The Additional Hetero Ring And The Bicyclo Ring System Are Attached Directly To The Same Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 548/468)
  • Patent number: 9598712
    Abstract: The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1?R,3?S)-5,7?-dichloro-6?-fluoro-3?-methyl-2?,3?,4?,9?-tetrahydrospiro[indoline-3,1?-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof.
    Type: Grant
    Filed: March 22, 2013
    Date of Patent: March 21, 2017
    Assignee: Novartis AG
    Inventors: Michael Crowe, Michael Foulkes, Giancarlo Francese, Dominique Grimler, Ernst Kuesters, Kurt Laumen, Yunzhong Li, Changxue Lin, Jovana Nazor, Thomas Ruch, Derek Smith, Shiwei Song, Shangjun Teng
  • Patent number: 9067915
    Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: June 30, 2015
    Assignee: Teva Pharmaceutical Industries LTD.
    Inventors: Alexandr Jegorov, Ales Gavenda, Pavel Vraspir, Augusto Canavesi, Francesca Scarpitta
  • Publication number: 20150112085
    Abstract: The present invention relates to pure crystalline Form II of an L-malic acid salt of sunitinib and a process for its preparation. The invention further provides crystalline Form II of an L-malic acid salt of sunitinib having a purity of at least 97.0%. The invention also provides crystalline Form II of an L-malic acid salt of sunitinib substantially free of an anti-oxidant. The invention also provides crystalline Form II of L-malic acid salt of sunitinib which remains chemically pure on storage at 25° C.±2° C. and 40° C.±2° C. at a relative humidity of 60%±5% and 75%±5%, respectively, for at least 1 month.
    Type: Application
    Filed: January 6, 2014
    Publication date: April 23, 2015
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Hari Babu MATTA, Mahavir Singh KHANNA, Mohan PRASAD
  • Publication number: 20150111940
    Abstract: The present invention relates to an ascorbic acid salt of sunitinib and a process for its preparation. The present invention further provides a crystalline Form I of an L-ascorbic acid salt of sunitinib.
    Type: Application
    Filed: January 6, 2014
    Publication date: April 23, 2015
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Hari Babu MATTA, Mahavir Singh KHANNA, Mohan PRASAD
  • Publication number: 20150094330
    Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 2, 2015
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 8987320
    Abstract: The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1, 2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders.
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: March 24, 2015
    Assignee: Zoetis LLC
    Inventors: Changquan C. Sun, Michael Hawley
  • Patent number: 8957066
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 17, 2015
    Assignee: Biomarin Pharmaceutical Inc.
    Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20150045562
    Abstract: The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1?R,3?S)-5,7?-dichloro-6?-fluoro-3?-methyl-2?,3?,4?,9?-tetrahydrospiro[indoline-3,1?-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 12, 2015
    Applicant: Novartis AG
    Inventors: Michael Crowe, Michael Foulkes, Giancarlo Francese, Dominique Grimler, Ernst Kuesters, Kurt Laumen, Yunzhong Li, Changxue Lin, Jovana Nazor, Thomas Ruch, Derek Smith, Shiwei Song, Shangjun Teng
  • Publication number: 20150030618
    Abstract: The present application relates to new binder-drug conjugates (ADCs) of N,N-dialkylauristatins that are directed against the target C4.4a, to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for treating and/or preventing illnesses, and also to the use of these ADCs for producing medicaments for treating and/or preventing illnesses, more particularly hyperproliferative and/or angiogenic diseases such as, for example, cancer diseases. Such treatments may be practised as a monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: May 5, 2014
    Publication date: January 29, 2015
    Applicant: SEATTLE GENETICS, INC.
    Inventors: Hans-Georg LERCHEN, Lars Linden, Sherif El Sheikh, Jörg Willuda, Charlotte C. Kopitz, Joachim Schuhmacher, Simone Greven, Christoph Mahlert, Beatrix Stelte-Ludwig, Sven Golfier, Rudolf Beier, Iring Heisler, Axel Harrenga, Karl-Heinz Thierauch, Sandra Bruder, Heike Petrul, Hannah Jörissen, Sandra Borkowski
  • Publication number: 20150025252
    Abstract: The present invention relates to an improved process for the preparation of Sunitinb. The process involves the activation of 5-((Z)-(5-fluoro-2-oxoindolin-3-ylidene) methyl)-2,4-dimethyl-1H-pyrrole-3carboxylic acid to corresponding suitable carboxylic acid activating group. The present invention also relates to novel acid addition salts of Sunitinb and preparation thereof.
    Type: Application
    Filed: March 22, 2013
    Publication date: January 22, 2015
    Inventors: Sanjay Kumar Dehury, Venkata Lakshmi Narasimha Dammalapati, Venkata Sunil Kumar Indukuri, Seeta Ramanjaneyulu Gorantla
  • Publication number: 20150018380
    Abstract: The present invention provides methods for obtaining specific and non-toxic inhibitors of AID nuclear import. The methods comprise a primary screen and a counter screen to identify a pool of AID specific nuclear import inhibitors that do not have off-target of toxic effects. AID specific nuclear import inhibitors identified by the screens of the invention prevent nuclear entry, limit the access of AID to genomic DNA, and inhibit AID mutagenic activity. Preparations, including pharmaceutical preparations, comprising specific nuclear import inhibitors, used for example, to inhibit cancer progression, are also encompassed in the invention.
    Type: Application
    Filed: February 7, 2013
    Publication date: January 15, 2015
    Applicant: University of Rochester
    Inventor: Harold C. Smith
  • Patent number: 8933247
    Abstract: The present invention provides a succinimide compound represented by the following formula (1-1) or (1-2), and a lubricating oil additive and a lubricating oil composition which contain the succinimide compound. wherein R represents an alkyl group or an alkenyl group having a number-average molecular weight of 500 or greater and less than 5000. wherein R represents an alkyl group or an alkenyl group having a number-average molecular weight of 500 or greater and less than 5000.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: January 13, 2015
    Assignee: JX Nippon Oil & Energy Corporation
    Inventors: Kazuo Tagawa, Miho Endou
  • Patent number: 8916716
    Abstract: The present invention relates to stable crystalline Form II of L-malic acid salt of sunitinib and its preparation.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: December 23, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Sudhir Singh Sanwal, Saridi Madhava Dileep Kumar, Swargam Sathyanarayana
  • Publication number: 20140371138
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
  • Publication number: 20140371198
    Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, 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, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.
    Type: Application
    Filed: June 23, 2014
    Publication date: December 18, 2014
    Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédict Pourbaix-L'ebraly
  • Publication number: 20140296292
    Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 2, 2014
    Inventors: Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, C. Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
  • Patent number: 8846953
    Abstract: The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: September 30, 2014
    Assignee: Scinopharm Taiwan, Ltd.
    Inventors: Julian P. Henschke, Yung-Fa Chen
  • Patent number: 8841464
    Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: September 23, 2014
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Publication number: 20140275033
    Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
  • Patent number: 8829039
    Abstract: Disclosed are dihydroindolone compounds which can modulate the activity of protein tyrosine kinases, a method for preparing the same, and pharmaceutical compositions comprising the same. Also disclosed are use of such compounds and pharmaceutical compositions thereof in the treatment and/or prophylaxis of protein tyrosine kinase associated diseases in an organism, particularly in the treatment and/or prophylaxis of tumors and fibroblast proliferation associated diseases.
    Type: Grant
    Filed: May 25, 2009
    Date of Patent: September 9, 2014
    Assignees: Shanghai Institute of Pharmaceutical Industry, Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd.
    Inventors: Zhedong Yuan, Xiaomin Zhang, Hubo Wang, Xueyan Zhu, Hongjiang Xu, Hui Fu, Wei Song
  • Patent number: 8815903
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: August 26, 2014
    Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Publication number: 20140171629
    Abstract: Provided is a medicinal agent for medical applications, which can act on the function of a target cell specifically. The medicinal agent for medical applications comprises: a cell-incorporated substance that can be incorporated into a target cell specifically; and an acting substance that can act on the function of the target cell and is bound to the cell-incorporated substance.
    Type: Application
    Filed: August 9, 2012
    Publication date: June 19, 2014
    Applicants: HITACHI ALOKA MEDICAL, LTD., THE NIPPON DENTAL UNIVERSITY
    Inventors: Minako Suzuki, Taka Nakahara, Hiroshi Ishikawa, Akihiro Oyama
  • Publication number: 20140170564
    Abstract: There is provided an actinic ray-sensitive or radiation-sensitive resin composition containing (A) a compound represented by the following formula (1-1); an actinic ray-sensitive or radiation-sensitive film using the composition; and a pattern forming method: in the formula, R1, R2, R3, R4 and Y? are the same as those in formula (1-1) set forth in the description.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Tomoki MATSUDA, Yoko TOKUGAWA, Akinori SHIBUYA
  • Patent number: 8754239
    Abstract: A process for preparation of eletriptan hydrobromide having ?-form of formula (I) is described that includes reducing 3-((R)-1-methylpyrrolidin-2-yl)methyl)-5-((E)-2-(phenylsulfonyl)vinyl)-1H-indole of formula (II) in presence of a metal catalyst to the product of formula (III) and then converting to hydrobromide salt having ?-form of formula (I).
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: June 17, 2014
    Assignee: SMS Pharmaceuticals Limited
    Inventors: Srinivasa Rao Venturi, Hari Prasad Kodali, Hariharakrishnan Venkata Subhramanian, Venkata Srihari Tadimalla, Ramesh Babu Potluri
  • Patent number: 8748601
    Abstract: Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: June 10, 2014
    Assignee: The Regents of the University of California
    Inventors: Jack Taunton, Michael Cohen, Kevan Shokat, Chao Zhang
  • Publication number: 20140142308
    Abstract: Receptor type oligothiopene compounds, methods of preparing the compounds, and use of the compounds in photoelectric materials.
    Type: Application
    Filed: March 27, 2012
    Publication date: May 22, 2014
    Applicant: NANKAI UNIVERSITY
    Inventors: Yongsheng Chen, Xiangjian Wan, Yongsheng Liu, Zhi Li, Jiaoyan Zhou, Fei Wang, Guangrui He, Guankui Long
  • Patent number: 8703967
    Abstract: A process for the preparation of a new crystal form of sunitinib malate, along with pharmaceuticals comprising the same are described.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: April 22, 2014
    Assignee: LEK Pharmaceuticals D.D.
    Inventor: Lovro Selic
  • Publication number: 20140107339
    Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.
    Type: Application
    Filed: September 4, 2013
    Publication date: April 17, 2014
    Applicant: Cornell University
    Inventors: Geoffrey W. Coates, John W. Kramer
  • Patent number: 8686023
    Abstract: Pharmaceutically acceptable salts of sunitinib, processes of making sunitinib salts, as well as related pharmaceuticals and methods of treating are described.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: April 1, 2014
    Assignee: Lek Pharmaceuticals D.D.
    Inventor: Lovro Selic
  • Patent number: 8686022
    Abstract: The present invention provides compounds according to general formula (I) which are proposed for the treatment of respiratory complaints, particularly asthma and COPD.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: April 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Birgit Jung, Frank Himmelsbach, Rolf Goeggel, Georg Dahmann
  • Patent number: 8686024
    Abstract: The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group.
    Type: Grant
    Filed: February 3, 2010
    Date of Patent: April 1, 2014
    Assignees: Kyoto University, Tokyo Institute of Technology
    Inventors: Hachiro Sugimoto, Jun Takahashi, Takashi Takahashi, Ichiro Hijikuro
  • Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Publication number: 20140039030
    Abstract: The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.
    Type: Application
    Filed: December 23, 2011
    Publication date: February 6, 2014
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Antoni Kozlowski, Sean M. Culbertson, Xiaoming Shen, Samuel P. Mcmanus, Mark A. Wilson
  • Patent number: 8642770
    Abstract: The present invention provides an indole derivative having a melanin-concentrating hormone receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: February 4, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shinichi Masada, Yoshito Terao, Toshiki Murata
  • Patent number: 8637681
    Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: January 28, 2014
    Assignee: Qilu Pharmaceutical Co., Ltd.
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Boyan Xu, Shousheng Yan, Zongru Guo, Minghui Zhang, Dong Lin, Zhantao Zhang, Haojie Zhou
  • Patent number: 8637685
    Abstract: The invention provides fluorescent schweinfurthin analogs of formula (I) which are useful as probes and for the treatment of cancer and other diseases.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: January 28, 2014
    Assignee: University of Iowa Research Foundation
    Inventors: David F. Wiemer, Jeffrey D. Neighbors, Raymond J. Hohl, Craig Kuder
  • Patent number: 8633239
    Abstract: The present invention relates to a novel process for the preparation of (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole and its intermediates thereof.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Biophore India Pharmaceuticals Private Limited
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Neelam Naidu, Nagaraju Maddela, Radha Nagarapu, Pulla Rao Polagani
  • Publication number: 20140011855
    Abstract: The invention relates to (among other things) polymer-semaxanib moiety conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over the semaxanib moiety in unconjugated form.
    Type: Application
    Filed: December 23, 2011
    Publication date: January 9, 2014
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Jennifer Riggs-Sauthier, Stephanie Allums-Donald, Sean M. Culbertson
  • Publication number: 20140005165
    Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Inventors: Anilkumar G. Nair, Jose S. Duca, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Patent number: 8618309
    Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: December 31, 2013
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Alexandr Jegorov, Ales Gavenda, Pavel Vraspir, Augusto Canavesi, Francesca Scarpitta
  • Publication number: 20130331425
    Abstract: The invention relates to (among other things) polymer-sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over sunitinib in unconjugated form.
    Type: Application
    Filed: December 23, 2011
    Publication date: December 12, 2013
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Sean M. Culbertson, Antoni Kozlowski, Tony Drew Vinson
  • Publication number: 20130331413
    Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Erik DE LEEUW, Alexander D. MACKERELL, JR.
  • Publication number: 20130317003
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: March 15, 2013
    Publication date: November 28, 2013
    Inventor: Repligen Corporation
  • Publication number: 20130317065
    Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.
    Type: Application
    Filed: January 24, 2012
    Publication date: November 28, 2013
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Publication number: 20130296575
    Abstract: Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate.
    Type: Application
    Filed: July 17, 2013
    Publication date: November 7, 2013
    Inventors: Alexandr JEGOROV, Ales Gavenda, Pavel Vraspir, Augusto Canavesi, Francesca Scarpitta
  • Publication number: 20130296561
    Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.
    Type: Application
    Filed: January 13, 2012
    Publication date: November 7, 2013
    Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
    Inventors: Karin Henderika Maria Bessembinder, Dennis Heemskerk, Ben De Lange
  • Publication number: 20130289090
    Abstract: Substituted indole derivatives of formula (I) wherein the radicals have e.g. the following meaning: R1 is hydrogen, C1-6-alkyl, R2 is hydrogen, —C1-6-alkyl or cycloC3-12-alkyl; R3 is OR R4 is hydrogen or halogen, R5 is hydrogen, —C1-6-alkyl R6 is hydrogen, —C1-6-alkyl R is hydrogen or —C1-6-alkyl; X is a group —C(O)CH2— or —CH?CH—; R7 is hydrogen are potent inhibitors of Abeta peptide polymerization and can be used for the treatment of e.g. Alzheimers disease or ocular disorders.
    Type: Application
    Filed: October 27, 2011
    Publication date: October 31, 2013
    Applicant: MERZ PHARMA GMBH & CO. KGAA
    Inventor: Ulrich Abel
  • Publication number: 20130289075
    Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.
    Type: Application
    Filed: June 25, 2013
    Publication date: October 31, 2013
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Publication number: 20130281451
    Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.
    Type: Application
    Filed: April 3, 2013
    Publication date: October 24, 2013
    Applicant: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
  • Publication number: 20130259830
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
    Type: Application
    Filed: June 24, 2011
    Publication date: October 3, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien