompanyInventors: James Knobelsdorf, Sheryl Hays, Charles J. Stankovic, Kimberly S. Para, Michael K. Connolly, Paul Galatsis, William Harter, Aurash B. Shahripour, Mark Stephen Plummer, Beth Lunney, Bernd Janssen, Jay Bradford Fell