Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I), wherein n is 1 or 2; m is 0, 1, 2, 3, or 4; q is 0 or 1; t is 0 or 1; R1 is hydrogen, halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; R2 is alkyl having from 1 to 3 carbon atoms; R3 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; one of R4 and R5 is hydrogen or hydroxy and the other is hydrogen; or R4 and R5 together are ?O; R6 is hydrogen or alkyl having one, two, three, four or five carbon atoms; or a pharmaceutically acceptable salt of the compound. Alternatively, the agent can be a pharmaceutically acceptable salt of the compound of Formula (I).
Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
Type:
Grant
Filed:
October 10, 2007
Date of Patent:
May 24, 2011
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Julian Adams, Mark L. Behnke, Alfredo C. Castro, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Tao Liu, Daniel A. Snyder, Thomas T. Tibbitts
Abstract: Disclosed herein are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with hyperthermia treatment. Also disclosed are methods of treating a proliferative disease, such as cancer, with bis(thio-hydrazide amides) or a tautomer, pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, in combination with radiotherapy.
Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4, R5, R6 and X have defined meanings.
Type:
Grant
Filed:
November 18, 2004
Date of Patent:
April 19, 2011
Inventors:
Dominique Jean-Pierre Mabire, Jérôme Emile Georges Guillemont, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
Abstract: A method of treating a resistant or refractory cancer in a mammal includes administering an effective amount of a compound of to the mammal. In preferred aspects, the cancer is resistant or refractory to CPT-11 or CPT therapy.
Abstract: Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
April 19, 2011
Assignee:
Board of Regents of the University of Texas System
Inventors:
Robert A. Kirken, Barry D. Kahan, Stanislaw M. Stepkowski, Waldemar Priebe, Izabela Fokt, Szymon Kosinski
Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.
Abstract: A method and composition for the treatment of diabetic neuropathy is disclosed. The composition comprises a cold compounded mixture of a compound that promotes synthesis of nerve growth factor, an aldose reductase inhibitor and an antioxidant formulated in a pharmaceutically acceptable carrier. It has been found that this combination of active agents provides significant, effective relief of the symptoms of diabetic neuropathy, as well as at least partial recovery of lost neurological function in some cases. In view of the consensus in the art that effective combinations of various active agents have not been demonstrated to be effective for the treatment of diabetic neuropathy, the present invention provides a surprising and unexpected effect. In addition, the topical compositions of the present invention, when used in effective amounts to treat diabetic neuropathy, do not exhibit the severe side effects of many prior art compositions proposed for treatment of this ailment.
Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
Type:
Grant
Filed:
March 19, 2008
Date of Patent:
March 22, 2011
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Helen E. Blackwell, Grant D. Geske, Jennifer C. O'Neill
Abstract: The present invention provides a combination of antioxidants that effectively stabilize different types of fats utilized in a ruminant diet. When included in a ruminant feed ration or water source, the antioxidant combination typically increases nutrient digestion, such as fiber and protein, improves rumen fermentation, improves microbial growth, improves microbial efficiency, increases milk production and/or milk fat, improves antioxidant status of the ruminant, and attenuates the negative effects of some fats in the ruminant animal.
Abstract: The hair wax product with liquid or creamy consistency for treating or setting up a human hairstyle contains at least 40% by weight of an aqueous or aqueous-alcoholic carrier medium, at least 5 percent by weight of an emulsifier and at least 2 percent by weight of wax. The weight ratio of emulsifier to wax is greater than 1, preferably 1.1 to 4. The invention also includes methods for styling and re-styling human hair-dos or hairstyles using the hair wax product according to the invention.
Type:
Grant
Filed:
July 25, 2003
Date of Patent:
March 15, 2011
Assignee:
Wella AG
Inventors:
Sarah Maillefer, Andre Rehmann, Benedikt Zenhaeusern
Abstract: Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
Type:
Grant
Filed:
April 27, 2005
Date of Patent:
March 15, 2011
Assignee:
Rottapharm S.p.A.
Inventors:
Francesco Makovec, Roberto Artusi, Antonio Giordani, Simona Zanzola, Lucio Claudio Rovati
Abstract: Association comprising agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, in association with a thymoregulatory agent. Medicinal products containing the same which are useful in the treatment of mood disorders.
Abstract: Disclosed is a method for treating PPAR (peroxisome proliferator activated receptor)-mediated diseases, such as diabetes mellitus, which includes administering to a subject an effective amount of macelignan represented by the following Formula (I): or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 27, 2006
Date of Patent:
March 8, 2011
Assignee:
Newtree Co., Ltd.
Inventors:
Jae-Kwan Hwang, Kyu-Lee Han, Jong-Hee Sohn, Ah-Jin Kim, Jeong-Han Choo, Jae-Young Lee, Jeong-Hwan Kim, Do Un Kim, Heechul Chung, Jae Youn Chung
Abstract: A formulation effective in reducing the pH in a menstruating vagina or in a tampon inserted therein to below pH 5.5, comprising (a) 3-100% by weight of glycolide; (b) optionally 97-15% by weight of a solid organic acid; and (c) optionally 5-30% of a wetting agent. Also disclosed is a catamenial tampon for insertion in a human vagina which comprises the pH reducing formulation.
Abstract: An ointment containing a compound represented by formula (I): [wherein R1 represents any group of a group represented by the formula: —(CH2)4—S—CH2—CO2H, a group represented by the formula: —(CH2)4—S—CH2—CO2CH3, a group represented by the formula: —(CH2)4—C?C—CO2H, a group represented by the formula: —CH2—S—(CH2)2—S—CH2—CO2H, and a group represented by the formula: —CH2—S—(CH2)4—CO2H], and an oleaginous base, is an ointment containing a compound which is effective for atopic symptoms, and is an ointment having low skin irritancy and excellent storage stability, thus, can be used as a pharmaceutical product effective for the pruritus caused by atopy or the like.
Abstract: A method of treating organophosphorous (OP) poisoning comprising administering to a mammal at risk for OP poisoning an OP poisoning-inhibiting amount of galantamine.
Type:
Grant
Filed:
September 23, 2005
Date of Patent:
February 15, 2011
Assignee:
Universtiy of Maryland, Baltimore
Inventors:
Edson X. Albuquerque, Michael Adler, Edna F. R. Pereira
Abstract: The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.
Abstract: The invention relates to the delta and epsilon crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide (the compound of formula I, see below), certain processes for their preparation, pharmaceutical compositions containing these crystal forms, and their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.
Abstract: Polyamine macrocyclic compounds, e.g. of 10 to 15 ring members and 3 to 6 ring amine nitrogens, linked through methylene groups to an aromatic moiety, show high selective activity against HIV.
Type:
Grant
Filed:
December 16, 1992
Date of Patent:
February 15, 2011
Assignee:
Genzyme Corporation
Inventors:
Gary J. Bridger, Sreenivasan Padmanbhan, Renato Skerlj, David M. Thornton