Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/366)
-
Patent number: 8569347Abstract: Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.Type: GrantFiled: May 20, 2004Date of Patent: October 29, 2013Assignee: Bristol-Myers Squibb CompanyInventor: Francis Y. F. Lee
-
Publication number: 20130281497Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as methods of modulating bone processes, and methods of treating bone-related disease, disorders, and symptoms thereof.Type: ApplicationFiled: May 23, 2011Publication date: October 24, 2013Applicants: University of Florida Research Foundation, Inc., Korea Research Institute of Chemical Technology, Duke UniversityInventors: Hendrik Luesch, Jiyong Hong, Seong Hwan Kim
-
Patent number: 8557810Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: January 24, 2012Date of Patent: October 15, 2013Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
-
Publication number: 20130267543Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 8, 2011Publication date: October 10, 2013Applicants: CHAPERONE THERAPEUTICS, INC., DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
-
Patent number: 8552037Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.Type: GrantFiled: October 23, 2012Date of Patent: October 8, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Tatsuki Koike, Yasutaka Hoashi, Takafumi Takai
-
Patent number: 8551963Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: November 5, 2009Date of Patent: October 8, 2013Assignee: Ambit Biosciences CorporationInventors: Julius L. Apuy, Darren E. Insko, Joyce J. James
-
Publication number: 20130252962Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: March 6, 2013Publication date: September 26, 2013Inventors: Mikhail CHAFEEV, Sultan CHOWDHURY, Lauren FRASER, Jianmin FU, Jonathan LANGILLE, Shifeng LIU, Jianyu SUN, Shaoyi SUN, Serguei SVIRIDOV, Mark WOOD, Alla Yurevna ZENOVA, Qi JIA, Jean-Jacques Alexandre CADIEUX, Simon J. GAUTHIER, Amy Frances DOUGLAS, Tom HSIEH, Nagasree CHAKKA, Zoran CIKOJEVIC
-
Publication number: 20130236447Abstract: Inhibition of eIF-2? phosphorylation can be used to improve cognitive function and/or to treat dementia, including Alzheimer's Disease. In particular, this can be achieved by inhibiting the kinase activity of PKR in a non-toxic manner.Type: ApplicationFiled: December 17, 2012Publication date: September 12, 2013Applicant: CARMEL-HAIFA UNIVERSITY ECONOMIC CORP., LTD.Inventors: Yaacov ROSENBLUM, Elad STERN, Yifat SEGEV
-
Publication number: 20130217666Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: February 15, 2013Publication date: August 22, 2013Applicant: Genentech, Inc.Inventor: Genentech, Inc.
-
Patent number: 8513290Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.Type: GrantFiled: June 7, 2012Date of Patent: August 20, 2013Assignees: Colorado State University Research Foundation, Dana-Farber Cancer Institute, Inc., University of Notre Dame du LacInventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Olaf G. Wiest
-
Patent number: 8501793Abstract: It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.Type: GrantFiled: September 24, 2010Date of Patent: August 6, 2013Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Yoshihisa Kamanaka, Hidekazu Matsuya
-
Publication number: 20130184218Abstract: A targeted osmotic lysis (TOL) of tumor cells that over-express voltage-gated sodium channels (VGSCs) has been developed that uses a combined therapy of a drug that blocks sodium, potassium-adenosine triphosphatase (Na+, K+-ATPase) that is then followed by an activation of VGSCs, for example, by electrical or pharmacological stimulation. Activation of VGSCs conducts sodium into the cancer cells in much greater amounts than non-cancer cells. Water follows this sodium gradient into the cancer cells, causing swelling and lysis. Because non-cancerous cells do not over-express VGSCs, less sodium and less water will enter the cells, and the non-cancerous cells will not lyse. This method is applicable to all cells that over-express VGSCs, including, but not limited to, highly invasive breast cancer, prostate cancer, small cell lung cancer, non-small cell lung carcinoma, lymphoma, mesothelioma, neuroblastoma, and cervical cancer.Type: ApplicationFiled: July 19, 2012Publication date: July 18, 2013Inventors: Dennis J. Paul, Harry J. Gould
-
Publication number: 20130178505Abstract: Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.Type: ApplicationFiled: June 28, 2011Publication date: July 11, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Michael Chorev, Bertal Huseyin Aktas, Jose A. Halperin, Gerhard Wagner
-
Publication number: 20130158082Abstract: The disclosure relates to methods of managing blood sugar levels and compositions related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diabetes, insulin resistance, or hyperglycemia comprising administering to a subject diagnosed with, at risk of or exhibiting symptoms of diabetes, insulin resistance, or hyperglycemia a pharmaceutical composition comprising a compound comprising formula I.Type: ApplicationFiled: September 27, 2011Publication date: June 20, 2013Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
-
Publication number: 20130143910Abstract: A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.Type: ApplicationFiled: November 14, 2012Publication date: June 6, 2013Inventor: Zhang Weihua
-
Publication number: 20130123263Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 10, 2013Publication date: May 16, 2013Applicants: F. HOFFMANN - LA ROCHE AG, GENENTECH, INC.Inventors: GENENTECH, INC., F. HOFFMANN - LA ROCHE AG
-
Patent number: 8426372Abstract: The invention relates to novel fungicidally active compound combinations of 2?-cyano-3,4-dichloroisothiazole-5-carboxanilide of the formula and active compounds listed in the disclosure.Type: GrantFiled: May 13, 2010Date of Patent: April 23, 2013Assignee: Bayer Cropscience AGInventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Rolf Pontzen, Lutz Assmann, Haruko Sawada
-
Patent number: 8420679Abstract: Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotrophin releasing factor (CRF) antagonists.Type: GrantFiled: April 25, 2007Date of Patent: April 16, 2013Assignee: SanofiInventors: Evelyne Fontaine, Michel Geslin, Danielle Gully, Antoine Pradines, Pierre Roger
-
Publication number: 20130090360Abstract: Method for protecting rice from being infected by harmful fungi, wherein the fungi, their habitat, rice plants, their seed, rice plant propagation material or the soil on which rice is grown or intended to be grown, is treated with epoxiconazole and tricyclazole in synergistically effective amounts; use of a composition comprising epoxiconazole, tricyclazole and optionally a further commercially available fungicide, for preparing a composition suitable for protecting rice from being infected by harmful fungi.Type: ApplicationFiled: June 17, 2011Publication date: April 11, 2013Applicant: BASF SEInventor: Reinhard Stierl
-
Publication number: 20130085143Abstract: Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.Type: ApplicationFiled: November 28, 2012Publication date: April 4, 2013Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE LORRAINE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S), UNIVERSITAT DE BARCELONA, ORESTE PICCOLO STUDIO DI CONSULENZA SCIENTIFICAInventors: Universite D'aix-Marseille, Universite De Lorraine, Oreste Piccolo Studio Di Consulenza Scientifica, Universitat De Barcelona, Centre National De La Recherche Scientifique (C.
-
Publication number: 20130079374Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.Type: ApplicationFiled: October 23, 2012Publication date: March 28, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: TAKEDA PHARMACEUTICAL COMPANY LIMITE
-
Patent number: 8399495Abstract: Novel metabolites of talarazole of formula (I) have been isolated and characterized, wherein R?H, OH, OSO3H or O-gly; R1, ?H, OH, OSO3H, O-gly or =0; and gly=a glucuronate, or a pharmaceutically acceptable salt thereof. These compounds are targeted for the treatment of various skin-, hair- and nail-associated disorders.Type: GrantFiled: May 21, 2012Date of Patent: March 19, 2013Assignee: Stiefel Laboratories, Inc.Inventor: Debra Barrett
-
Patent number: 8389736Abstract: The invention provides compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The compositions pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The compositions and pharmaceutical preparations of the invention may comprise one or more bithiazole-containing compounds of the invention, or an analog or derivative thereof.Type: GrantFiled: September 5, 2008Date of Patent: March 5, 2013Assignee: The Regents of the University of CaliforniaInventors: Mark J. Kurth, Alan S. Verkman
-
Patent number: 8357690Abstract: Provided herein are methods of treating a proliferative disease in a subject, comprising administering to the subject a therapeutically effective amount of AC220 and a nucleoside analog, a topoisomerase inhibitor or an anthracycline, or a combination thereof.Type: GrantFiled: March 23, 2010Date of Patent: January 22, 2013Assignee: Ambit Biosciences CorporationInventors: Robert C. Armstrong, Barbara A. Belli
-
Patent number: 8357707Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: July 2, 2010Date of Patent: January 22, 2013Assignee: Novartis AGInventors: Robin Alec Fairhurst, Marc Gerspacher, Robert Mah
-
Patent number: 8357708Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.Type: GrantFiled: December 20, 2011Date of Patent: January 22, 2013Assignees: University of Florida Resesarch Foundation, Inc., Smithsonian InstitututionInventors: Hendrik Luesch, Taori Kanchan, Valerie J. Paul
-
Publication number: 20130012488Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 7, 2012Publication date: January 10, 2013Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
-
Patent number: 8349879Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.Type: GrantFiled: March 14, 2011Date of Patent: January 8, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Tatsuki Koike, Yasutaka Hoashi, Takafumi Takai
-
Publication number: 20120322770Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: ApplicationFiled: August 21, 2012Publication date: December 20, 2012Inventor: Robert P. RICCIARDI
-
Patent number: 8334262Abstract: Inhibition of eIF-2? phosphorylation can be used to improve cognitive function and/or to treat dementia, including Alzheimer's Disease. In particular, this can be achieved by inhibiting the kinase activity of PKR in a non-toxic manner.Type: GrantFiled: June 30, 2010Date of Patent: December 18, 2012Assignee: Carmel-Haipa University Economic Corp. Ltd.Inventors: Yaacov Rosenblum, Elad Stern, Yifat Segev
-
Publication number: 20120316157Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more heterocyclic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.Type: ApplicationFiled: March 2, 2011Publication date: December 13, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
-
Patent number: 8318784Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.Type: GrantFiled: March 14, 2011Date of Patent: November 27, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Uchikawa, Tatsuki Koike, Yasutaka Hoashi, Takafumi Takai
-
Patent number: 8309582Abstract: Bcl-xL/Bcl-2 binding inhibitors useful in the treatment of unwanted proliferating cells, including cancers and precancers, in subjects in need of such treatment. Also provided are methods of treating a subject having unwanted proliferating cells comprising administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject in need of such treatment. Also provided are methods of preventing the proliferation of unwanted proliferating cells, such as cancers and precancers, in a subject comprising the step of administering a therapeutically effective amount of a Bcl-xL/Bcl-2 binding inhibitor described herein to a subject at risk of developing a condition characterized by unwanted proliferating cells.Type: GrantFiled: January 5, 2010Date of Patent: November 13, 2012Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Chung-Wai Shiau
-
Patent number: 8304556Abstract: 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 characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: January 11, 2012Date of Patent: November 6, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Darryl McConnell, Maria Impagnatiello, Dirk Kessler, Oliver Kraemer, Siegfried Schneider, Lars Van Der Veen, Ulrike Weyer-Czernilofsky, Tobias Wunberg
-
Publication number: 20120276047Abstract: The present invention relates to novel fused tricyclic compounds, compositions comprising at least one fused tricyclic compound, and methods of using fused tricyclic compounds for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 23, 2010Publication date: November 1, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge
-
Publication number: 20120264794Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.Type: ApplicationFiled: June 7, 2012Publication date: October 18, 2012Applicants: DANA-FARBER CANCER INSTITUTE, INC., COLORADO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Ann E. Youngman
-
Publication number: 20120245166Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.Type: ApplicationFiled: October 14, 2010Publication date: September 27, 2012Applicant: Southern Research InstituteInventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
-
Patent number: 8263631Abstract: Method of treating persons having carcinoma, sarcoma or hematopoietic cancer by administering (i) a compound of the formula (I) and (ii) an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and pharmaceutical compositions for use in said method. A method for treating gastric cancer, colon cancer, lung cancer, breast cancer, pancreas cancer, kidney cancer, prostate cancer, medulloblastoma, rhabdomyosarcoma, Ewing sarcoma, liposarcoma, multiple myeloma and leukemia by administering a compound of the formula (I).Type: GrantFiled: July 30, 2008Date of Patent: September 11, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Kosaku Fujiwara, Naomi Shimazaki
-
Patent number: 8247401Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: GrantFiled: October 29, 2008Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
-
Publication number: 20120196852Abstract: The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.Type: ApplicationFiled: August 5, 2010Publication date: August 2, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun O. Liu, Omonike Arike Olaleye, Shridhar Bhat
-
Publication number: 20120178750Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Subharekha Raghavan, Steven L. Colletti, Fa-Xiang Ding, Hong Shen, James R. Tata, Ashley Rouse Lins, Abigail Lee Smenton, Weichun Chen, Darby Rye Schmidt, George Scott Tria
-
Publication number: 20120172402Abstract: Substituted tricyclic diproline analogues of the formula (I): wherein the variables are as defined herein. Also disclosed are methods for the production thereof, the use thereof for the induction of an alpha-helix conformation in peptides and/or proteins, pharmaceuticals containing said compounds, methods for the production of a peptide library containing said compounds, and peptide libraries containing said compounds.Type: ApplicationFiled: July 9, 2010Publication date: July 5, 2012Applicants: FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITAT ZU KOLNInventors: Hans-Günther Schmalz, Ronald Kuhne, Verena Hack, Cédric Reuter
-
Patent number: 8203001Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: GrantFiled: June 13, 2007Date of Patent: June 19, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
-
Patent number: 8188124Abstract: Novel metabolites of talarazole of formula (I) have been isolated and characterized, wherein R?H, OH, OSO3H or O-gly; R1, ?H, OH, OSO3H, O-gly or =0; and gly=a glucuronate, or a pharmaceutically acceptable salt thereof. These compounds are targeted for the treatment of various skin-, hair- and nail-associated disorders.Type: GrantFiled: October 17, 2007Date of Patent: May 29, 2012Assignee: Stiefel Laboratories, Inc.Inventor: Debra Barrett
-
Publication number: 20120129850Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: ApplicationFiled: January 24, 2012Publication date: May 24, 2012Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
-
Publication number: 20120129811Abstract: This invention relates to tricycle I and its therapeutic and prophylactic uses, wherein the variables C1, C2, Z1, Z2, Q, J, R1, and R3 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Aihua WANG, Yan Zhang, Kristi Anne Leonard, Michael Hawkins, Brett Andrew Tounge, Umar S.M. Maharoof, Joseph Kent Barbay
-
Publication number: 20120122852Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: ApplicationFiled: January 24, 2012Publication date: May 17, 2012Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
-
Publication number: 20120108618Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X 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 medicament having the above-mentioned properties.Type: ApplicationFiled: April 22, 2010Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl Mcconnell, Siegfried Schneider, Matthias Grauert, Andreas Schoop, Tobias Wunberg
-
Publication number: 20120095065Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.Type: ApplicationFiled: December 20, 2011Publication date: April 19, 2012Applicant: University of Florida Research Foundation, Inc.Inventors: Hendrik Luesch, Taori Kanchan, Valerie J. Paul
-
Patent number: 8148411Abstract: The present invention relates to 2-hetarylthiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereofType: GrantFiled: December 9, 2008Date of Patent: April 3, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Ulrich Bothe, Arne Von Bonin, Duy Nguyen, Ulf Bomer, Judith Guenther