Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 546/281.1)
-
Publication number: 20130256645Abstract: A compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode are disclosed, the compound being represented by the following Chemical Formula 1:Type: ApplicationFiled: June 3, 2013Publication date: October 3, 2013Inventors: Soo-Hyun MIN, Eun-Sun YU, Hyung-Sun KIM, Mi-Young CHAE
-
Publication number: 20130261130Abstract: The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is —CON—R3R4, —NR5COR6, —NHR7, —OR8, —SR9, —CH2NR10R11, —(CH2)2-R12, —CH?CH—R12, —C?C—R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.Type: ApplicationFiled: October 31, 2011Publication date: October 3, 2013Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Hans Allgeier
-
Publication number: 20130197013Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.Type: ApplicationFiled: July 27, 2011Publication date: August 1, 2013Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
-
Publication number: 20130172339Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.Type: ApplicationFiled: September 19, 2011Publication date: July 4, 2013Applicant: KANCERA ABInventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
-
Publication number: 20130131321Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
-
Publication number: 20130123265Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
-
Publication number: 20130099208Abstract: A condensed-cyclic compound represented by Formula 1 below, a method for preparing the condensed-cyclic compound, and an organic light-emitting device including the condensed-cyclic compound. wherein R1 through R8, a ring A, and X1 are defined as in the specification.Type: ApplicationFiled: April 24, 2012Publication date: April 25, 2013Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Sun-Young Lee, Yoon-Hyun Kwak, Bum-Woo Park, Se-Jin Cho
-
Publication number: 20130079313Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: September 26, 2012Publication date: March 28, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
-
Publication number: 20130053369Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: ApplicationFiled: October 26, 2012Publication date: February 28, 2013Applicant: Astellas Pharma Inc.Inventor: Astellas Pharma Inc.
-
Publication number: 20130042918Abstract: Compounds of Formula (I): Wherein: R1 and R2 are independently selected from the group consisting of optionally substituted C1-C20 alkyl, optionally substituted C3-C8 cycloalkyl, optionally substituted aromatic, and optionally substituted heteroaromatic groups or R1 and R2 together with the nitrogen atom to which they are attached comprise an optionally substituted saturated or unsaturated ring which may optionally contain further heteroatoms selected from the group consisting of O, N and S, and may optionally be further fused to one or more other rings; Ar is selected from the group consisting of optionally substituted aromatic and optionally substituted heteroaromatic groups; L is a linker which is a direct bond or is selected from the group consisting of optionally substituted C2 alkenylene and optionally substituted C2 alkynylene; T is independently selected from the group consisting of: R3, R4 and R9 are independently selected from the group consisting of hydrogen, optionally substitutedType: ApplicationFiled: May 5, 2011Publication date: February 21, 2013Inventors: Richard Evans, Akhil Gupta, Abdelselam Saeed Ali
-
Publication number: 20120316195Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 16, 2010Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
-
Publication number: 20120295920Abstract: HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.Type: ApplicationFiled: December 10, 2010Publication date: November 22, 2012Inventors: Genadiy Kalayanov, Bart Rudolf Romanie Kesteleyn, Kevin Parkes, Bengt Bertil Samuelsson, Wim Bert Griet Schepens, Johannes Wilhelmus J. Thuring, Hans Kristian Wallberg, Jörg Kurt Wegner
-
Patent number: 8283479Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: GrantFiled: April 4, 2011Date of Patent: October 9, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, Jr., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
-
Publication number: 20120245184Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a compound. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal patched pathway or agonizing smoothened or hedgehog activity.Type: ApplicationFiled: June 8, 2012Publication date: September 27, 2012Inventors: Shirley Ann Brunton, Oivin M. Guicherit, Lawrence I. Kruse
-
Publication number: 20120214794Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: October 13, 2011Publication date: August 23, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
-
Publication number: 20120214994Abstract: The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salt thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to ?-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease.Type: ApplicationFiled: September 14, 2010Publication date: August 23, 2012Inventors: Dae-Yoon Chi, Byoung-Se Lee, Sirion Uthaiwan, So-Young Chu, Yu-Jin Bae, Chansoo Park, Dae-Hyuk Moon, Jin-Sook Ryu, Jae-Seung Kim, Seung-Jun Oh
-
Patent number: 8242142Abstract: Compounds having the formula I, their methods of synthesis, and pharmaceutically acceptable salts of certain of them are provided in which the variables have the definitions described herein. Compositions including the compounds having the formula I-A in which the variables have the definitions described herein, and methods of using the compositions for the treatment of certain diseases mediated by the up-regulation of Smo are also disclosed.Type: GrantFiled: August 18, 2009Date of Patent: August 14, 2012Assignees: The Regents of the University of California, Peking University Shenzhen Graduate SchoolInventors: Shuo Lin, Zhen Yang
-
Publication number: 20120202817Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
-
Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
-
Publication number: 20120148955Abstract: A resist composition including: a base component (A) which exhibits changed solubility in a developing solution under action of acid; a nitrogen-containing organic compound component (C) containing a compound (C1) represented by general formula (c1) shown below; and an acid generator component (B) which generates acid upon exposure, provided that the compound (C1) is excluded from the acid generator component (B): wherein RN represents a nitrogen-containing heterocyclic group which may have a substituent; X0 represents a linear or branched divalent aliphatic hydrocarbon group of 1 to 10 carbon atoms, a cyclic divalent aliphatic hydrocarbon group of 3 to 20 carbon atoms or a divalent aliphatic hydrocarbon group of 3 to 20 carbon having a cyclic partial structure, or any one of these groups in which some or all of the hydrogen atoms thereof have been substituted with fluorine atoms; and M+ represents an organic cation.Type: ApplicationFiled: December 6, 2011Publication date: June 14, 2012Applicant: TOKYO OHKA KOGYO CO., LTD.Inventors: Yoshiyuki Utsumi, Kenichiro Miyashita, Akiya Kawaue
-
Patent number: 8163778Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 24, 2008Date of Patent: April 24, 2012Assignee: Hoffmann-LA Roche Inc.Inventors: Wolfgang Haap, Paul Hebeisen, Eric Argirios Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
-
Patent number: 8158655Abstract: The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, R1 to R2?, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.Type: GrantFiled: January 8, 2008Date of Patent: April 17, 2012Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Harald Mauser, Rudolf E. Minder, Hans P. Wessel
-
Patent number: 8129532Abstract: Amino(oligo)thiophene dyes useful for studying the electrophysiology of organelles, cells, and tissues are described. Compared to previously known dyes, the amino(oligo)thiophene dyes exhibit improved (faster) response to membrane potential changes, as well as the ability to be excited by 1064 nanometer femtosecond pulses. Methods of preparing the amino( oligo )thiophene dyes are also described.Type: GrantFiled: July 30, 2008Date of Patent: March 6, 2012Assignee: The University of ConnecticutInventors: Leslie M. Loew, Ping Yan
-
Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
-
Patent number: 8067602Abstract: Asymmetric cyanine fluorescent dyes are represented by general formula I. These kinds of dyes may be used as a staining agent for nucleic acids, with the spectra at 600-900 nm in the near-infrared region and without interference from background fluorescence. These kinds of dyes may be useful with small-type red semiconductor lasers as the light source (such as 633 nm). Compositions comprising these dyes and methods for staining biological samples using these dyes or compositions are also provided.Type: GrantFiled: December 12, 2008Date of Patent: November 29, 2011Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventor: Jianhui Shao
-
Patent number: 8058446Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: GrantFiled: September 11, 2007Date of Patent: November 15, 2011Assignee: Gilead Connecticut, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Tony Lee, James W. Darrow, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt
-
Patent number: 8039532Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: GrantFiled: August 15, 2008Date of Patent: October 18, 2011Assignee: Fujifilm CorporationInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
-
Publication number: 20110212983Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 18, 2009Publication date: September 1, 2011Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
-
Publication number: 20110190283Abstract: Compounds of the Formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.Type: ApplicationFiled: July 6, 2010Publication date: August 4, 2011Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, JR., Dalia R. Jakas
-
Publication number: 20110184177Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: ApplicationFiled: April 4, 2011Publication date: July 28, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, JR., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
-
Publication number: 20110177007Abstract: The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienopyrrole core. In some embodiments, dyes of the present invention are dithienopyrrole dyes having a dithienopyrrole core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.Type: ApplicationFiled: September 29, 2009Publication date: July 21, 2011Inventors: Raghavan Rajagopalan, William L. Neumann, Amruta Poreddy, John N. Freskos, Richard B. Dorshow
-
Publication number: 20110177006Abstract: The invention provides optical agents, including compositions, preparations and formulations, and methods of using and making optical agents. Optical agents of the present invention include dyes, and derivatives thereof, having a fused ring backbone structure having dithienofuran core. In some embodiments, dyes of the present invention are dithienofuran dyes having a dithienofuran core optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.Type: ApplicationFiled: September 29, 2009Publication date: July 21, 2011Inventors: Raghavan Rajagopalan, William L. Neumann, Amruta Poreddy, John N. Freskos, Richard B. Dorshow
-
Publication number: 20110160247Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereo. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.Type: ApplicationFiled: June 8, 2009Publication date: June 30, 2011Applicants: JIANGSU GOWORTH INVESTMENT CO. LTD, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRYInventors: Jianqi Li, Kai Gao, Wangping Cai, Yongyong Zheng
-
Patent number: 7928140Abstract: The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: August 1, 2008Date of Patent: April 19, 2011Assignee: Amgen Inc.Inventors: Shon Booker, Noel D'Angelo, Derin C. D'Amico, Tae-Seong Kim, Longbin Liu, Kristin Meagher, Mark H. Norman, Kathleen Panter, Laurie B. Schenkel, Adrian L. Smith, Nuria A. Tamayo, Douglas A. Whittington, Ning Xi, Kevin Yang
-
Patent number: 7915295Abstract: Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(?O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(?O)ORx, —NRxOH; —C(?O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(?O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(?O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(?O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)q-O—Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, —S(?O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8?)n-D-(CR8R8?)m-; D is a bond, —NR9—, -0-, —S—, —S(=0)- or —S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.Type: GrantFiled: December 30, 2004Date of Patent: March 29, 2011Assignee: Medivir ABInventors: Christian Sund, Nathalie Roue, Stefan Lindstrom, Dmitry Antonov, Christer Sahlberg, Katarina Jansson
-
Publication number: 20110052643Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: January 7, 2009Publication date: March 3, 2011Applicant: Synta Pharmaceuticals Corp.Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen, Lijun Sun
-
Publication number: 20110044938Abstract: Compounds of a certain formula I, in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and apoptosis inducing activity.Type: ApplicationFiled: August 15, 2007Publication date: February 24, 2011Applicant: NYCOMED GMBHInventors: Bjorn Bartels, Mathias Schmidt, Klaus Pekari, Thomas Beckers, Astrid Zimmermann, Volker Gekeler
-
Publication number: 20100311582Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
-
Patent number: 7838537Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: November 30, 2007Date of Patent: November 23, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Marc-André Poupart, Pierre Louis Beaulieu, Jean Rancourt
-
Publication number: 20100261727Abstract: 2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for ?-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight ?-amyloid peptide binding compound, generation of malignant high-molecular weight ?-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.Type: ApplicationFiled: October 15, 2009Publication date: October 14, 2010Inventors: Dae Yoon Chi, Byoung Se Lee, Youjung Jung, Uthaiwan Sirion, Yoo Jin Lim, Yu Jin Bae, Heejun Kim, So Young Chu, Dae Hyuk Moon, Jin-Sook Ryu, Jae Seung Kim, Seung Jun Oh
-
Publication number: 20100237334Abstract: Triphenylene containing benzo-fused thiophene compounds are provided. Additionally, triphenylene containing benzo-fused furan compounds are provided. The compounds may be useful in organic light emitting devices, particularly as hosts in the emissive layer of such devices, or as materials for enhancement layers in such devices, or both.Type: ApplicationFiled: August 7, 2008Publication date: September 23, 2010Applicant: UNIVERSAL DISPLAY CORPORATIONInventors: Bin Ma, Yonggang Wu, Chun Lin, Raymond Kwong
-
Publication number: 20100234428Abstract: The invention relates to substituted 2-mercapto-3-aminopyridines, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
-
Publication number: 20100210762Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: ApplicationFiled: August 15, 2008Publication date: August 19, 2010Applicant: FUJIFILM CORPORATIONInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
-
Publication number: 20100204219Abstract: The invention relates to novel compounds of formula (I) wherein X, Y, Z represent independently from one another C or N, n stands for 1, 2, 3, m is 0 or 1, p stands for 0 or an integer from 1 to 6, R1, R2 represent independently from one another hydrogen, a halogen atom, a hydroxyl group, a C1-C3 alkyl group and a C1-C3 alkoxy group, R3 represents, independently from one another if p is not 0, hydrogen, halogen, a C1-C5 linear or branched alkyl, a carboxylyl, a carbomethoxyl, carboethoxyl, a benzyl, an acyl, a hydroxyl, a C1-C4 linear or branched alkoxyl, a trifluoromethyl, a cyano, a morpholino, a 1,3-dioxolyl, an N-acetylamidyl or an amidoyl group, a saturated 5-8 membered ring, a heterocyclic ring, optionally substituted by a C1-C3 alkyl, a hydroxyl or a benzyl group, a C1-C6 alkylsulfonyl, a mono or disubstituted C1-C5 alkyl group, a branched or a cyclic amine, R6 is H or part of a alicyclic, heteroalicyclic ring system, if m is 0 then C represents CF3 or a branched or unbranched C1-C4 alkyl group, if m=1Type: ApplicationFiled: December 11, 2007Publication date: August 12, 2010Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Guy Lemaillet, Leonardo Scapozza
-
Publication number: 20100197684Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: February 9, 2010Publication date: August 5, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
-
Publication number: 20100137306Abstract: The invention relates to compounds of formulae I(a)-I(d): and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: October 22, 2009Publication date: June 3, 2010Inventor: Laykea Tafesse
-
Publication number: 20100123123Abstract: A thin-film transistor comprises a semiconducting layer comprising a semiconducting material selected from Formula (I) or (II): wherein X, R1, R2, R3, R4, R5 a, b, and n are as described herein. Semiconducting compositions of Formula (I) or (II) are also described.Type: ApplicationFiled: November 19, 2008Publication date: May 20, 2010Applicant: Xerox CorporationInventors: Yuning Li, Yiliang Wu, Ping Liu, Paul F. Smith
-
Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
-
Publication number: 20100048637Abstract: Compounds having the formula I, their methods of synthesis, and pharmaceutically acceptable salts of certain of them are provided in which the variables have the definitions described herein. Compositions including the compounds having the formula I-A in which the variables have the definitions described herein, and methods of using the compositions for the treatment of certain diseases mediated by the up-regulation of Smo are also disclosed.Type: ApplicationFiled: August 18, 2009Publication date: February 25, 2010Inventors: Shuo Lin, Zhen Yang
-
Publication number: 20100041891Abstract: A compound having GPR52 agonist activity or a salt thereof is provided. The compound can be provided as a preventive/therapeutic agent for schizophrenia or the like. The compound is represented by the following formula: wherein A represents —CONRa— or —NRaCO—, Ra represents a hydrogen atom or the like, B represents a hydrogen atom or the like, a ring Cy1 represents a six-membered aromatic ring which may have one or more substituents in addition to a group represented by -A-B, a ring Cy2 represents a six-membered ring which may be substituted with a halogen atom or the like, a ring Cy3 represents a five- or six-membered ring which may have one or more substituents; X represents C1-2 alkylene or the like, m represents an integer of 0 to 2, and a ring Cy4 represents a six-membered aromatic ring which may have one or more substituents.Type: ApplicationFiled: August 11, 2009Publication date: February 18, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Masaki Setoh, Mitsunori Kouno, Yuhei Miyanohana, Masakuni Kori