The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/373)
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Publication number: 20130030173Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: ApplicationFiled: September 13, 2012Publication date: January 31, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Ke Ding, Guoping Wang
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Publication number: 20130025618Abstract: The present invention relates to a cationic 4-aminoindole of general formula (I), addition salts thereof with an acid and solvates thereof: in which: R1 is a linear or branched, saturated C2-C20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic 4-aminoindole, to the compositions, the uses, the hair dyeing processes and the devices using this cationic 4-aminoindole.Type: ApplicationFiled: December 6, 2010Publication date: January 31, 2013Inventor: Aziz Fadli
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Publication number: 20130029970Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: July 9, 2010Publication date: January 31, 2013Applicant: IRONWOOD PHARMACEUTICALS, INCInventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
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Patent number: 8362001Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: January 29, 2013Assignee: Janssen Pharmaceutica NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Patent number: 8362249Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R6, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: April 21, 2010Date of Patent: January 29, 2013Assignee: Boehringer Ingelheim International GmbHInventors: John David Ginn, Daniel Richard Marshall, Anthony S. Prokopowicz, Sabine Schlyer, Robert Sibley, Michael Robert Turner, Di Wu, Frank Wu
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Publication number: 20130023522Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: July 17, 2012Publication date: January 24, 2013Applicant: MERCK PATENT GMBHInventors: Henry YU, Jiezhen LI, Thomas E. RICHARDSON, Pandi BHARATHI, Brian H. HEASLEY, Andreas GOUTOPOULOS
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Publication number: 20130012522Abstract: The present invention relates to a compound of formula (I) wherein: R1 and R2 are selected from among H and C1-C10 alkyl; R3 is selected from among H, —OR4, N, —CN, —C(O)R4, —C(O)OR4, —C(O)N4R5, —C?NR4, —OC(O)R4, —NR4R5, —NR4C(O)R5, —NO2, —N?CR4R5, halogen and C1-C10 alkyl, wherein R4 and R5 are selected from among H, alkyl, alkenyl, cycloalkyl and aryl; X, Y, Z1, Z2 and Z3 are selected independently from among CH and N; A is selected from among (CH2)n, NH, O and CO, wherein n is an integer between 1 and 6, to the procedure for the obtainment of said compounds, to a pharmaceutical composition comprising said compound, and to the use thereof in the treatment of a neurodegenerative disease, more particularly treatment of Alzheimer's or Parkinson's disease.Type: ApplicationFiled: March 18, 2011Publication date: January 10, 2013Applicants: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS, UNIVERSIDAD DE BARCELONA, UNIVERSITAT AUTÓNOMA DE BARCELONAInventors: Abdelouahid Samadi, José Luis Marco Contelles, Irene Bolea Tomás, Francisco Javier Luque Garriga, Mercedes Unzeta López
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Patent number: 8338590Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substitutes A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.Type: GrantFiled: May 20, 2011Date of Patent: December 25, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Hervé Geneste, Andrea Hager-Wernet, legal representative
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Publication number: 20120323006Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: June 28, 2010Publication date: December 20, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli
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Patent number: 8318744Abstract: 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: GrantFiled: April 12, 2011Date of Patent: November 27, 2012Assignee: Merck PatentgesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Patent number: 8318725Abstract: The present invention relates to novel aryl indolyl sulfonamide compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.Type: GrantFiled: March 3, 2009Date of Patent: November 27, 2012Assignee: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Rama Sastri Kambhampati, Anil Karbhari Shinde, Ishtiyaque Ahmad, Nagaraj Vishwottam Kandikere, Venkateswarlu Jasti
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Publication number: 20120295884Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: January 2, 2012Publication date: November 22, 2012Applicant: NOVARTIS AGInventors: Eva ALTMANN, Ulrich HOMMEL, Edwige Liliane Jeanne LORTHIOIS, Juergen Klaus MAIBAUM, Nils OSTERMANN, Jean Quancard, Stefan Andreas RANDL, Olivier ROGEL, Oliver SIMIC, Anna VULPETTI, Veronique Stark-Rogel
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Patent number: 8304541Abstract: The present invention relates to a process for the manufacture of a specific indolinone derivative and a pharmaceutically acceptable salt thereof, namely 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone and its monoethanesulfonate, to new manufacturing steps and to new intermediates of this process.Type: GrantFiled: December 2, 2008Date of Patent: November 6, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Joern Merten, Guenter Linz, Juergen Schnaubelt, Rolf Schmid, Werner Rall, Svenja Renner, Carsten Reichel, Robert Schiffers
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Publication number: 20120277238Abstract: The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is —O—, etc., n is an integer of 0 to 6; X is —N(R7)— or —O—; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is —C(R8)? or —N?; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is ?O, ?S, etc.; B ring is a ring represented by the following formula: wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: July 29, 2010Publication date: November 1, 2012Applicant: Shionogi & Co., LtdInventors: Yuuki Tachibana, Masayoshi Miyagawa, Tsutomu Masuda, Tsuyoshi Hasegawa
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Publication number: 20120270859Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 14, 2012Publication date: October 25, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias TREU, Ulrich GUERTLER, Thomas KARNER, Oliver KRAEMER, Jens Juergen QUANT, Stephan Karl ZAHN
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Publication number: 20120269766Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H? function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.Type: ApplicationFiled: October 12, 2010Publication date: October 25, 2012Applicant: Yale UniversityInventors: David Spiegel, Christopher Parker
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Publication number: 20120252807Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of arboviruses.Type: ApplicationFiled: March 19, 2012Publication date: October 4, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Scott Larsen, Janice Sindac, Scott Barraza, David J. Miller
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Publication number: 20120245143Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: July 6, 2010Publication date: September 27, 2012Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Elena Casale, Alexander Khvat, Mikhail Yurievitch Krasavin, Paolo Orsini, Helena Posteri, Alessandra Scolaro
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Publication number: 20120245142Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: July 6, 2010Publication date: September 27, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Alexander Khvat, Mikhail Yurievitch Krasavin, Barbara Forte, Fabio Zuccotto
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Patent number: 8268831Abstract: The present invention describes a series of derivatives of 2-(3-methylenedioxy)-benzoyl indol, their mixtures, their pharmaceutically acceptable salts, their enantiomers, pharmaceutical compositions comprising them, processes for preparing them, use in the prophylactic and/or curative treatment of sexual dysfunction. More specifically, the invention describes derivatives (R)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione, and S)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione.Type: GrantFiled: September 30, 2009Date of Patent: September 18, 2012Assignee: Biolab Sanus Farmaceutica Ltda.Inventors: Sérgio Luiz Sacurai, Carlos Eduardo Da Costa Touzarim, Marcio Henrique Zaim
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Patent number: 8268828Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.Type: GrantFiled: August 6, 2010Date of Patent: September 18, 2012Assignee: SanofiInventors: David Squire Thorpe, Martin Smrcina, Dagmar Dasha Cabel
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Patent number: 8258139Abstract: The invention relates to a medicament or a method for treating mental disorders, in detail, ADHD comprising lurasidone, or a combination of lurasidone and a D4 receptor agonist.Type: GrantFiled: May 23, 2011Date of Patent: September 4, 2012Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Kazuhito Ikeda, Takeo Ishiyama
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Publication number: 20120214817Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Inventors: Bruce E Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20120202775Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: August 4, 2011Publication date: August 9, 2012Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Patent number: 8236804Abstract: 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: GrantFiled: May 4, 2011Date of Patent: August 7, 2012Assignee: Merck PatentgesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Publication number: 20120197014Abstract: The present invention generally relates to inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt), in particularly to compounds that inhibit Icmt activity and pharmaceutical compositions thereof. The invention also relates to methods of disease treatment using the same.Type: ApplicationFiled: July 30, 2010Publication date: August 2, 2012Inventors: Jo Lene Leow, Mei-Wang Casey, Patrick J. Casey, Mei Lin Go, Kumar Gorla Suresh
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Patent number: 8232312Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: GrantFiled: March 14, 2008Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Publication number: 20120178829Abstract: The instant invention pertains to novel bi- or tricyclic sterically hindered alkoxyamines, their precursors, a process for their preparation and their use as light stabilizers for polymers or coatings, as flame retardants, as peroxide substitutes (rheology modifiers) or carbon radical scavengers.Type: ApplicationFiled: August 3, 2010Publication date: July 12, 2012Applicant: BASF SEInventors: Stefan Hauck, Walter Fischer, Kai-Uwe Schoening
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Patent number: 8217044Abstract: There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.Type: GrantFiled: March 28, 2011Date of Patent: July 10, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jing Zhang, Zhuming Zhang
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Patent number: 8211885Abstract: The present invention relates to cyclic indole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: July 28, 2010Date of Patent: July 3, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Bodo Scheiper, Hans Matter, Hans Ulrich Stilz, Gary McCort
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Publication number: 20120157463Abstract: The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.Type: ApplicationFiled: August 31, 2010Publication date: June 21, 2012Applicant: PIERRE FABRE MEDICAMENTInventors: Pierre Sokoloff, Thierry Imbert, Jean-François Patoiseau, Jean-Pierre Rieu
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Patent number: 8202871Abstract: The present application discloses compounds of the formula: and pharmaceutical compositions containing same and their use for treating and preventing various pathologies, including obesity, appetite disorders, excess weight and diabetes.Type: GrantFiled: January 24, 2011Date of Patent: June 19, 2012Assignee: Sanofi-AventisInventors: Marco Baroni, Letizia Puleo
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Patent number: 8202870Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, R3, Y1, Y2, m, n, W, X, B and Z are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseasesType: GrantFiled: March 23, 2006Date of Patent: June 19, 2012Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Hervé Geneste
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Patent number: 8198274Abstract: This application discloses compounds of generic Formula I: or pharmaceutically acceptable salts thereof, wherein A, R1, R2, R3, R4, Q, X, Y, m, p, and q are defined as described herein, useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: July 15, 2009Date of Patent: June 12, 2012Assignee: Roche Palo Alto LLCInventors: Eun Kyung Lee, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20120142687Abstract: 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: February 8, 2012Publication date: June 7, 2012Inventors: Akira KUGIMIYA, Yuki Tachibana
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Patent number: 8193195Abstract: 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: GrantFiled: November 12, 2010Date of Patent: June 5, 2012Assignee: Merck PatentgesellschaftInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Patent number: 8188087Abstract: The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms.Type: GrantFiled: April 24, 2007Date of Patent: May 29, 2012Assignee: Merck Patent GmbHInventors: Susan Marie Reutzel-Eden, Gregory Alan Stephenson
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Publication number: 20120129100Abstract: An actinic ray-sensitive or radiation-sensitive resin composition including: (PA) a compound having a proton acceptor functional group and undergoing decomposition upon irradiation with an actinic ray or radiation to generate a compound reduced in or deprived of proton acceptor property or changed to be acidic from being proton acceptor-functioning, wherein a molar extinction coefficient ? of the compound (PA) at a wavelength of 193 nm as measured in acetonitrile solvent is 55,000 or less, and a pattern forming method using the composition are provided.Type: ApplicationFiled: August 17, 2010Publication date: May 24, 2012Applicant: FUJIFILM CORPORATIONInventors: Akinori Shibuya, Shuhei Yamaguchi, Shohei Kataoka, Michihiro Shirakawa, Takayuki Kato, Naohiro Tango
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Patent number: 8183374Abstract: Compounds of general formula (Ia): in which R1, A1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.Type: GrantFiled: January 22, 2007Date of Patent: May 22, 2012Assignee: M's Science CorporationInventors: Connie L. Sun, Xiaoyuan Li
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Publication number: 20120122839Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Applicant: Priaxon AGInventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
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Publication number: 20120122868Abstract: Derivatives of 2,5-piperazinedione of formula (I) are apoptotic peptidase activating factor 1 (Apaf-1) inhibitors, therefore they are useful as active pharmaceutical ingredients for the prophylaxis and/or treatment of a pathological and/or physiological condition associated with an increase of apoptosis.Type: ApplicationFiled: July 29, 2010Publication date: May 17, 2012Applicant: LABORATORIOS SALVAT, S.A.Inventors: Ángel Messeguer Pyepoch, Alejandra Moure Fernández, Daniel Gonzáles Pinacho, Isabel Masip Masip, Enrique Pérez Payá, Natividad García, Ester Monlleó Mas, Juanlo Catena Ruiz
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Publication number: 20120108815Abstract: A precursor for the deposition of a thin film by atomic layer deposition is provided. The compound has the formula MxLy where M is a metal and L is an amidrazone-derived ligand or an amidate-derived ligand. A process of forming a thin film using the precursors is also provided.Type: ApplicationFiled: April 21, 2010Publication date: May 3, 2012Applicant: WAYNE STATE UNIVERSITYInventor: Aloke K. Dutta
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Publication number: 20120108607Abstract: The present invention relates to the enantiomers of 5,7-dichloro-3-{4-[4-(4-chlorophenyl)-piperazin-1-yl]butyl}-3-ethyl-1,3-dihydro-2H-indol-2-one of the Formula (II) pharmaceutically acceptable salts thereof, process for the preparation thereof, medicinal products containing said enantiomers and the use thereof and their pharmaceutically acceptable salts in the treatment of the disorders of the central nervous system.Type: ApplicationFiled: February 5, 2010Publication date: May 3, 2012Inventors: Balázs Volk, József Barkóczy, István Gacsalyi, Elemér Fogassy, József Schindler, Gábor Gigler, Hajnalka Kompagne, Iidikó Nagyné Gyoenos, Katalin Pallagi, Márta Porcs-Makkay, Gábor Szénási, Tibor Mezel, Gyula Lukács, Gyoergy Lévay, András Egyed, László Gábor Hársing
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Publication number: 20120064090Abstract: Provided are a pharmaceutical composition which enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, wherein the cancer has resistance to the molecular target drug, and a cancer therapeutic agent effective against a cancer having resistance to a molecular target drug, such as gefitinib and erlotinib. The pharmaceutical composition comprising an HGF-MET receptor pathway inhibitor enhances the sensitivity of a cancer to a molecular target drug, such as gefitinib and erlotinib, even though the cancer has resistance to the molecular target drug. The cancer therapeutic agent comprising a molecular target drug in combination with an HGF-MET receptor pathway inhibitor is effective against a cancer having resistance to the molecular target drug.Type: ApplicationFiled: October 9, 2009Publication date: March 15, 2012Applicant: KRINGLE PHARMA INC.Inventors: Seiji Yano, Kunio Matsumoto
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Publication number: 20120058996Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: November 9, 2011Publication date: March 8, 2012Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Patent number: 8119623Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: GrantFiled: September 15, 2009Date of Patent: February 21, 2012Assignee: Priaxon AGInventors: Christoph Burdack, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
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Publication number: 20120039913Abstract: The invention relates to Histamine H4 receptor antagonists or inhibitors of Histamine H4 receptor gene expression for the treatment and/or the prevention of vestibular disorders.Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: INSERM (institut National de la Sante de la Recher Medicale)Inventors: Gilles Desmadryl, Christian Chabbert
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Publication number: 20120040996Abstract: The invention relates to 3-benzofuranyl-indol-2-one derivatives substituted at the 3 position and of the formula (I) where R1, R2, R3, R4, R5 and n are such as defined in claim 1, to a method for preparing same, and to the therapeutic use of said compounds.Type: ApplicationFiled: February 9, 2010Publication date: February 16, 2012Applicant: SANOFIInventors: Marco Baroni, Letizia Puleo
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Publication number: 20120040990Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20120040958Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp