The Additional Ring Is A Hetero Ring Patents (Class 514/326)
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Publication number: 20150126486Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.Type: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Atsushi NAGANAWA, Kensuke KUSUMI, Kazuhiro OTSUKI, Tetsuya SEKIGUCHI, Akito KAKUUCHI, Koji SHINOZAKI, Hiroshi YAMAMOTO, Shigeyuki NONAKA
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Publication number: 20150126518Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.Type: ApplicationFiled: October 30, 2014Publication date: May 7, 2015Applicant: HANALL BIOPHARMA CO., LTD.Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
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Publication number: 20150119376Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.Type: ApplicationFiled: April 12, 2012Publication date: April 30, 2015Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
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Publication number: 20150119366Abstract: Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.Type: ApplicationFiled: March 27, 2013Publication date: April 30, 2015Inventors: Yanming Du, Xiaodong Xu, Hong Ye, Jinhong Chang, Timothy M. Block
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Patent number: 9018224Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: November 9, 2012Date of Patent: April 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
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Patent number: 9018200Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: GrantFiled: October 18, 2012Date of Patent: April 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
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Patent number: 9018380Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: GrantFiled: August 23, 2013Date of Patent: April 28, 2015Assignee: Boar of Regents, The University of Texas SystemInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Christopher L. Carroll, Joe Marszalek, Barbara Czako, Ryan Johnson, Jay Theroff
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Publication number: 20150111922Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conditions.Type: ApplicationFiled: May 29, 2013Publication date: April 23, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Colm Carroll, Anne Goldby, Martin Teall
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Publication number: 20150111893Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.Type: ApplicationFiled: May 9, 2013Publication date: April 23, 2015Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
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Patent number: 9012362Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: GrantFiled: August 19, 2014Date of Patent: April 21, 2015Assignee: Bayer Intellectual Property GmbHInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20150105424Abstract: Compositions, systems and methods for administration of small volume sufentanil drug dosage forms to the sublingual mucosa of a subject for treatment of pain using a device are disclosed.Type: ApplicationFiled: October 17, 2014Publication date: April 16, 2015Applicant: AcelRx Pharmaceuticals, Inc.Inventors: Pamela Palmer, Thomas Schreck, Stelios Tzannis, Larry Hamel, Andrew I. Poutiatine
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Publication number: 20150105354Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLCInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
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Patent number: 9006268Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: GrantFiled: June 6, 2011Date of Patent: April 14, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: John S. Debenham, Jinlong Jiang, Christina B. Madsen-Duggan, Dong-Ming Shen
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Patent number: 9006446Abstract: This document discloses molecules having the following formula (“Formula I”):Type: GrantFiled: November 14, 2012Date of Patent: April 14, 2015Assignee: Dow AgroSciences LLCInventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl Deamicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, Jr., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
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Patent number: 9006228Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: June 11, 2012Date of Patent: April 14, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
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Publication number: 20150099733Abstract: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.Type: ApplicationFiled: December 11, 2014Publication date: April 9, 2015Applicant: AJINOMOTO CO., INC.Inventors: Takahiro KOSHIBA, Munetaka TOKUMASU, Taisuke ICHIMARU, Koji OHSUMI, Tadakiyo NAKAGAWA, Tatsuhiro YAMADA, Kayo MATSUMOTO, Tamotsu SUZUKI
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Publication number: 20150099785Abstract: The present invention provides compositions containing efinaconazole, butylated hydroxytoluene, a salt of ethylenediaminetetraacetic acid, and optional citric acid. The compositions exhibit stable color profiles and are useful in the treatment of fungal infections.Type: ApplicationFiled: October 2, 2014Publication date: April 9, 2015Inventors: Varsha Bhatt, Nayan Desai, Radhakrishnan Pillai
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Patent number: 9000174Abstract: The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: October 14, 2005Date of Patent: April 7, 2015Assignee: Purdue Pharma L.P.Inventors: Elfrida R. Benjamin, Zhengming Chen, Deyou Sha, Laykea Tafesse, Samuel F. Victory, John W. F. Whitehead
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Patent number: 9000010Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.Type: GrantFiled: January 19, 2011Date of Patent: April 7, 2015Assignee: SanofiInventors: Ahmed Abouabdellah, Antoine Ravet
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Publication number: 20150094337Abstract: The present invention provides a heterocyclic group contained amino-methanol derivative, and salt, a preparation method and use thereof, and belongs to the medical field. The heterocyclic group contained amino-methanol derivative and the salt thereof of the present invention are used for preparing medicines for immune suppression and for the treatment of organ transplant rejection, or medicines for treating immune mediated inflammatory diseases, such as multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventors: Xingmin Zhang, Ensi Wang, Jing Guo, Shengxiu Niu, Zhuolin Dai, Nan Zheng, Liping Ji, Zhenfang Wang, Tie Liang
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Publication number: 20150094520Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Sanath K. MEEGALLA, M. Jonathan RUDOLPH, Mark J. WALL, Kenneth J. WILSON, Renee Louise DESJARLAIS, Carl M. MANTHEY, Christopher J. MOLLOY
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Publication number: 20150094284Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.Type: ApplicationFiled: December 3, 2014Publication date: April 2, 2015Inventors: Jean-Luc GIRARDET, Yung-Hyo KOH, Martha DE LA ROSA, Esmir GUNIC, Zhi HONG, Stanley LANG, Woo-Hong KIM
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Patent number: 8993556Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 16, 2010Date of Patent: March 31, 2015Assignee: Nerviano Medical Sciences S.R.L.Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
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Patent number: 8993597Abstract: Provided are peptides, compositions thereof, and methods for treating or preventing dyslipidemia, a cardiovascular disease, endothelial dysfunction, a macrovascular disorder, or a microvascular disorder.Type: GrantFiled: February 13, 2013Date of Patent: March 31, 2015Assignee: Cerenis Therapeutics Holding SAInventors: Jean-Louis Dasseux, Anna Shenderova Schwendeman, Lingyu Zhu
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Patent number: 8993567Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: March 27, 2014Date of Patent: March 31, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
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Publication number: 20150087675Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds corresponding to general formula (I) are disclosed. Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.Type: ApplicationFiled: October 26, 2012Publication date: March 26, 2015Applicant: GLADERMA RESEARCH & DEVELOPMENTInventors: Branislav Musicki, Jerôme Aubert, Patricia Rossio, Marlène Schuppli-Nollet, Laurence Clary, Jean-Guy Boiteau
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Publication number: 20150087629Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein saidType: ApplicationFiled: December 5, 2014Publication date: March 26, 2015Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
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Publication number: 20150087642Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Inventors: Bronislava GEDULIN, Andrew A. YOUNG, Howard E. GREENE
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Publication number: 20150087628Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.Type: ApplicationFiled: April 10, 2013Publication date: March 26, 2015Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
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Patent number: 8987313Abstract: The present application provides for a compound of formula I, or a salt thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional therapeutic agent.Type: GrantFiled: December 20, 2011Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Hon Chung Hui, Hongtao Liu, Jianyu Sun, Lianhong Xu
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Patent number: 8987248Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumor disorders.Type: GrantFiled: March 12, 2010Date of Patent: March 24, 2015Assignee: Bayer Intellectual Property GmbHInventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
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Patent number: 8987276Abstract: The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: March 22, 2012Date of Patent: March 24, 2015Assignees: Janssen Pharmaceuticals, Inc., Cellzome LimitedInventors: Francois Paul Bischoff, Adriana Ingrid Velter, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
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Publication number: 20150080364Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.Type: ApplicationFiled: March 15, 2013Publication date: March 19, 2015Applicants: Abide Therapeutics, Inc., The Scripps Research InsitituteInventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
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Publication number: 20150080349Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: ApplicationFiled: July 10, 2014Publication date: March 19, 2015Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL
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Publication number: 20150080296Abstract: Nutritive proteins are provided. In some embodiments the nutritive proteins comprise a protein digestibility corrected amino acid score (PDCAAS) that exceeds a benchmark protein. Also provided are nucleic acids encoding the proteins, recombinant microorganisms that make the proteins, methods of making the proteins using recombinant microorganisms, compositions that comprise the proteins, and methods of using the proteins, among other things.Type: ApplicationFiled: March 15, 2013Publication date: March 19, 2015Inventors: Nathaniel W. Silver, Geoffrey von Maltzahn, Michael J. Hamill, David Arthur Berry
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Publication number: 20150072970Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: ApplicationFiled: May 19, 2014Publication date: March 12, 2015Applicant: MELINTA THERAPEUTICS, INC.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Publication number: 20150072959Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
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Publication number: 20150073020Abstract: Methods and compositions for treating disorders of the nail and nail bed. Such compositions contain a vehicle in which all components of the composition are dissolved, suspended, dispersed, or emulsified, a non-volatile solvent, a wetting agent, and a pharmaceutically active ingredient that is soluble in the non-volatile solvent and/or a mixture of the vehicle and the non-volatile solvent, which composition has a surface tension of 40 dynes/cm or less and has continuing spreadability, and which composition is effective in treating a disorder of the nail or nail bed.Type: ApplicationFiled: September 19, 2014Publication date: March 12, 2015Inventors: Gareth Winckle, Gregory T. Fieldson
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Publication number: 20150072006Abstract: The invention relates to drug preparations with controlled active ingredient released in the form of microtablets which contain, as active ingredient, flupirtin or one of its physiologically compatible salts, and to processes for their production.Type: ApplicationFiled: March 1, 2013Publication date: March 12, 2015Inventors: Katrin Moschner, Torsten Hoffmann, Mario Weingart, Annegret Hildebrand-Cyrener
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Publication number: 20150065541Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X and G are each as defined in the description, and agrochemically active salts, metal complexes and N-oxides thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: September 12, 2014Publication date: March 5, 2015Inventors: Pierre CRISTAU, Sebastian HOFFMANN, Joachim KLUTH, Tomoki TSUCHIYA, Pierre WASNAIRE, Jurgen BENTING, Daniela PORTZ, Ulrike WACHENDORFF-NEUMANN, Stefan Hillebrand
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Publication number: 20150065519Abstract: This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.Type: ApplicationFiled: August 28, 2014Publication date: March 5, 2015Inventors: Sarvajit Chakravarty, Roopa Rai, Son Minh Pham, Brahmam Pujala, Ramniwas Jangir, Rambabu Guguloth, Vijay Kumar Sharma
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Publication number: 20150065542Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Inventors: Allan C. Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
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Publication number: 20150057278Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.Type: ApplicationFiled: September 10, 2012Publication date: February 26, 2015Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
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Patent number: 8962658Abstract: The present invention relates to compounds of Formula (I) wherein R1 is chosen among the following radicals: and n=1 or 2 and m=1 or 2 with the proviso that m=2 when R1 is The present invention also relates to the use thereof as drugs, more particularly in the treatment of mycobacterial infections and more particularly in the treatment of tuberculosis.Type: GrantFiled: October 24, 2012Date of Patent: February 24, 2015Assignee: Universite de Droit et de la Sante de Lille 2Inventors: Benoit Deprez, Nicolas Willand, Marion Flipo, Matthieu Desroses, Alain Baulard, Florence Leroux
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Patent number: 8962676Abstract: The present invention is directed to the treatment of demyelination as an underlying cause of the disease of multiple sclerosis (MS) in a mammal, the method comprising promoting remyelination of myelination of axonal cells by administering to the mammal a 2-oxopyrrolidine compound having a general formula I: wherein R?R??H, and R??CH2CONH-(2,6CH3)C6H3 or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 22, 2010Date of Patent: February 24, 2015Assignee: University College Dublin, National University of Ireland, DublinInventors: Mark Pickering, Keith Murphy
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Patent number: 8962846Abstract: Melanocortin receptor antagonist compounds, processes for preparing them and uses thereof in human medicine and cosmetics are described. Melanocortin receptor antagonist compounds corresponding to the general formula (I): compositions containing them, and processes for their preparation and their use in pharmaceutical or cosmetic compositions are also described.Type: GrantFiled: November 4, 2009Date of Patent: February 24, 2015Assignee: Galderma Research & DevelopmentInventors: Claire Bouix-Peter, Isabelle Carlavan, Catherine Soulet, Veronique Parnet, Johannes Voegel
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Publication number: 20150051193Abstract: Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.Type: ApplicationFiled: October 5, 2012Publication date: February 19, 2015Inventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
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Publication number: 20150051248Abstract: The present invention is directed to imidazolyl methyl piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: ApplicationFiled: March 26, 2013Publication date: February 19, 2015Inventors: Craig W. Lindsley, William D. Shipe
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Publication number: 20150051249Abstract: This disclosure features compounds and pharmaceutically acceptable salts thereof that inhibit MCL-1 and/or BFL-1/A1 and compositions containing the same. This disclosure also features combinations that include one or more of the MCL-1/BFL-1/A1 inhibitor compounds described herein, or a pharmaceutically acceptable salt thereof; and one or more additional therapeutic agents (e.g., one or more chemotherapeutic agents (including small molecule and/or anti-body based chemotherapy and/or radiation); e.g., one or more therapeutic agents that modulate apoptosis; e.g., one or more therapeutic agents that bind to and inhibit anti-apoptotic proteins or modulate them indirectly; e.g., one or more therapeutic agents that bind to and inhibit, or indirectly modulate, anti-apoptotic BCL-2, BCL-XL, BCL-w, MCL-1, and/or BFL-1/A1; e.g., one or more therapeutic agents that directly bind to and inhibit anti-apoptotic BCL-2/BCL-XL; e.g., agents such as ABT-199, ABT-263 and ABT-737; e.g.Type: ApplicationFiled: March 14, 2013Publication date: February 19, 2015Inventor: Loren D. Walensky
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Publication number: 20150051247Abstract: Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor.Type: ApplicationFiled: August 16, 2012Publication date: February 19, 2015Inventor: Samy O. Meroueh