Indole Ring System (including Hydrogenated) Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/254.09)
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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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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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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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Patent number: 8211935Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: GrantFiled: December 17, 2010Date of Patent: July 3, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas P. Termin, Esther Ann Martinborough, Nicole Hilgraf, Charles J. Cohen, Corey Anderson
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Publication number: 20120157472Abstract: The present invention relates to a method of treating patients suffering from colorectal cancer characterized by coadministration of BIBF 1120 and BIBW 2992, wherein in said method BIBF 1120 is administered according to a continuous daily regimen and BIBW 2992 is administered according to a weekly alternating on-off regimen, pharmaceutical compositions and kits suitable for this method as well as their preparation.Type: ApplicationFiled: January 13, 2010Publication date: June 21, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Annette Larsen, Anke Baum, Frank Hilberg, Flavio Solca
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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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Publication number: 20120142703Abstract: The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of an inhibitor of vascular endothelial growth factor receptors (VEGFRs) in conjunction with a thrombin inhibitor.Type: ApplicationFiled: May 11, 2010Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joanne Van Ryn, Frank Hilberg, Pilar Garin-Chesa
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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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Publication number: 20120136004Abstract: The invention relates to new methods for the treatment of oncological and fibrotic diseases comprising the combined administration of a receptor tyrosine kinase inhibitor in conjunction with a thrombin inhibitor.Type: ApplicationFiled: May 11, 2010Publication date: May 31, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joanne Van Ryn, Pilar Garin-Chesa, Flavio Solca
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Patent number: 8188088Abstract: Compounds of the formula (I), which are suitable for use as microbiocides, and in which A is A1, or A is A2, or A is A3, or A is A4 and B is a phenyl, naphthyl or quinolinyl group.Type: GrantFiled: June 14, 2007Date of Patent: May 29, 2012Assignees: Syngenta Participations AG, Syngenta LimitedInventors: Daniel Stierli, John Taylor, Harald Walter, Paul Anthony Worthington
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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: 20120129853Abstract: This invention pertains to methods of treating systemic lupus erythematosus, lupus nephritis or Sjogren's Syndrome with compounds that selectively inhibit the activity of Bcl-2 anti-apoptotic proteins. Specifically, the current invention is directed to treatment with compounds that selectively inhibit the activity of Bcl-2 proteins, with a lesser affinity for inhibiting the activity of other BCL-2 family proteins, including Bcl-xL.Type: ApplicationFiled: November 22, 2011Publication date: May 24, 2012Applicant: Abbott LaboratoriesInventors: Steven Elmore, Andrew Souers, Li Chun Wang, Tariq Ghayur, Stuart J. Perper
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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: 20120115778Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 10, 2012Applicant: The Trustees of Columbia University in the City of New YorkInventors: Gerard Karsenty, Vijay Yadav, Franck Oury
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Publication number: 20120107304Abstract: The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of a cell signalling and/or angiogenesis inhibitor in conjunction with an Aurora kinase inhibitor.Type: ApplicationFiled: April 19, 2011Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Flavio Solca, Ulrich Guertler, Ulrike Tontsch-Grunt
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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: 20120077825Abstract: 1-[4-(5-cyanoindo1-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof is used for the manufacture of a medicament for the treatment of sub-type anxiety disorders chosen from the sub-types panic disorder with or without agoraphobia, agoraphobia. obsessive-compulsive spectrum disorders, social phobia, posttraumatic stress disorder, acute stress indication or generalized-anxiety disorder, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, anorexia and fibromyalgia. A preferred salt is 1-[4-(5-cyanoindo1-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride.Type: ApplicationFiled: May 26, 2011Publication date: March 29, 2012Applicant: Merck PatentgesellschaftInventors: Gerd Bartoszyk, Christoph Seyfried, Christoph Von Amsterdam, Henning Boettcher, Ewen Sedman
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Publication number: 20120071461Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.Type: ApplicationFiled: September 22, 2011Publication date: March 22, 2012Applicant: GRUENENTHAL GmbHInventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
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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: 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: 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: 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
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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: 20120034186Abstract: Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. A high throughput screen identified compounds that inhibit the PTP Shp2. Several compounds were identified that selectively inhibit Shp2 over Shp1 with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.Type: ApplicationFiled: October 17, 2011Publication date: February 9, 2012Applicants: University of South Florida, H. Lee Mofffitt Cancer Center and Research Institute, Inc.Inventors: Jie Wu, Nicholas James Lawrence, Said M. Sebti, Harshani Rithma Lawrence
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Publication number: 20120028963Abstract: The present invention relates to hydroxamate derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, a method of treating disease using the compositions, and a method for preparing the hydroxamate derivatives.Type: ApplicationFiled: March 18, 2010Publication date: February 2, 2012Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Sung Sook Lee, Kyung Joo Lee, Chang Sik Lee, Hyun Mo Yang, Do Hoon Kim, Dae Kyu Choi, Ho Jin Choi, Dal Hyun Kim, In Chang Hwang, Mi Jeong Kim, Byeong Hoon Han
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Publication number: 20120028920Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20120028990Abstract: A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.Type: ApplicationFiled: April 14, 2010Publication date: February 2, 2012Inventors: Takashi Fujimura, Hiroyuki Kishino, Takashi Mizutani, Shunji Sakuraba, Takahide Sasaki, Nagaaki Sato
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Patent number: 8106057Abstract: This invention provides methods for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): and in particular, those of subgenus VIIa These compounds inhibit or modulate the activity of the heat shock protein Hsp90.Type: GrantFiled: May 19, 2010Date of Patent: January 31, 2012Assignee: Astex Therapeutics, Ltd.Inventors: Gianni Chessari, Maria Grazia Carr, Miles Stuart Congreve, Robert Downham, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
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Publication number: 20120022078Abstract: A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is a hydrogen atom, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, or haloC1-6alkyloxy; R2 represents C1-6alkyl or haloC1-6alkyl; R3 represents a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents an aryl or heteroaryl, wherein the aryl or the heteroaryl may be substituted with 1 to 3 substituents such as halogen, C1-6alkyl, haloC1-6alkyl, and C1-6alkyloxy.Type: ApplicationFiled: April 7, 2010Publication date: January 26, 2012Applicant: MSD K.K.Inventors: Hiroyuki Kishino, Sayaka Mizutani, Shunji Sakuraba, Nagaaki Sato
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Patent number: 8101608Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-II, Rsk1, SGK, TrkA, TrkB and TrkC kinases.Type: GrantFiled: November 7, 2005Date of Patent: January 24, 2012Assignee: IRM LLC, a Delware Limited CorporationInventors: Yongqin Wan, Yuan Mi, Yi Fan, Dai Cheng, Yi Liu, Nathanael S. Gray, Pamela Albaugh
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Publication number: 20120015959Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumours.Type: ApplicationFiled: March 3, 2010Publication date: January 19, 2012Inventors: Wolfgang Staehle, Kai Schiemann, Melanie Schultz
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Publication number: 20120004224Abstract: 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: June 29, 2011Publication date: January 5, 2012Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elisc Rioux, Sasmita Tripathy, Terrance W. Deyle
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Publication number: 20120004202Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.Type: ApplicationFiled: March 31, 2011Publication date: January 5, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John Edward PARK, Nveed CHAUDHARY, Gerald Juergen ROTH, Armin HECKEL, Thorsten LEHMANN-LINTZ, Joerg KLEY
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Patent number: 8088768Abstract: The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.Type: GrantFiled: August 10, 2010Date of Patent: January 3, 2012Assignee: The Research Foundation of The State University of New YorkInventors: David G. Hangauer, Jr., Moustafa E. El-Araby, Karen L. Milkiewicz
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Patent number: 8084440Abstract: This invention is in the field of animal food, in particular food for female animals in their reproductive phase. Food according to the invention improves the fertility of animals and increases their chances on a pregnancy. It was found that the fertility of animals may be improved by feeding the animal with a certain amount of naturally occurring immune enhancing ingredients such as beta-glucans and/or phytohormones like auxin or gibberellic acid. Also, combinations of these substances, in particular the combination of beta-glucans and phytohormones, were shown to have a synergistic effect in that they improved the fertility of the animal more than these individual components on their own.Type: GrantFiled: April 19, 2006Date of Patent: December 27, 2011Assignee: Desol B.V.Inventors: Wilhelmus Hubertus Henricus Antonius Van Den Elshout, Rudi Ludovicus Florent Forier
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Publication number: 20110312945Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.Type: ApplicationFiled: October 1, 2009Publication date: December 22, 2011Inventors: James Jia, Ara Mermerian, Charles Kim, Regina Graul, Joel Moore
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Publication number: 20110312971Abstract: 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 12, 2011Publication date: December 22, 2011Applicant: Merck PatentgesellschaftInventors: Andreas BATHE, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning BÖTTCHER
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Publication number: 20110312972Abstract: The invention relates to disubstituted 3-benzofuranyl-indol-2-one-3-acetamidopiperazine derivatives of the general formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R9 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: December 22, 2011Applicant: SANOFIInventors: Marco Baroni, Letizia Puleo
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Publication number: 20110301177Abstract: The present invention relates to a suspension formulation containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate, to a capsule pharmaceutical dosage form containing said suspension formulation, to a process for preparing said suspension formulation, to a process for preparing said capsule comprising said suspension formulation and to the packaging material for the finished capsule.Type: ApplicationFiled: June 4, 2009Publication date: December 8, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roman Messerschmid, Rudolf Binder, Thomas Bock, Werner Brox
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Patent number: 8071602Abstract: Compounds of general formula (I) in which R1, 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: October 10, 2006Date of Patent: December 6, 2011Assignee: M's Science CorporationInventor: Connie L. Sun
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Publication number: 20110294822Abstract: The invention relates to a substituted phenylpiperazine aryl alkanol derivative represented by the following general formula and its salt and hydrate, wherein C1 and C2 represent chiral carbon atoms, and the compound is one of the six isomers: (1RS, 2SR), (1RS, 2RS), (1R, 2S), (1S, 2S), (1R, 2R) or (1S, 2R); and R, R1, R2, R3 and Ar are as defined in the specification. The derivative is non-opioid analgesic, has good analgesic effect and relatively small side effects. The invention also relates to a composition comprising the derivative and its use.Type: ApplicationFiled: December 22, 2009Publication date: December 1, 2011Applicant: NHWA PHARMA. CORPORATIONInventors: Jianqi Li, Guan Wang, Guisen Zhang, Xiangping Yang, Peng Xie, Linjie Zhang, Xiangqing Xu, Yumei Wang