Five-membered Hetero Ring Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen Patents (Class 544/366)
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Patent number: 7812025Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whicType: GrantFiled: August 11, 2006Date of Patent: October 12, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
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Publication number: 20100256357Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: ApplicationFiled: July 30, 2007Publication date: October 7, 2010Inventors: Wesley Kwan Mung Chong, Andrew M. Haidle, Martha Alicia Ornelas, Lin Li, Seiji Nukui, Eugene Yuanjin Rui, Min Teng, William Francois Vernier, Joe Zhongxiang Zhou
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Patent number: 7807671Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity useful for the treatment of HIV and AIDS.Type: GrantFiled: April 10, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini
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Patent number: 7807672Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.Type: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
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Publication number: 20100216809Abstract: The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-mType: ApplicationFiled: June 5, 2008Publication date: August 26, 2010Applicant: Janssen Pharmaceutica N.V.Inventors: Jean-Pierre André Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
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Publication number: 20100190762Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: April 2, 2010Publication date: July 29, 2010Applicant: CHEMOCENTRYX, INC.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Publication number: 20100168359Abstract: Described herein are tri-functional compounds useful in the production of ophthalmic lenses. The compounds are composed of UV absorber having a polymerization initiator directly or indirectly bonded to the ultraviolet absorber, and an olefinic group directly or indirectly bonded to the ultraviolet absorber. Also described herein are polymers and ophthalmic lenses produced from the tri-functional compounds described herein.Type: ApplicationFiled: December 17, 2009Publication date: July 1, 2010Inventors: Angelika Maria Domschke, Lynn Cook Winterton, Troy Vernon Holland, Richard Charles Turek
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Publication number: 20100160323Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: December 22, 2009Publication date: June 24, 2010Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
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Publication number: 20100152047Abstract: The present invention relates to piperazine compounds of the general formula I defined below and to their use as herbicides. Moreover, the invention relates to compositions for crop protection and to a method for controlling unwanted vegetation.Type: ApplicationFiled: June 11, 2008Publication date: June 17, 2010Applicant: BASF SEInventors: Eike Hupe, Thomas Seitz, Matthias Witschel, Dschun Song, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Trevor William Newton, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Michael Rack, Elmar Kibler
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Publication number: 20100144712Abstract: A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.Type: ApplicationFiled: June 12, 2008Publication date: June 10, 2010Applicants: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, CHEMON INC.Inventors: Bum Tae Kim, Yong Ki Min, Jung Nyoung Heo, Hyuk Lee, Sung Youn Chang, No Kyun Park, Si-Whan Song, Jung-Ja Oh
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Patent number: 7728009Abstract: Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: GrantFiled: February 16, 2006Date of Patent: June 1, 2010Assignee: Neurogen CorporationInventors: Wallace C. Pringle, John M. Peterson, Linghong Xie, Ping Ge, Yang Gao, Joseph W. Ochterski, Jiong Lan
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Publication number: 20100130509Abstract: The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds, variants of bis(1-aryl-5-tetrazolyl)methanes, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.Type: ApplicationFiled: April 3, 2008Publication date: May 27, 2010Applicant: Nederlandse Organisatie voor toegepast-natuurwe- tenschappelijk onderzoek TNOInventors: Frank Henri Johan Schuren, Roy Christiaan Montijn
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Publication number: 20100113447Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: August 10, 2009Publication date: May 6, 2010Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Patent number: 7700586Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.Type: GrantFiled: September 4, 2002Date of Patent: April 20, 2010Assignee: Axikin Pharmaceuticals, Inc.Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
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Publication number: 20100056543Abstract: Improved posaconazole-based compositions and methods of treating and preventing fungal infections, cancer or metastatic diseases are disclosed. In preferred aspects, the conjugates are PEG-posaconazole conjugates in which the PEG has a molecular weight of about 20,000 daltons.Type: ApplicationFiled: November 13, 2009Publication date: March 4, 2010Applicant: Enzon Pharmaceuticals, Inc.Inventor: Hong ZHAO
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Publication number: 20100056779Abstract: Methyl nonactate is converted into a variety of different triazoloamide antibacterial agents by a reaction scheme involving (1) inversion of the secondary alcohol of the methyl nonactate to produce the corresponding azidoester, (2) converting the azido ester to the corresponding azidoamide, and (3) converting the azido group of the azidoamide to a triazole to produce the corresponding triazoloamide.Type: ApplicationFiled: September 11, 2007Publication date: March 4, 2010Applicant: OHIO UNIVERSITYInventors: Stephen C. Bergmeier, Nigel D. Priestley
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Patent number: 7667037Abstract: Provided are processes for preparing ziprasidone from CEI and BIPT.Type: GrantFiled: October 25, 2004Date of Patent: February 23, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Gideon Pilarsky, Natalia Shenkar, Marioara Mendelovici, Tamar Nidam, Anna Balanov
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Publication number: 20100041655Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2— or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).Type: ApplicationFiled: February 5, 2007Publication date: February 18, 2010Inventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato
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Patent number: 7662813Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: GrantFiled: August 17, 2006Date of Patent: February 16, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, David James, Shijie Zhang, Teresa Przewloka, Elena Kostik, Junghyun Chae, Howard P Ng, Zhenjian Du, James Barsoum, Dinesh Chimmanamada, Chi-Wan Lee, Kevin Foley
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Patent number: 7659276Abstract: Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.Type: GrantFiled: February 6, 2009Date of Patent: February 9, 2010Assignee: Amgen, Inc.Inventors: Christopher Hulme, Paul Tempest, Vu Ma, Thomas Nixey, Guity Balow
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Publication number: 20100029620Abstract: The present invention concerns substituted triazolone, tetrazolone and imidazolone 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: December 20, 2005Publication date: February 4, 2010Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Joaquin Pastor-Fernández, Xavier Jean,Michel Langlois, Julen Oyarzabal-Santamarina, Juan Antonio Vega-Ramiro
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Publication number: 20100022540Abstract: Novel triazole derivatives of the formula (I) in which R1—R6 and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: April 20, 2007Publication date: January 28, 2010Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Patent number: 7645775Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 21, 2005Date of Patent: January 12, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, Cornelia Forster, Michael Arnost, Jian Wang
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Publication number: 20100004265Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,3-triazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis or pain.Type: ApplicationFiled: November 7, 2007Publication date: January 7, 2010Inventors: Nadine Jagerovic, Cristina Ana Gomez-De La Oliva, Maria Pilar Goya-Laza, Alberto Dordal Zueras, Maria Rosa Cuberes-Altisent
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Publication number: 20090326220Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: August 18, 2009Publication date: December 31, 2009Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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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: 7612060Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: October 11, 2005Date of Patent: November 3, 2009Assignee: Amgen Inc.Inventors: Toshihiro Aya, Guolin Cai, Jian J. Chen, Derin D'Amico, Thomas Nguyen, Wenyuan Qian
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Patent number: 7605162Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: GrantFiled: October 27, 2008Date of Patent: October 20, 2009Assignee: Solvay PharmaceuticalsInventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Patent number: 7595320Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.Type: GrantFiled: August 29, 2007Date of Patent: September 29, 2009Assignee: Aventis Pharma S.A.Inventors: Claude Barberis, Jean-Christophe Carry, Gilles Doerflinger, Dominique Barbalat-Damour, Francois Clerc, Herve Minoux
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Publication number: 20090239877Abstract: The invention provides 1,2,4-triazole compounds, compositions containing those compounds, methods of treating diseases and/or disorders with those compounds and processes of manufacturing 1,2,4-triazole compounds.Type: ApplicationFiled: March 17, 2009Publication date: September 24, 2009Applicants: AETERNA ZENTARIS GmbH, CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE, University of Montpellier I, University of Montpellier IIInventors: Jean-Alain Fehrentz, Mathieu Bibian, Aline Moulin, Jean Martinez
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Publication number: 20090227791Abstract: In some embodiments, this invention pertains to active esters of N-substituted piperazine acetic acid, including isotopically enriched versions thereof. In some embodiments, this invention pertains to methods for the preparation of active esters of N-substituted piperazine acetic acid, including isotopically enriched versions thereof.Type: ApplicationFiled: March 5, 2009Publication date: September 10, 2009Inventors: Subhakar Dey, Darryl J.C. Pappin, Subhasish Purkayastha, Sasi Pillai, James M. Coull
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Patent number: 7582761Abstract: Therapeutic benzimidazoles having the general structure: and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gasType: GrantFiled: October 16, 2003Date of Patent: September 1, 2009Assignee: Amgen Inc.Inventors: Chenera Balan, Yunxin Bo, Celia Dominguez, Christopher H. Fotsch, Vijay K. Gore, Vu Van Ma, Mark H. Norman, Vassil I. Ognyanov, Yi-xin Qian, Xianghong Wang, Ning Xi, Shimin Xu
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Patent number: 7579352Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,Type: GrantFiled: October 29, 2007Date of Patent: August 25, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
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Patent number: 7569568Abstract: Disclosed are compounds of formula (I) Where Ar1, X, R3, R4, R5 and R6 are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: September 7, 2006Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek A. Cogan, Ming-Hong Hao, Kevin Chungeng Qian, Alan David Swinamer
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Publication number: 20090130117Abstract: The present invention provides tetrazole compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the tetrazole compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of the present invention.Type: ApplicationFiled: October 14, 2008Publication date: May 21, 2009Applicant: ARQULE, INC.Inventors: Rui-Yang Yang, Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Rocio Palma, Neil Westlund
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Patent number: 7524848Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: GrantFiled: March 22, 2007Date of Patent: April 28, 2009Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
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Patent number: 7514438Abstract: Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.Type: GrantFiled: August 11, 2004Date of Patent: April 7, 2009Assignee: Amgen, Inc.Inventors: Christopher Hulme, Paul A. Tempest, Vu Van Ma, Thomas Nixey, Guity Balow
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Patent number: 7511046Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: July 21, 2006Date of Patent: March 31, 2009Assignee: Aventis Hoklings Inc.Inventors: David M Fink, Brian S Freed, Nicholas J Hrib, Raymond W Kosley, George E Lee, Gregory H Merriman, Barbara S Rauckman
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Publication number: 20090082363Abstract: The present application describes deuterium-enriched posaconazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090076028Abstract: The present application describes deuterium-enriched itraconazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7504400Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hyper-triglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: GrantFiled: March 7, 2005Date of Patent: March 17, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Libuse Jaroskova, Peter Walter Maria Roevens, Louis Jozef Elisabeth Van Der Veken, Marcel Viellevoye, Joannes Theodorus Maria Linders
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Publication number: 20090069561Abstract: The high efficiency and fidelity of click chemistry permits a large number of diverse dendrimers encompassing a wide variety of functionalities at the chain ends, repeat units, and/or core to be prepared. Almost quantitative yields were obtained during the synthesis. In some cases, filtration or solvent extraction was the only method required for purification. These features represent a significant advancement in dendrimer chemistry and demonstrate an evolving synergy between organic chemistry and functional materials.Type: ApplicationFiled: June 30, 2005Publication date: March 12, 2009Applicant: The Scripps Research InstituteInventors: Valery Fokin, K. Barry Sharpless, Peng Wu, Alina Feldman
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Patent number: 7501422Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: May 30, 2008Date of Patent: March 10, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Bo Han, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
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Publication number: 20090062294Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 23, 2008Publication date: March 5, 2009Inventors: Richard Apodaca, J. Guy Breitenbucher, Natalie A. Hawryluk, William M. Jones, John M. Keith, Jeffrey E. Merit, Mark S. Tichenor, Amy K. Timmons
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Patent number: 7482344Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart disease, hypertension, rheumatoid arthritis or inflammation, comprising administering to a patient in thereof an effective amount of a compound of Formula (I).Type: GrantFiled: December 15, 2004Date of Patent: January 27, 2009Assignee: Eli Lilly and CompanyInventors: Michael Joseph Coghlan, Prabhakar Kondaji Jadhav, James Joseph Droste, Jonathan Edward Green, Donald Paul Matthews
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Patent number: 7468371Abstract: Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: March 24, 2005Date of Patent: December 23, 2008Assignee: Abbott Laboratories Inc.Inventors: Lee D. Arnold, Jürgen Dinges, Richard W. Dixon, Stevan W. Djuric, Anna M. Ericsson, Kimba Fischer, Alan F. Gasiecki, Vijaya J. Gracias, James H. Holms, Makoto Takeshita, Michael R. Michaelides, Melanie A. Muckey, Paul Rafferty, Douglas H. Steinman, Carol K. Wada, Zhiren Xia, Irini Akritopoulou-Zanze, Henry Q. Zhang
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Publication number: 20080306089Abstract: The present invention relates to a compound of formula I wherein R1, R2, R3, and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These compounds are NK3 receptor antagonists, useful for the treatment of such disorders as depression, pain, bipolar disorders, psychosis, Parkinson's disease, schizophrenia, anxiety, and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: May 30, 2008Publication date: December 11, 2008Inventors: Bo Han, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
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Publication number: 20080249084Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome.Type: ApplicationFiled: October 27, 2004Publication date: October 9, 2008Inventors: Jay P. Powers, Mario G. Cardozo, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
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Publication number: 20080249106Abstract: The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor.Type: ApplicationFiled: April 8, 2008Publication date: October 9, 2008Inventors: Benny C. Askew, Jian J. Chen, Derin C. D'Amico, Thomas Nguyen, Kevin Yang
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Patent number: 7429659Abstract: Certain furan compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: GrantFiled: March 31, 2005Date of Patent: September 30, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson