Additional Six-membered Hetero Ring Consisting Of Five Ring Carbons And One Ring Nitrogen Attached Directly Or Indirectly To The 1,3-diazine By Nonionic Bonding Patents (Class 514/252.18)
-
Publication number: 20130303461Abstract: The technology described herein is directed to methods of determining oligonucleotide sequences, e.g. by enriching target sequences prior to sequencing the sequences.Type: ApplicationFiled: March 11, 2013Publication date: November 14, 2013Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Anthony John Iafrate, Long Phi Le, Zongli Zheng
-
Publication number: 20130303526Abstract: The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: September 16, 2011Publication date: November 14, 2013Applicant: Purdue Pharma L.P.Inventors: Chiyou NI, Bin Shao, Laykea Tafesse, Jiangchao Yao, Jianming Yu, Xiaoming Zhou
-
Publication number: 20130303512Abstract: This disclosure is directed, in part, to a method of determining whether a subject having cancer is at risk for developing metastasis of the cancer. In one embodiment, the method comprises (a) obtaining a biological sample from the subject having cancer; (b) determining CCR5 expression level and/or expression level of at least one of CCR5 ligands in the biological sample; and (c) if the expression level of CCR5 and/or of at least one of CCR5 ligands determined in step (b) is increased compared to CCR5 expression level and/or expression level of at least one of CCR5 ligands in a control sample, then the subject is identified as likely at risk for developing metastasis of the cancer.Type: ApplicationFiled: May 14, 2013Publication date: November 14, 2013Inventor: Richard G. PESTELL
-
Patent number: 8580794Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: November 22, 2010Date of Patent: November 12, 2013Assignee: AbbVie Inc.Inventors: George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Andrew J. Souers, Zhi-Fu Tao, Gary T. Wang, Le Wang, Robert Mantei, Todd M. Hansen
-
Publication number: 20130296302Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.Type: ApplicationFiled: May 3, 2013Publication date: November 7, 2013Applicant: Samumed, LLCInventors: John Hood, Sunil Kumar KC, David Mark Wallace
-
Publication number: 20130296296Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.Type: ApplicationFiled: February 4, 2013Publication date: November 7, 2013Inventor: ASTRAZENECA AB
-
Publication number: 20130296327Abstract: The present invention relates to substituted heterocyclic compounds of Formula I or XI: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.Type: ApplicationFiled: July 8, 2013Publication date: November 7, 2013Inventors: Jincong Zhuo, Thomas P. Maduskuie, Ding-quan Qian, Wenqing Yao
-
Patent number: 8575163Abstract: Pyrrolopyridinylpyrimidin-2-ylamine derivatives of the formula (I), in which R1-R6 and R1 have the meanings indicated in claim 1, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: GrantFiled: November 12, 2010Date of Patent: November 5, 2013Assignee: Merck Patent GmbHInventors: Margarita Wucherer-Plietker, Christina Esdar, Brian Hodous
-
Publication number: 20130287730Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: April 24, 2013Publication date: October 31, 2013Inventors: Daniel D. Long, Robert Murray McKinnell, Lori Jean Van Orden, Gavin Ogawa, Donna Wilton
-
Publication number: 20130287833Abstract: Medical devices having a catalyst capable of catalyzing the generation of nitric oxide in vivo and methods of treating a vascular condition using the devices are provided.Type: ApplicationFiled: June 21, 2013Publication date: October 31, 2013Inventors: Thierry Glauser, Stephen D. Pacetti, Paul M. Consigny
-
Publication number: 20130289014Abstract: The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of a cell signalling and/or angiogenesis inhibitor in conjunction with an Aurora kinase inhibitor.Type: ApplicationFiled: June 28, 2013Publication date: October 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Flavio SOLCA, Ulrich GUERTLER, Ulrike TONTSCH-GRUNT
-
Patent number: 8569305Abstract: The present invention relates to the use of PDGF receptor tyrosine kinase or bcr-abl tyrosine kinase inhibitors, especially of N-phenyl-2-pyrimidine-amine derivatives of formula I, in which the symbols and substituents have the meaning as defined herein in free form or in pharmaceutically acceptable salt form, in the manufacture of a pharmaceutical composition for the treatment of tuberous sclerosis associated neoplasms; to a method of treatment of warm-blooded animals, including humans, suffering from a tuberous sclerosis associated neoplasms.Type: GrantFiled: November 22, 2006Date of Patent: October 29, 2013Assignee: Emory UniversityInventor: Jack Arbiser
-
Patent number: 8569306Abstract: Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH—R2 Or N—SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 19, 2010Date of Patent: October 29, 2013Assignee: Hoffmann-La Roche, Inc.Inventors: Bernd Buettelmann, Bindu Goyal, Wylie Solang Palmer
-
Publication number: 20130281402Abstract: The disclosure includes hydroxamic compounds of Formula I: (Formula I) wherein Z, L, R1, R2, and R3 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: ApplicationFiled: January 6, 2012Publication date: October 24, 2013Applicant: CRYSTAL BIOPHARMACEUTICAL LLCInventors: Yi Chen, Yu Chen
-
Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
-
Publication number: 20130281431Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: April 23, 2013Publication date: October 24, 2013Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
-
Publication number: 20130281429Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: March 26, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl ZAHN, Guido BOEHMELT, Andreas MANTOULIDIS, Ulrich REISER, Matthias TREU, Ulrich GUERTLER, Andreas SCHOOP, Flavio SOLCA, Ulrike TONTSCH-GRUNT, Ralph BRUECKNER, Charlotte REITHER, Lars HERFURTH, Oliver KRAEMER, Heinz STADTMUELLER, Harald ENGELHARDT
-
Publication number: 20130267491Abstract: C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKK? and/or TBK-1: in which: R1 represents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; R2 represents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of R3 and R4 independently represents a hydrogen atom or a C1-4 alkyl group.Type: ApplicationFiled: July 18, 2011Publication date: October 10, 2013Applicant: DOMAINEX LIMITEDInventors: Trevor Robert Perrior, Gary Karl Newton, Mark Richard Stewart, Rehan Aqil
-
Publication number: 20130267533Abstract: A method of treating and/or lowering elevated cholesterol by administering a therapeutically effective amount of at least one 5HT1A receptor agonist to a subject in need thereof as either a short term or long term therapy. Also, a method of maintaining clinically acceptable cholesterol levels, or cholesterol levels below an elevated amount, by administering a therapeutically effective amount of at least one 5HT1A receptor agonist to a subject in need thereof as either a short term or long term therapy.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Applicant: FABRE-KRAMER PHARMACEUTICALS, INC.Inventors: Louis F. FABRE, Stephen J. KRAMER, Lou SMITH
-
Patent number: 8546390Abstract: Compounds of the formula (I), in which R1, R2, R3 and R4 have the meanings indicated in claim (1), are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumors.Type: GrantFiled: May 23, 2008Date of Patent: October 1, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Margarita Wucherer-Plietker, Lars T. Burgdorf, Christian Sirrenberg, Christina Esdar, Thomas J. J. Mueller, Eugen Merkul
-
Patent number: 8546399Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: GrantFiled: May 26, 2010Date of Patent: October 1, 2013Assignee: Abbvie Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
-
Publication number: 20130251702Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: SNU R&DB FOUNDATIONInventors: Doo Hyun CHUNG, Sae Jin OH, Ji Hyung KIM
-
Publication number: 20130252941Abstract: The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy.Type: ApplicationFiled: May 16, 2013Publication date: September 26, 2013Applicant: F. Hoffmann-La Roche AGInventors: Toby Blench, Simon Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven Magnuson, Vickie Tsui, Karen Williams, Birong Zhang
-
Publication number: 20130252939Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 30, 2013Publication date: September 26, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, John Studley, Ronald Knegtel, Luca Settimo, Christopher John Davis, Damien Fraysse, Philip N. Collier, Guy Brenchley, Dean Boyall, Andrew Miller, Heather Twin, Stephen Young
-
Publication number: 20130243754Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: ApplicationFiled: December 20, 2012Publication date: September 19, 2013Applicant: TARGEGEN, INC.Inventors: Wolfgang WRASIDLO, Elena DNEPROVSKAIA
-
Publication number: 20130244999Abstract: The present invention relates to substituted heterocyclic compounds of Formula I: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.Type: ApplicationFiled: May 6, 2013Publication date: September 19, 2013Applicant: Incyte CorporationInventors: Colin Zhang, Ding-quan Qian, Jincong Zhuo, Wenqing Yao
-
Patent number: 8536180Abstract: Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, L1, R2, R3, n, p, Ar1, and Ar2 are defined in the description. Methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-1R are also disclosed.Type: GrantFiled: May 26, 2010Date of Patent: September 17, 2013Assignee: AbbVie Inc.Inventors: Richard F. Clark, Nwe Y. Ba-maung, Scott A. Erickson, Steve D. Fidanze, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang, Randy L. Bell
-
Publication number: 20130237516Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: April 25, 2013Publication date: September 12, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Wannamaker W. Wannamaker, Tiansheng Wang
-
Publication number: 20130236511Abstract: The present invention provides methods for impregnating a porous carrier with an active pharmaceutical ingredient (“AP”), the methods comprising steps: a) dissolving at least one API in a solvent to form an API solution; b) contacting a porous carrier with the at least one API of step (a) in a contactor to form an API impregnated porous carrier; and c) drying the at least one API impregnated porous carrier.Type: ApplicationFiled: August 19, 2011Publication date: September 12, 2013Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Fernando J. Muzzio, Benjamin J. Glasser, Plamen I. Grigorov
-
Publication number: 20130231336Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.Type: ApplicationFiled: February 13, 2013Publication date: September 5, 2013Applicant: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
-
Publication number: 20130230511Abstract: Copy number gains detected in tumors and associated with drug sensitivity and resistance in vivo and in vitro can be used as biomarkers to select, predict and monitor drug treatment outcomes in cancer patients treated with tyrosine kinase inhibitors. Methods to identify patients with NSCLC or other malignancies who are more likely to benefit from tyrosine kinase inhibitors such as VEGF or VEGFR inhibitors when used either as monotherapy or in combination with other therapies such as chemotherapy or EGFR inhibitors, and who are in the advanced stages of disease and/or who have undergone adjuvant therapy are also provided herein.Type: ApplicationFiled: February 4, 2013Publication date: September 5, 2013Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventor: Board of Regents, The University of Texas System
-
Publication number: 20130225596Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 9, 2011Publication date: August 29, 2013Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
-
Publication number: 20130225598Abstract: The invention relates to the stabilized amorphous form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)-pyrimidin-2-ylamino)-pheny]-benzamide, pharmaceutical compositions such as capsules or tablets containing this form, the use of such form in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans, and the use of formulation principles stabilizing the amorphous form of Imatinib mesylate as an intermediate for the preparation of pharmaceutical compositions.Type: ApplicationFiled: April 17, 2013Publication date: August 29, 2013Applicant: Novartis AGInventors: Elisabete Goncalves, Oskar Kalb, Michael Mutz, Wolfgang Wirth, Jay Parthiban Lakshman
-
Publication number: 20130224186Abstract: Disclosed are new substituted oxazole and thiazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: ApplicationFiled: April 13, 2011Publication date: August 29, 2013Inventors: Paul A. Barsanti, Yu Ding, Wooseok Han
-
Publication number: 20130224288Abstract: The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, certain processes for their preparation, pharmaceutical compositions containing these crystal forms, their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.Type: ApplicationFiled: July 15, 2011Publication date: August 29, 2013Inventor: Michael Mutz
-
Publication number: 20130225575Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from certain neurological conditions.Type: ApplicationFiled: June 16, 2011Publication date: August 29, 2013Applicant: AFRAXIS, INC.Inventors: Jay Lichter, David Campbell, Sergio G. Duron, Benedikt Vollrath
-
Publication number: 20130225555Abstract: The present invention provides compounds of formula (I) wherein Ra, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: March 14, 2013Publication date: August 29, 2013Applicants: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca ABInventors: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
-
Publication number: 20130224195Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: April 3, 2013Publication date: August 29, 2013Inventors: Abran Costales, Teresa Hansen, Barry H. Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Joelle Verhagen
-
Publication number: 20130225553Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: ApplicationFiled: March 7, 2013Publication date: August 29, 2013Applicant: ASTELLAS PHARMA INC.Inventor: ASTELLAS PHARMA INC.
-
Publication number: 20130224255Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.Type: ApplicationFiled: February 23, 2012Publication date: August 29, 2013Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Paul M. Consigny
-
Publication number: 20130216498Abstract: New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: December 23, 2010Publication date: August 22, 2013Inventors: Paul Robert Eastwood, Jacob Gonzales Rodriguez, Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Juan Francisco Caturla Javaloyes, Victor Giulio Matassa
-
Patent number: 8513237Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: March 21, 2012Date of Patent: August 20, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noëlle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
-
Patent number: 8513256Abstract: The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(?) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.Type: GrantFiled: February 8, 2012Date of Patent: August 20, 2013Assignee: Novartis AGInventors: Hans Michael Bürger, Paul William Manley, Michael Mutz
-
Patent number: 8513233Abstract: The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compounds. The compounds are useful as PPAR? agonist, through activating PPAR-RXR heterodimers that interacts with specific DNA response elements within promoter regions of target gene, particularly in the treatment and prevention of polycystic kidney and cancer.Type: GrantFiled: October 11, 2007Date of Patent: August 20, 2013Assignee: Shanghai Institute of Materia Medica, CASInventors: Jianhua Shen, Changlin Mei, Hualiang Jiang, Bin Dai, Yangliang Ye, Xishan Xiong, Jing Tang, Lili Fu
-
Publication number: 20130209488Abstract: The present invention relates to methods, compositions, and diagnostic tests for treating and diagnosing cancer and other related diseases that result in dysregulation of malic enzyme 2. In particular, the methods and compositions include combination therapy, such as with a combination of two or more ME2 inhibitors or a combination of an ME2 inhibitor and an anticancer agent.Type: ApplicationFiled: August 5, 2011Publication date: August 15, 2013Applicant: BETH ISRAEL DEACONESS MEDICAL CENTER, INCInventors: Vikas P. Sukhatme, Jian-Guo Ren
-
Publication number: 20130210771Abstract: This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.Type: ApplicationFiled: February 13, 2013Publication date: August 15, 2013Applicant: IRM LLCInventor: Novartis AG
-
Publication number: 20130210818Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: February 14, 2012Publication date: August 15, 2013Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
-
Publication number: 20130210800Abstract: The present application relates to compounds of Formula (I), and Formula (II), or pharmaceutically acceptable salt thereof, wherein A, X, Y, Z, e, f, R1, R2, R3, R4, R5, R5b, R6, R7, R8, R9, R10, R11, R20, R21, R22 and R23 are defined herein. These novel pyridine derivatives that are useful in therapy, in particular for treating diseases or conditions mediated by Smo, including the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to methods of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: October 19, 2011Publication date: August 15, 2013Applicant: PFIZER INC.Inventors: Sajiv Krishnan Nair, Simon Paul Planken
-
Publication number: 20130210811Abstract: Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11?-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11?-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human-derived 11?-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LADA), insulin tolerance syndromes, obesity, impaired glucose tolerance (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.Type: ApplicationFiled: May 4, 2011Publication date: August 15, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Je Ho Ryu, Shin Ae Kim, Keun Ho Ryu, Jae Sun Kim, Nam Ho Kim, Hye Young Han, Yong Hyuk Kim, Won-No Youn, Yoon-Jung Lee, Hyun Joo Son, Bong-Yong Lee, Sung Hoon Park, Ju Young Lee, Hyun Jung Lee, Hoe Chul Jung, Young Ah Shin, Jung A Lee, Bo Ram Lee, Joon Ho Sa
-
Patent number: 8507485Abstract: A method of treating a disease associated with angiogenesis by administering a therapeutically effective amount of a compound represented by the formula (1) or a salt thereof wherein the ring X represents R1 and R2 independently represent a hydrogen atom, an alkyl, an aryl or an aromatic heterocyclic; R3 represents a hydrogen atom, a halogen atom, a hydroxy, an alkoxy, an aryloxy, an alkyl, an aryl, an amino, an alkylamino, a cycloalkylamino, an arylamino, an alkylcarbonylamino, an arylcarbonylamino, a mercapto, an alkylthio, an arylthio, an alkylsulfinyl or a nonaromatic heterocyclic; A1 represents a sulfur atom, a sulfinyl or a sulfonyl; and A2 represents an alkylene.Type: GrantFiled: January 24, 2011Date of Patent: August 13, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hisashi Tajima, Takahiro Honda, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto