Abstract: The present invention is phthalocyanine compounds with peripheral siloxane substitution, as well as methods for making these compounds and various uses thereof, having the basic structure: wherein —W—X—Y-Z are peripheral groups comprising individual W, X, Y, and Z subgroups; W is a linkage represented by the formula: -D-(R1)0,1—, where D=S or O; X is: —(CH2)n—, n=2 to 8; Y is a siloxane chain; Z is an aryl or alkyl terminal cap; M is two protons or a metal ion; and forms a transparent film of high optical quality with large nonlinear absorption and thermal refraction, free of scattering from solid or liquid crystalline domains making them highly suitable for use as the active component in thin films, protective eye wear, and optical data storage applications.
Type:
Grant
Filed:
September 25, 2002
Date of Patent:
August 23, 2005
Assignee:
The United States of America as represented by the Secretary of the Navy
Inventors:
Arthur W. Snow, James S Shirk, Eva M Maya, Richard G. S. Pong, Steven R. Flom
Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.
Type:
Grant
Filed:
August 13, 2002
Date of Patent:
August 16, 2005
Assignee:
Nitromed, Inc.
Inventors:
David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p??(1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH??(2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX??(3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.
Abstract: Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.
Type:
Grant
Filed:
January 14, 2000
Date of Patent:
August 9, 2005
Assignee:
Novo Nordisk A/S
Inventors:
Min Teng, Larry Kenneth Truesdale, Dilip Bhumralkar, Dan Kiel, Michael D. Johnson, Christine Thomas, Anker Steen Jorgensen, Peter Madsen, Preben Houlberg Olesen, Liselotte Bjerre Knudsen, Ingrid Vivika Petterson, Johannes Cornelis de Jong, Carsten Behrens, Janos Tibor Kodra, Jesper Lau
Abstract: The invention provides dicarboxylic acid-substituted heteroaryl derivatives of the formula G1-(C(R1)R2)n-Q1-B-Q2-(C(R3)R4)m-G2??I or a pharmaceutically acceptable salt thereof, wherein G1, G2, R1, R2, R3, R4, n, m, Q1, Q2, and B are as defined in the specification. The invention compounds are inhibitors of matrix metalloproteinase enzymes, including MMP-13. This invention also provides pharmaceutical compositions and methods of treating diseases mediated by MMP-13, including arthritis, asthma, heart disease, atherosclerosis, and osteoporosis, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to compounds of the general formula: NO2-A-B wherein A is a saturated or unsaturated hydrocarbon chain of 14-26 carbon atoms and B is (CH2)n(COOH)m in which n is an integer from 0 to 2 and m is an integer from 0 to 2; or of general formula (I), wherein A? is a saturated or unsaturated hydrocarbon chain of 9-26 carbon atoms, X is oxygen or is absent and B? is (CH2)j(COOH)k in which j is an integer from 1 to 3 and k is 0 or 1; and the derivatives thereof in which the hydrocarbon chain includes one or more than one substitution selected from the group consisting of hydroxy, hydroperoxy, epoxy and peroxy. These compounds have biological activity, e.g. as anti-infective or anti-inflammatory agents.
Type:
Grant
Filed:
March 18, 2002
Date of Patent:
August 2, 2005
Assignees:
Children, Youth and Women's Health Service Incorporated, Peptech Limited
Inventors:
Antonio Ferrante, Christopher J. Easton, Ling Xia
Abstract: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.
Type:
Grant
Filed:
February 21, 2003
Date of Patent:
August 2, 2005
Assignee:
Pfizer Inc.
Inventors:
Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be replaced; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.
Type:
Grant
Filed:
June 20, 2000
Date of Patent:
August 2, 2005
Assignee:
Janssen Pharmacatica, N.V.
Inventors:
Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
Type:
Grant
Filed:
January 23, 2003
Date of Patent:
August 2, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Dhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Chunguang Wang, Hans Pluempe, Achim Feurer, Samir Bennabi
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
Abstract: The invention relates to substituted tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid trans: protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease.
Type:
Grant
Filed:
December 23, 2002
Date of Patent:
August 2, 2005
Assignee:
Pfizer Inc.
Inventors:
James A. Sikorski, Richard C. Durley, Melvin L. Rueppel, Deborah A. Mischke, Barry L. Parnas
Abstract: There is provided a preventive or therapeutic agent for diseases accompanied by abnormal vascular function in which lipid deposition in the blood vessel is involved, said agent comprising a chymase inhibitor as an active ingredient. As the chymase inhibitor, a quinazoline derivative represented by the following formula is used. In the above formula, the ring A represents an aromatic ring.
Abstract: The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts.
Type:
Grant
Filed:
June 9, 2003
Date of Patent:
July 26, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Hans-Christian Militzer, Boris Bosch, Markus Eckert, Benjamin Meseguer
Abstract: 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:
Grant
Filed:
August 19, 2002
Date of Patent:
July 19, 2005
Assignee:
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
Abstract: Compounds of the formula wherein X1 is C(O), —S(O)—, or —S(O)2—; X2 is CR3 or N; X3 is —NH—, —O—, or —S—; X4 is CR4 or N; X5 is CR5 or N; and X6 is CR6 or N are useful as inhibitors of IMPDH enzyme. Thus, these compounds can be used as therapeutic agents for IMPDH-associated disorders.
Type:
Grant
Filed:
April 23, 2001
Date of Patent:
July 19, 2005
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Edwin J. Iwanowicz, Scott H. Watterson, T. G. Murali Dhar, William J. Pitts, Henry H. Gu
Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.
Type:
Grant
Filed:
December 3, 2002
Date of Patent:
July 19, 2005
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jiacheng Zhou, Lynette M. Oh, Philip Ma, Hui-Yin Li, Pasquale Confalone
Abstract: The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl m
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
July 12, 2005
Assignee:
OSI Pharmaceuticals, Inc.
Inventors:
Arlindo Castelhano, Bryan McKibben, Arno Steinig, Eric Collington
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.