The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
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Patent number: 7547703Abstract: The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.Type: GrantFiled: September 7, 2006Date of Patent: June 16, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Gerald Juergen Roth, Armin Heckel, Thorsten Lehmann-Lintz, Joerg Kley, Frank Hilberg, Jacobus C. A. Van Meel, Ulrike Tontsch-Grunt
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Patent number: 7544685Abstract: The invention relates to compounds of the formula I wherein the variables are as defined in the claims. The compounds are useful in the treatment of a disease where a D4 receptor and/or a 5-HT2A receptor is implicated.Type: GrantFiled: August 15, 2006Date of Patent: June 9, 2009Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Krestian Larsen, Niels Mørk
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Publication number: 20090143406Abstract: 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: ApplicationFiled: October 27, 2008Publication date: June 4, 2009Inventors: 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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Publication number: 20090137570Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: ApplicationFiled: January 28, 2009Publication date: May 28, 2009Applicant: IRM LLCInventors: Hong LIU, Arnab K. CHATTERJEE, David C. TULLY, Phillip B. ALPER, Badry BURSULAYA, Jianhua GUO, David H. WOODMANSEE, Daniel MUTNICK, Donald S. KARANEWSKY, Yun HE
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Publication number: 20090124634Abstract: The invention relates to a novel class of dipodazine derivatives, suitable for use as surface on-growth inhibiting agents.Type: ApplicationFiled: June 9, 2006Publication date: May 14, 2009Inventors: Lars Bohlin, Jan Bergman, Martin Sjogren, Ulf Goransson
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Publication number: 20090118301Abstract: The invention provides compounds useful for treating or effecting prophylaxis of cancers, particularly cervical cancer.Type: ApplicationFiled: October 30, 2008Publication date: May 7, 2009Applicant: Arbor Vita CorporationInventors: Peter S. Lu, Michael P. Belmares, Jingjing Wang, Johannes Schweizer, Aida A. Fantaye
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Patent number: 7524839Abstract: The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.Type: GrantFiled: February 11, 2005Date of Patent: April 28, 2009Inventors: Patrizia Caldirola, Björn M. Nilsson, Gary Johansson
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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: 20090105274Abstract: The present invention provides an indolecarboxylic acid 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 (I): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of -X1=X2-X3=X4- is a formula of —C(R1)?C(R2)—C(R3)?C(R4)— etc.; X5 is C(R5) or N; R1, R2, R3, R4 and R5 is independently a hydrogen atom, a halogen atom etc; R6 is a formula of -Z-R10 etc. wherein Z is alkylene etc., and R10 is carboxy etc.; R7 is optionally substituted alkyloxy etc.; R8 is independently a halogen atom etc.; R9 is independently optionally substituted alkyl etc.; Y is a single bond etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: September 4, 2006Publication date: April 23, 2009Inventors: Akira Kugimiya, Yuki Tachibana
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Publication number: 20090093469Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, 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: ApplicationFiled: December 15, 2008Publication date: April 9, 2009Applicant: WYETHInventors: Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
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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: 7514433Abstract: The present invention relates to the compounds of formula I: wherein R1 to R4 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: July 19, 2007Date of Patent: April 7, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Olivier Roche
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Publication number: 20090082346Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: July 29, 2008Publication date: March 26, 2009Applicant: Pfizer Italia S.r.l.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Patent number: 7504399Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and azaindole piperazine enamine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to a compound of Formula I useful for the treatment of HIV and AIDS.Type: GrantFiled: May 15, 2007Date of Patent: March 17, 2009Assignee: Bristol-Meyers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell
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Publication number: 20090069328Abstract: The present invention relates to ?-alkyl substituted N-acyltryptophanols of the formula I in which R1, R2, R3, R4, R5, R6, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: August 14, 2008Publication date: March 12, 2009Inventors: Lars Wortmann, Marcus Koppitz, Hans Peter Muhn, Anna Schrey, Ronald Kuehne
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Patent number: 7501419Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with 4-squarylpiperazine derivatives that possess unique antiviral activity.Type: GrantFiled: April 19, 2007Date of Patent: March 10, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Daniel H. Deon, Edward H. Ruediger
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Patent number: 7498328Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.Type: GrantFiled: July 17, 2006Date of Patent: March 3, 2009Assignee: Laboratorias Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Publication number: 20090054407Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I): {wherein W represents a nitrogen atom or —CH—; X represents —C(?O)— or —CHR4— (wherein R4 represents a hydrogen atom, or the like); R1 represents a group represented by the following formula: [wherein Q1 represents a nitrogen atom or —CR8— (wherein R8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like). Q2 represents —NR15— (wherein R15 represents a hydrogen atom, or the like) and R5 and R6 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like]; and R2 and R3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: April 19, 2006Publication date: February 26, 2009Applicant: Kyowa Hakko Kogyo Co., Ltd.Inventors: Chikara Murakata, Nobuyoshi Amishiro, Toshiyuki Atsumi, Yoshinori Yamashita, Takeshi Takahashi, Ryuichiro Nakai, Hisashi Tagaya, Hiroko Takahashi, Jun Funahashi, Junichiro Yamamoto, Yuichi Fukuda
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Publication number: 20090054402Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.Type: ApplicationFiled: April 16, 2008Publication date: February 26, 2009Applicant: Abbott LaboratoriesInventors: Xilu Wang, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
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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: 20090036444Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: May 18, 2006Publication date: February 5, 2009Applicant: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Shintaro Hirashima, Takahiro Oka, Kenta Aoki, Satoru Noji, Izuru Ando, Toshihiro Sato, Yasushi Niwa
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Publication number: 20090029971Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.Type: ApplicationFiled: September 4, 2008Publication date: January 29, 2009Applicant: KALYPSYS, INC.Inventors: Stewart A. Noble, Guy Oshiro, James W. Malecha, Cunxiang Zhao, Carmen Robinson, Sergio G. Duron, Michael Sertic, Andrew K. Lindstrom, Andrew K. Shiau, Christopher D. Bayne, Mehmet Kahraman, Boliang Lou, Steve P. Govek
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Publication number: 20090030014Abstract: The present invention creates an indole 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 generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.Type: ApplicationFiled: July 20, 2006Publication date: January 29, 2009Inventors: Akira Kugimiya, Michitaka Shichijo, Yoshiharu Hiramatsu, Natsuki Ishizuka
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Publication number: 20090023749Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: ApplicationFiled: April 28, 2008Publication date: January 22, 2009Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Bottcher
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Publication number: 20090018141Abstract: Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.Type: ApplicationFiled: June 9, 2008Publication date: January 15, 2009Inventors: Robert Shoemaker, John Cardellina, Michael Currens, Sudhir Kondapaka, Yves Pommier, Andy Jobson, Dominic Scudiero, David Waugh, George Lountos, Charles M. Cook, Guangtao Zhang, Andrew Colasanti, Christopher R. Self, Janet Cicariello Cook
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Publication number: 20080318941Abstract: The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, R6, B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: May 21, 2008Publication date: December 25, 2008Applicant: MEMORY PHARMACEUTICALS CORPORATIONInventors: Robert Dunn, Truc Minh Nguyen, Wenge Xie, Ashok Tehim
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Publication number: 20080318973Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: ApplicationFiled: June 5, 2008Publication date: December 25, 2008Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20080318902Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.Type: ApplicationFiled: July 18, 2008Publication date: December 25, 2008Applicant: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
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Patent number: 7459557Abstract: The present invention relates to substituted isoindole-1,3-dione compounds of Formula (I) and pharmaceutically acceptable forms thereof, as ?1a/?1d adrenoreceptor modulators for the treatment of benign prostatic hypertrophy and lower urinary tract symptoms. The present invention also relates to pharmaceutical compositions comprising said new compounds, new processes to prepare these new compounds and new uses as a medicine as well as methods of treatment.Type: GrantFiled: June 12, 2006Date of Patent: December 2, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: George Chiu, Peter J. Connolly, Jessica J. Liu, Steven A. Middleton, Virginia L. Pulito, Shengjian Li
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Patent number: 7456182Abstract: 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: June 12, 2006Date of Patent: November 25, 2008Assignee: Solvay Pharmaceuticals, Inc.Inventors: 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: 7456183Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.Type: GrantFiled: April 8, 2002Date of Patent: November 25, 2008Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
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Patent number: 7456184Abstract: A melanocortin receptor-specific compound of the general formula of structure I: where X, R1, R2a, R2b, R3, R4a, R4b, R5a and R5b are as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.Type: GrantFiled: April 30, 2004Date of Patent: November 25, 2008Assignee: Palatin Technologies Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit, Annette M. Shadiack, Papireddy Purma, Kevin D. Burris
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Publication number: 20080280923Abstract: The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence.Type: ApplicationFiled: March 17, 2006Publication date: November 13, 2008Applicant: N.V. OrganonInventors: Phillip Martin Cowley, Samuel George Gibson, Grant Wishart
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Publication number: 20080275041Abstract: Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.Type: ApplicationFiled: September 21, 2004Publication date: November 6, 2008Applicant: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg
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Publication number: 20080261917Abstract: A compound of formula or a prodrug and/or a pharmaceutically acceptable salt thereof, wherein X is O, N or S; R1 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroaralkyl; R2 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; R3 is hydrogen, halo, hydroxy, substituted or unsubstituted alloy substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; and R4-R7, is used to represent groups R4, R5, R6 and R7 which are H, OH, alkyl, alkoxy, alkylamine, hydroxyalkyl, hType: ApplicationFiled: August 26, 2005Publication date: October 23, 2008Inventors: Hendrika Maria Gerarda Willems, Per Kallblad, Ian Robert Hardcastle, Robert John Griffin, Bernard Thomas Golding, John Lunec, Martin E.M. Noble, David R. Newell, Alan H. Calvert
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Publication number: 20080261978Abstract: The invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula (I).Type: ApplicationFiled: March 7, 2008Publication date: October 23, 2008Inventors: Michael P. Clark, Mark A. Lockwood, Florence F. Wagner, Michael G. Natchus
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Publication number: 20080261944Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: ApplicationFiled: June 8, 2005Publication date: October 23, 2008Inventors: Stefania Colarusso, Immacolata Conte, Joerg Habermann, Frank Narjes, Simona Ponzi
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Publication number: 20080260685Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.Type: ApplicationFiled: June 23, 2008Publication date: October 23, 2008Applicant: ImmunoGen Inc.Inventors: Robert Yongxin ZHAO, Ravi V.J. Chari
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Patent number: 7439371Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 11, 2006Date of Patent: October 21, 2008Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Richard C. Yee
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Publication number: 20080255350Abstract: The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: ApplicationFiled: June 17, 2008Publication date: October 16, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: John Z. JIANG, Jack Roger KOEHL, Shujaath MEHDI, Neil MOORCROFT, Kwon Yon MUSICK, Philip Marvin WEINTRAUB, Paul Robert EASTWOOD
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Publication number: 20080255102Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, 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, fibromyalgia 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: ApplicationFiled: June 23, 2008Publication date: October 16, 2008Applicant: WyethInventors: An Thien Vu, Paige Erin Mahaney, Stephen Todd Cohn
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Patent number: 7432255Abstract: The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds of the present invention are useful for the treatment and/or prevention of diseases which are associated with the modulation of histamine 3 (H3) receptors.Type: GrantFiled: April 26, 2007Date of Patent: October 7, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Heinrich Nettekoven, Olivier Roche
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Publication number: 20080242662Abstract: The invention relates to substituted 3,4- or higher substituted piperazine compounds, the use thereof for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; pharmaceutical formulations or products comprising said compounds, and/or a method of treatment comprising administering said compounds, a method for the manufacture of said compounds as well as novel intermediates, starting materials and/or partial steps for their synthesis. The compounds are especially of the formula I, wherein R1, R2, R11, C, E and D are as defined in the specification.Type: ApplicationFiled: May 29, 2006Publication date: October 2, 2008Inventors: Atsuko Nihonyanagi, Atsushi Toyao, Yuki Iwaki, Keiichi Masuya
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Publication number: 20080234260Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.Type: ApplicationFiled: January 6, 2005Publication date: September 25, 2008Inventors: Magnus Nilsson, Xiao-Xiong Zhou, Lourdes Oden, Bjorn Classon, Rolf Noren, Urszula Grabowska, Philip Jackson, Philip Fallon, Andrew Carr, Mark Liley, Matt Tozer, Tony Johnson, Victor Diaz, Laia Crespo, Jussi Kangasmetsa, Thierry Bonnaud
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Publication number: 20080234289Abstract: A melanocortin receptor-specific compound of the general formula of structure I: where X, R1, R2a, R2b, R3, R4a, R4b, R5a and R5b are as defined in the specification, which compound binds with high affinity to one or more melanocortin receptors and is optionally an agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist, and may be employed for treatment of one or melanocortin receptor-associated conditions or disorders, and methods for the use of the compounds of the invention.Type: ApplicationFiled: June 2, 2008Publication date: September 25, 2008Applicant: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Ramesh Rajpurohit, Zhijun Wu, Papireddy Purma, Annette M. Shadiack, Kevin D. Burris
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Patent number: 7427632Abstract: Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of thrombotic disorders.Type: GrantFiled: December 22, 2003Date of Patent: September 23, 2008Assignee: Eli Lilly and CompanyInventors: Scott Martin Sheehan, Brian Morgan Watson, John Walter Liebeschuetz
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Patent number: 7423058Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: December 21, 2006Date of Patent: September 9, 2008Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
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Publication number: 20080214542Abstract: The invention concerns compounds of general formula (I), a method for preparing same, as well as their use as therapeutic agent.Type: ApplicationFiled: November 29, 2005Publication date: September 4, 2008Applicant: BIOPROJETInventors: Marc Capet, Denis Danvy, Catherine Dartois, Nicolas Levoin, Marcel Morvan, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Patent number: 7419980Abstract: The present invention is directed to fused-aryl and heteroaryl 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: September 2, 2008Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
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Publication number: 20080206886Abstract: The present invention relates to a diagnostic contrast agent comprising a water dispersible, near-infrared tricarbocyanine, enamine-functionalized dye having a Stoke shift of greater than 50 and represented by five general formulae. The present invention also relates to a method for making a dye-conjugate utilizing the novel dye and a method of identifying a biological compound using the novel dye conjugate.Type: ApplicationFiled: February 28, 2007Publication date: August 28, 2008Inventors: Ruizheng Wang, John W. Harder, David A. Stegman, William J. Harrison, Hans F. Schmitthenner