The Substituent Nitrogen Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Nonionic Bonding Patents (Class 564/164)
  • Patent number: 9527805
    Abstract: The invention provides for novel compounds which are inhibitors of lysine-specific demethylase 1 (LSD1) such as those according to Formula II. Such compounds may be used to treat disorders, including cancer.
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: December 27, 2016
    Inventors: Robert A. Casero, Ian Bytheway, Patrick M. Woster
  • Patent number: 9259403
    Abstract: The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: February 16, 2016
    Inventors: Rahul Surana, Mahendra G. Dedhiya
  • Publication number: 20150148424
    Abstract: The present invention relates to stable dosage forms of levomilnacipran and pharmaceutically acceptable salts thereof. Processes for the preparation of these dosage forms and methods of using these dosage forms are also described.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Inventors: Anil Chhettry, Murali Divi, Rahul Surana
  • Patent number: 8987464
    Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., W is oxygen atom or sulfur atom, etc., X is halogen atom, C1-C6haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is —CH?NOR1a, —C(O)OR1c, —C(O)NHR1d, phenyl substituted with (Z)p1, D-14, D-52, D-53, D-55 to D-59, etc., R1a is C1-C6alkyl, etc., R1c is C1-C6alkyl, etc., R1d is hydrogen atom, —C(O)R15, —C(O)OR15, etc., R2 is C1-C6alkyl, —CH2R14a, C1-C6alkynyl, —C(O)R15, —C(O)OR15, etc., further when R1 is —CH?NOR1a, —C(O)OR1c or —C(O)N(R1e)R1d, R2 may be hydrogen atom, R3 is C1-C6haloalkyl, etc., R14a is cyano, —OR25, etc., R15 is C1-C6alkyl, C1-C6haloalkyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl, etc., R25 is C1-C4alkyl, C1-C4haloalkyl, —C(O)R32 or —C(O)OR32, etc., R32 is C1-C6alkyl or C3-C6cycloalkyl, etc., Z is halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, etc.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: March 24, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Yuki Furukawa, Ken-ichi Toyama, Manabu Yaosaka, Eitatsu Ikeda, Yoshihide Masuzawa, Mitsuaki Komoda
  • Publication number: 20150038574
    Abstract: Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: February 5, 2015
    Applicant: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Judd Berman, Tan Quach
  • Publication number: 20150038587
    Abstract: The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Rahul Surana, Mahendra G. Dedhiya
  • Patent number: 8946297
    Abstract: To provide an anthranilamide formulation compound for improving pest controlling effects. A solid composition for pest control which comprises an amorphous anthranilamide compound or its salt as a pesticidal active ingredient, a nonionic surfactant and/or an anionic surfactant and a mineral carrier.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: February 3, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Masayuki Morita, Takao Awazu, Akira Nakagawa, Taku Hamamoto
  • Patent number: 8946296
    Abstract: The invention relates to compounds of Formula (I): (A?)x-(A)-(B)—(Z)-(L)-C(?O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A?), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: February 3, 2015
    Assignee: Oryzon Genomics S.A.
    Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
  • Publication number: 20140357634
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: BERT NOLTE, WOLFGANG SCHRÖDER, KLAUS LINZ, WERNER ENGLBERGER, HANS SCHICK, HEINZ GRAUBAUM, BIRGIT ROLOFF, SIGRID OZEGOWSKI, JÓZSEF BÁLINT, HELMUT SONNENSCHEIN
  • Patent number: 8883945
    Abstract: A compound of the formula R1.[(AO)n.—R2]m (I) where: R1 is the residue of a group having at least m active hydrogen atoms; AO is an alkylene oxide residue; each n is independently from 1 to 100; m is at least 2; and each R2 is independently H, a C1 to C21 hydrocarbyl, or an acyl group —OC.R3, where R3 is a C1 to C21 hydrocarbyl group, wherein on average greater than one of the R2 groups is or comprises a C4 to C21 hydrocarbyl group comprising at least two ethylenic double bonds. The compounds are particularly suitable for use in preparing aqueous emulsions or dispersions of resins and polymers, especially alkyd resins.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: November 11, 2014
    Assignees: Croda International PLC, Croda Americas LLC
    Inventors: William Harry McNamee, Trevor Graham Blease, Johnny Denis Grade, Hanamanthsa Shankarsa Bevinakatti
  • Patent number: 8865937
    Abstract: The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
    Type: Grant
    Filed: November 8, 2010
    Date of Patent: October 21, 2014
    Inventors: Mahendra G. Dedhiya, Rahul Surana
  • Patent number: 8853453
    Abstract: The present invention relates to processes for reducing impurities in lacosamide during the preparation of lacosamide. The invention provides processes for minimizing or removing impurities such as (2R)-2-(acetylamino)-3-(benzylamino)-3-oxopropyl acetate of Formula II or (2R)-2-propanoylamino-N-benzyl-3-methoxypropionamide of Formula III in lacosamide.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: October 7, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Hari Mohan Sriram, Mukesh Kumar Madhra, Mukesh Kumar Sharma
  • Publication number: 20140256743
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Applicants: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
  • Patent number: 8809280
    Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 19, 2014
    Assignee: Lytix Biopharma AS
    Inventors: Morten Strom, Terkel Hansen, Martina Havelkova, Veronika Torfoss
  • Patent number: 8754215
    Abstract: The present disclosure describes a novel, cost-effective process for preparation of a 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2,1-a]isoquinoline derivatives. Specifically, it discloses a process for the preparation of the anthelmintic drug praziquantel through the use of a novel intermediate, 2-[(2,2-dimethoxyethyl)benzyl amino]-N-phenethylacetamide. This present disclosure also describes a novel crystalline form of 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: June 17, 2014
    Assignee: Sequent Scientific Limited
    Inventors: Lingappa Balaya, Mahalinga Manjathuru, Yogeesh Derambala, Pejakala Kakrannaya Vasudeva, Thangavel Arulmoli
  • Patent number: 8722896
    Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: May 13, 2014
    Assignee: The Regents of the University of California
    Inventors: Qun-Yong Zhou, Jia-Da Li, Qi Huang
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Publication number: 20140117280
    Abstract: An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.
    Type: Application
    Filed: May 16, 2012
    Publication date: May 1, 2014
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Kentaro Ishii, Ryoji Otaki, Takafumi Oda, Shota Arakawa
  • Publication number: 20140066500
    Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Seema BHAT
  • Publication number: 20140044708
    Abstract: A process of lowering the viscosity of a solution includes preparing a solution comprising a compound of formula I, at a concentration in the final formulation of between 10 and 250 mM, and a protein having at least one antibody fragment whose concentration is between 50 and 350 mg/mL and whose pH is between 5 and 8. The compound lowers the viscosity of the solution, which is difficult to inject, by a value of at least 15% relative to the viscosity of a solution of at least one protein having at least one antibody fragment of the same concentration and of the same pH not containing the compound.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Inventors: Emmanuel DAUTY, Thomas BALLET, Remi Soula
  • Patent number: 8604241
    Abstract: The present invention relates to a method for synthesizing a pharmaceutically acceptable acid addition salt of (1S, 2R)-milnacipran comprising the following successive steps: (a) reaction of phenylacetonitrile and of (R)-epichlorhydrin in the presence of a base containing an alkaline metal, followed by a basic treatment, and then by an acid treatment in order to obtain a lactone; (b) reaction of said lactone with MNEt2, wherein M represents an alkaline metal, or with NHEt2 in the presence of a Lewis acid-amine complex, in order to obtain an amide-alcohol; (c) reaction of said amide-alcohol with thionyl chloride in order to obtain a chlorinated amide; (d) reaction of said chlorinated amide with a phthalimide salt in order to obtain a phthalimide derivative; (e) hydrolysis of the phthalimide group of said phthalimide derivative in order to obtain (1S, 2R)-milnacipran, and (f) salification of (1S, 2R)-milnacipran in a suitable solvent system in the presence of a pharmaceutically acceptable acid.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: December 10, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Marc Nicolas, Paul Hellier, Catherine Diard, Laurent Subra
  • Patent number: 8598386
    Abstract: The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20° C.
    Type: Grant
    Filed: October 17, 2011
    Date of Patent: December 3, 2013
    Assignee: Euticals GmbH
    Inventors: Richard Wisdom, Joerg Jung, Andreas Meudt
  • Publication number: 20130317110
    Abstract: A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.
    Type: Application
    Filed: May 23, 2013
    Publication date: November 28, 2013
    Applicant: FUJITSU LIMITED
    Inventors: Nozomu Kamiya, Atsushi Tomonaga, Hajime Sugiyama
  • Patent number: 8530521
    Abstract: A compound having the structure wherein Y is selected from the group consisting of —C(O)OR2, —C(O)NHR8, —C(CH2)1-2OR3, OH, and or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: September 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Robert K. Baker, Kathleen M. Rupprecht, Michael Man-Chu Lo, Brent Whitehead
  • Publication number: 20130210919
    Abstract: The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Inventor: Forest Laboratories Holdings Ltd.
  • Patent number: 8466318
    Abstract: The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of formula (1) and wherein A and R1—R4 are defined herein.
    Type: Grant
    Filed: May 15, 2007
    Date of Patent: June 18, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenter Linz, Gerd Kraemer, Zeno A. Leuter, Markus Ostermeier, Werner Rall, Claudia Ochs, Rolf Schmid
  • Patent number: 8378142
    Abstract: The present invention is concerned with novel compounds and their use for the preparation of lacosamide. The present invention also contemplates processes for the preparation of lacosamide employing the novel compound of general Formula II, Formula IIa or Formula IIb as intermediate. Wherein R1 is —OH or —OMe; R2 is —OH or —NH—CH2—C6H5.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: February 19, 2013
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Chandra Has Khanduri
  • Publication number: 20130035296
    Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
    Type: Application
    Filed: November 2, 2010
    Publication date: February 7, 2013
    Applicant: LYTIX BIOPHARMA AS
    Inventors: Morten Strom, Terkel Hansen, Martina Havelkova, Veronika Torfoss
  • Patent number: 8367732
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: February 5, 2013
    Assignee: Virobay, Inc.
    Inventors: John O. Link, Craig J. Mossman, Jie Liu, Soon Hyung Woo
  • Patent number: 8318779
    Abstract: The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.
    Type: Grant
    Filed: May 30, 2007
    Date of Patent: November 27, 2012
    Assignee: Janssen R&D Ireland
    Inventors: Tim Hugo Maria Jonckers, Inge Dierynck, Stefaan Julien Last, Herman De Kock
  • Publication number: 20120289744
    Abstract: The present invention relates to an improved and commercially, viable process for the resolution of racemic cis milnacipran of formula I and its pharmaceutically acceptable salts of formula II. The present invention comprises using racemic cis milnacipran or its pharmaceutically acceptable salts as starting material, a low cost and commercially available resolving agent of formula III and industrially safe and economically low cost material such as water as a solvent. The said process results into optical isomers of racemic cis milnacipran having excellent optical purity without involving multiple crystallization steps. The present invention also comprises the concept of green chemistry as the invention works well with water as a solvent thereby minimizing the use of any other solvent.
    Type: Application
    Filed: December 20, 2010
    Publication date: November 15, 2012
    Applicant: ARCH PHARMALABS LIMITED
    Inventors: Ganesh Gurpur Pai, Arun Kanti Mandal, Kamlesh Jayantilal Ranbhan, Vikram Sarjerao Jagtap, Dayaghan Gangadhar Patil, Yuvraj Kashinath Zunjarrao
  • Publication number: 20120264760
    Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
    Type: Application
    Filed: June 6, 2012
    Publication date: October 18, 2012
    Applicants: University of Georgia Research Foundation, Inc., Brandeis University
    Inventors: Lizbeth K. Hedstrom, Boris Striepen
  • Publication number: 20120252792
    Abstract: The invention provides methods, compositions, and kits for the inhibition of members of the Rho GTPase family. Specifically, the invention provides methods, compositions and kits for the inhibition of RhoA and/or RhoC transcriptional signalling. The invention finds use in treatment of Rho-mediated disease states (e.g., tumor metastasis, inflammation, inflammatory disease), Rho-mediated biological conditions, and in cell signaling research.
    Type: Application
    Filed: September 17, 2010
    Publication date: October 4, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Richard Neubig, Chris Evelyn, Jenny Ryu, Scott Larsen, Jessica Bell
  • Publication number: 20120184774
    Abstract: The present invention relates to an improved process for the preparation of pharmaceutically acceptable salts of milnacipran by mutual acid radical exchange.
    Type: Application
    Filed: December 20, 2011
    Publication date: July 19, 2012
    Inventors: Vikram Sarjerao Jagtap, Ravindra Baburao Chache, Kamiesh Jayantital Ranbhan, Yuvaraj Kashinath Zunjarrao, Pushpalata Sarjekar, Arun Kanti Mandal, Ganesh Gurpur Pai
  • Patent number: 8222454
    Abstract: The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to resolve.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: July 17, 2012
    Assignee: Zhejiang Haisen Pharmaceutical Co., Ltd.
    Inventors: Lin Ai, Xiao Liu
  • Publication number: 20120172426
    Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: July 1, 2011
    Publication date: July 5, 2012
    Applicant: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan Bhat, Kouacou Adiey
  • Publication number: 20120149910
    Abstract: The object of the present invention is to provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Disclosed are the carboxamides represented by the following Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite controlling agents.
    Type: Application
    Filed: August 3, 2010
    Publication date: June 14, 2012
    Applicant: Bayer CropScience AG
    Inventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Yukiyoshi Watanabe, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Gorgens
  • Publication number: 20120142646
    Abstract: The present invention provides compounds of formula (I) wherein k, Ar, R2, R3, R4, R5, R4?, R5?, R6, R7, A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 19, 2007
    Publication date: June 7, 2012
    Inventors: Lilian Alcaraz, Roger Victor Bonnert, Stephen Connolly, Anthony Ronald Cook, Adrian Fisher, Alexander Humphries, Piotr Raubo
  • Publication number: 20120108515
    Abstract: Novel compounds which may be for treatment, prevention or alleviation of a condition associated with bone loss or low bone density or to inhibit osteoclast differentiation and stimulation, bone resorption, or loosening of a prosthetic device.
    Type: Application
    Filed: June 17, 2010
    Publication date: May 3, 2012
    Applicant: NEOBIOTICS AB
    Inventors: Anders Grubb, Franciszek Kasprzykowski, Ulf Lerner, Beata Zolnowska, Regina Kasprzykowska
  • Publication number: 20120095251
    Abstract: The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20° C.
    Type: Application
    Filed: October 17, 2011
    Publication date: April 19, 2012
    Inventors: Richard WISDOM, Joerg JUNG, Andreas MEUDT
  • Publication number: 20120065208
    Abstract: A method for treating, preventing or ameliorating a hyperliferative disease and/or disorder in a mammal, comprises administering a therapeutically effective amount of one or more compounds selected from the group consisting of a compound of Formula (III), a compound of Formula (IV), and a pharmaceutically acceptable salt of Formula (III) or Formula (IV): wherein R2 is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, vinyl and allyl.
    Type: Application
    Filed: September 28, 2011
    Publication date: March 15, 2012
    Inventors: Gilles Klopman, Suman K. Chakravarti
  • Publication number: 20120041036
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: February 16, 2012
    Inventors: Isao Kinoyama, Yohei Koganemaru, Takehiro Miyazaki, Takuya Washio
  • Publication number: 20120029013
    Abstract: The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C1-C6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3? each independently or together are a hydrogen atom or C1-C6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.
    Type: Application
    Filed: April 2, 2010
    Publication date: February 2, 2012
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Stéphane Cuisiat, Adrian Newman-Tancredi, Olivier Vitton, Bernard Vacher
  • Patent number: 8093426
    Abstract: The present invention is concerned with novel compounds and their use for the preparation of lacosamide. The present invention also contemplates processes for the preparation of lacosamide employing the novel compound of general Formula II, Formula IIa or Formula IIb as intermediate. Wherein R1 is —OH or —OMe; R2 is —OH or —NH—CH2—C6H5.
    Type: Grant
    Filed: December 3, 2008
    Date of Patent: January 10, 2012
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Chandra Has Khanduri
  • Publication number: 20110275615
    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or un
    Type: Application
    Filed: October 29, 2010
    Publication date: November 10, 2011
    Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
  • Patent number: 8053452
    Abstract: There is provided a novel pest control agent (pesticide), particulally insecticide or miticide. A substituted isoxazoline compound or a substituted enone oxime compound represented by Formula (1) or (2), and apest control agent containing them: wherein A1, A2, A3 and A4 are C or N, G1 is a benzene ring, etc., G2 is 1-trazolyl, etc., X and Y are halogen atom, etc., R3 is haloalkyl, etc., R3a is halogen atom, etc., R3b and R3c are H, etc., is haloalkyl, etc., m is 0-5, n is 0-4.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: November 8, 2011
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Kenichi Toyama, Yuki Furukawa, Mitsuaki Komoda
  • Publication number: 20110269986
    Abstract: The invention relates to pharmaceutical chemistry notably to new biologically active substances (BAS) and their properties. In particular, the invention relates to Creatine derivatives having a general formula: NH?C(NH2)—N(CH3)—CH2—CO—NH—R*X, wherein R—amino acid residue of aliphatic, aromatic or heteroaromatic L-amino acid or its derivative representing a salts of amino acid, amino acid esters, amino acid amides or peptides; X—lower organic or mineral acid or water. New substances are prepared by interaction of aforesaid amides of sarcosine having a general formula of HN(CH3)—CH2—CO—NH—R*X, wherein: R is amino acid residue or substituted amino acid residue; X is low-molecular-weight organic acid or mineral acid or water, with a guanidinylating agents with the in organic solvents at temperature not exceeding 50° C. New chemical compounds can be used as a remedy possessing a neuroprotective activity.
    Type: Application
    Filed: December 24, 2008
    Publication date: November 3, 2011
    Inventors: Sergej Vladimirovich Burov, Natalia Vasilyevna Khromova, Anna Alexandrovna Khromova, Petr Alekseevich Khromov
  • Publication number: 20110263658
    Abstract: The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: August 18, 2008
    Publication date: October 27, 2011
    Inventors: Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Rejean Fortin, Patrick Lacombe, Daniel McKay, Tom Yao-Hsiang Wu
  • Publication number: 20110262994
    Abstract: A compound of the general formula X-[Q-W—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represent an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.
    Type: Application
    Filed: July 1, 2011
    Publication date: October 27, 2011
    Applicant: Polytherics Limited
    Inventor: Antony GODWIN
  • Publication number: 20110263604
    Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: October 27, 2011
    Applicant: Oryzon Genomics, S.A.
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria