Chalcogen And Acyclic Nitrogen Bonded Directly To The Same Carbon Patents (Class 546/291)
  • Patent number: 10149842
    Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
    Type: Grant
    Filed: May 31, 2018
    Date of Patent: December 11, 2018
    Assignee: Akebia Therapeutics, Inc.
    Inventors: James Densmore Copp, Ann W. Newman, Anne Luong
  • Patent number: 9273005
    Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: March 1, 2016
    Assignee: BioTheryX, Inc.
    Inventors: Frank Mercurio, Kyle W. H. Chan
  • Publication number: 20150133670
    Abstract: The present invention provides a novel process for the preparation of sorafenib tosylate polymorph III.
    Type: Application
    Filed: May 21, 2013
    Publication date: May 14, 2015
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao, Bandi Vamsi Krishna
  • Patent number: 9029401
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20150119425
    Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 30, 2015
    Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
  • Publication number: 20150099883
    Abstract: The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R1 represents an ethyl group or the like, R2 represents a hydrogen atom or the like, R3 and R4 represents a methyl group or the like, X1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X2 represents a methyl group or the like, m2 is an integer of 0 to 3.
    Type: Application
    Filed: April 8, 2013
    Publication date: April 9, 2015
    Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Jun Kanazawa, Katsunori Tanaka, Asaho Nagagata
  • Publication number: 20150099786
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150099762
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Inventors: Hilary Schenck EIDAM, Kaushik RAHA, Zhen GONG, Huiping Amy GUAN, Chengde WU, Haiying YANG, Haiyu YU, Zhiliu ZHANG, Mui CHEUNG
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150051399
    Abstract: The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent.
    Type: Application
    Filed: March 29, 2013
    Publication date: February 19, 2015
    Inventors: Iontcho Radoslavov Vlahov, Hari Krishna R. Santhapuram, Paul Joseph Kleindl, Christopher Paul Leamon, Fei You
  • Patent number: 8952039
    Abstract: The present invention relates to a compound having the general formula (II), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: February 10, 2015
    Assignees: European Molecular Biology Laboratory, F. Hoffmann-La Roche AG, Savira pharmaceuticals GmbH
    Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley
  • Publication number: 20140357670
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Application
    Filed: May 28, 2014
    Publication date: December 4, 2014
    Inventors: Saleem Ahmad, Lidet A. Negash
  • Patent number: 8900797
    Abstract: The present invention provides a cross-linking agent capable of preventing formation of scum from a bottom anti-reflective coating, and also provides a composition for forming a bottom anti-reflection coating containing the agent. The cross-linking agent is a nitrogen-containing aromatic compound having at least one vinyloxy group or N-methoxymethylamide group, and the composition contains the cross-linking agent. The cross-linking agent of the formula (1) can be produced by reaction of a nitrogen-containing aromatic compound, a halogen compound having a vinyloxy group or N-methoxymethylamide group and a basic compound.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: December 2, 2014
    Assignee: AZ Electronic Materials (Luxembourg) S.A.R.L.
    Inventors: Shigemasa Nakasugi, Shinji Miyazaki, Munirathna Padmanaban, Alberto D. Dioses
  • Publication number: 20140343031
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joesph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Patent number: 8877933
    Abstract: The present invention relates to a novel form, thermodynamically stable at room temperature, of the tosylate salt of 4-{4-[({[4-chloro-3-(trifluoromethyl)phenyl]amino}carbonyl)amino]phenoxy}-N-methylpyridine-2-carboxamide, to processes for its preparation, to medicaments comprising it and to its use in the control of disorders.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: November 4, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Alfons Grunenberg, Jana Lenz
  • Patent number: 8871976
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: October 28, 2014
    Assignees: National University of Singapore, Agency for Science, Technology and Research
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Publication number: 20140315879
    Abstract: The present invention relates to sulfonamide derivatives, of formula (I): or a pharmaceutically acceptable salts thereof, wherein X, Z, R1a, R1b, R2, R3, R4 and R5 are as defined in the description, and to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. The compounds of formula (I) are Nav1.7 inhibitors useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Publication number: 20140315949
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 19, 2012
    Publication date: October 23, 2014
    Applicant: CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Nasveschuk
  • Patent number: 8865736
    Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Biota Scientific Pty Ltd
    Inventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
  • Publication number: 20140296208
    Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicants: Topivert Pharma Limited, Respivert Limited
    Inventors: Thomas Matthew BAKER, Matthew Colin Thor FYFE, Gareth William HARBOTTLE, Vedran HASIMBEGOVIC, Premji MEGHANI, Aaron RIGBY, Colin SAMBROOK-SMITH, Stephen Malcolm THOM
  • Publication number: 20140288086
    Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Applicants: PFIZER INC., AGOURON PHARMACEUTICALS, INC.
    Inventors: Jingrong Jean CUI, Lee Andrew FUNK, Lei JIA, Pei-Pei KUNG, Jerry Jialun MENG, Mitchell David NAMBU, Mason Alan PAIRISH, Hong SHEN, Michelle TRAN-DUBE
  • Publication number: 20140275111
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck EIDAM, Kaushik Raha, Zhen Gong, Huiping Guan, Chengde Wu, Haiying Yang, Haiyu Yu, Zhiliu Zhang, Mui CHEUNG
  • Publication number: 20140235608
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 26, 2012
    Publication date: August 21, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: John Lloyd, Jeniffer X. Qiao, Heather Finlay, James Neels, Zulan Pi, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20140221661
    Abstract: The present invention relates to a process for preparing 4-(4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy)-N-methylpyridine-2-carboxamide, its salts and monohydrate.
    Type: Application
    Filed: April 15, 2014
    Publication date: August 7, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Juergen STIEHL, Werner HEILMANN, Michael L.GERS, Joachim REHSE, Michael GOTTFRIED, Saskia WICHMANN
  • Publication number: 20140221404
    Abstract: In order to identify a gene that can serve as an indicator for predicting the effectiveness of a drug treatment of cancer and to provide a novel method for predicting the effectiveness of a drug treatment targeting said gene, lung adenocarcinomas were subjected to whole-transcriptome sequencing. As a result, in-frame fusion transcripts between the KIF5B gene and the RET gene were identified. The KIF5B-RET gene fusions were detected in 6 out of 319 (2%) LADC specimens from Japanese individuals and 1 out of 80 (1%) LADC specimens from U.S.A. individuals. None of the seven subjects revealed known activating mutations such as EGFR, KRAS or ALK oncogenes; thus, said gene fusions were found to be responsible mutations (driver mutations) for oncogenesis. Since said gene fusions are considered to induce constitutive activation of RET tyrosine kinase protein, it was found that treatments with RET tyrosine kinase inhibitors are effective in patients with detection of said gene fusions.
    Type: Application
    Filed: August 3, 2012
    Publication date: August 7, 2014
    Applicants: LSIP, LLC, NATIONAL CANCER CENTER
    Inventors: Takashi Kohno, Koji Tsuta
  • Publication number: 20140213569
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: March 31, 2014
    Publication date: July 31, 2014
    Applicant: GRUNENTHAL GMBH
    Inventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER, Simon LUCAS
  • Publication number: 20140206875
    Abstract: Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same for inhibiting human 11-?-hydroxy steroid dehydrogenase type 1 (11?-HSD1). The disclosed compound and the pharmaceutical composition including the same for inhibiting human 11-?-hydroxy steroid dehydrogenase type 1 (11?-HSD1) are excellent in activity and solubility, and is more efficient in formulation and transfer.
    Type: Application
    Filed: August 6, 2012
    Publication date: July 24, 2014
    Applicant: HYUNDAI PHARM CO., LTD.
    Inventors: Inhee Lee, Doohyeok Pyeon, Myounghyeon Shin, Jeongun Hwang, Changmin Park, Sehoan Kim, Heeil Chae, Soonyoung Moon, Soyoun Kim, Jaekeol Rhee
  • Publication number: 20140194476
    Abstract: The present invention relates to a compound having the general formula (II), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Application
    Filed: January 7, 2014
    Publication date: July 10, 2014
    Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley
  • Patent number: 8748622
    Abstract: The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: June 10, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Juergen Stiehl, Werner Heilmann, Michael Lögers, Joachim Rehse, Michael Gottfried, Saskia Wichmann
  • Publication number: 20140148468
    Abstract: The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
    Type: Application
    Filed: November 27, 2013
    Publication date: May 29, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
  • Publication number: 20140113898
    Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.
    Type: Application
    Filed: November 4, 2011
    Publication date: April 24, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
  • Patent number: 8703801
    Abstract: New chiral and achiral oxy-substituted cyclopentyl pyridinone diketocarboxamides and their derivatives and methods for their preparations are disclosed. The compounds include tautomers, regioisomers and geometric isomers. These complex carboxamides are designed as inhibitors of HIV replication through inhibition of HIV integrase. The compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: April 22, 2014
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Vasu Nair, Maurice O. Okello, Abdumalik A. Nishonov, Sanjaykumar Mishra
  • Publication number: 20140088157
    Abstract: Provided are an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient, and a method for controlling endoparasites, comprising orally or parenterally administering the endoparasite control agent.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 27, 2014
    Applicants: NIHON NOHYAKU CO., LTD., THE UNIVERSITY OF TOKYO
    Inventors: Kiyoshi Kita, Akiyuki Suwa
  • Publication number: 20140087311
    Abstract: The present invention provides a cross-linking agent capable of preventing formation of scum from a bottom anti-reflective coating, and also provides a composition for forming a bottom anti-reflection coating containing the agent. The cross-linking agent is a nitrogen-containing aromatic compound having at least one vinyloxy group or N-methoxymethylamide group, and the composition contains the cross-linking agent. The cross-linking agent of the formula (1) can be produced by reaction of a nitrogen-containing aromatic compound, a halogen compound having a vinyloxy group or N-methoxymethylamide group and a basic compound.
    Type: Application
    Filed: September 26, 2012
    Publication date: March 27, 2014
    Applicant: AZ ELECTRONIC MATERIALS (LUXEMBOURG) S.A.R.L.
    Inventors: Shigemasa NAKASUGI, Shinji MIYAZAKI, Munirathna PADMANABAN, Alberto D. DIOSES
  • Publication number: 20140088311
    Abstract: Disclosed are an intermediate compound of N-(1,1,1-trideuterated methyl)phthalimide, and its use in the preparation of deuterated diphenylurea derivative.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SUZHOU ZELGEN BIOPHARMACEUTICAL CO., LTD.
    Inventors: Weidong FENG, Xiaoyong GAO, Xiaojun DAI
  • Publication number: 20140088156
    Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.
    Type: Application
    Filed: February 14, 2012
    Publication date: March 27, 2014
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
  • Publication number: 20140072517
    Abstract: Compounds and uses of the compounds are provided. The compounds can be used as Fe(II) sequestering compounds. For example, these compounds can be used to sequester Fe(II) in cells, organs, vasculature, or tissues. Also, provided are compositions and methods of using the them for sequestering Fe(II) in an individual. The compounds can be used as MRI paraCEST contrast agents.
    Type: Application
    Filed: May 11, 2012
    Publication date: March 13, 2014
    Applicant: The Research Foundation of State University of New
    Inventors: Janet Morrow, Pavel Tsitovich
  • Publication number: 20140051727
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 20, 2014
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20140045903
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: July 30, 2013
    Publication date: February 13, 2014
    Applicant: Intrexon Corporation
    Inventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Publication number: 20140044806
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20140031376
    Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.
    Type: Application
    Filed: October 3, 2013
    Publication date: January 30, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Shigeyuki ITOH, Atsushi IWATA
  • Publication number: 20140005405
    Abstract: Processes are provided which create an aldehyde methylene, or hydrated or hemiacetal methylene attached to a heteroatom of a 6 membered ring without going through an olefinic group and without the necessity of using an osmium reagent. In particular, a compound of formula (I) can be produced from (II) and avoid the use of an allyl amine: (formulae I and II) where R, P1 P3, R3 and Rx are as described herein.
    Type: Application
    Filed: September 5, 2013
    Publication date: January 2, 2014
    Applicants: VIIV Healthcare Company, Sionogi & Co., Ltd.
    Inventors: Brian JOHNS, Maosheng DUAN, Toshikazu HAKOGI
  • Patent number: 8618141
    Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: December 31, 2013
    Assignee: Bayer Healthcare LLC
    Inventors: Jacques Dumas, William J. Scott, James Elting, Holia Hatoum-Makdad
  • Patent number: 8609854
    Abstract: The present invention provides a process for the preparation of sorafenib tosylate, comprising contacting sorafenib free base with p-toluenesulphonic acid in water.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: December 17, 2013
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
  • Publication number: 20130327251
    Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
    Type: Application
    Filed: March 7, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF HOUSTON SYSTEM
    Inventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
  • Publication number: 20130315847
    Abstract: The invention relates to a cosmetic process for depigmenting, lightening and/or whitening keratin materials, in particular the skin, which comprises the application of a cosmetic composition comprising a compound of formula (I): or its tautomer form of formula (I) in which: R1 and R2, which may be identical or different, denote a radical chosen from: a) a hydrogen atom; b) a C1-C20 alkyl group optionally interrupted with N, S or O, optionally substituted with one or more group(s) chosen from —OR3, —SR3, —NR3R4, —CONHR3; —COOR3; and an aryl group optionally substituted with one or more hydroxyls and/or with one or more C1-C8 alkoxy radicals; c) a C1-C8 alkyl group substituted with a C5-C12 aryl radical optionally substituted with one or more hydroxyls and/or with one or more C1-C8 alkoxy radicals; d) a phenyl group optionally substituted with one or more hydroxyls and/or with one or N more C1-C8 alkoxy radicals; R3 denoting H or a C1-C5 alkyl group, R4 denoting H, a C1-C5 hydrocarbon-based group or an acetyl g
    Type: Application
    Filed: December 8, 2011
    Publication date: November 28, 2013
    Applicant: L'OREAL
    Inventor: Xavier Marat
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130252957
    Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: December 28, 2012
    Publication date: September 26, 2013
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
  • Patent number: 8541402
    Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: September 24, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt