Plural 1,4-diazine Rings Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/252.11)
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Publication number: 20100160331Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: April 30, 2008Publication date: June 24, 2010Inventors: Ki Ho Lee, Han Ju Yi, Hyeon Cho, Dae Joong Im, Eun Hee Chae, Yeon Jung Choi
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Publication number: 20100152197Abstract: The present invention relates to compounds of formula (I) The compounds act via antagonism of the CCR2b receptor and may be used to treat inflammatory disease and/or neuropathic pain.Type: ApplicationFiled: December 10, 2009Publication date: June 17, 2010Applicant: ASTRAZENECA ABInventors: John Cumming, Alan Wellington Faull, David Waterson
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Patent number: 7737143Abstract: A compound of general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating kinase-associated disease states using the compound of formula (I) is also described.Type: GrantFiled: December 3, 2004Date of Patent: June 15, 2010Assignee: YM Biosciences Australia Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Xianyong Bu
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Patent number: 7737142Abstract: The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.Type: GrantFiled: January 20, 2006Date of Patent: June 15, 2010Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Eva Againe Csongor, Janos Galambos, Katalin Nogradi, Istvan Vago, Istvan Gyertyan, Bela Kiss, Istvan Laszlovszky, Judit Laszy, Katalin Saghy
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Publication number: 20100144704Abstract: Disclosed are methods of reducing amyloid-? peptide levels in a subject. The method involves administering to the subject a therapeutically effective amount of a bisdioxopiperazine or a pharmaceutically acceptable salt thereof to reduce ?-amyloid peptide levels.Type: ApplicationFiled: June 8, 2007Publication date: June 10, 2010Inventors: Nigel H. Greig, Kurt Hellmann
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Publication number: 20100144710Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof, wherein A, B, D, Ar1, Ar2, R2, R3, R4, a, m and n are defined in the specification, methods for the use thereof, processes for making and pharmaceutical compositions containing the same.Type: ApplicationFiled: February 28, 2008Publication date: June 10, 2010Applicant: ASTRAZENECA ABInventors: Jalaj Arora, Methvin Isaac, Abdelmalik Slassi, Louise Edwards, Satheesh Nair, Fupeng Ma
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Publication number: 20100137329Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.Type: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Applicant: SANOFI-EVENTISInventors: Ahmed ABOUABDELLAH, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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Publication number: 20100135999Abstract: The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is 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: ApplicationFiled: October 5, 2009Publication date: June 3, 2010Applicant: SANOFI-AVENTISInventors: Marc Nazaré, Gernot ZECH, Melitta JUST, Tilo WEISS, Gerhard HESSLER, Joerg Czech
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Publication number: 20100137330Abstract: The present invention relates to a new use of a compound of the formula (I) wherein R1 is NH2, piperazin-1-yl, 4-methylpiperazin-1-yl, 4-methyl-1,4-diazepan-1-yl or 4-ethylpiperazin-1-yl; R2 is hydrogen, fluoro, CH3, CH2CH3, OCH3, CF3 or OCF3; R3 is hydrogen, CH3 or fluoro; as a free base or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the prevention and/or treatment of bone-related disorders, osteoporosis and increasing bone formation, bone mineral density. The present invention further relates to a method of prevention and/or treatment of these disorders.Type: ApplicationFiled: August 12, 2009Publication date: June 3, 2010Inventors: Ratan Bhat, Anna-Lena Berg
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Publication number: 20100130506Abstract: A compound of Formula I in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: December 10, 2008Publication date: May 27, 2010Inventors: Gurdip BHALAY, Emma Budd, Graham Charles Bloomfield, Stephen Paul Collingwood, Andrew Dunstan, Lee Edwards, Peter Gedeck, Catherine Howsham, Peter Hunt, Thomas Anthony Hunt, Paul Oakley, Nichola Smith
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Publication number: 20100130447Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: November 15, 2007Publication date: May 27, 2010Inventors: Christopher John Burns, Michael Francis Harte, James T. Palmer
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100125075Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Publication number: 20100120785Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)? or N?, provided that at least one of A and B is —N?, n is 1-3, m is 0-3, and R14 are as defined herein.Type: ApplicationFiled: May 7, 2008Publication date: May 13, 2010Applicant: ELI LILLY AND COMPANYInventors: Valentina O. Badescu, Anne Marie Camp, Barry Peter Clark, Michael Philip Cohen, Sandra Ann Filla, Peter Thaddeus Gallagher, Sarah Lynne Hellman, Michael Philip Mazanetz, Marta Maria Pineiro-Nunez, John Mehnert Schaus, Patrick Gianpietro Spinazze, Maria Ann Whatton
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Publication number: 20100120769Abstract: The present invention relates to compounds of formula I wherein s, R1a and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Matthias Nettekoven, Jean-Marc ` Plancher, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Patent number: 7709475Abstract: The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: May 19, 2005Date of Patent: May 4, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Jun Shibata, Tadashi Shimamura, Hideki Kurihara, Takashi Mita, Nobuhiko Kawanishi, Takashi Hashihayata, Mikako Kawamura, Takeshi Sagara, Sachie Arai, Hiroshi Hirai
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Publication number: 20100105654Abstract: A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structures VA, VB, VIIA and VIIB where the values of the variables are defined herein.Type: ApplicationFiled: October 23, 2009Publication date: April 29, 2010Inventors: Rustum S. BOYCE, Natalia Aurrecoechea, Daniel Chu, Aaron Smith, Christopher R. Conlee, Brian D. Thompson, Judith de Armas Kuntz, David L. Musso, Kevin K. Barvian, Stephen A. Thomson, William R. Swain, Kien S. Du, Brian A. Chauder, Jason D. Speake, Michael J. Bishop
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Publication number: 20100105682Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a piperazine ring and a cyclopropyl ring are disclosed of the general formula (I) where X1 and X2 are linkers.Type: ApplicationFiled: October 12, 2007Publication date: April 29, 2010Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Ramesh Kaul
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Publication number: 20100105660Abstract: A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M1, M2, L1, L2, W1, W2, X1, X2, Y1, Y2, A, R5 and R5a are as defined herein for the for treatment of conditions treatable by the blockade of an epithelial sodium channel, particularly conditions benefiting from mucosal hydration.Type: ApplicationFiled: May 5, 2008Publication date: April 29, 2010Inventors: Robin Alec Fairhurst, Rebecca Fraser, Paul Oakley, Stephen Paul Collingwood, Nichola Smith, Emily Stanley, Maria Ines Rodriguez Perez
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Publication number: 20100105693Abstract: The present invention relates to substituted piperazine compounds that are useful modulators of muscarinic receptors. The present invention also provides compositions comprising such compounds, and methods for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: January 5, 2010Publication date: April 29, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lewis Makings, Dennis Hurley, Miguel Gracia-Guzman Blanco, Daniele Bergeron, Akiko Nakatani
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Publication number: 20100105694Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in claim 1, having selective 2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: October 10, 2007Publication date: April 29, 2010Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernández, Juan Antonio Vega-Ramiro, Francisca Delgado-Jiménez, Wilhelmus Helena Ignatius Maria Drinkenburg
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Publication number: 20100105652Abstract: Substituted heteroaryl nitrile salt of Formula I, processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.Type: ApplicationFiled: February 28, 2008Publication date: April 29, 2010Inventors: Jose Miguel Coteron-Lopez, Beatriz Diaz-Hernandez, Jose Maria Fiandor-Roman, Maria Marco-Martin
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Patent number: 7704995Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.Type: GrantFiled: May 2, 2003Date of Patent: April 27, 2010Assignee: Exelixis, Inc.Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
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Patent number: 7700583Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: GrantFiled: October 6, 2005Date of Patent: April 20, 2010Assignee: High Point Pharmaceuticals, LLCInventors: Anette Gundertofte, Anker Steen Jorgensen, Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen, Inge Thoger Christensen, Kilburn Paul John
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Publication number: 20100093703Abstract: The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Ruediger Streicher, Matthias Eckhardt, Annette Schuler-Metz, Alexander Pautsch, Corinna Schoelch
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Publication number: 20100081665Abstract: The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.Type: ApplicationFiled: July 28, 2009Publication date: April 1, 2010Inventors: Richard W. Scott, Doron Greenbaum, Dahui Liu, Xiaodong Fan, Yongjiang Xu, Haizhong Tang, Ehab Khalil
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Publication number: 20100075976Abstract: The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)? or —N?; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.Type: ApplicationFiled: August 19, 2008Publication date: March 25, 2010Inventors: Michael Philip Cohen, Sarah Lynne Hellman, Sean Patrick Hollinshead, Sandra Ann Filla, Michael Wade Tidwell
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Patent number: 7678791Abstract: Substituted rifamycin derivatives in which a nitroimidazole, nitrothiazole or nitrofuran pharmacophore is covalently bonded to a rifamycin, methods of using the rifamycin derivatives, and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.Type: GrantFiled: July 12, 2007Date of Patent: March 16, 2010Assignee: Cumbre IP Ventures, L.P.Inventors: Charles Z. Ding, In Ho Kim, Jiancheng Wang, Zhenkun Ma, Yafei Jin, Keith D. Combrink, Genliang Lu, A. Simon Lynch
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Publication number: 20100034784Abstract: The present invention provides a group of compounds found to increase the number of neurons derived from stem cells for use as a therapeutic agent in neurological conditions or diseases. In one embodiment of the present invention, the compounds are used to detect the mechanism by which the number of neurons is increased.Type: ApplicationFiled: July 9, 2009Publication date: February 11, 2010Applicant: NEURALSTEM, INC.Inventors: Judith KELLEHER-ANDERSSON, Karl K. JOHE
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Publication number: 20100029605Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.Type: ApplicationFiled: September 24, 2007Publication date: February 4, 2010Applicants: Novartis AGInventors: Pamela Albaugh, Gregory S. Chopiuk, Qiang Ding, Shenlin Huang, Zuosheng Liu, Shifeng Pan, Pingda Ren, Xia Wang, Xing Wang, yongping Xie, Chengzhi Zhang, Qiong Zhang, Guobao Zhang, Daniel Poon, Paul Renhowe, Martin Sendzik
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Publication number: 20100022539Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: September 15, 2009Publication date: January 28, 2010Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20100022528Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: October 2, 2007Publication date: January 28, 2010Applicant: ERIMOS PHARMACEUTICALS LLC.Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
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Publication number: 20100022512Abstract: Compositions containing at least one Chk1 inhibitor and at lease one cyclodextrin are disclosed. Also disclosed are methods of treating a cancer or potentiating a cancer treatment with a composition comprising at least one Chk1 inhibitor and at least one cyclodextrin.Type: ApplicationFiled: October 2, 2007Publication date: January 28, 2010Inventors: Wendy A. Wisdom, Anita A. Colvin, Sandy Koppenol
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Patent number: 7652011Abstract: The invention relates to 4-[(arylmethyl)aminomethyl]piperidine derivatives of general formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparation process and therapeutic application.Type: GrantFiled: May 26, 2006Date of Patent: January 26, 2010Assignee: sanofi-aventisInventors: Michael Bosch, Jean Wagnon
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Patent number: 7648979Abstract: The present invention relates to compounds of formula I wherein A, G and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: January 28, 2008Date of Patent: January 19, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Jean-Marc Plancher, Hans Richter, Olivier Roche, Sven Taylor
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Publication number: 20100009987Abstract: Compounds of formula (I): inhibit microtubule affinity regulating kinase (MARK) and therefore find use in treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.Type: ApplicationFiled: June 1, 2007Publication date: January 14, 2010Inventors: Michela Bettati, Ian Churcher, Peter Alan Hunt, Victoria Alexandra Steadman
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Publication number: 20100009962Abstract: The present invention is directed to benzyl-substituted quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of diseases in which the M1 receptor is involved.Type: ApplicationFiled: June 27, 2007Publication date: January 14, 2010Inventors: Craig Lindsley, William D. Shipe, Feng Yang, Jaime Lynn Bunda
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Publication number: 20100004231Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.Type: ApplicationFiled: July 1, 2009Publication date: January 7, 2010Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
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Patent number: 7642259Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: July 3, 2006Date of Patent: January 5, 2010Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20090317360Abstract: Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: June 11, 2008Publication date: December 24, 2009Inventors: Roopa Rai, Franz Ulrich Schmitz, Christopher Don Roberts, Irina Slobodov, Martin Robert Leivers
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Publication number: 20090312309Abstract: Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.Type: ApplicationFiled: June 30, 2006Publication date: December 17, 2009Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Rolf Hohlweg, Knud Erik Andersen, Jan Lindy Sorensen, Jane Marie Lundbeck
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Publication number: 20090306091Abstract: The technical field of the present invention relates to antimalarial therapy using a synthetic artemisinin derivative and bisquinoline derivative.Type: ApplicationFiled: May 17, 2007Publication date: December 10, 2009Inventors: Vyas Madhavrao Shingatgeri, Venkatesha Udupa
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Publication number: 20090306070Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.Type: ApplicationFiled: October 2, 2007Publication date: December 10, 2009Applicant: Erimos Pharmaceuticals LLCInventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
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Patent number: 7629341Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.Type: GrantFiled: June 11, 2003Date of Patent: December 8, 2009Assignee: Symphony Evolution, Inc.Inventors: Lynne Canne Bannen, Erick W. Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew, Shumeye Mamo, Zhaoyang Wen, Wei Xu
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Publication number: 20090298831Abstract: The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal.Type: ApplicationFiled: May 29, 2009Publication date: December 3, 2009Inventors: Yonggil Kim, Nahmryune Cho, Yunhee Kim, Joon Heo, Seonmin Dong, Mi Kyung Ji, Man-Young Cha, Kiho Lee
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Patent number: 7625889Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.Type: GrantFiled: July 25, 2007Date of Patent: December 1, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
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Patent number: 7625902Abstract: The invention is concerned with novel imidazolidinone derivatives of formula (I): wherein R1 to R11 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used in pharmaceutical compositions.Type: GrantFiled: March 24, 2008Date of Patent: December 1, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Ulrike Obst Sander, Stephan Roever, Tanja Schulz-Gasch, Matthew Wright
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Patent number: 7622497Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 17, 2004Date of Patent: November 24, 2009Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Songchun Jiang, Han-Zhong Zhang
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Publication number: 20090281099Abstract: The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective ?2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are usefull for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: May 21, 2007Publication date: November 12, 2009Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Lourdes Linares De La Morena, Sonia Martinez Gonzalez, Julen Oyarzabal Santamarina, Joaquin Pastor-Fernàndez, Juan Antonio Vega Ramiro, Francisca Delgado-Jiménez, Wilhelmus Helena Drinkenburg
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Publication number: 20090281087Abstract: 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: ApplicationFiled: December 5, 2008Publication date: November 12, 2009Applicant: Biovitrum ABInventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom, Viet-Anh Anne Horgan (nee Nguyen), Jaqueline Ouzman, Iain Simpson