The Hetero Ring Is Five-membered Patents (Class 514/461)
  • Patent number: 7410999
    Abstract: The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure according to Formulas (I)-(VI) as recited throughout the application.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: August 12, 2008
    Assignees: University of North Carolinia at Chapel Hill, Georgia State University Research Foundation, Inc., Auburn University
    Inventors: Christine C. Dykstra, Maurice Daniel Givens, David A. Stringfellow, Kenny Brock, David Boykin, Arvid Kumar, W. David Wilson, Richard R. Tidwell, Chad F. Stephens
  • Publication number: 20080188528
    Abstract: Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.
    Type: Application
    Filed: December 21, 2007
    Publication date: August 7, 2008
    Inventors: Ronald J. Biediger, Huong M. Bui, Jie Chen, Kevin M. Henry, Thomas Thrash
  • Patent number: 7407989
    Abstract: There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R1, R2 and R3 are each independently selected from OH, C1-6alkyl, OC1-6alkyl, OC(O)C1-6alkyl, C(O)OC1-6alkyl, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), C(O)NHC1-6alkyl, C(O)N(C1-6alkyl)(C1-6alkyl), SH, SC1-6alkyl, NO2, CF3, OCF3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1-4 substituents independently selected from OH, C1-6alkyl, C1-6alkoxy, C1-3alkylenedioxy, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), SH, S—C1-6alkyl, NO2, CF3, OCF3 and halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: August 5, 2008
    Assignee: The Hospital for Sick Children
    Inventors: Chaim Roifman, Peter Demin, Olga Rounova, Tom Grunberger
  • Patent number: 7405311
    Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
    Type: Grant
    Filed: March 28, 2007
    Date of Patent: July 29, 2008
    Assignee: Magnesium Diagnostics, Inc.
    Inventor: Ibert Clifton Wells
  • Publication number: 20080176912
    Abstract: The invention is directed to compounds of Formula (I) useful as GPR40 agonists. Pharmaceutical compositions and methods of treating one or more conditions including, but not limited to, insulin resistance, hyperglycemia, obesity, diabetes such as NIDDM, and other disorders related to lipid metabolism, energy homeostasis, and complications thereof, using compounds of the invention are also described.
    Type: Application
    Filed: November 13, 2007
    Publication date: July 24, 2008
    Inventors: Gee-Hong Kuo, Fengbin Song, Joseph Gunnet, Keith Demarest
  • Publication number: 20080171757
    Abstract: The invention relates to methods of screening for inhibitors of diseases or biological processes that involve peptide or protein polymerization. Included in the methods of the invention are methods to identify inhibitors of deoxyhemoglobin S polymerization. Also included in the invention are diagnostic and therapeutic methods.
    Type: Application
    Filed: January 11, 2007
    Publication date: July 17, 2008
    Applicant: Government of the US, as represented by the Secretary, Department of Health and Human Serivces
    Inventors: William A. Eaton, H. J. Hofrichter, Jeffrey F. Smith
  • Publication number: 20080167331
    Abstract: The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.
    Type: Application
    Filed: March 14, 2008
    Publication date: July 10, 2008
    Inventor: Robert M. Burk
  • Patent number: 7396843
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: July 8, 2008
    Assignee: Glaxo Group Limited
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Suzanne Joy Merrick, Ann Louise Walker
  • Patent number: 7393846
    Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: July 1, 2008
    Assignee: Glenmark Pharmaceuticals, S.A.
    Inventors: Balasubramanian Gopalan, Laxmikant Atmaram Gharat, Aftab Dawoodbhai Lakdawala, Usha Karunakaran
  • Publication number: 20080146659
    Abstract: Drugs containing Taxiresinol, (7?R)-7?-Hydroxylariciresinol, Secoisolariciresinol and Isotaxiresinol, which are lignans contained in Hongdoushan, as the active ingredients. Drugs containing an extract, which is obtained by extracting a Hongdoushan plant with water and further extracting the obtained extract with an organic solvent, as the active ingredient. These drugs are useful particularly as a hypoglycemic agent, a liver protecting agent and an anticancer agent.
    Type: Application
    Filed: February 8, 2008
    Publication date: June 19, 2008
    Applicant: KOTOSUGI INC.
    Inventors: Shigetoshi Kadota, Takahiro Nobukawa
  • Publication number: 20080146624
    Abstract: The present invention is directed to amidino heterocyclic compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Application
    Filed: September 18, 2007
    Publication date: June 19, 2008
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Eddy Wai Tsun Yue
  • Publication number: 20080146622
    Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.
    Type: Application
    Filed: December 23, 2004
    Publication date: June 19, 2008
    Applicant: SRZ Properties, Inc.
    Inventor: Dieter Scheller
  • Publication number: 20080139599
    Abstract: Compounds of the formula (1) in which R1, R2,X, Y and Z are as defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.
    Type: Application
    Filed: December 22, 2005
    Publication date: June 12, 2008
    Inventors: Michel Brunet, Nathalie Adje, Valerie Guyard-Dangremont, Francis Contard
  • Patent number: 7384962
    Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: June 10, 2008
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Balasubramanian Gopalan, Laxmikant Atmaram Gharat, Aftab Dawoodbhai Lakdawala, Usha Karunakaran
  • Patent number: 7378529
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: January 10, 2005
    Date of Patent: May 27, 2008
    Assignee: Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
  • Patent number: 7371396
    Abstract: The present invention relates to a dermatological and/or cosmetic composition comprising a furfuryl derivative of formula (I), and its use in the treatment of dermatological disorders especially when caused by free radicals.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: May 13, 2008
    Assignee: Relivia SRL
    Inventor: Carlo Ghisalberti
  • Patent number: 7371777
    Abstract: The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. Wherein a, b and c are the same as or different from one another and each represents 0 to 4; R1 to R6 are the same as or different from one another and each represents a hydrogen atom, a hydroxyl group, a cyano group, a halogen atom, etc.; A1 and A2 are the same as or different from each other and each represents a single bond, an oxygen atom, etc.; L, M and T each represent a single bond, an alkylene group having one to six carbon atoms, etc.; W represents a carboxyl group; the partial structure represented by the formula: represents a single bond or a double bond; X represents a single bond, an oxygen atom, —NRx1CQ1O—, etc.; Y represents Y1—Y2— (wherein Y1 represents a 5 to 14-membered aromatic ring having one to four substituents, etc.
    Type: Grant
    Filed: August 16, 2002
    Date of Patent: May 13, 2008
    Assignee: Eisai Co., Ltd.
    Inventors: Richard Clark, Fumiyoshi Matsuura, Eita Emori, Masanobu Shinoda, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Takashi Inoue, Sadakazu Miyashita, Taro Hihara
  • Patent number: 7368475
    Abstract: The synthesis and study of biological activity of a series of new molecules with potential antimicrobial activity are described. The molecules are bicyclic carbohydrates, based on furanose sugars. Their antimicrobial activity against viruses is demonstrated, next to cytostatic effects. Significantly, a high and selective activity against Cytomegalovirus was observed.
    Type: Grant
    Filed: January 20, 2004
    Date of Patent: May 6, 2008
    Assignee: Kemin Pharma BVBA
    Inventors: Benedikt Sas, Johan Van hemel, Jan Vandenkerckhove, Eric Peys, Johan Van der Eycken, Steven Van Hoof
  • Patent number: 7365089
    Abstract: The present invention relates to adenosine A3? receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and theirs salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and to the preparation thereof.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: April 29, 2008
    Assignee: Sanofi-Aventis
    Inventors: Peter Aranyi, Laszlo Balazs, Sandor Batori, Judit Bence, Kinga Boer, Felix Hajdu, Zoltan Kapui, Endre Mikus, Tibor Szabo, Lajos T. Nagy, Geza Timari, Katalin Urban-Szabo, Erzsebet Walcz
  • Patent number: 7361679
    Abstract: The present invention relates to a 2-phenyl-3-heteroarylpropionic acid derivative or a salt thereof, and also relates to a pharmaceutical agent and a VLA-4 and/or LPAM-1 antagonist each of which contains the same as an active ingredient.
    Type: Grant
    Filed: September 3, 2002
    Date of Patent: April 22, 2008
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Satoru Ikegami, Yoichiro Hoshina
  • Publication number: 20080090900
    Abstract: This invention describes a new antibiotic, hereinafter designated as bushrin, having the formula C16H16O2, which is 7-(3-furyl)-3,7-dimethyl-7,8-dihydro-1-naphthalenol, its production method by fermentation, and the methods related to its recovery, concentration and purification from the crude solutions. The invention includes within its scope the agent in dilute form, as a crude concentrate, and in pure form. The invention also relates to the use of the compound according to the invention in antimicrobial compositions and as antiseptics or disinfectants.
    Type: Application
    Filed: October 12, 2006
    Publication date: April 17, 2008
    Applicant: University of Karachi
    Inventors: Nuzhat Ahmed, Bushra Uzair, Viqar Uddin Ahmad, Farzana Kousar
  • Patent number: 7354604
    Abstract: An aqueous disinfecting solution and dry powdered composition which may be dissolved in water to provide the solution. The solution has a pH of from 0.6 to 7 and comprises (a) hydrogen peroxide in a concentration of from 0.01 to 6% w/w; and (b) at least one component chosen from cyclic carboxylic acids and aromatic alcohols, in a concentration of from 0.01 to 4 w/w %, all based on the total weight of the solution. The cyclic carboxylic acids are preferably 2-furan carboxylic acid, benzoic acid and salicylic acid. Furthermore, the solution preferably contains at least one C6-C12 alkyl diphenyl oxide sulfonate surfactant and a nonionic surfactant. Additional optional ingredients include anionic surfactants, corrosion inhibitors, cation sequestering agents, and buffers.
    Type: Grant
    Filed: November 17, 2003
    Date of Patent: April 8, 2008
    Assignee: Virox Technologies Inc.
    Inventors: Jose A. Ramirez, Navid Omidbakhsh
  • Patent number: 7335673
    Abstract: 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.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: February 26, 2008
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Yoichiro Hoshina, Satoru Ikegami, Akihiko Okuyama, Tatsuhiro Harada, Atsushi Matsuo
  • Patent number: 7332518
    Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH?CHR2, CH?C?CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7cycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.
    Type: Grant
    Filed: January 24, 2002
    Date of Patent: February 19, 2008
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Harald Walter, Stephan Trah
  • Publication number: 20080015219
    Abstract: Disclosed and described herein are compounds of the formula or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed and described.
    Type: Application
    Filed: May 14, 2007
    Publication date: January 17, 2008
    Inventors: DAVID W. OLD, VINH X. NGO
  • Patent number: 7317039
    Abstract: The invention concerns deuterated substituted dihydrofuranones and pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated substituted dihydrofuranones for the treatment of symptoms for the irritating states of degenerative joint disorders, of acute pain and primary dysmenorrhea. In addition, the invention discloses pharmaceutical compositions, which contain deuterated substituted dihydrofuranones as well as their physiologically compatible salts, in addition to pharmaceutically compatible adjuvants and/or additives, for the treatment of symptoms for the irritating states of degenerative joint disorders, of acute pain and primary dysmenorrhea.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: January 8, 2008
    Assignee: BDD Berolina Drug Development GmbH
    Inventor: Rudolf-Giesbert Alken
  • Patent number: 7317125
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
    Type: Grant
    Filed: January 31, 2006
    Date of Patent: January 8, 2008
    Assignee: Hoffman-La Roche Inc.
    Inventors: David Robert Bolin, Christophe Michoud
  • Publication number: 20070293565
    Abstract: An ester compound represented by the formula (I): has excellent pest controlling activity and is useful as an active ingredient for a pest controlling agent.
    Type: Application
    Filed: May 21, 2007
    Publication date: December 20, 2007
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Tatsuya MORI
  • Patent number: 7297714
    Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: November 20, 2007
    Assignee: IRM LLC
    Inventors: Hong Liu, Phillip Alper, Daniel Mutnick, Donald Karanewsky
  • Patent number: 7294639
    Abstract: Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPAR? receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: November 13, 2007
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Laurence Clary, Eric Terranova
  • Patent number: 7294641
    Abstract: Heterocyclic compounds useful for stimulating/inducing the growth of keratinous fibers, notably human hair/eyelashes, and/or slowing the loss of same, have the following structural formula (I) or salt thereof: in which Hy is a heterocycle of 4 to 7 atoms, optionally comprising carbonyl/thiocarbonyl functional groups, and G is O, S or NH.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: November 13, 2007
    Assignee: L'Oreal
    Inventors: Christophe Boulle, Roger Rozot, Maria Dalko
  • Patent number: 7288567
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: March 26, 2001
    Date of Patent: October 30, 2007
    Assignee: Methylgene Inc.
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
  • Patent number: 7285571
    Abstract: The present invention relate to a novel synergistic composition of lignans exhibiting anticancer activities for breast, cervix, neuroblastoma, colon, liver, lung, mouth, ovary and prostate cancer obtained from the plant extract of Cedrus deodra, said composition comprising of (?)-Matairesinol in the range of 9 to 13% by weight, (?)-Wikstromol in the range of 75 to 79% by weight, Dibenzylbutyrolactol in the range of 7 to 11% by weight, and Unidentified material in the range of 2.6 to 3% by weight; further, the synergistic composition of lignan is used in combination with pharmaceutically acceptable carriers for inhibiting growth of various human cancer cell lines selected from breast, cervix, neuroblastoma, colon, liver, lung, mouth, ovary and prostate tissues.
    Type: Grant
    Filed: June 17, 2003
    Date of Patent: October 23, 2007
    Assignee: Council of Scientific and Industrial Research
    Inventors: Janaswamy Madhusudana Rao, Pullela Venkata Srinivas, Jhillu Singh Yadav, Kondapuram Vijaya Raghavan, Ajit Kumar Saxena, Mutiah Shanmugavel, Himani Kampasi, Gulam Nabi Qazi
  • Patent number: 7282519
    Abstract: The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent.
    Type: Grant
    Filed: August 20, 2004
    Date of Patent: October 16, 2007
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, Manuel Worcel, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Subhash P. Khanapure, Chia-En Lin, Ramani R. Ranatunge, Cheri A. Stevenson
  • Patent number: 7271289
    Abstract: Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: September 18, 2007
    Assignee: SmithKline Beecham Corporation
    Inventor: Nicola Mary Aston
  • Patent number: 7264822
    Abstract: One aspect of the invention is a system for treating vascular conditions, including a catheter, a stent coupled to the catheter, and a polymeric coating on the stent comprising at least one conjugated drug. Each conjugated drug includes a control agent and a bioactive agent, where the control agent controls the elution rate of the bioactive agent.
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: September 4, 2007
    Assignee: Poly-Med, Inc.
    Inventors: Shalaby W. Shalaby, Todd Campbell
  • Patent number: 7256203
    Abstract: A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR17, where R17 is hydrogen or lower alkyl; A and Y are CH, N, NR17, O, or S; C1 and C2 are each C or N, wherein C1 and C2 are the same or different; D1 and D2 are each C or N, wherein D1 and D2 are the same or different; B and Z are CH, N, or NR17, provided that B, Z, or both B and Z are not present when A, Y, or both A and Y are O, S, or NR17; R13, R14, R1 and R8 can be present or absent, and when present are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R15 and Rare selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R3 and R6 are each independently selected from the group consisting of H, hydroxy, lower alkyl, cycloalkyl, aryl, aralkyl, alkoxyl, hydroxycycloalkyl, alkoxycycloalkyl, hydroxyalkyl, aminoalkyl, acyloxy, acetoxy, and alkylaminoalkyl; and R2, R4, R5 and R7 are each independently selected fr
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: August 14, 2007
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: David W. Boykin, Richard R. Tidwell, Mohamed A. Ismail, Reto Brun
  • Patent number: 7244753
    Abstract: The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: July 17, 2007
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Subhash P. Khanapure, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder
  • Patent number: 7235690
    Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: June 26, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
  • Patent number: 7223791
    Abstract: The present invention provides a retinoid-related receptor (except retinoic acid receptors) function regulating agent comprising a compound represented by the formula: wherein one of R1 and R2 is an optionally substituted monocyclic aromatic hydrocarbon group or an optionally substituted monocyclic aromatic heterocyclic group containing one heteroatom, and the other is a hydrogen atom and the like; B is a 5- or 6-membered heterocycle (except 1,3-azole); A is an optionally substituted aromatic hydrocarbon group or an optionally substituted aromatic heterocyclic group; and R3 is a hydrogen atom and the like, or a salt thereof, which is useful as an agent for the prophylaxis or treatment of diabetes mellitus, hyperlipidemia, impaired glucose tolerance or the like.
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: May 29, 2007
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuyoshi Maekawa, Jun Kunitomo, Hiroyuki Odaka, Hiroyuki Kimura
  • Patent number: 7214701
    Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: May 8, 2007
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Patent number: 7208629
    Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1–6alkyl and —(CH2)n-C3–7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1–6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: April 24, 2007
    Assignee: Glaxo Group Limited
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, George Stuart Cockerill, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
  • Patent number: 7202383
    Abstract: There is described compounds of Formula I, and salts, solvates and hydrates thereof: wherein: R1, R2 and R3 are each independently selected from OH, C1-6alkyl, OC1-6alkyl, OC(O)C1-6alkyl, C(O)OC1-6alkyl, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6alkyl), C(O)NHC1-6alkyl, C(O)N(C1-6alkyl)(C1-6alkyl), SH, SC1-6alkyl, NO2, CF3, OCF3 and halogen; and Ar is an aromatic or heteroaromatic group chosen from benzene, naphthalene, quinoline, isoquinoline, indole, pyridine, pyrasine, pyrimidine, imidazole, furan and thiophene, unsubstituted or substituted with 1–4 substituents independently selected from OH, C1-6alkyl, C1-6alkoxy, C1-3alkylenedioxy, NH2, NH—C1-6alkyl, N(C1-6alkyl)(C1-6)(C1-6alkyl), SH, S—C1-6alkyl, NO2, CF3, OCF3 and halogen. The compounds of Formula I are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.
    Type: Grant
    Filed: September 14, 2004
    Date of Patent: April 10, 2007
    Assignee: The Hospital For Sick Children
    Inventors: Chaim Roifman, Peter Demin, Olga Rounova, Tom Grunberger
  • Patent number: 7202247
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: April 10, 2007
    Assignee: AtheroGenics, Inc.
    Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten
  • Patent number: 7199148
    Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5a and R5b is C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5a and R5b may also be hydrogen, aryl, Het1, Het2; R6 is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms.
    Type: Grant
    Filed: August 14, 2003
    Date of Patent: April 3, 2007
    Assignee: Tibotec Pharmaceuticals Ltd
    Inventors: Abdellah Tahri, Piet Tom Bert Paul Wigerinck
  • Patent number: 7192940
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: July 16, 2004
    Date of Patent: March 20, 2007
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Patent number: 7189753
    Abstract: A method of preventing the headache phase of migraine in a human comprises administration of a 5HT1 receptor agonist or administration of an over-the-counter or nonprescription drug to said human exhibiting prodrome symptoms of migraine. Suitably, the method comprises administration of a migraine headache phase-preventing effective amount of the 5HT1 agonist or over-the-counter or nonprescription drug. There is disclosed a preemptive prophylaxis migraine method using the following cognitive tests: Simple Reaction Time; Running Memory Continuous Performance Task; Matching to Sample; Mathematical Processing Task; and interpreting the results as a percent of baseline indicator of need for prophylaxis.
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: March 13, 2007
    Inventors: Roger K. Cady, Donna Lee Gutterman, Stephen Venson O'Quinn
  • Patent number: 7186742
    Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
    Type: Grant
    Filed: May 12, 2004
    Date of Patent: March 6, 2007
    Assignee: Pfizer Inc
    Inventors: Mark A Dombroski, Allen J. Duplantier, Chakrapani Subramanyam
  • Patent number: 7183297
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: February 27, 2007
    Assignee: Glaxo Group Limited
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Stephen Sean Flack, Dramane Ibrahim Lainé, Ann Louise Walker
  • Patent number: 7183300
    Abstract: Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula I wherein the variables A, R1, R2, R3, R4, X, Y, Z, A5, A6, A7, R8, R9, R12, and R13 are defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: February 27, 2007
    Inventors: Michael F. Summers, Atul Agarwal, Xi Chen, Milind Deshpande