Patents Examined by Sun Jae Y Loewe
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Patent number: 7432392Abstract: A therapeutic agent for hyperlipidemia which has no side effects on the liver unlike conventional MTP inhibitors and has excellent MTP inhibitory activity. Also, provided is an ester compound represented by the general formula (1): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 27, 2006Date of Patent: October 7, 2008Assignee: Japan Tobacco Inc.Inventors: Atsushi Hagiwara, Taku Ikenogami, Yasuko Mera, Yukako Sumida, Akio Iida, Toshio Taniguchi, Mitsuru Takahashi
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Patent number: 7423160Abstract: A method of making a metal complex comprises combining a 1-monoacyldipyrromethane with a compound of the formula R1R2MX, wherein M is boron, R1 and R2 are each independently organic substituents; and X is an anion leaving group; to produce a metal complex of the formula DMR1R2 wherein DH is a 1-monoacyldipyrromethane. The methods and complexes are useful for the purification and synthesis of dipyrromethanes and porphyrins.Type: GrantFiled: August 29, 2007Date of Patent: September 9, 2008Assignee: North Carolina State UniversityInventors: Jonathan S. Lindsey, Kannan Muthukumaran, Marcin Ptaszek, H. Z. Syeda Huma
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Patent number: 7417147Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.Type: GrantFiled: November 13, 2006Date of Patent: August 26, 2008Inventor: Nicholas S. Bodor
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Patent number: 7414131Abstract: Amine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: GrantFiled: December 23, 2004Date of Patent: August 19, 2008Assignee: Renovis, Inc.Inventors: Michael G. Kelly, Satyanarayana Janagani, Guoxian Wu, John Kincaid, David Lonergan, YunFeng Fang, Zhi-Liang Wei
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Patent number: 7414141Abstract: There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P1 represents hydrogen or a protecting group, and W represents =0 or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents —OP2, deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents ?O, or compound of formula (6) to ring-opening, and removal of any remaining protectingType: GrantFiled: July 23, 2004Date of Patent: August 19, 2008Assignee: Avecia Pharmaceuticals, Ltd.Inventors: David John Moody, Jonathan Willian Wiffen
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Patent number: 7411072Abstract: The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.Type: GrantFiled: June 13, 2003Date of Patent: August 12, 2008Assignee: Eli Lilly and CompanyInventors: Michael Joseph Coghlan, Jonathan Edward Green, Timothy Alan Grese, Prabhakar Kondaji Jadhav, Donald Paul Matthews, Mitchell Irvin Steinberg, Kevin Robert Fales, Michael Gregory Bell
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Patent number: 7411083Abstract: The present invention relates generally to substituted acetic acid derivatives and methods of using them.Type: GrantFiled: September 23, 2004Date of Patent: August 12, 2008Assignee: WyethInventors: Ariamala Gopalsamy, Scott Lee Kincaid
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Patent number: 7402683Abstract: The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis in illnesses in people or animals, especially diseases of bacterial infection.Type: GrantFiled: April 14, 2003Date of Patent: July 22, 2008Assignee: Bayer HealthCare AGInventors: Nina Brunner, Christoph Freiberg, Thomas Lampe, Ben Newton, Michael Otteneder, Josef Pernerstorfer, Jens Pohlmann, Guido Schiffer, Mitsuyuki Shimada, Niels Svenstrup, Rainer Endermann, Peter Nell
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Patent number: 7402676Abstract: This invention relates to a compound of Formula I, a method for its preparation and its use in the preparation of a compound of Formula II wherein R1, R2, R3, X and n are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein R1, R2, R6, R7, R8 and n are as defined in the disclosure. Also disclosed are certain intermediates of Formula 4 for the preparation of compounds of Formula I wherein X is N and R2, R3 and n are as defined in the disclosure.Type: GrantFiled: April 26, 2007Date of Patent: July 22, 2008Assignee: E.I. du Pont de Nemours and CompanyInventor: John Herbert Freudenberger
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Patent number: 7399869Abstract: Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: May 18, 2006Date of Patent: July 15, 2008Assignee: Genentech, Inc.Inventors: Frederick Cohen, Wayne J. Fairbrother, Clifford Quan, Daniel P. Sutherlin, Beni B. Wolf
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Patent number: 7399861Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.Type: GrantFiled: November 13, 2006Date of Patent: July 15, 2008Inventor: Nicholas S. Bodor
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Patent number: 7396958Abstract: Disclosed are compounds having the general formula (I) as defined herein, the preparation thereof, and the use thereof for the prophylaxis or treatment of any disease involving a dysfunction associated with the orexin 2 receptor such as obesity, appetite or taste disorders including cachexia, anorexia and bulimia, diabetes, metabolic syndromes, vomiting and nausea, depression and anxiety, addictions, mood and behaviour disorders, schizophrenia, sleep disorders, restless legs syndrome, memory learning disorders, sexual and psychosexual dysfunctions, pain, visceral or neuropathic pain, hyperalgesia, allodynia, digestive disorders, irritable bowel syndrome, neuronal degenerescence, ischaemic or haemorrhagic attacks, Cushing's disease, Guillain-Barré syndrome, myotonic dystrophy, urinary incontinence, hyperthyroidism, pituitary function disorders, hypertension or hypotension.Type: GrantFiled: February 2, 2007Date of Patent: July 8, 2008Assignee: Sanofi AventisInventors: Gilles Courtemanche, Pierre Despeyroux, Evelyne Fontaine, Pierrick Rochard, Claudine Serradeil-Le Gal
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Patent number: 7393960Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.Type: GrantFiled: August 28, 2003Date of Patent: July 1, 2008Assignee: Merck & Co., Inc.Inventors: John J. Acton, III, Peter T. Meinke, Harold B. Wood, Regina M. Black
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Patent number: 7385073Abstract: A process for reducing the level of an aliphatic monounsaturated amine (IV) in a mixture (V) containing an aminonitrile (I) or a diamine (II) or a dinitrile (III) or mixtures thereof as well as said mine (IV) by a) reacting said mixture (V) with an anionic nucleophile (VI) which contains a nucleophilic atom selected from the group consisting of oxygen, nitrogen and sulfur, which is capable of taking up an H+ ion to form an acid having a pKa value in the range from 7 to 11, as measured in water at 25° C., and which has a relative nucleophilicity, as measured in methyl perchlorate/methanol at 25° C., in the range from 3.4 to 4.7 when said nucleophilic atom is oxygen, in the range from 4.5 to 5.8 when said nucleophilic atom is nitrogen, and in the range from 5.5 to 6.8 when said nucleophilic atom is sulfur, in an amount in the range from 0.01 to 10 mol per mole of said amine (IV) in said mixture (V) at a temperature in the range from 50 to 200° C.Type: GrantFiled: May 21, 2003Date of Patent: June 10, 2008Assignee: BASF AktiengesellschaftInventors: Stefan Maixner, Christoph Benisch, Hermann Luyken, Peter Baβler, Rolf-Hartmuth Fischer, Johann-Peter Melder, Andreas Ansmann
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Patent number: 7378532Abstract: A fused pyrazolyl compound of the following formula: wherein A, Ar1, Ar2, R1, R2, R3, and R4, are as defined herein. Also disclosed is a pharmaceutical composition containing an effective amount of the above-described fused pyrazolyl compound.Type: GrantFiled: November 29, 2004Date of Patent: May 27, 2008Assignee: Yung Shin Pharmaceutical Ind. Co., Ltd.Inventors: Sheng-Chu Kuo, Fang-Yu Lee, Che-Ming Teng, Li-Jiau Huang, Li-Chen Chou, Jih-Hwa Guh, Shiow-Lin Pan
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Patent number: 7375237Abstract: Pyrrolizine compounds having the formula (I), or pharmaceutically-acceptable salts thereof, are effective in treating inflammatory or immune diseases, where A is a four- to seven-membered saturated ring, K is O or S, and R1, R2, R3 n, and M are defined in the specification.Type: GrantFiled: August 18, 2005Date of Patent: May 20, 2008Assignees: Bristol-Myers Squibb Company, Cerep SAInventors: T. G. Murali Dhar, Dharmpal S. Dodd, Dominique Potin, Michele Launay
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Patent number: 7368578Abstract: The present invention provides a compound represented by the formula: wherein R1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is —(CH2)n-Z1- or -Z1-(CH2)n— (n is an integer of 0 to 8, Z1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R2 is a hydrogen atom, a cyano group, —PO(OR9)(OR10) (R9 and R10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R9 and R10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic actiType: GrantFiled: September 9, 2003Date of Patent: May 6, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Yu Momose, Nobuyuki Takakura, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
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Patent number: 7365225Abstract: The present invention is related to aryl dicarboxamides 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, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs.Type: GrantFiled: July 20, 2004Date of Patent: April 29, 2008Assignee: Laboratoires Serono SAInventors: Russel J. Thomas, Dominique Swinnen, Jean-Francois Pons, Agnes Bombrun
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Patent number: 7358370Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: GrantFiled: February 27, 2006Date of Patent: April 15, 2008Assignee: Serenex, Inc.Inventors: Kenneth He Huang, Jeron Eaves, Gunnar J. Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
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Patent number: 7351823Abstract: The present invention relates to a process for preparing 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide starting from 2-[(2S)-2-oxiranylmethyl]-1H-isoindole-1,3(2H)-dione, 4-(4-aminophenyl)-3-morpholinone and 5-chlorothiophene-2-carbonyl chloride.Type: GrantFiled: January 10, 2005Date of Patent: April 1, 2008Assignee: Bayer HealthCare AGInventors: Mathias Berwe, Christian Thomas, Joachim Rehse, Dirk Grotjohann