Chalcogen Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/253.11)
  • Publication number: 20120115778
    Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.
    Type: Application
    Filed: July 15, 2010
    Publication date: May 10, 2012
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Gerard Karsenty, Vijay Yadav, Franck Oury
  • Publication number: 20120114765
    Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
    Type: Application
    Filed: March 31, 2010
    Publication date: May 10, 2012
    Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
  • Publication number: 20120115837
    Abstract: Provided is a solid preparation comprising (i) a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, (ii) a sugar alcohol, and (iii) a calcium antagonist, which is superior in the dissolution property and stability.
    Type: Application
    Filed: April 28, 2010
    Publication date: May 10, 2012
    Inventors: Wataru Hoshina, Makoto Fukuta, Shigeyuki Marunaka
  • Publication number: 20120077818
    Abstract: Provided herein are methods of and compositions for, treating, preventing and managing various neurological disorders. The methods comprise administering a transnorsertraline in combination with a serotonin receptor IA agonist, antagonist or modulator.
    Type: Application
    Filed: May 12, 2010
    Publication date: March 29, 2012
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Una Campbell, Judith Dunn
  • Publication number: 20120077802
    Abstract: Provided herein are spiro-cyclic compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2010
    Publication date: March 29, 2012
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Publication number: 20120071487
    Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
    Type: Application
    Filed: May 26, 2010
    Publication date: March 22, 2012
    Inventors: Vladimir Kogan, Lev Tabachnik
  • Patent number: 8129393
    Abstract: Compounds of general formula: as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain, depression and anxiety.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: March 6, 2012
    Assignee: AstraZeneca AB
    Inventors: William Brown, Andrew Griffin, Thomas Hudzik, Carla Maciag, Gennady Smagin, Christopher Walpole
  • Publication number: 20120046277
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloakyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is no
    Type: Application
    Filed: March 9, 2010
    Publication date: February 23, 2012
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Publication number: 20120028920
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: October 11, 2011
    Publication date: February 2, 2012
    Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
  • Patent number: 8097624
    Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: January 17, 2012
    Assignee: Apotex Inc.
    Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
  • Patent number: 8097629
    Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.
    Type: Grant
    Filed: February 5, 2005
    Date of Patent: January 17, 2012
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Heike Gielen-Haertwig, Barbara Albrecht, Marcus Bauser, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
  • Publication number: 20110319393
    Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.
    Type: Application
    Filed: March 17, 2010
    Publication date: December 29, 2011
    Inventors: Christophe Pierre Alain Chassaing, Thorsten Meyer
  • Publication number: 20110312958
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: May 16, 2011
    Publication date: December 22, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • Patent number: 8071600
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: December 6, 2011
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
  • Publication number: 20110281871
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Application
    Filed: July 26, 2011
    Publication date: November 17, 2011
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • 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
  • Publication number: 20110263611
    Abstract: The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed.
    Type: Application
    Filed: July 7, 2011
    Publication date: October 27, 2011
    Inventors: Lon T. Spada, Jane Guo Shiah, Patrick Hughes, Thomas C. Malone, Gerald W. Devries, Jeffrey L. Edelman, Julie A. Wurster
  • Publication number: 20110230487
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 17, 2011
    Publication date: September 22, 2011
    Inventors: Tai Wei LY, Garrett Thomas Potter, Jared Andrew Forrester
  • Publication number: 20110224210
    Abstract: The invention relates to novel bis-amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
    Type: Application
    Filed: November 18, 2009
    Publication date: September 15, 2011
    Inventors: Hamed Aissaoui, Christoph Boss, Olivier Corminboeuf, Marie-Celine Frantz, Corinna Grisostomi
  • Publication number: 20110224189
    Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Application
    Filed: May 19, 2011
    Publication date: September 15, 2011
    Inventors: Yun-Long Li, Jincong Zhuo, David Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Patent number: 8012969
    Abstract: The invention relates to “C-labeled compounds, their preparation, compositions comprising an effective amount of a “C-labeled compound, and the use of a “C-labeled compound as a radiopharmaceutical for positron emission tomography.
    Type: Grant
    Filed: January 11, 2006
    Date of Patent: September 6, 2011
    Assignee: GE Healthcare Limited
    Inventors: Christopher John Helal, Gunnar Antoni, Bengt Langstrom, Jia Zhi Sheng, Susan Beth Sobolov-Jaynes, Timothy James McCarthy
  • Publication number: 20110212946
    Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
    Type: Application
    Filed: November 3, 2009
    Publication date: September 1, 2011
    Inventors: James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman
  • Publication number: 20110212973
    Abstract: [Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that a piperazine-1-carboxylate compound, in which benzimidazol-2-ylcarbonyl, benzofuran-2-ylcarbonyl or the like binds to the 4-position of the piperazine, has an excellent FAAH inhibitory activity and further has an action to increase the effective bladder capacity, an action to ameliorate sleep disorders, an anti-diuretic action, and an analgesic activity on lower urinary tract pain including bladder pain and the like, thereby completed the present invention.
    Type: Application
    Filed: November 5, 2009
    Publication date: September 1, 2011
    Inventors: Takahiro Ishii, Takashi Sugane, Ryosuke Munakata, Satoshi Aoki, Masahide Higaki, Akiyoshi Someya
  • Patent number: 8008305
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20110201589
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Application
    Filed: August 10, 2009
    Publication date: August 18, 2011
    Applicant: EVOTEC AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xialou Wang
  • Publication number: 20110183966
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: February 4, 2011
    Publication date: July 28, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Francois Maltais, Guy W. Bemis, Tiansheng Wang, Juan Miguel Jimenez, Luca Settimo, Stephen Young, Dean Boyall, Damien Fraysse, Christopher John Davis
  • Publication number: 20110178062
    Abstract: Certain substituted indole and benzothiophene compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
    Type: Application
    Filed: February 28, 2008
    Publication date: July 21, 2011
    Inventors: Brett D. Allison, Cheryl A. Grice, Kelly J. McClure, Alejandro Santillan, JR.
  • Publication number: 20110172229
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: March 23, 2011
    Publication date: July 14, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Fredrick van Goor
  • Patent number: 7973038
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: July 5, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark T. Miller, Peter D. J. Grootenhuis, Brian Richard Bear, Jason McCartney, Jinglan Zhou
  • Publication number: 20110150833
    Abstract: Compounds useful as Rho kinase inhibitors of formula (1) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.
    Type: Application
    Filed: December 18, 2008
    Publication date: June 23, 2011
    Applicant: The Scripps Research Institute
    Inventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Yen Ting Chen, Yan Yin, Hampton Sessions, Michael P. Smolinski, Lei Yao, Bo Wang, Bozena Frackowiak-Wojtasek
  • Patent number: 7964602
    Abstract: The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.
    Type: Grant
    Filed: December 1, 2006
    Date of Patent: June 21, 2011
    Assignee: Glaxo Group Limited
    Inventors: Gregor James MacDonald, Darren Jason Mitchell, Mervyn Thompson, Susan Marie Westaway
  • Publication number: 20110144122
    Abstract: The present invention relates to derivatives of 4-{2-[phenyl-3,6-dihydropyridin-1-yl]-2-oxoalkyl}-1-piperazin-2-one and 4-{2-[phenyl-2,5-dihydropyrrol-1-yl]-2-oxoalkyl}-1-piperazin-2-one having general formula (I): in which A, B, m, R3 and n are as defined herein. The invention also relates to the preparation thereof and to the therapeutic use thereof.
    Type: Application
    Filed: December 13, 2010
    Publication date: June 16, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Marco BARONI, Francoise BONO, Sandrine DELBARY-GOSSART
  • Patent number: 7956052
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: June 7, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Fredrick van Goor
  • Publication number: 20110118263
    Abstract: The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.
    Type: Application
    Filed: June 30, 2009
    Publication date: May 19, 2011
    Applicant: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co. Ltd.
    Inventors: Jianqi Li, Kai Gao, Na Lv
  • Publication number: 20110118233
    Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Application
    Filed: May 6, 2009
    Publication date: May 19, 2011
    Inventors: Peter A. Blomgren, David R. Brittelli, Kevin S. Currie, Seung H. Lee, Jeffrey E. Kropf, Scott A. Mitchell, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Zhongdong Zhao, Pavel E. Zhichkin
  • Patent number: 7943622
    Abstract: Disclosed are novel piperazine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
    Type: Grant
    Filed: June 6, 2007
    Date of Patent: May 17, 2011
    Assignee: Cornerstone Therapeutics, Inc.
    Inventors: Roger B. Clark, Daniel Elbaum
  • Publication number: 20110112075
    Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Application
    Filed: August 18, 2010
    Publication date: May 12, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Markus FOLLMANN, Volkmar WEHNER, Jerome MENEYROL, Jean-Michel ALTENBURGER, Frédéric PETIT, Gilbert LASSALLE, Jean-Pascal HERAULT
  • Publication number: 20110077244
    Abstract: The present invention relates to synthetic studies of a novel thiophenediamine derivative having a urea structure and to finding pharmaceutical actions thereof. The present invention provides a compound represented by the following general formula (1) or a salt thereof. In the formula (1), R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, etc. R3 represents a hydroxy group, a lower alkoxy group which may have a substituent, a lower cycloalkyloxy group which may have a substituent, etc. R4 and R5 are the same or different and represent a halogen atom, a lower alkyl group, a hydroxy group, etc. X represents a lower alkylene group which may have a substituent, etc. Y represents a single bond or a lower alkylene group which may have a substituent, etc. W1-W2 represents N—CH, CH—N, etc. and l and m are the same or different and represent 0, 1, etc.
    Type: Application
    Filed: May 25, 2009
    Publication date: March 31, 2011
    Applicant: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyaki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe
  • Patent number: 7915253
    Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: March 29, 2011
    Assignee: Kalypsys, Inc
    Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen K. Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
  • Publication number: 20110059968
    Abstract: The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
    Type: Application
    Filed: December 29, 2008
    Publication date: March 10, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Wilfried Hornberger, Helmut Mack, Andreas Kling, Achim Moeller, Barbara Vogg, Jürgen Delzer, Gisela Backfisch, Armin Beyerbach
  • Publication number: 20110059944
    Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Application
    Filed: November 4, 2010
    Publication date: March 10, 2011
    Inventors: Peter A. Blomgren, Kevin S. Currie, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Zhongdong Zhao, Pavel E. Zhichkin, Douglas G. Stafford, Jeffrey E. Kropf
  • Publication number: 20110053917
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the Al adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
    Type: Application
    Filed: November 4, 2010
    Publication date: March 3, 2011
    Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
  • Publication number: 20110009420
    Abstract: The present invention provides compounds of the formula wherein R1, R2 and B are as herein described, pharmaceutical compositions comprising these compounds, use of these compounds for the preparation of pharmaceutical compositions and methods of use thereof for the treatment and/or prevention of disorders and diseases wherein modulation of the H3 receptor is beneficial.
    Type: Application
    Filed: September 16, 2010
    Publication date: January 13, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventor: Knud Erik Andersen
  • Publication number: 20110009421
    Abstract: An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.
    Type: Application
    Filed: February 27, 2009
    Publication date: January 13, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masaki Setoh, Toshitake Kobayashi, Toshio Tanaka, Atsuo Baba
  • Publication number: 20100331341
    Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.
    Type: Application
    Filed: June 28, 2010
    Publication date: December 30, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Johan ANDERSSON, Helena GYBÄCK, Anh JOHANSSON, Christian Erik LINDE, Jonas MALMSTRÖM, Gunnar NORDVALL, Tatjana WEIGELT, Gitte TERP
  • Patent number: 7851471
    Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: December 14, 2010
    Assignee: AstraZeneca AB (PUBL)
    Inventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
  • Publication number: 20100305090
    Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
    Type: Application
    Filed: March 5, 2008
    Publication date: December 2, 2010
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
  • Patent number: 7834001
    Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
    Type: Grant
    Filed: November 8, 2005
    Date of Patent: November 16, 2010
    Assignee: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
  • Publication number: 20100278897
    Abstract: The present disclosure generally provides intraocular implants including at least one therapeutic bioactive agent and a molecular partitioning system. The molecular partitioning system comprises at least two phases wherein the first phase has an inherent viscosity equal or greater than the inherent viscosity of a second phase. The molecular partitioning system allows the intraocular implants to controllably release the at least one therapeutic bioactive agent into the surrounding tissues once implanted.
    Type: Application
    Filed: May 1, 2009
    Publication date: November 4, 2010
    Applicant: ALLERGAN, INC.
    Inventors: Ruiwen SHI, Patrick M. Hughes
  • Patent number: 7816362
    Abstract: Novel piperazine derivatives are provided having the formula wherein R1 is cyano, nitro, trifluoromethyl or halogen, or pharmaceutically acceptable acid addition salts thereof, which are useful as 5-HT1A receptor antagonists.
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: October 19, 2010
    Assignee: Wyeth LLC
    Inventors: Wayne Everett Childers, Michael Kelly, Sharon Joy Rosenzweig-Lipson