Chalcogen Or Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/491)
-
Patent number: 7652020Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: June 1, 2005Date of Patent: January 26, 2010Assignee: Schering CorporationInventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, Jr., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
-
Patent number: 7645886Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula (I), or especially of amides of the formula (II), wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: GrantFiled: December 12, 2003Date of Patent: January 12, 2010Assignee: Ciba Specialty CorporationInventors: Ulrich Berens, Oliver Dosenbach, Daniel Sprenger
-
Patent number: 7638513Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: December 1, 2005Date of Patent: December 29, 2009Assignee: Schering CorporationInventors: M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga A. Reddy, Vincent S. Madison
-
Publication number: 20090318528Abstract: New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals.Type: ApplicationFiled: March 11, 2009Publication date: December 24, 2009Applicant: AJINOMOTO CO., INCInventors: Kenichi MORI, Eriko ONO
-
Publication number: 20090318492Abstract: Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.Type: ApplicationFiled: November 3, 2006Publication date: December 24, 2009Inventors: Han-Ting Chang, Dominique Charmot, Tomasz Glinka, Michael James Cope, Elizabeth Goka, Jun Shao, Shiah-yun Chen, Jerry M. Buysse
-
Publication number: 20090318527Abstract: Novel indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds.Type: ApplicationFiled: February 11, 2009Publication date: December 24, 2009Inventors: Howard Sard, Yiliang Zhang, Jie Li, Louis Shuster, Bryan Roth, Niels Jensen
-
Publication number: 20090305410Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.Type: ApplicationFiled: December 12, 2008Publication date: December 10, 2009Applicant: Biotium, Inc.Inventors: Fei Mao, Wai-Yee Leung, Ching-Ying Cheung, Hye Eun Hoover
-
Publication number: 20090291989Abstract: Provided herein are compositions of matter and pharmaceutical compositions thereof, for use in inhibiting the growth of various microbial pathogens, including bacteria, fungi, protozoa, and viral pathogens. Also provided herein are methods of treating microbial diseases/infections and cancer with the compositions. The compositions are additionally useful in wood preservation and food preservation by inhibition of microbial growth.Type: ApplicationFiled: July 6, 2007Publication date: November 26, 2009Applicant: University of Medicine and Dentistry of New JerseyInventors: Arkady Mustaev, Natalia Kurepina
-
Patent number: 7612065Abstract: The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: March 28, 2007Date of Patent: November 3, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Susanne Wilke, Francesco Salituro, Edmund Harrington, Jingrong Cao, Guy Bemis, Huai Gao
-
Publication number: 20090259020Abstract: Disclosed are compounds having the structure: wherein R1a and R1b are independently H, alkyl, F, or fluoroalkyl; wherein R2a, R2b, R2a?, and R2b? are independently H, alkyl, F, fluoroalkyl, aryl, or alkenyl; wherein R3 is OH, alkoxyl, NH2, alkylamino, or dialkylamino; wherein R4a and R4b are independently H, alkyl, acyl, or alkyloxycarbonyl; wherein R11, R12, R13, R21, R22, and R23 are independently H, alkyl, F, or fluoroalkyl; and wherein C0, C1, C2, and C2? are independently chiral or achiral. Also disclosed are processes for making a fluorinated ?-amino acid comprising the steps of: providing a diol; treating the diol with a thionyl halide with oxidative workup; reacting the product with an azide salt to yield an azido group; oxidizing the product to yield a carboxyl group; and reducing the azido group to yield an amino group. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: September 14, 2007Publication date: October 15, 2009Applicant: University of Utah Research FoundationInventors: Bruce Yu, Zhong-Xing Jiang
-
Patent number: 7582771Abstract: A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH2; Y represents C1-C6alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF3, OCF3, OH, C1-C6alkyl, C1-C6alkoxy, C1-C6thioalkyl, NH2, N(C1-C6alkyl)2, NH(C1-C6alkyl), NC(O)—(C1C6alkyl), and NO2. In his process, a compound of formula (II) is reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).Type: GrantFiled: August 31, 2004Date of Patent: September 1, 2009Assignee: WyethInventors: Christoph M. Dehnhardt, Sreenivasulu Megati, Ronald S. Michalak, Panolil Raveendranath, Jianxin Ren, Charles C. Wu, Yangzhong Wu
-
Publication number: 20090215025Abstract: The present invention pertains to compounds that show a high affinity to Factor VIII and Factor VIII-like proteins, and their uses. The compounds are characterized by the general Formula B-Q-X, wherein B represents a dipeptide, tripeptide, or a peptidomimetic; Q represents a spacer and X represents an anchoring molecule; Q and X are optional. These compounds can be used for coating a solid support material. The resulting coated solid support material can be used for purifying Factor VIII by means of affinity chromatography methods. In addition, the compounds of the present invention may be used for stabilizing Factor VIII and for enhancing its activity. The present invention thus pertains also to methods for manufacturing a stabilized Factor VIII containing medicament of increased activity. The inventive compounds can furthermore be used in diagnostic kits and as research tools.Type: ApplicationFiled: December 7, 2006Publication date: August 27, 2009Applicant: TECHNISCHE UNIVERSITAT MUNCHENInventors: Sebastian Knor, Horst Kessler, Charlotte Hauser, Alexey Khrenov, Evgueni Saenko
-
Publication number: 20090216023Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: August 8, 2008Publication date: August 27, 2009Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
-
Patent number: 7560591Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta pType: GrantFiled: April 30, 2008Date of Patent: July 14, 2009Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
-
Publication number: 20090176111Abstract: The present invention relates to a splayant, that is, an intercalant/exfoliant, comprising an azinium compound capable of splaying a layered material.Type: ApplicationFiled: March 11, 2009Publication date: July 9, 2009Inventors: Debasis Majumdar, Deepak Shukla
-
Publication number: 20090142832Abstract: Indole derivatives and analog compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat a cancer.Type: ApplicationFiled: November 29, 2007Publication date: June 4, 2009Inventors: James Dalton, Duane Miller, Sunjoo Ahn, Charles Duke, III, Dong Jin Hwang, Jun Yang
-
Publication number: 20090137570Abstract: 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: ApplicationFiled: January 28, 2009Publication date: May 28, 2009Applicant: IRM LLCInventors: Hong LIU, Arnab K. CHATTERJEE, David C. TULLY, Phillip B. ALPER, Badry BURSULAYA, Jianhua GUO, David H. WOODMANSEE, Daniel MUTNICK, Donald S. KARANEWSKY, Yun HE
-
Publication number: 20090118169Abstract: A compound comprising the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: wherein N1 represents an atom to which a donative hydrogen atom in a hydrogen-bond donating group is bonded or a hydrogen-bond accepting atom in a hydrogen-bond accepting group; N3 represents a hydrogen-bond accepting atom in a hydrogen-bond accepting group; and N2, N4 and N5 independently represents an arbitrary carbon atom constituting a hydrophobic group and defined by the interatomic distances between N1, N2, N3, N4 and N5; and, in the optimized three-dimensional structure thereof, the distances between the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, in the optimized steric structure thereof, are the interatomic distances in a pharmacophore; or a salt thereof; inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases iType: ApplicationFiled: November 16, 2007Publication date: May 7, 2009Applicant: TOYAMA CHEMICAL CO., LTD.Inventors: Hisaaki Chaki, Tadakazu Takakura, Keiichi Tsuchida, Hironori Kotsubo, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
-
Patent number: 7517899Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: March 28, 2005Date of Patent: April 14, 2009Assignee: WyethInventors: Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
-
Publication number: 20090082419Abstract: The present application describes deuterium-enriched tegaserod, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Publication number: 20090075938Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent paiType: ApplicationFiled: February 9, 2007Publication date: March 19, 2009Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
-
Patent number: 7498328Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.Type: GrantFiled: July 17, 2006Date of Patent: March 3, 2009Assignee: Laboratorias Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
-
Publication number: 20090054235Abstract: The present invention relates to novel benzoheterocyclylethylbenzamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: July 6, 2006Publication date: February 26, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
-
Publication number: 20090047246Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: February 11, 2008Publication date: February 19, 2009Applicant: InterMune, Inc.Inventors: Leonid Beigelman, Brad Buckman, Vladimir Serebryany, Guangyi Wang, Jasenka Matulic-Adamic, Antitsa Dimitrova Stoycheva, Steven W. Andrews, Shawn Maurice Misialek, P.T. Ravi Rajagopalan, Andrew M. Fryer, Indrani Gunawardana, Julia Haas, Lily Huang, Machender R. Madduru, Gan Zhang, Karl Kossen, Scott D. Seiwert, Lawrence M. Blatt
-
Patent number: 7491744Abstract: The presently disclosed subject matter provides derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) that are characterized by substantially reduced cyclooxygenase inhibiting activity, yet retain the ability to interact with and modulate the activities of other polypeptides such as the class of peroxisome proliferators-activated receptors (PPARs) and ?-secretase. Also provided are methods of using the derivatives to treat pathological disorders.Type: GrantFiled: April 26, 2005Date of Patent: February 17, 2009Assignee: Vanderbilt UniversityInventors: Lawrence J. Marnett, Jeffery J. Prusakiewicz, Andrew S. Felts, Chuan Ji
-
Publication number: 20090036501Abstract: 2-cyclopenten-1-one oxime derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof inhibit the production of TNF-? or PDE4, and therefore show therapeutic effect in inflammatory or immunological disorders mediated through TNF-? or PDE4.Type: ApplicationFiled: November 30, 2005Publication date: February 5, 2009Applicant: AmorePacific CorporationInventors: Yeonjoon Kim, Sun-Young Kim, Jung Sun Hwang, Kyoung Min Lim, Miyoung Park, Hyun Ju Koh, Sa-yong Hong, Song Seok Shin, Jin Kyu Choi, Joo Hyun Moh, Chin Chung, Byoung Young Woo, Sung II Kim
-
Publication number: 20090035810Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
-
Publication number: 20090035809Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: May 29, 2008Publication date: February 5, 2009Applicant: INVITROGEN CORPORATIONInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
-
Publication number: 20090023797Abstract: The present invention relates to agonists of the S1P4 receptor, which are selective for the S1P4 receptor over one or more of the S1P1, S1P2, S1P3 or S1P5 receptors of at least 10 fold, in particular new indol-alanine derivatives of structure 1, process for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them wherein R1 is phenyl or naphthyl, wherein phenyl is substituted by one or two of halogen, C1-6alkyl, C1-6alkoxy or phenylC1-6alkyl; and R2 is hydrogen or C1-6alkyl; in free or salt form.Type: ApplicationFiled: January 20, 2005Publication date: January 22, 2009Inventors: Kamal Azzaoui, Rochdi Bouhelal, Peter Buehlmayer, Danilo Guerini, Manuel Koller
-
Publication number: 20090023798Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase. Also described herein are methods of using such HDAC inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC activity.Type: ApplicationFiled: June 16, 2008Publication date: January 22, 2009Applicant: PHARMACYCLICS, INC.Inventors: Darren Magda, Zhong Wang
-
Publication number: 20090012112Abstract: This invention relates to novel compounds that are dihydroindoles derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel dihydroindoles derivatives that are derivatives of silodosin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?-1A-adrenoreceptor antagonist, such as silodosin.Type: ApplicationFiled: February 26, 2008Publication date: January 8, 2009Inventor: Julie F. Liu
-
Publication number: 20080317744Abstract: The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: October 14, 2005Publication date: December 25, 2008Applicant: CHIRON CORPORATIONInventors: Rustum S. Boyce, Yi Xia, Hongyan Guo, Kris G. Mendenhall, Annette O. Walter, Weibo Wang
-
Publication number: 20080318874Abstract: A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity.Type: ApplicationFiled: July 26, 2005Publication date: December 25, 2008Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Hiroharu Matsuoka, Tsutomu Sato, Masahiro Nishimoto, Nobuo Shimma
-
Publication number: 20080319044Abstract: Indole boronic acid compounds, and analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-?) in a subject in need thereof.Type: ApplicationFiled: October 27, 2005Publication date: December 25, 2008Applicant: NUADA, LLCInventors: John R. Didsbury, Tatyana A. Dyakonov, Simon N. Haydar, Michael L. Jones, Francine F. Li, Christopher J. Markworth, Jessymol Mathew, Frank J. Schoenen, Jan J. Scicinski, David Middlemiss
-
Publication number: 20080312308Abstract: The present invention relates generally to substituted acetic acid derivatives and methods of using them.Type: ApplicationFiled: July 7, 2008Publication date: December 18, 2008Applicant: WyethInventors: Ariamala Gopalsamy, Scott Lee Kincaid
-
Patent number: 7462640Abstract: The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic) optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, at any mixing ratio or their salts, preferably the corresponding, physiologically acceptable salts, or corresponding solvates; to the process for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.Type: GrantFiled: July 29, 2004Date of Patent: December 9, 2008Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Ramon Merce Vidal, Xavier Codony Soler, Alberto Dordal Zueras
-
Publication number: 20080300240Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: wherein m, n, p, x, R, R1, R2, R3, R4, R5, A and B, are defined herein, including pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE 10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: May 20, 2008Publication date: December 4, 2008Applicant: Omeros CorporationInventors: John E. Bergmann, Neil S. Cutshall, Rene Onrust, Hongkui Zeng, Jennifer Lynn Gage, Derek Johnston, Sandor Cseh, Laszlo Urogdi, Akos Papp
-
Publication number: 20080300291Abstract: Compounds and methods for treating cancer and inducing apoptosis in unwanted rapidly proliferating cells. The compounds are shown in formula I: wherein X is hydroxyl or amino; Y is carboxyl or sulfonyl; R1, R2, R3, and R4 can be the same or different and are selected from hydrogen, halogen, methoxy, trifluoromethyl, hydroxyl and combinations thereof, R5, R6, and R7 may be the same or different and are selected from hydrogen, chloro, bromo, nitro, phenyl, amino, methoxy, and combinations thereof, and derivatives or metabolites thereof.Type: ApplicationFiled: May 9, 2008Publication date: December 4, 2008Applicant: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Dasheng Wang, Jing-Ru Weng
-
Patent number: 7453010Abstract: The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optionaType: GrantFiled: May 26, 2003Date of Patent: November 18, 2008Assignee: Sanofi AventisInventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
-
Publication number: 20080280923Abstract: The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence.Type: ApplicationFiled: March 17, 2006Publication date: November 13, 2008Applicant: N.V. OrganonInventors: Phillip Martin Cowley, Samuel George Gibson, Grant Wishart
-
Publication number: 20080269200Abstract: Indole carboxamide compounds of Formula (I): are provided as inhibitors of kinase activity, in particular IKK2 activity as well as compositions and medicaments containing them, for use in inflammatory and tissue repair disorders.Type: ApplicationFiled: January 13, 2005Publication date: October 30, 2008Applicant: SmithKline Beecham CorporationInventors: Ian Robert Baldwin, Paul Bamborough, John Andrew Christopher, Jeffrey K Kerns, Timothy Longstaff, David Drysdale Miller
-
Publication number: 20080262245Abstract: The present invention relates to a novel process for the preparation of the HMG-CoA reductase inhibitor, fluvastatin, more specifically to a process for the preparation of amorphous form of fluvastatin sodium.Type: ApplicationFiled: October 5, 2004Publication date: October 23, 2008Inventors: Sumithra Srinath, Tom Thomas Puthiaprampil, Ravindra Chandrapa, Sambasivam Ganesh
-
Publication number: 20080255201Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: March 5, 2008Publication date: October 16, 2008Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
-
Publication number: 20080249091Abstract: There is provided compounds of formula I, wherein X1, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: December 22, 2005Publication date: October 9, 2008Inventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris
-
Patent number: 7429612Abstract: The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.Type: GrantFiled: July 16, 2003Date of Patent: September 30, 2008Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Shouji Kamiya, Miho Ikai, Kenji Takahash, Tadatsugu Tarumi, Masayasu Kasai, Akihisa Yoshimi, Hiroaki Shirahase
-
Publication number: 20080227823Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a diamide and aromatic functionality are disclosed of the general formula (1) where X1 and X2 are linkers.Type: ApplicationFiled: March 4, 2008Publication date: September 18, 2008Inventors: Hassan Pajouhesh, Nagasree Chakka, Yuanxi Zhou, Francesco Belardetti
-
Publication number: 20080214646Abstract: This invention provides a prodrug that help arthritis patients without increasing cardiovascular and gastrointestinal risk. A novel group of hybrid nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs), moiety attached via a one -carbon methylene spacer to the carboxylic acid group of the traditional NSAIDs aspirin, ibuprofen and indomethacin were synthesized. The ester prodrugs showed equipotent anti-inflammatory activities in vivo to that of the parent aspirin, ibuprofen and indomethacin. The simultaneous release of parent drug and nitric oxide from the NO- prodrugs constitutes a potentially beneficial property for the prophylactic prevention of thrombus formation and adverse cardiovascular events such as stroke and myocardial infarction. Data acquired in an in vivo ulcer index (UI) assay showed that this group of ester prodrugs in which no lesions were observed when compared to the parent drugs at equivalent doses.Type: ApplicationFiled: May 16, 2006Publication date: September 4, 2008Inventors: Edward E. Knaus, Carlos Velazquez
-
Publication number: 20080207920Abstract: The present invention provides a process for selectively producing an enantiomer at position 4 of an optically active compound in the cross aldol reaction of pyruvic acid and indole-3-pyruvic acid. The process comprises the step of reacting pyruvic acid with indole-3-pyruvic acid in the presence of an optically active ?-amino acid containing a secondary amine and a metal ion.Type: ApplicationFiled: February 8, 2008Publication date: August 28, 2008Applicant: Ajinomoto Co., Inc.Inventors: Shigeru KAWAHARA, Yusuke Amino, Masakazu Sugiyama
-
Publication number: 20080207919Abstract: Disclosed herein are novel polymorphic forms of Fluvastatin sodium, wherein said polymorphic forms are designated as JF, JF1, JF2, JF3 and are characterized by their powder X-ray diffraction patterns, Infrared absorption spectrums, thermo gravimetric analysis and differential scanning calorimetry. The processes for preparing said polymorphic forms are also disclosed. The present invention also relates to process for preparing amorphous form of Fluvastatin sodium.Type: ApplicationFiled: February 10, 2006Publication date: August 28, 2008Applicant: Jubliant Organosys LimitedInventors: Bhausaheb Chavhan, Arun Kumar Awasthi, Richa Aggarwal, Rani S. Beena, Soumendu Paul, Rajesh Kumar Thaper, Sushil Kumar Dubey
-
Patent number: 7414070Abstract: The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salts, preferably the corresponding, physiologically acceptable salts, or corresponding solvates; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.Type: GrantFiled: July 29, 2004Date of Patent: August 19, 2008Assignee: Laboratorios del Dr. ESTEVE S.A.Inventors: Ramon Merce Vidal, Xavier Codony Soler, Alberto Dordal Zueras