Bicyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos (e.g., Octahydroindoles, Etc.) Patents (Class 548/452)
  • Patent number: 11753382
    Abstract: The invention in this disclosure is related to the processes of making Bindarit or derivatives thereof. Specifically, the present invention provides, in part, new processes for making 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid and its derivatives. By way of non-limiting example, synthesis and purification processes of 2-((1-benzyl-1H-indazol-3-yl)methoxy)-2-methylpropanoic acid are provided by the invention in this disclosure.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: September 12, 2023
    Assignee: TRANSLATUM MEDICUS INC.
    Inventors: Xiangdong Jiao, Kanjai Khumtaveeporn
  • Patent number: 11339136
    Abstract: In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured; Formula (I), Formula (II) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: May 24, 2022
    Assignee: Novartis AG
    Inventors: Gary Glick, Shomir Ghosh, William R. Roush
  • Patent number: 9527813
    Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (?)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: December 27, 2016
    Assignee: EUTHYMICS BIOSCIENCE, INC.
    Inventors: Jerry A. Murry, Edward G. Corley, Feng Xu, Bryon Simmons
  • Patent number: 9150511
    Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.
    Type: Grant
    Filed: April 29, 2014
    Date of Patent: October 6, 2015
    Assignee: Apicore US LLC
    Inventors: Ravishanker Kovi, KeshavRao Rapole, Ashish Naik, Jayaraman Kannapan, Muralikrishna Madala, Sanjay Thakor
  • Patent number: 9067881
    Abstract: The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: June 30, 2015
    Assignee: NOVARTIS AG
    Inventors: Joachim Nozulak, Dieter Oser
  • Publication number: 20150141465
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: Calvin W. YEE, Zhe Li
  • Patent number: 9029567
    Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof. The invention relates to novel amino acid derivatives of the formula (1), wherein, A is amino acid B is peptide bond R-NH- wherein R is defined in the specification.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: May 12, 2015
    Assignee: Cadila Pharmaceuticals Limited
    Inventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
  • Patent number: 9018397
    Abstract: The present invention relates to compounds of the formula I wherein the substituents are as defined in claim 1, and their use as organic semiconductor in organic devices, like diodes, organic field effect transistors and/or a solar cells. The compounds of the formula I have excellent solubility in organic solvents. High efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when said compounds are used in semiconductor devices or organic photovoltaic (PV) devices (solar cells).
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: April 28, 2015
    Assignee: BASF SE
    Inventors: Zhimin Hao, Beat Schmidhalter, Jean-Luc Budry, Margherita Fontana, Matheiu G. R. Turbiez, Frank Bienewald, Mathias Duggeli, Oliver Frederic Aebischer, Pascal Hayoz, Marta Fondrodona Turon
  • Publication number: 20150112084
    Abstract: Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.
    Type: Application
    Filed: April 22, 2013
    Publication date: April 23, 2015
    Inventor: RAMAMOHAN RAO DAVULURI
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20150087686
    Abstract: It comprises a cocrystal of saxagliptin hydrochloride and a compound selected from the group consisting of saxagliptin, glycolic acid, malonic acid, and urea; or a solvate thereof, or a hydrate thereof. It also comprises a salt of saxagliptin with glycolic acid 1:1 hydrate. It also comprises their preparation processes, as well as their use as antidiabetics.
    Type: Application
    Filed: April 24, 2013
    Publication date: March 26, 2015
    Applicant: ENANTIA, S.L.
    Inventors: Nicolas Tesson, Montserrat Trilla Castaño, Lydia Cárdenas Romaña, Llorenç Rafecas Jané
  • Patent number: 8980935
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: March 17, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • Publication number: 20150057443
    Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
    Type: Application
    Filed: August 21, 2014
    Publication date: February 26, 2015
    Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
  • Patent number: 8901157
    Abstract: The present invention discloses compositions and a method of improving the pharmacokinetics of pharmaceutical agents (or pharmaceutically acceptable salts, esters, and prodrugs thereof) which are metabolized by cytochrome P450 monoxygenase comprising coadministering ritonavir or a pharmaceutically acceptable salt, ester, and prodrug thereof.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: December 2, 2014
    Assignee: AbbVie Inc.
    Inventors: Dale J. Kempf, Kennan C. Marsh
  • Publication number: 20140336393
    Abstract: The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 13, 2014
    Inventors: Narendra Bhalchandra Ambhaikar, Robert Hughes, Dennis James Hurley, Elaine Chungmin Lee, Benjamin Littler, Mehdi Numa, Stefanie Roeper, Urvi Sheth
  • Patent number: 8865915
    Abstract: Process for the preparation of the compound of formula (I):
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: October 21, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Julie Linol, Stéphane Laurent, Arnaud Grenier, Sébastien Mathieu
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Publication number: 20140288142
    Abstract: The invention relates to nitric oxide donor compounds and their use for treating cardiovascular diseases, inflammation, pain, fever, gastrointestinal disorders, ophthalmic diseases, hepatic disorders, renal diseases, respiratory disorders, immunological diseases, bone metobolisms dysfunctions, central and peripheral nervous system diseases, sexual dysfunctions, infectious diseases, for the inhibition of platelet aggregation and platelet adhesion, for treating pathological conditions resulting from abnormal cell proliferation, vascular diseases. The invention also relates to compositions comprising at least one nitric oxide releasing compounds of the invention and composition comprising at least one nitric oxide releasing compounds according to the invention and at least one 15 therapeutic agent.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Inventors: Nicoletta ALMIRANTE, Stefano BIONDI, Ennio ONGINI, Laura STORONI, Alessia NICOTRA
  • Publication number: 20140275025
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
  • Publication number: 20140275155
    Abstract: This invention relates to bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias GRAUERT, Ralf ANDERSKEWITZ, Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS
  • Patent number: 8835652
    Abstract: Delta crystalline form of the compound of formula (I): characterised by its X-ray powder diffraction diagram. Medicinal products containing the same which are useful in the treatment of cardiovascular diseases.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: September 16, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Julie Linol, Stephane Laurent, Arnaud Grenier, Sebastien Mathieu
  • Patent number: 8809365
    Abstract: This invention provides 2-azabicyclo[3.1.1]heptyl derivatives, and methods for producing them, which are useful therapeutic agents for preventing or treating central nervous system disorders and disease mediated by a Nicotinic Acetylcholine Receptor such as, but not limited to, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy, dementia, pain and nicotine addiction.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: August 19, 2014
    Assignee: Universiteit Gent
    Inventors: Christian Stevens, Ann De Blieck, Thomas Heugebaert
  • Patent number: 8802715
    Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
    Type: Grant
    Filed: December 27, 2013
    Date of Patent: August 12, 2014
    Assignee: AstraZeneca AB
    Inventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
  • Patent number: 8796469
    Abstract: The present invention relates to polymers comprising one or more (repeating) unit(s) of the formula (I) which are characterized in that Ar1 and Ar1? are independently of each other are an annulated (aromatic) heterocyclic ring system, containing at least one thiophene ring, which may be optionally substituted by one, or more groups, and their use as organic semiconductor in organic devices, especially in organic photovoltaics (solar cells) and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers according to the invention have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.
    Type: Grant
    Filed: March 22, 2010
    Date of Patent: August 5, 2014
    Assignee: BASF SE
    Inventors: Pascal Hayoz, Olivier Frédéric Aebischer, Mathias Düggeli, Hans Jürg Kirner, Marta Fonrodona Turon
  • Publication number: 20140213788
    Abstract: The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: Vereniging voor Christelijk hoger onderwijs, wetenschappelijk onderzoek en patiëntenzorg
    Inventors: Eelco RUIJTER, Romano ORRU, Anass ZNABET, Marloes POLAK, Nicholas TURNER
  • Publication number: 20140200252
    Abstract: The present invention relates to novel polymorphic forms of Saxagliptin Hydrochloride. The present invention also relates to methods of making polymorphic forms of Saxagliptin Hydrochloride.
    Type: Application
    Filed: October 2, 2013
    Publication date: July 17, 2014
    Applicant: SANDOZ AG
    Inventors: Arthur Pichler, Josef Wieser, Christoph Langes, Milica Vukicevic
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Patent number: 8748631
    Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.
    Type: Grant
    Filed: May 24, 2012
    Date of Patent: June 10, 2014
    Assignee: Apicore, LLC
    Inventors: Ravishanker Kovi, KeshavRao Rapole, Ashish Naik, Jayaraman Kannapan, Murali Krishna Madala, Sanjay F. Thakor
  • Patent number: 8748446
    Abstract: Halo-organic heterocyclic compounds are described, which have the formulas Ring A is an aromatic ring bound to at least two halogen atoms, at least one of which is iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Grant
    Filed: March 3, 2012
    Date of Patent: June 10, 2014
    Assignee: Nanoquantum Sciences, Inc.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20140135504
    Abstract: The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form ? and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form ? with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process.
    Type: Application
    Filed: January 23, 2014
    Publication date: May 15, 2014
    Applicant: MYLAN LABORATORIES LIMITED
    Inventors: Ramakoteswara Rao Jetti, Chetan Kanaiyalal Raval, Aggi Ramireddy Bommareddy, Debashish Datta
  • Patent number: 8716326
    Abstract: The present invention relates to an amide compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The inventive amide compound facilitates bone formation and inhibits bone loss, and is therefore useful for preventing and treating bone disorders such as osteoporosis, osteodystrophy, bone fracture, periodontal disease, Paget's disease, bone metastasis, and rheumatoid arthritis.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: May 6, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Bum Tae Kim, Hyuk Lee, Sung Youn Chang, Zang Hee Lee, Seong Hwan Kim, Hyun-Mo Ryoo
  • Publication number: 20140121155
    Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
    Type: Application
    Filed: December 27, 2013
    Publication date: May 1, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
  • Patent number: 8710049
    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 agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: April 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
  • Patent number: 8691865
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: April 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
  • Patent number: 8686021
    Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.
    Type: Grant
    Filed: May 3, 2006
    Date of Patent: April 1, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
  • Patent number: 8686161
    Abstract: The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form ? and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form ? with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: April 1, 2014
    Assignee: Mylan Laboratories Limited
    Inventors: Ramakoteswara Rao Jetti, Chetan Kanaiyalal Raval, Aggi Ramireddy Bommareddy, Debashish Datta
  • Patent number: 8680294
    Abstract: Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: March 25, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Traverse, William M. Leong, Steven P. Miller, Jennifer Albaneze-Walker, Thomas J. Hunter, Lijun Wang, Hongbiao Liao, Ashok Arasappan, Scott T. Trzaska, Randi M. Smith, Azzeddine Lekhal, Stephane L. Bogen, Jianshe Kong, Frank Bennett, F. George Njoroge, Marc Poirier, Shen-Chun Kuo, Yonggang Chen, Kenneth S. Matthews, Patrice Demonchaux, Amadeo Ferreira
  • Publication number: 20140080802
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Application
    Filed: October 28, 2013
    Publication date: March 20, 2014
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
  • Patent number: 8664443
    Abstract: The present invention relates to an improved process for the preparation of (1S,3S,5S)-2-[2(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its intermediates.
    Type: Grant
    Filed: September 4, 2012
    Date of Patent: March 4, 2014
    Assignee: Divi's Laboratories Ltd.
    Inventors: Murali Krishna Prasad Divi, Gundu Rao Padakandla, Nageswara Rao Bolneni, Gopinarayana Bodala
  • Patent number: 8653071
    Abstract: The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: February 18, 2014
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Kana Ram Kumawat, Ishtiyaque Ahmad, Pradeep Jayarajan, Anil Karbhari Shinde, Nagaraj Vishwottam Kandikere, Koteshwara Mudigonda, Venkateswarlu Jasti
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Patent number: 8633316
    Abstract: Provided is a method for producing a nitrogen-containing condensed heterocyclic compound containing the step of: reacting a compound represented by Formula (1a) or Formula (1b) with a compound represented by Formula (2) under existence of cupper or a cupper ion, and a ligand to produce a nitrogen-containing condensed heterocyclic compound represented by Formula (3a) or Formula (3b):
    Type: Grant
    Filed: January 20, 2011
    Date of Patent: January 21, 2014
    Assignee: Konica Minolta Holdings, Inc.
    Inventors: Shuichi Sugita, Eisaku Katoh, Rie Fujisawa
  • Patent number: 8618158
    Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: December 31, 2013
    Assignee: Cancer Research Technology Limited
    Inventors: Bernard Thomas Golding, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcastle, Eric Valeur, Anna Frances Watson, Martin Noble
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8598370
    Abstract: The present invention provides a process for producing Droxidopa or a pharmaceutically acceptable salt thereof comprising a step of reacting threo-N-phthaloyl-3-(3,4-dihydroxyphenyl)-L-serine represented by the formula (1) with methylamine, whereby a process for producing threo-3-(3,4-dihydroxyphenyl)-L-serine (common name: Droxidopa), which is useful as an agent for treatment of peripheral orthostatic hypotension or an agent for treatment of Parkinson's disease, with high production efficiency and without requiring troublesome operations.
    Type: Grant
    Filed: June 29, 2010
    Date of Patent: December 3, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Toshikazu Yagi, Koji Koyama, Masanori Itoh
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130317235
    Abstract: The present invention relates to an improved process for the preparation of (1S,3S,5S)-242(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its intermediates.
    Type: Application
    Filed: September 4, 2012
    Publication date: November 28, 2013
    Applicant: DIVI'S LABORATORIES LIMITED
    Inventors: Murali Krishna Prasad Divi, Gundu Rao Padakandla, Nageswara Rao Bolneni, Gopinarayana Bodala
  • Publication number: 20130296554
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: March 13, 2013
    Publication date: November 7, 2013
    Inventors: Ny Sin, Zheng Liu, Jacob Swidorski, Sing-Yuen Sit, Jie Chen, Yan Chen, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Publication number: 20130274294
    Abstract: The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: December 19, 2011
    Publication date: October 17, 2013
    Inventors: David Carcache, Manuel Koller, Silvio Ofner, David Orain, Johanne Renaud
  • Patent number: 8552051
    Abstract: The use of mesembrenone and medicaments and dietary supplements containing mesembrenone. The applicant has surprisingly found that mesembrenone exhibits potent PDE-4 inhibition properties and, in addition to being useful in treating conditions that respond to treatment with a PDE-4 inhibitor, has dual activity on account of its serotonin-uptake inhibition properties. Mesembrenone is extracted and isolated, for example as a pure compound, from plant material of the plant family Mesembryanthemaceae. Preferably a plant or plants from the genus Sceletium, more preferably, Sceletium tortuosum(L) N.E.Br is used.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: October 8, 2013
    Assignee: H. L. Hall & Sons Limited
    Inventors: Alan Harvey, Nigel Gericke, Alvaro Viljoen