Plural Nitrogens In The Additional Five-membered Hetero Ring Patents (Class 514/254.05)
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Patent number: 7728029Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: March 14, 2007Date of Patent: June 1, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Kevin William Anderson, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Jr., Kevin Richard Guertin, Nancy-Ellen Haynes, Michael Paul Myers, Sherrie Lynn Pietranico-Cole, Lida Qi, Pamela Loreen Rossman, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Qiang Zhang
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Publication number: 20100130464Abstract: The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: June 21, 2006Publication date: May 27, 2010Applicants: ASTEX THERAPEUTICS LIMITED, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Thomas Glanmor Davies, Robert George Boyle, Ian Collins, Michelle Dawn Garrett
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Publication number: 20100130509Abstract: The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds, variants of bis(1-aryl-5-tetrazolyl)methanes, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.Type: ApplicationFiled: April 3, 2008Publication date: May 27, 2010Applicant: Nederlandse Organisatie voor toegepast-natuurwe- tenschappelijk onderzoek TNOInventors: Frank Henri Johan Schuren, Roy Christiaan Montijn
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Publication number: 20100125075Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: ApplicationFiled: December 14, 2006Publication date: May 20, 2010Applicant: British Biotech Pharmaceuticals Ltd.Inventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Publication number: 20100125064Abstract: The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula I, wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.Type: ApplicationFiled: March 27, 2008Publication date: May 20, 2010Applicant: NOVARTIS AGInventors: Andreas Boettcher, Nicole Buschmann, Pascal Furet, Jean-Marc Groell, Jorg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Lorenz Mayr, Andrea Vaupel
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Publication number: 20100119622Abstract: The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 15, 2009Publication date: May 13, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100113447Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: August 10, 2009Publication date: May 6, 2010Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Publication number: 20100105665Abstract: Compounds, pharmaceutical compositions, kits, article of manufacture, methods of using, and method of preparing of compounds having the formula of: wherein the variables are as defined herein.Type: ApplicationFiled: January 9, 2008Publication date: April 29, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Lily Kwok, Betty Lam, Zhe Li, Zhiyuan Zhang
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Publication number: 20100105684Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the treatment or prophylaxis of various disorders of humans or animals.Type: ApplicationFiled: March 28, 2008Publication date: April 29, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover, Helmut Buschmann
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Patent number: 7705007Abstract: There are provided compounds of the formula I wherein R, V1, V2 and Ring A are described herein. The compounds exhibit anticancer activity.Type: GrantFiled: January 17, 2007Date of Patent: April 27, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Gregory Jay Haley, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
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Patent number: 7700586Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.Type: GrantFiled: September 4, 2002Date of Patent: April 20, 2010Assignee: Axikin Pharmaceuticals, Inc.Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
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Publication number: 20100075966Abstract: The invention relates to dihydroimidazoles of formula rac-(I), wherein the radicals and symbols are as defined herein; their use as inhibitors of the interaction of the MDM2 protein with a p53-like peptide, new pharmaceutical formulations comprising said compounds, said compounds for use in the therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of proliferative diseases or for the manufacture of pharmaceutical formulations useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide, a pharmaceutical formulation e.g. useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide comprising said compound, methods of treatment comprising administration of said compounds to a warm-blooded animal, and/or processes for the manufacture of said compounds.Type: ApplicationFiled: November 26, 2007Publication date: March 25, 2010Inventors: Sylvie Chamoin, Hans- Jorg Roth, Juerg Zimmermann, Thomas Zoller
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Publication number: 20100069353Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV replication, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: December 3, 2007Publication date: March 18, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christiane Yoakim, Patrick Deroy, Martin Duplessis, Alexandre Gagnon, Sylvie Goulet, Oliver Huecke, Christopher Lemke, Simon Surprenant
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Publication number: 20100069400Abstract: A method for treating an inflammatory condition or immune disorder comprises administering to a subject having such a condition or disorder a therapeutically effective amount of at least one compound selected from irindalone, physiologically active enantiomers thereof, and pharmaceutically acceptable salts thereof. The invention further provides a method for elevating levels of anti-inflammatory cytokines such as IL-10 and IL-13 while inhibiting expression of pro-inflammatory cytokines. A pharmaceutical composition, useful for example in topical treatment of psoriasis, comprises a therapeutically effective amount of at least one compound selected from irindalone, physiologically active enantiomers thereof, and pharmaceutically acceptable salts thereof, in a vehicle comprising at least one pharmaceutically acceptable excipient, the vehicle being adapted for topical administration to skin of a subject.Type: ApplicationFiled: July 10, 2009Publication date: March 18, 2010Applicant: Ore Pharmaceuticals Inc.Inventors: Scott Malstrom, Hellen Mulomi Amuguni, Clary Clish, Amy Anderson Deik, David White
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Publication number: 20100069386Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting form hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. Such methods and reagents may also inhibit the hedgehog pathway in normal cells, e.g., where normal levels of hedgehog signalling are unwanted.Type: ApplicationFiled: September 14, 2009Publication date: March 18, 2010Inventors: Philip A. Beachy, James K. Chen, Anssi Jussi Nikolai Taipale
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Publication number: 20100062972Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound has superior HSD1 inhibitory activity, and is useful as an HSD1 inhibitor, a therapeutic drug of diabetes or a therapeutic drug of obesity or a therapeutic drug of metabolic syndrome.Type: ApplicationFiled: November 19, 2009Publication date: March 11, 2010Inventors: JAY P. POWERS, Mario G. CARDOZO, Hiroyuki GOTO, Kazuhito HARADA, Katsuaki IMAMURA, Makoto KAKUTANI, Isamu MATSUDA, Yasuhiro OHE, Shinji YATA
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Publication number: 20100056498Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: November 9, 2009Publication date: March 4, 2010Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
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Publication number: 20100041655Abstract: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2— or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).Type: ApplicationFiled: February 5, 2007Publication date: February 18, 2010Inventors: Naoya Ono, Tetsuo Takayama, Fumiyasu Shiozawa, Hironori Katakai, Tetsuya Yabuuchi, Tomomi Ota, Makoto Yagi, Masakazu Sato
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Patent number: 7662816Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: August 4, 2004Date of Patent: February 16, 2010Assignee: Schering CorporationInventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Patent number: 7659276Abstract: Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein A, W, X, Z, R1-R3, and R8 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.Type: GrantFiled: February 6, 2009Date of Patent: February 9, 2010Assignee: Amgen, Inc.Inventors: Christopher Hulme, Paul Tempest, Vu Ma, Thomas Nixey, Guity Balow
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Publication number: 20100029620Abstract: The present invention concerns substituted triazolone, tetrazolone and imidazolone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective ?2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.Type: ApplicationFiled: December 20, 2005Publication date: February 4, 2010Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Joaquin Pastor-Fernández, Xavier Jean,Michel Langlois, Julen Oyarzabal-Santamarina, Juan Antonio Vega-Ramiro
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Publication number: 20100022540Abstract: Novel triazole derivatives of the formula (I) in which R1—R6 and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: April 20, 2007Publication date: January 28, 2010Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Publication number: 20100021420Abstract: A combination comprising (a) a compound of formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NR9(C?O) or 0(C?O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 to 3 carbon atoms; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or an optionally substituted C1-8 hydrocarbyl group wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; and (b) a compound of formulType: ApplicationFiled: July 13, 2007Publication date: January 28, 2010Applicant: ASTEX THERAPEUTICS LIMITEDInventors: John Francis Lyons, Matthew Simon Squires, Neil Thomas Thompson, Neil James Gallagher
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Publication number: 20100016313Abstract: Disclosed are modulators, i.e., activators and inhibitors, of Intestinal Alkaline Phosphatase (IAP). Also disclosed are methods for treating bacterial infections of the intestinal tract and methods for maintaining the health of the intestinal tract using IAP activators. Further disclosed are methods to assist in weight gain of emaciated patients and those having reduced or negligible fat absorption using IAP inhibitors.Type: ApplicationFiled: May 19, 2009Publication date: January 21, 2010Applicant: Burnham Institute for Medical ResearchInventors: Jose Luis Millan, Sonoko Narisawa, Eduard Sergienko
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Patent number: 7645775Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 21, 2005Date of Patent: January 12, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Davies, Cornelia Forster, Michael Arnost, Jian Wang
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Publication number: 20100004263Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: ApplicationFiled: December 22, 2008Publication date: January 7, 2010Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Libuse Jaroskova, Peter Walter Maria Roevens, Louis Jozef Elisabeth Van Der Veken, Marcel Viellevoye, Joannes Theodorus Maria Linders
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Publication number: 20100004264Abstract: Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: October 2, 2007Publication date: January 7, 2010Inventors: Yifeng Xiong, Martin C. Cherrier, Jin Sun Karoline Choi, Peter I. Dosa, Brian M. Smith, Sonja Strah-Pleynet, Brett Ullman, Bradley Teegarden
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Publication number: 20100004265Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,3-triazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis or pain.Type: ApplicationFiled: November 7, 2007Publication date: January 7, 2010Inventors: Nadine Jagerovic, Cristina Ana Gomez-De La Oliva, Maria Pilar Goya-Laza, Alberto Dordal Zueras, Maria Rosa Cuberes-Altisent
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Publication number: 20090325974Abstract: Novel 1,5-diphenylpyrazole derivatives of the formula (I) in which R1-R6 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: April 20, 2007Publication date: December 31, 2009Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Publication number: 20090325979Abstract: Disclosed are novel imidazolylalkylcarbonyl derivatives useful as calcium channel modulators and a preparation method of the same. Also disclosed is a method for the treatment of diseases by administering the above compounds based on their inhibitory activity against calcium channel.Type: ApplicationFiled: June 26, 2009Publication date: December 31, 2009Inventors: Kyung Il CHOI, Ghilsoo Nam, Hye Ran Kim, Hyewhon Rhim, Seon Hee Seo, Yoon Jee Kim, Hee Sup Shin, Dong Jin Kim, Ae Nim Pae, Hye Jin Chung, Yong Seo Cho, Hyunah Choo, Eun Joo Roh, Soon Bang Kang, Kye Jung Shin, Hoh Gyu Hahn, Dong Yun Shin, Chan Seong Cheong, Kee Dal Nam, Yong Koo Kang, Jae Kyun Lee, Woong Seo Park, Youngsoo Kim, Eunice Eun-Kyeong Kim, Key-Sun Kim, Hesson Chung, Gyo Chang Keum, Cheolju Lee, Kee Hyun Choi
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Patent number: 7638546Abstract: The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonist or antagonists of somatostatin receptors.Type: GrantFiled: October 29, 2007Date of Patent: December 29, 2009Assignee: IPSEN Pharma S.A.S.Inventors: Christophe Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Thomas D. Gordon, Barry A. Morgan, Christophe Philippe Moinet, Dennis C. H. Bigg
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Publication number: 20090318468Abstract: There is provided novel compounds of formula (Ia) or (Ib): or pharmaceutically acceptable salsts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: June 19, 2009Publication date: December 24, 2009Applicant: AstraZeneca ABInventors: David Buttar, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20090312341Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24) (R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Type: ApplicationFiled: June 24, 2009Publication date: December 17, 2009Inventors: Jared N. Cumming, Ying Huang, Guoqing Li, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Jianping Pan, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie
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Publication number: 20090306039Abstract: 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 B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: ApplicationFiled: July 20, 2007Publication date: December 10, 2009Inventors: Shifeng Pan, Yi Liu, Yun Feng Xie, Dai Cheng, yongqin Wan, Dong Han, Yang Yang, Wenqi Gao, Jiqing Jiang, Badry Bursulaya, Philip Chamberlain, Donald Karanewsky, Xia Wang
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Publication number: 20090298785Abstract: It has now been found that the p53 pathway is inactivated in ocular cancers such as retinoblastoma. As such, the present invention is a method for inducing ocular cancer cell death using a p53 activator. In particular embodiments, the p53 activator blocks the interaction between DM2 or DMX and p53. As the p53 activator induces ocular cancer cell death, a method for preventing or treating ocular cancer is also provided.Type: ApplicationFiled: July 24, 2007Publication date: December 3, 2009Inventors: Michael A. Dyer, Jean-Christophe Marine, Aart Gerrit Jochemsen
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Patent number: 7625902Abstract: The invention is concerned with novel imidazolidinone derivatives of formula (I): wherein R1 to R11 and X are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds bind to LXR alpha and LXR beta and can be used in pharmaceutical compositions.Type: GrantFiled: March 24, 2008Date of Patent: December 1, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Ulrike Obst Sander, Stephan Roever, Tanja Schulz-Gasch, Matthew Wright
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Publication number: 20090291963Abstract: Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R1, D, E, R12, p, X1, E, G, X2 and Z are as defined in claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolytics and/or antihypertonics.Type: ApplicationFiled: July 29, 2009Publication date: November 26, 2009Inventors: Oliver SCHADT, Henning Böttcher, Joachim Leibrock, Kai Schiemann, Timo Heinrich, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
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Publication number: 20090286771Abstract: Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.Type: ApplicationFiled: July 16, 2009Publication date: November 19, 2009Inventors: Yingfu Li, Kevin Bacon, Hiromi Sugimoto, Keiko Fukushima, Kentaro Hashimoto, Makiko Marumo, Toshiya Moriwaki, Noriko Nunami, Naoki Tsuno, Klaus Urbahns, Nagahiro Yoshida
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Patent number: 7618971Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 27, 2005Date of Patent: November 17, 2009Assignee: Merck & Co. Inc.Inventors: Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, George D. Hartman, John Schreier
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Publication number: 20090275595Abstract: There is to provide is an agent for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion comprising an effective amount of 2-[4-[2-(benzimidazole-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide (hereinafter, referred to as compound 1), its pharmaceutically acceptable salt or a hydrate thereof and Pitavastatin, and a pharmaceutically acceptable carrier, wherein the agent is intended to be simultaneously administered, or separately administered with interval of time to a patient in need thereof.Type: ApplicationFiled: December 9, 2005Publication date: November 5, 2009Applicant: KOWA CO., LTD.Inventors: Hideyuki Kobayashi, Yasunobu Yoshinaka, Kimiyuki Shibuya
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Publication number: 20090275563Abstract: Patients suffering from serotonin-mediated diseases or conditions, such as depression, may be treated by administering an effective combined amount of a 5-HT7 receptor antagonist and a serotonin reuptake inhibitor.Type: ApplicationFiled: October 18, 2006Publication date: November 5, 2009Inventor: Pascal Bonaventure
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Patent number: 7612060Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: October 11, 2005Date of Patent: November 3, 2009Assignee: Amgen Inc.Inventors: Toshihiro Aya, Guolin Cai, Jian J. Chen, Derin D'Amico, Thomas Nguyen, Wenyuan Qian
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Publication number: 20090263398Abstract: The invention provides a combination comprising an ancillary compound and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NR9(C?O) or 0(C?O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy; or a C1-4 hydrocarbyl group optionally substituted byType: ApplicationFiled: July 13, 2007Publication date: October 22, 2009Applicant: Astex Therapeutics LimitedInventors: John Francis Lyons, Matthew Simon Squires, Neil Thomas Thompson, Neil James Gallagher, Jayne Elizabeth Curry
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Publication number: 20090264442Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: March 1, 2007Publication date: October 22, 2009Applicant: Laboratorios Del Dr. Esteves, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20090264416Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.Type: ApplicationFiled: August 19, 2008Publication date: October 22, 2009Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
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Publication number: 20090257950Abstract: The membrane scaffold proteins (MSP) of the present invention assemble with hydrophobic or partially hydrophobic proteins to form soluble nanoscale particles which preserve native structure and function; they are improved over liposomes and detergent micelles, both in terms of stability and preservation of biological activity and native conformation. In the presence of phospholipid, MSPs form nanoscopic phospholipid bilayer disks, with the MSP stabilizing the particle at the perimeter of the bilayer domain. The particle bilayer structure allows manipulation of incorporated proteins in solution or on solid supports, including for use with such surface-sensitive techniques as scanning probe microscopy or surface plasmon resonance. The nanoscale particles, which are robust in terms of integrity and maintenance of biological activity of incorporated proteins, facilitate pharmaceutical and biological research, structure/function correlations, structure determinations, bioseparations, and drug discovery.Type: ApplicationFiled: October 10, 2007Publication date: October 15, 2009Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Stephen G. Sligar, Timothy H. Bayburt, Mary A. Schuler, Natanya R. Civjan, Yelena V. Grinkova, Ilia G. Denisov, Stephen James Grimme
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Publication number: 20090253673Abstract: Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of the ghrelin receptor, such as obesity, diabetes, and metabolic syndrome.Type: ApplicationFiled: July 6, 2007Publication date: October 8, 2009Inventors: Min Ge, Eric Cline, Lihu Yang, Sander G. Mills
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Patent number: 7598250Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Type: GrantFiled: August 4, 2004Date of Patent: October 6, 2009Assignee: Schering CorporationInventors: Jared N. Cumming, Ying Huang, Guoqing Li, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Jianping Pan, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie
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Publication number: 20090247525Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: March 2, 2007Publication date: October 1, 2009Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20090239877Abstract: The invention provides 1,2,4-triazole compounds, compositions containing those compounds, methods of treating diseases and/or disorders with those compounds and processes of manufacturing 1,2,4-triazole compounds.Type: ApplicationFiled: March 17, 2009Publication date: September 24, 2009Applicants: AETERNA ZENTARIS GmbH, CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE, University of Montpellier I, University of Montpellier IIInventors: Jean-Alain Fehrentz, Mathieu Bibian, Aline Moulin, Jean Martinez