The Hetero Ring Is Five-membered Patents (Class 514/461)
  • Patent number: 7589121
    Abstract: The invention relates to the use of one or several synthetic or natural furan alkyls for preparing a drug preventing and/or treating obesity or overweight. The use of one or several synthetic or natural furan alkyls for cosmetically treating local excessive weight is also disclosed. Said furan alkyls preferably correspond to formula (I), wherein identical or different R1, R2, R3et R4 are independently of each other a hydrogen atom, a C1-C35alkyl radical, C1-C35 alcenyl radical or a C1-C35 alcynyl radical, preferably C10-C22, wherein said alkyl, alcenyl and alcynyl radicals are substitutable and R1, R2, R3 are preferably a hydrogen atom.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: September 15, 2009
    Assignee: Laboratoires Expanscience
    Inventors: Antoine Piccirilli, Philippe Msika, Nathalie Piccardi
  • Patent number: 7582677
    Abstract: A topical formulation which includes a lignan or lignan ester in a dermatologically acceptable vehicle. The formulation can be either a cosmetic formulation or a pharmaceutical formulation.
    Type: Grant
    Filed: May 15, 2003
    Date of Patent: September 1, 2009
    Assignee: Hormos Medical Corp.
    Inventors: Helena Korte, Veli-Matti Lehtola, Mikko Unkila, Mervi Hiilovaara-Teijo, Markku Ahotupa
  • Publication number: 20090215623
    Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.
    Type: Application
    Filed: July 21, 2006
    Publication date: August 27, 2009
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
  • Patent number: 7569602
    Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii) an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: August 4, 2009
    Assignee: Asterand UK Limited
    Inventors: David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark
  • Patent number: 7569603
    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: Grant
    Filed: May 21, 2007
    Date of Patent: August 4, 2009
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Tatsuya Mori
  • Publication number: 20090176837
    Abstract: Disclosed herein are novel compounds with activity at RAR? 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.
    Type: Application
    Filed: July 12, 2006
    Publication date: July 9, 2009
    Applicant: SONY CORPORATION
    Inventors: Roger Olsson, Fabrice Piu, Birgitte Lund
  • Patent number: 7557247
    Abstract: The invention provides a novel ?2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel ?2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with ?2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
    Type: Grant
    Filed: May 26, 2004
    Date of Patent: July 7, 2009
    Assignee: Theravance, Inc.
    Inventors: Ioanna Stergiades, Edward Yost
  • Publication number: 20090170895
    Abstract: The present invention relates to a medicine, and more particularly to novel arylamidrazone derivatives having an antagonistic action against S1P3 receptors and a medicine containing thereof as an active ingredient.
    Type: Application
    Filed: October 11, 2006
    Publication date: July 2, 2009
    Applicant: TOA EIYO LTD.
    Inventors: Shin-ya Ohnuma, Takeshi Hasegawa, Tomoyuki Sada
  • Patent number: 7553867
    Abstract: The present invention provides a compound represented by the formula (I): [wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, p is 0, 1 or 2, and when p is 2, each R may be the same or different, R1 is a hydrogen atom or an optionally substituted hydrocarbon group, R2 is an optionally substituted aromatic group, Ring A is an optionally substituted monocyclic aromatic ring or optionally substituted bicyclic aromatic fused ring, X1 is an oxygen atom or a sulfur atom, X2 is a bond, an oxygen atom or —S(O)n— (wherein n is 0, 1 or 2), Y is a bond, an oxygen atom, —S(O)m—, —C(?O)—N(R3)— or —N(R3)—C(?O)— (R3 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, and m is 0, 1 or 2), M1, M2 and M3 may be the same or different and are each independently a bond or an optionally substituted divalent aliphatic hydrocarbon group, and M4 is an optionally substituted divalent aliphatic hydrocarbon group] or a
    Type: Grant
    Filed: September 4, 2003
    Date of Patent: June 30, 2009
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazumasa Hamamura, Shigekazu Sasaki, Yuichiro Amano, Junichi Sakamoto, Kohji Fukatsu
  • Publication number: 20090163582
    Abstract: Pesticide concentrates are provided containing an emulsifier that is an EPA list 4 inert and is a polyglycerol fatty acid ester, a sorbitan fatty acid ester or a combination thereof, a pesticide and a solvent that is either a EPA list 3 inert of acetyl ester, EPA list 4 inert of a methyl fatty ester, an acetyltributyl citrate, white mineral oil or a combination thereof. The pesticide can be a water-insoluble synthetic pyrethroid, natural pyrethrum, channel blocking insecticide, acetylcholinesterase inhibitor, oxadiazine, organophosphate, neonicotinoid insecticide, thiamethoxam, imidacloprid, acetamiprid, thiacloprid, clothianidin, nitenpyran, insect growth regulator, juvenile hormone mimic, fermentation insecticide, plant oil insecticide acaracide, miticide, fungicide, herbicide and combinations thereof. The pesticide concentrate is diluted with a hydrocarbon solvent, a white mineral oil or a combination thereof and mixed with water.
    Type: Application
    Filed: April 4, 2006
    Publication date: June 25, 2009
    Inventors: Yueh Wang, Ian R. Gecker, John Lucas, Ashish Shah
  • Publication number: 20090149531
    Abstract: The present invention is a chemical composition including: Use of the compound with the chemical formula can be applied in pharmaceutical compositions for the treatment of psoriasis.
    Type: Application
    Filed: December 10, 2008
    Publication date: June 11, 2009
    Applicant: APOTEKNOS PARA LA PIEL, S.L.
    Inventors: Juan Pablo PIVEL RANIERI, Juan Manuel Ferrer Cuesta, Fernando Martinez Galan, Juan Manuel Irache, Jose Luis Novella Robisco, Juan Jose Perez Rueda, Ma Paz Maria Martin, Julio Alvarez-Builla Gomez, Jaime Bermejo, Fernando Vidal Vanaclocha
  • Patent number: 7544667
    Abstract: The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agents.
    Type: Grant
    Filed: September 15, 2004
    Date of Patent: June 9, 2009
    Assignee: Lipideon Biotechnology AG
    Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder
  • Publication number: 20090137664
    Abstract: Compounds and compositions that effectively block hypoxia-inducible factor-1 function, and methods of use thereof. The compounds and compositions of the present invention are useful in the prevention and treatment of cancer, stroke, heart disease, ocular neovascular diseases, and arthritis.
    Type: Application
    Filed: October 20, 2008
    Publication date: May 28, 2009
    Inventors: Dale G. Nagle, Yu-Dong Zhou, Chowdhury Faiz Hossain, Tyler W. Hodges
  • Publication number: 20090131474
    Abstract: The present invention describes an improved method for screening compounds for activity in inhibiting the enzymatic activity of Akt1 protein kinase, also known as Protein Kinase B, an enzyme that is believed to play a key role in the inhibition of apoptosis and thus in the etiology of cancer and other conditions, including neurodegenerative diseases.
    Type: Application
    Filed: March 2, 2006
    Publication date: May 21, 2009
    Inventors: Martino Forino, Dawoon Jung, Maurizio Pellecchia
  • Patent number: 7534768
    Abstract: The synergistic combination of a loop diuretic and a cardiac glycoside is useful in the treatment of DNA viral infections.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: May 19, 2009
    Assignee: Henderson Morely Research and Development Ltd.
    Inventor: Christopher Edward Hartley
  • Publication number: 20090118269
    Abstract: Methods for using tetracycline compounds for the treatment of spinal muscular atrophy are described.
    Type: Application
    Filed: April 14, 2008
    Publication date: May 7, 2009
    Inventors: Joel Berniac, Todd Bowser, Michael Draper, Stuart B. Levy, Mark L. Nelson
  • Patent number: 7528274
    Abstract: Certain thiol and acylthiol compounds inhibit retrovirus growth by attacking the highly conserved zinc finger regions of essential viral proteins. These compounds, compositions containing them, and methods of using them to treat retroviral infections such as HIV are described. These compounds are also useful for preparation of vaccines comprised of inactivated retroviruses such as HIV, prevention of the transmission of such retroviruses, and detection of retroviral proteins.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: May 5, 2009
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: John K. Inman, Atul Goel, Ettore Appella, Jim Turpin, Marco Schito
  • Patent number: 7528166
    Abstract: Novel phenolic esters of lignans, and pharmaceutical compositions, dietary supplements, and food products containing these esters.
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: May 5, 2009
    Assignee: Hormos Medical Corporation
    Inventors: Patrik Eklund, Mervi Hiilovaara-Teijo, Arja Kalapudas, Lauri Kangas, Anna Lindholm, Rainer Sjohölm, Marja Södervall, Mikko Unkila
  • Publication number: 20090111870
    Abstract: An acetone extract, chloroform extract or hexane extract of Angelicae sinensis and/or the active components purified therefrom, such as n-butylidenephthalide, are administered alone or in combination with one or more chemotherapy drugs and are effective in treating cancers.
    Type: Application
    Filed: October 29, 2008
    Publication date: April 30, 2009
    Applicant: BUDDHIST TZU CHI GENERAL HOSPITAL
    Inventors: Jiann-Kuan Luo, Horng-Jyh Harn, Wen-Liang Chang, Shinn-Zong Lin, Yeung-Leung Cheng, Nu-Man Tsai
  • Patent number: 7517893
    Abstract: Novel dicationic bichalcophene compounds are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: April 14, 2009
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: Richard R. Tidwell, David W. Boykin, Chad Stephens, Mohamed A. Ismail, W. David Wilson, Reto Brun, Karl Werbovetz
  • Publication number: 20090093519
    Abstract: Small molecules and their derivatives are described for the treatment and/or prevention of intestinal fluid loss. Also disclosed are methods of using said molecules and their derivatives to treat and/or prevent conditions associated with increased levels of 3?,5?-adenosine monophosphate. Specific compositions of the invention are also novel.
    Type: Application
    Filed: June 13, 2008
    Publication date: April 9, 2009
    Applicants: Mission Pharmacal Co., Board of Regents, The University of Texas System
    Inventors: Catherine H. Schein, Scott R. Gilbertson, Johnny W. Peterson, Deliang Chen, Maria Estrella-Jimenez, Mary A. Walter, Jian Gao
  • Publication number: 20090093538
    Abstract: The invention relates to a method of treating cancer in a subject, comprising administering to the subject an anti-cancer therapy and a compound that increases the oxidative stress of the cancer cells and activates p38.
    Type: Application
    Filed: December 27, 2007
    Publication date: April 9, 2009
    Applicant: Synta Pharmaceuticals Corp
    Inventors: John Bertin, Jessica R. Kirshner, Zhenjian Du
  • Patent number: 7511073
    Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke.
    Type: Grant
    Filed: May 23, 2006
    Date of Patent: March 31, 2009
    Assignee: Sepracor, Inc.
    Inventors: Brian M. Aquila, Seth C. Hopkins, Curtis A. Lockshin, Fengjiang Wang
  • Patent number: 7507817
    Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.
    Type: Grant
    Filed: November 13, 2007
    Date of Patent: March 24, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo, Wha-Bin Im
  • Publication number: 20090053175
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.
    Type: Application
    Filed: August 22, 2008
    Publication date: February 26, 2009
    Inventors: Yat Sun Or, Ce Wang, Jiang Long, Lu Ying, Yao-Ling Qiu
  • Patent number: 7495024
    Abstract: The method of treating patients be administering phenylalkyl N-hydroxurea derivatives for combating atherosclerotic plaque and cardiovascular diseases and compositions for this use.
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: February 24, 2009
    Assignee: VIA Pharmaceuticals, Inc.
    Inventors: Raymond Tabibiazar, Melisa Cooper, Thomas Quertermous, Adeoye Olukotun
  • Patent number: 7485752
    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: May 5, 2006
    Date of Patent: February 3, 2009
    Assignee: Hoffman-La Roche Inc.
    Inventor: Christophe Michoud
  • Publication number: 20090030015
    Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) or (IIa) or (IIb) and a pharmaceutically acceptable carrier wherein the symbols and substituents have the following meaning —X— is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    Type: Application
    Filed: September 20, 2006
    Publication date: January 29, 2009
    Applicant: REVOTAR BIOPHARMACEUTICALS AG
    Inventors: Remo Kranich, Ewald M. Aydt, Anke S. Busemann
  • Publication number: 20090018145
    Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreating carcinomas) and mesotheliomas.
    Type: Application
    Filed: October 18, 2005
    Publication date: January 15, 2009
    Applicant: Compass Pharmaceuticals LLC
    Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
  • Publication number: 20090018167
    Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiogenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.
    Type: Application
    Filed: August 22, 2008
    Publication date: January 15, 2009
    Applicants: J. Phillip Bowen, Emory University
    Inventors: J. Phillip Bowen, Thomas Philip Robinson, Tedman Ehlers, David Goldsmith, Jack Arbiser
  • Publication number: 20090011059
    Abstract: The present invention relates to the use of a ginger extract on its own or in combination with pharmaceutical compositions for inhibiting human drug transporters for positively influencing the oral bioavailability and pharmacokinetics of active substances.
    Type: Application
    Filed: December 20, 2006
    Publication date: January 8, 2009
    Inventors: Naoki Ishiguro, Wataru Kishimoto, Thomas Ebner, Willy Roth
  • Publication number: 20080319015
    Abstract: The present invention relates to the use of an insect repellent, preferably selected from the group 2-(2-hydroxyethyl)-1-methylpropyl 1-piperidinecarboxylate, N,N-diethyl-3-methylbenzamide, dimethyl phthalate, butopyronoxyl, 2,3,4,5-bis(2-butylene)-tetrahydro-2-furaldehyde, N,N-diethylcaprylamide, N,N-diethylbenzamide, o-chloro-N,N-diethylbenzamide, dimethyl carbate, di-n-propyl isocinchomeronate, 2-ethylhexane-1,3-diol, N-octylbicycloheptenedicarboximide or piperonyl butoxide, particularly preferably 2-(2-hydroxyethyl)-1-methylpropyl 1-piperidinecarboxylate, as action enhancer for a second insect repellent, to corresponding compositions, and to the preparation thereof.
    Type: Application
    Filed: November 24, 2006
    Publication date: December 25, 2008
    Inventors: Hans-Werner Gruenewald, Alexandra Axt
  • Publication number: 20080312293
    Abstract: The present invention relates to selected (R)-2-phenyl-propionamides and (R)-2-phenyl-sulfonamides with a hydrogen bond acceptor atom/group in a well defined position in the chemical space. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Application
    Filed: December 13, 2005
    Publication date: December 18, 2008
    Applicant: Dompe' PHA.R.MA.S.P.A.
    Inventors: Marcello Allegretti, Riccardo Bertini, Andrea Beccari, Alessio Moriconi, Andrea Aramini, Cinzia Bizzarri, Francesco Colotta
  • Publication number: 20080300178
    Abstract: The present invention relates to a method for treating patients having Huntington's disease by a drug increasing the phosphorylation of huntingtin at position S421, thereby decreasing the polyQ-huntingtin-induced toxicity.
    Type: Application
    Filed: January 18, 2007
    Publication date: December 4, 2008
    Applicants: Insitut Curie, Centre National De La Recherche Scientifique
    Inventors: Raul Pardo, Sandrine Humbert, Frederic Saudou
  • Publication number: 20080293764
    Abstract: A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof.
    Type: Application
    Filed: April 30, 2008
    Publication date: November 27, 2008
    Inventors: Masahiko Terakado, Shinji Nakade, Takuya Seko, Yoshikazu Takaoka
  • Publication number: 20080293739
    Abstract: Disclosed are compounds and compositions that modulate T-cells. Such compounds can be used to treat T-cell mediated disease like T-ALL, rheumatoid arthritis, multiple sclerosis, and graft-vs-host disease (GvHD), to name but a few. The compounds have a general structure as shown in Formula I. Ar1-L-Ar2??I wherein Ar1 and Ar2, are independent of one another, a substituted aryl, unsubstituted aryl, substituted heteroaryl, or unsubstituted heteroaryl; and L is a bond or a linker spanning two, three, four, or five atoms.
    Type: Application
    Filed: April 11, 2008
    Publication date: November 27, 2008
    Inventor: Nikolaus S. Trede
  • Publication number: 20080287442
    Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-8)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.
    Type: Application
    Filed: January 11, 2007
    Publication date: November 20, 2008
    Applicant: Nabriva Therapeutics Forschungs GmbH
    Inventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
  • Publication number: 20080287430
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof wherein X, Z, R1, R2a, R2b, R3, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
    Type: Application
    Filed: April 24, 2006
    Publication date: November 20, 2008
    Inventors: Rino Antonio Bit, Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Tiziana Scoccitti
  • Patent number: 7449481
    Abstract: 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 that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: November 11, 2008
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Marie-Edith Gourdel, Greg Hostetler, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet, Eric Riguet, Dominique Schweizer, Christophe Yue
  • Publication number: 20080275103
    Abstract: The invention relates to a compound represented by general formula (I) wherein Z represents N, O or S, and A represents a CH group, a nitrogen atom or an NL+ group wherein L represents a straight-chained or branched C1-C12 alkyl group. The invention also relates to a method for the preparation thereof and the use thereof as an antimitotic.
    Type: Application
    Filed: May 13, 2005
    Publication date: November 6, 2008
    Inventors: Yannick Arlot, Benedicte Martin, Jean-Guy Delcros, Gilles Alcaraz, Olivier Paulus
  • Patent number: 7438900
    Abstract: A pharmaceutical composition comprising an active agent bound to a scaffold for dendritic encapsulation wherein said scaffold is covalently or non-covalently attached to a polysaccharide. More specifically, the invention is directed to active agent complexes or conjugates which utilize dendritic encapsulation alone or in combination with other delivery systems to improve and target active agent release.
    Type: Grant
    Filed: July 8, 2004
    Date of Patent: October 21, 2008
    Assignee: Shire LLC
    Inventors: Thomas Piccariello, Travis Mickle, Barney Bishop
  • Publication number: 20080255198
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, m, n, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.
    Type: Application
    Filed: June 13, 2008
    Publication date: October 16, 2008
    Inventors: Chang An Chu, Paul Gillespie, Jefferson Wright Tilley
  • Patent number: 7435750
    Abstract: The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: October 14, 2008
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Han-Zhong Zhang, John A. Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Kristin P. Ollis
  • Patent number: 7432289
    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: October 7, 2008
    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, Suzanne Joy Merrick, Kathryn Jane Smith, Ann Louise Walker
  • Publication number: 20080234199
    Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.
    Type: Application
    Filed: November 22, 2006
    Publication date: September 25, 2008
    Inventor: Subba Reddy Katamreddy
  • Publication number: 20080221205
    Abstract: The present invention relates to furan derivatives and pharmaceutical compositions containing them to prevent and cure osteoporosis. The furan derivatives of the present invention have effect on bone proliferation with the side effect reduced, so that they can be used for bone disease.
    Type: Application
    Filed: May 22, 2008
    Publication date: September 11, 2008
    Inventors: Jung-Keun Kim, Se-Won Kim, Kwi-Ok Oh, Seon Yle Ko, Jong Yeo Kim, Byung-Eui Lee, Bum Tae Kim, Yeon Soo Lee, Yong Ki Min, No Kyun Park
  • Publication number: 20080214660
    Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
    Type: Application
    Filed: May 15, 2008
    Publication date: September 4, 2008
    Inventors: Russell M. Medford, Patricia K. Somers, Lee K. Hoong, Charles O. Meng
  • Patent number: 7420000
    Abstract: Aminophosphonate and amino bisphosphonate compounds and methods for their preparation are provided. Also provided are pharmaceutical and agricultural compositions containing the compounds. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease, cardiovascular disease, bacterial infection, viral disease, abnormal cell proliferation, bone resorption disease, osteoporosis, or parasitic disease and in various agricultural methods, including, methods of eradicating weeds.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: September 2, 2008
    Assignee: University of Southern California
    Inventor: Nicos A. Petasis
  • Patent number: 7417068
    Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii)an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: August 26, 2008
    Assignee: Asterand UK Limited
    Inventors: David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark
  • Publication number: 20080194678
    Abstract: A process to obtain synthetic and semi-synthetic derivatives of lignans, especially dibenzylbutyrolactonic, tetrahydrofuranic, aryltetralynic, furofuranic and dibenzocyclooctanic lignans obtained by means of partial synthesis and/or full synthesis or also by isolation from plant extracts. It refers to a process to obtain synthetic and semi-synthetic derivatives of (?)-cubebin, such as: (?)-O-acetylcubebin; (?)-O-methylcubebin; (?)-O—N,N-(dimethylamino-ethyl)-cubebin; (?)-hinokinin; (?)-6,6?-dinitroinokinine; (?)-O-benzylcubebin; (?)-6,6?-diaminoinokinin, (?)-6,6?-dinitroinokinin, as well as to obtain dibenzocyclooctanic lignans from dibenzylbutyrolactoinic lignans by means of structural modifications in the positions 7, 7?, 8, 8?, 9? and in the aromatic rings (introduction and/or substitution of functional groups such as: —OH, —CO2H, —CO2CH3, —NO2, —NH2, —OCH3, —OAc, —SO2CH3, —SO2NH2, prenyl and halogens) is provided. A therapeutic method using the derivatives is also provided.
    Type: Application
    Filed: July 14, 2006
    Publication date: August 14, 2008
    Applicant: Fundacao de Amparo a Pesquissa do Estado de Aao Pa
    Inventors: Marcio Luis Andrade e Silva, Rosangela da Silva, Vanderlei Rodrigues, Olavo dos Santos Pereira, Ademar Alves da Silva Filho, Paulo Marcos Donate, Sergio Albuquerque, Jairo Kenupp Bastos