The Additional Hetero Ring Is Five-membered And Unsaturated (e.g., Thienyl Piperazines, Etc.) Patents (Class 544/379)
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Publication number: 20100234391Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: DOW AGROSCIENCES LLCInventors: Beth Anne Lorsbach, James Melvin Ruiz, Thomas Clarence Sparks, Michael Thomas Sullenberger, Irene Mae Morrison, Jeffery Dale Webster
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Publication number: 20100210618Abstract: The invention 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 —O—C(?O)—; —C(?O)—C(?O)—; —NRX—C(?O)—; —Z—C(?O)—; —Z—NRX—C(?O)—; —C(?O)—Z—; —NRX—C(?O)—Z—; —C(?S)—; —NRX—C(?S)—; —Z—C(?S)—; —Z—NRX—C(?S)—; —C(?S)—Z—; —NRX—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRX— or —NRX—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein saiType: ApplicationFiled: June 6, 2008Publication date: August 19, 2010Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Mieerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaret, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
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Publication number: 20100210635Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: March 23, 2007Publication date: August 19, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Andre A. Kiryanov, Stephen W. Kaldor
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Publication number: 20100179168Abstract: The present invention therefore provides compounds of formula (I) or pharmaceutically acceptable salts thereof: (I) processes for their preparation, pharmaceutical compositions containing the same and to their use in the treatment of gastrointestinal and other disorders.Type: ApplicationFiled: April 13, 2007Publication date: July 15, 2010Inventors: Emma Louise Blaney, David Kenneth Dean, Alessandra Gaiba, Nigel Paul King, Jason Witherington
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Patent number: 7754721Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, X, Y, Z, Ar, R1, R2, R3, R4, R5, R6 and R7 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: August 17, 2007Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Ryan Craig Schoenfeld, Robert James Weikert
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Patent number: 7750012Abstract: The present invention relates to a chemical genus of biaryl nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: GrantFiled: August 3, 2006Date of Patent: July 6, 2010Assignee: deCODE genetics ehfInventors: Vincent Sandanayaka, Jasbir Singh, Li-Ming Zhou, Mark E. Gurney
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Publication number: 20100168114Abstract: Methods for determining invertebrate- and insect-specific, such as mosquito-specific, residues of acetylcholinesterases are provided herein. The methods can be used to design pesticides and insecticides that are specific for the invertebrate or insect (e.g., mosquito) enzymes, resulting in reduced toxicity concerns for mammals. Compositions for inhibiting invertebrate and insect (e.g., mosquito) acetylcholinesterases and methods for preparing the same are also provided.Type: ApplicationFiled: December 18, 2009Publication date: July 1, 2010Inventor: Yuan-Ping Pang
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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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Patent number: 7741326Abstract: Compounds of formula I or formula II: or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1, R2, R4, and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds.Type: GrantFiled: November 8, 2007Date of Patent: June 22, 2010Assignee: Roche Palo Alto LLCInventors: Joe Timothy Bamberg, Counde O'Yang, Meng Sui, Shu-Hai Zhao
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Publication number: 20100145048Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.Type: ApplicationFiled: October 20, 2009Publication date: June 10, 2010Inventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, JR., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
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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: 20100121048Abstract: The present invention relates to a compound represented by the formula: (I) wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent (s); U, V and W are each independently C or N, provided that when any one of U, V and W is N, then the others should be C; Ra and Rb are each independently a cyclic group optionally having substituent(s), a C1-10alkyl group optionally having substituent(s), a C2-10 alkenyl group optionally having substituent(s), or a C2-10alkynyl group optionally having substituent(s); X is a bond, or a spacer having 1 to 6 atoms in the main chain; Y is a spacer having 1 to 6 atoms in the main chain; Rc is a hydrocarbon group optionally containing heteroatom(s) as the constituting atom(s), which optionally has substituent(s); m and n are each independently 1 or 2; and ring B optionally further has substituent(s), or a salt thereof.Type: ApplicationFiled: February 15, 2007Publication date: May 13, 2010Inventors: Takanobu Kuroita, Yasuhiro Imaeda, Naohiro Taya, Tsuneo Oda, Kouichi Iwanaga, Yasutomi Asano
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Publication number: 20100120789Abstract: There is provided a compound having Formula I R1—Z—R2 ??Formula I wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(?O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S?O, and S(?O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p- NR10—S(?O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)v-Y—(CR15R16)w- where Y is a heteroaryl group in which a bond in the heteroType: ApplicationFiled: September 7, 2009Publication date: May 13, 2010Inventors: Nigel Vicker, Xiangdong Su, Fabienne Praduax, Michael John Reed, Barry Victor Lloyd Potter
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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: 20100069638Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.Type: ApplicationFiled: November 20, 2009Publication date: March 18, 2010Inventors: Akira Kugimiya, Masahiko Fujioka, Yuki Tachibana, Takami Murashi
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Publication number: 20100063040Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.Type: ApplicationFiled: September 25, 2006Publication date: March 11, 2010Inventor: Akira Kugimiya
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Publication number: 20100029607Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.Type: ApplicationFiled: September 22, 2009Publication date: February 4, 2010Inventors: Eric J. Gilbert, Michael W. Miller, Jack D. Scott, Andrew W. Stamford, William J. Greenlee, Jay Weinstein
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Publication number: 20090281086Abstract: A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: HetA is a C5 arylene group, wherein the two substituent groups are on adjacent ring atoms, and where the group is further optionally substituted by one halo, amino or C1-7 alkoxy group; Y is —CRC1RC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2 together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; HetB is selected from: (i), where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and (ii), (aa), (bb) Q is O or S.Type: ApplicationFiled: June 15, 2007Publication date: November 12, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Muhammad Hashim Javaid, Xiao-Ling Fan Cockcroft, Keith Allan Menear, Niall Morrison Barr Martin
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Publication number: 20090281317Abstract: A compound represented by the formula (1): wherein A, B, R1, L1, R2, L2, L3, Y, L4, R3 and X are the same as defined in the description, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: December 7, 2005Publication date: November 12, 2009Applicant: NISSAN CHEMICAL INDUSTRIES LTD.Inventors: Katsuaki Miyaji, Yukihiro Shigeta, Satoshi Nakano, Shunuske Iwamoto, Yutaka Hirokawa, Hirofumi Ota, Kazufumi Yanagihara, Shingo Owada, Norihisa Ishiwata
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Publication number: 20090264416Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.Type: ApplicationFiled: August 19, 2008Publication date: October 22, 2009Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
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Publication number: 20090253656Abstract: The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by formula (1): wherein one of R1 and R2 represents a cyano group and the other represents a hydrogen atom; Ar1 represents a group selected from among the groups represented by formulas (2) to (4): and Ar2 represents an aromatic hydrocarbon group having a condensed ring which may be substituted by a halogen atom, or a group selected from among the groups represented by the following formulas (5) to (15): or a salt thereof.Type: ApplicationFiled: March 29, 2006Publication date: October 8, 2009Applicant: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Publication number: 20090253684Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.Type: ApplicationFiled: December 2, 2008Publication date: October 8, 2009Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 7592344Abstract: 3-cyanonaphthalene-1-carboxylic acid perhydroxyalkylmethyl-piperazine compounds of formula I which are antagonistic to tachykinin receptors, pharmaceutical compositions containing such compounds, methods of using such compounds for the treatment and/or inhibition of various diseases and disorders, processes for preparing such piperazine compounds, and intermediate products of these processes.Type: GrantFiled: November 30, 2006Date of Patent: September 22, 2009Assignee: Solvay Pharmaceuticals GmbHInventors: Jochen Antel, Daniel Jasserand, Uwe Schoen, Michael Firnges, Holger Sann, Reinhard Brueckner, Dania Reiche
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Patent number: 7582749Abstract: Various non-limiting embodiments disclosed herein relate generally to photochromic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. Other non-limiting embodiments relate to photochromic-dichroic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. For example, one non-limiting embodiment provides a thermally reversible, photochromic compound adapted to have at least a first state and a second state, wherein the thermally reversible, photochromic compound has an average absorption ratio greater than 2.3 in at least one state as determined according to CELL METHOD.Type: GrantFiled: October 26, 2007Date of Patent: September 1, 2009Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, Meng He, Terry A. Kellar, II, Forrest R. Blackburn
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Publication number: 20090203696Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: ApplicationFiled: December 15, 2008Publication date: August 13, 2009Applicant: SANOFI-AVENTISInventors: Jozsef Zsolt BOCSKEI, Gary MCCORT, Hans MATTER, Henning STEINHAGEN, Berangere THIERS
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Patent number: 7566717Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.Type: GrantFiled: July 9, 2008Date of Patent: July 28, 2009Assignee: Gilead Sciences, Inc.Inventors: Venkata Palle, Jeff Zablocki
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Publication number: 20090131659Abstract: The present invention provides compounds useful for prevention, treatment or alleviation of diseases against which activation of the thrombopoietin receptor is effective. A compound represented by the formula (1): wherein A, B, R1, L1, R2, L2, L3, Y, L4, R3 and X are the same as defined in the description, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: December 14, 2005Publication date: May 21, 2009Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Katsuaki Miyaji, Shunsuke Iwamoto, Satoshi Nakano, Hirofumi Ota, Yukihiro Shigeta, Yutaka Hirokawa, Kazufumi Yanagihara, Koji Toyama, Shingo Owada, Masato Horikawa, Norihisa Ishiwata
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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: 7524846Abstract: The present invention is directed to arylalkyl- and cycloalkylalkyl-piperazine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: April 28, 2009Assignee: WyethInventor: Paige Erin Mahaney
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Publication number: 20090105251Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: December 10, 2007Publication date: April 23, 2009Inventors: Benjamin Jones, Andrey A. Kiryanov, Stephen W. Kaldor
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Patent number: 7521473Abstract: Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted thiophene compounds such as, for example, 2-carboxyl, 3-carboxymethoxy, 5-aryl substituted thiophenes, can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.Type: GrantFiled: February 23, 2005Date of Patent: April 21, 2009Assignee: WyethInventors: Jinbo Lee, Zhao-Kui Wan, Douglas P. Wilson, Bruce C. Follows, Steven J. Kirincich, Michael J. Smith, Jun-Jun Wu, Kenneth W. Foreman, David V. Erbe, Yan-Ling Zhang, Weixin Xu, Steve Y. Tam
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Publication number: 20090099186Abstract: The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: October 10, 2006Publication date: April 16, 2009Inventors: Leonid Beigelman, Steven W. Andrews, Kevin R. Condroski, Indrani Gunawaradana, Julia Haas
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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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Publication number: 20090069335Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: September 5, 2008Publication date: March 12, 2009Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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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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Publication number: 20090062297Abstract: The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: January 8, 2007Publication date: March 5, 2009Inventors: Richard W. Heidebrecht, Thomas A. Miller, Kevin J. Wilson, David J. Witter, Jonathan Grimm
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Publication number: 20090062284Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.Type: ApplicationFiled: August 27, 2008Publication date: March 5, 2009Applicant: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Marie-Edith Gourdel, Greg A. Hostetler, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet, Eric Riguet, Dominique Schweizer, Christophe Yue
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Publication number: 20090054396Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer.Type: ApplicationFiled: September 8, 2008Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Susan Ashwell, Thomas Gero, Stephanos Ioannidis, James Janetka, Paul Lyne, Vibha Oza, Mei Su, Dingwei Yu, Stephanie Springer
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Patent number: 7491723Abstract: The present invention is directed to alkanoyl and cycloalkanoyl-amine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: February 17, 2009Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, William Jay Moore, Joseph Peter Sabatucci
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Publication number: 20090036439Abstract: The present invention provides a compound of formula I and the use thereof for the inhibition of bacterial cell wall biosynthesis and for the therapeutic treatment of bacterial infection or disease in a patient in need thereof. The present invention also provides the use of the formula I compound for the control of ecto- or endoparasites in homeothermic animals.Type: ApplicationFiled: September 19, 2008Publication date: February 5, 2009Applicant: WyethInventors: Craig Eugene Caufield, Schuyler Adam Antane, Koi Michele Morris, Shaughnessy McGrath Naughton, Dominick Anthony Quagliato, Patrick Michael Andrae, Annmarie Enos, John F. Chiarello
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Publication number: 20090012075Abstract: The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: January 8, 2007Publication date: January 8, 2009Inventors: Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Patent number: 7473692Abstract: The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's dissases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).Type: GrantFiled: September 25, 2002Date of Patent: January 6, 2009Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: János Galambos, Katalin Nógrádi, Éva Ágainé Csongor, György Miklós Keserü, István Vágó, György Domány, Béla Kiss, István Gyertyán, István Laszlovszky, Judit Laszy
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Publication number: 20080317671Abstract: Certain non-imidazole heterocyclic compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: August 20, 2008Publication date: December 25, 2008Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20080306087Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 3, 2006Publication date: December 11, 2008Applicant: ASTRAZENECA ABInventors: James R. Empfield, Michael Laplante, Megan Murphy King, Thomas R. Simpson, Maxime C. Tremblay, James M. Woods, Jingbo Yan
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Patent number: 7459558Abstract: A method of treating in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein the substituents are defined in accordance with the disclosure.Type: GrantFiled: April 13, 2005Date of Patent: December 2, 2008Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auquet, Jeremiah Harnett
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Publication number: 20080287430Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof wherein X, Z, R1, R2a, R2b, R3, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: April 24, 2006Publication date: November 20, 2008Inventors: Rino Antonio Bit, Gerard Martin Paul Giblin, Adrian Hall, David Nigel Hurst, Ian Reginald Kilford, Tiziana Scoccitti
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Patent number: 7449481Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.Type: GrantFiled: April 12, 2005Date of Patent: November 11, 2008Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, Marie-Edith Gourdel, Greg Hostetler, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet, Eric Riguet, Dominique Schweizer, Christophe Yue
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Patent number: 7442692Abstract: A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, or R1 represents a hydrogen atom, and R2 and R3 together with the carbon atoms carrying them form a benzene, naphthalene or quinoline ring structure, each of the ring structures being optionally substituted, n represents 1 or 2, —X— represents a group selected from —(CH2)m—O-Ak-, —(CH2)m—NR4-Ak-, —(CO)—NR4-Ak- and —(CH2)m—NR4-(CO)—, m represents an integer between 1 and 6 inclusive, Ak represents an optionally substituted alkylene chain, and R4 represents a hydrogen atom or an alkyl group, Ar represents an aryl or heteroaryl group, its enantiomers, diasteroisomers, and addition salts thereof with a pharmaceutically acceptable acid.Type: GrantFiled: March 29, 2006Date of Patent: October 28, 2008Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Mark Millan, Jean-Claude Ortuno, Clotilde Mannoury La Cour, Alain Gobert
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Publication number: 20080261996Abstract: The present invention relates to substituted propiolic acid amides, methods for the production thereof, medicaments containing these compounds and the use thereof for producing medicaments.Type: ApplicationFiled: June 26, 2008Publication date: October 23, 2008Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH, Saskia ZEMOLKA
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Publication number: 20080255144Abstract: The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.Type: ApplicationFiled: March 9, 2006Publication date: October 16, 2008Inventors: Daniel Marcus Bradley, Clive Leslie Branch, Wai Ngor Chan, Steven Coulton, Anthony William Dean, Paul Martin Doyle, Brian Evans, Martin Leonard Gilpin, Sharon Lisa Gough, Jacqueline Anne Macritchie, Howard Robert Marshall, David John Nash, Roderick Alan Porter, Simon Edward Ward