Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To A Piperidine Ring Patents (Class 546/189)
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Publication number: 20120088791Abstract: In one aspect, the invention relates to compounds having a general structure: Formula (I) which are useful as allosteric agonists of the M1 muscarinic receptor, synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: February 19, 2010Publication date: April 12, 2012Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, Jeffrey P. Corn, Charles David Weaver, Colleen M. Niswender, Evan P. Lebois, Thomas M. Bridges
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Publication number: 20120083499Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: December 12, 2011Publication date: April 5, 2012Applicant: ABBOTT LABORATORIESInventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
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Publication number: 20120065230Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: ApplicationFiled: March 21, 2011Publication date: March 15, 2012Applicant: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Publication number: 20120010242Abstract: The present invention relates to the use of low dose pipamperone and compositions comprising the same for the treatment of mood disorders.Type: ApplicationFiled: March 30, 2010Publication date: January 12, 2012Applicant: ALKERSTRAAT 30 AInventor: Erik Buntinx
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Publication number: 20110311447Abstract: Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for ?1 receptors. Some compounds are also highly selective for ?1 receptor compared to ?2 receptor. Compounds can comprise radioisotopes, including 18F or 11C. Radiolabeled compounds can be used as probes for imaging distribution of ?1 receptor in a subject such as a human using positron emission tomography (PET) scanning.Type: ApplicationFiled: June 21, 2011Publication date: December 22, 2011Applicant: WASHINGTON UNIVERSITYInventors: Zhude Tu, Robert H. Mach, Wei Wang, Stanley M. Parsons
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Publication number: 20110312965Abstract: The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis.Type: ApplicationFiled: December 21, 2009Publication date: December 22, 2011Inventors: Walter Cabri, Giuseppe Giannini, Gianfranco Battistuzzi, Domenico Alloatti, Claudio Pisano, Sabrina Dallavalle, Tiziana Brunetti
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Publication number: 20110301196Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.Type: ApplicationFiled: January 28, 2011Publication date: December 8, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
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Patent number: 8071624Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: June 23, 2005Date of Patent: December 6, 2011Assignee: Incyte CorporationInventors: Wenqing Yao, Meizhong Xu, Colin Zhang, Yanlong Li, Jincong Zhuo, Brian W. Metcalf
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Patent number: 8049042Abstract: To provide a resist polymer comprising, as a structural unit, an acid-decomposable unit having a structure represented by formula (1) or (2) which exhibits a small line edge roughness and produces little defects in DUV excimer laser lithography or the like.Type: GrantFiled: March 26, 2009Date of Patent: November 1, 2011Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Hikaru Momose, Atsushi Ootake, Tadashi Nakamura, Akifumi Ueda
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Patent number: 8030491Abstract: The invention relates to new compounds of formula (III): wherein R is a C1-C4 linear or branched alkyl group. The invention also relates to new compounds of formula (IV) wherein M is a metal. The invention also relates to methods of making compounds of formulas (III) and (IV) and to methods of making donepezil and pharmaceutically acceptable salts thereof, such as donepezil hydrochloride, using the compounds.Type: GrantFiled: January 3, 2007Date of Patent: October 4, 2011Assignee: Cipla LimitedInventors: Srinivas Laxminarayan Pathi, Vinod Acharya, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
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Publication number: 20110224185Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: May 23, 2011Publication date: September 15, 2011Inventors: Phillip B. Alper, Mihai Azimioara, Christopher Cow, Robert Epple, Songchun Jiang, Gerald Lelais, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin, Lucas Westcott-Baker
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Publication number: 20110201581Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: February 11, 2011Publication date: August 18, 2011Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
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Publication number: 20110190300Abstract: The invention relates to amide compounds of Formula I: (I) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl, etc.; R1 and R2 are each independently hydrogen, halogen, cyano, optionally substituted lower alky, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl etc. R3 and R4 are hydrogen, each optionally substituted lower alkyl, cycloalkyl, aryl or heterocyclyl etc.; X is ?O, optionally substituted lower alkyl, halogen, cyano, nitro etc., n is 0-5, m is 1 or 2 and p is 0-2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: May 30, 2008Publication date: August 4, 2011Inventors: Akira Matsumura, Hidenori Mikamiyama, Jiangchao Yao
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Patent number: 7989629Abstract: The present invention relates to a compound of formula (I), or a salt thereof wherein the naphthalene ring is substituted in the 2, 3, 4, 5, 6, 7 or 8 position by R1, and R1 represents —CH2CH2COOH or —CH?C(CH3)COOH, and to processes for their preparation, to compositions containing them and to their use in the treatment of various inflammatory and/or allergic diseases, such as diseases such as allergic rhinitis.Type: GrantFiled: December 19, 2006Date of Patent: August 2, 2011Assignee: Glaxo Group LimitedInventors: Simon Teanby Hodgson, Panayiotis Alexandrou Procopiou, Maria Victoria Vinader Brugarolas
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Publication number: 20110178104Abstract: The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.Type: ApplicationFiled: January 5, 2011Publication date: July 21, 2011Applicant: POLYMEDIX INC.Inventors: Richard W. Scott, Dahui Liu, Robert W. Kavash, Trevor Young, Michael J. Costanzo, Carol Ann Mulrooney
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Publication number: 20110178060Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.Type: ApplicationFiled: September 18, 2009Publication date: July 21, 2011Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
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Publication number: 20110171171Abstract: A compound of Formula 1.1A: 1.1A or salt thereof, as well as methods of making compounds of Formula 1.1A, methods of using compounds of Formula 1.1A to treat proliferative disorders such as cancer, and related compounds, composition, and methods.Type: ApplicationFiled: June 26, 2009Publication date: July 14, 2011Applicant: Aegera Therapeutics, Inc.Inventors: Alain Laurent, Melanie Proulx, Yannick Rose, James B. Jaquith, Stephen Morris
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Publication number: 20110129419Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.Type: ApplicationFiled: December 19, 2007Publication date: June 2, 2011Applicants: GE HEALTHCARE LIMITED, HAMMERSMITH IMANET LIMITEDInventors: Anthony Eamon Storey, Julie Davis, Erik Arstad, Benedicte Guilbert, Alessandra Gaeta
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Publication number: 20110118262Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.Type: ApplicationFiled: June 24, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
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Publication number: 20110105474Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; R1 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1 C6 haloalkoxy; R2, R3 are, independently, hydrogen; C1-C6 alkyl; aryl; or taken together with the carbon atoms to which they are bound form a bridged bicyclic ring or a fused heterocycle; X is CH or nitrogen; Y is a bond, oxygen, (CH2)mCR4R5(CH2)n, or (CH2)oNR6(CH2)p; m, n, o, p, R4, R5 and R6 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: June 8, 2009Publication date: May 5, 2011Inventors: Florian Thaler, Mario Varasi, Stefania Gagliardi, Andrea Colombo, Saverio Minucci, Ciro Mercurio
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Publication number: 20110098300Abstract: The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals, useful for the treatment and prevention of diseases or pathological conditions of the central nervous system including mild-cognitive impairments, Alzheimer's disease, learning and; memory disorders, cognitive disorders, attention deficit disorder, attention-deficit hyperactivity disorder, Parkinson's disease, schizophrenia, dementia, depression, epilepsy, seizures, convulsions, sleep/wake and arousal/vigilance disorders such as hypersomnia and narcolepsy, pain and/or obesity.Type: ApplicationFiled: June 2, 2009Publication date: April 28, 2011Applicant: UCB PHARMA, S.A.Inventors: Sylvain Celanire, Laurent Provins, Frederic Denonne, Anne Valade
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Publication number: 20110059154Abstract: Topical cream, ointment, lotion, gel, foam formulations and slow release formulations or devices are provided including certain CCR5 antagonists as prophylactics for the prevention, retardation or inhibition of transmission of Human Immunodeficiency Virus (HIV) infection from one human to another.Type: ApplicationFiled: February 24, 2009Publication date: March 10, 2011Inventor: Julie M. Strizki
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Selected CGRP-antagonists, processes for preparing them and their use as pharmaceutical compositions
Patent number: 7897603Abstract: The present invention relates to the CGRP-antagonists of general formula I wherein R1, R2, R3 and R4 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: June 16, 2009Date of Patent: March 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Marco Santagostino, Fabio Paleari, Henri Doods, Kirsten Arndt, Gerhard Schaenzle -
Publication number: 20110046106Abstract: The present invention relates to compounds of general formula I wherein A, B, R1, R2 and R3 are defined as in claim 1, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: February 5, 2009Publication date: February 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20110014226Abstract: A method to identify small molecules useful as therapeutics and/or vaccines to prevent, alleviate or ameliorate a pathogenic infection or an autoimmune disorder. The method can be used to screen small molecule test compounds for the ability to disrupt particular antigen-antibody interactions of interest. In one embodiment, the antigen is a pathogen-derived antigen and the antibody decreases or inhibits virulence of the pathogen when bound to the antigen (e.g., a neutralizing antibody, antibody with serum bactericidal activity, etc.). In another embodiment, the antigen is a self-antigen (autoantigen) and the antibody is an autoantibody that is known to be associated with a pathological condition (e.g., autoimmune disorder). Compounds that bind to the antigen or antibody disrupt binding can be used as therapeutics to decrease or inhibit the autoimmune disorder.Type: ApplicationFiled: March 17, 2009Publication date: January 20, 2011Inventors: Michael J. Caulfield, Michael D. Miller, Joseph G. Joyce, Paul D. Zuck, Krista L. Getty, Vadim Dudkin, Elizabeth A. Ottinger
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Publication number: 20100324025Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: September 21, 2009Publication date: December 23, 2010Applicant: University of WashingtonInventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
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Publication number: 20100311792Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: September 26, 2008Publication date: December 9, 2010Inventors: Bin Shao, Jiangchao Yao
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Publication number: 20100280005Abstract: Disclosed are compounds of Formula I, wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: November 4, 2010Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, John Gleason, Alexey V. Ishchenko, Brian Lawhorn, Gerard McGeehan, Jaclyn R. Patterson, Simon F. Semus, Robert D. Simpson, Suresh B. Singh, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Wei Zhao
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Publication number: 20100280034Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;Type: ApplicationFiled: December 28, 2007Publication date: November 4, 2010Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20100256126Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: March 11, 2010Publication date: October 7, 2010Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
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Publication number: 20100256359Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.Type: ApplicationFiled: October 6, 2009Publication date: October 7, 2010Inventors: Micheal D. Gaul, Bao-Ping Zhao, Daniel A. Hutta
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Publication number: 20100222387Abstract: The present invention is directed to 3-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.Type: ApplicationFiled: June 21, 2006Publication date: September 2, 2010Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhi-Qiang Yang
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Publication number: 20100210633Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: October 12, 2007Publication date: August 19, 2010Applicant: EPIX Delaware, Inc.Inventors: Jian Lin, Dongli Chen, Steffi Koerner, Rosa E. Melendez, Pradyumma Mohanty, Efrat Ben-Zeev, Merav Fichman, Yael Marantz, Oren Becker, Dilara McCauley, Pini Orbach, Ashis K. Saha, Sharon Shacham, Michael Xie
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Publication number: 20100179118Abstract: The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group and the like, R3 is a hydrogen atom, a C1-6 alkyl group and the like, R4 and R5 are the same or different and each is a hydrogen atom, a halogen atom, a hydroxy group, a C1-6 alkyl group and the like, X is a single bond or —C(R6)(R7)—, R6 and R7 are the same or different and each is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group and the like, or R6 and R7 optionally form, together with the carbon atom bonded thereto, an optionally substituted C3-8 cycloalkyl group and the like, ring group A is an azetidin-1-yl group and the like, m is 0, 1 or 2, and n is 0, 1 or 2.Type: ApplicationFiled: September 7, 2007Publication date: July 15, 2010Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Michinori Ozawa, Tomoya Shiro, Takaaki Sumiyoshi, Mari Itoh
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Patent number: 7754737Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: GrantFiled: October 7, 2005Date of Patent: July 13, 2010Assignee: Vitae Pharmaceuticals, Inc.Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Patent number: 7750156Abstract: The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity.Type: GrantFiled: March 25, 2005Date of Patent: July 6, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Kiyokawa, Shinji Aki
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Publication number: 20100168103Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of diaryl piperidine compounds are disclosed of the general formula (I) where X is a linker and Y may be C, O, S or N.Type: ApplicationFiled: September 14, 2007Publication date: July 1, 2010Applicant: NEUROMED PHARMACEUTICALS LTD.Inventors: Hassan Pajouhesh, Yanbing Ding, Hossein Pajouhesh, Richard Holland, Gabriel Hum
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Publication number: 20100160306Abstract: Certain novel 4 alkyl substituted N acylated piperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: ApplicationFiled: September 26, 2006Publication date: June 24, 2010Inventors: Raman K. Bakshi, Qingmei Hong, Ravi P. Nargund
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Publication number: 20100130471Abstract: Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiamo Ghirlanda, Xiaoping Hou, Alexey V. Ishebenko, Lara S. Kallander, Beth A. Knapp-Reed, Brian Lawhorn, Qing Lu, Gerard McGeehan, Simon Semus, Robert D. Simpson, Suresh B. Singh, Lamont R. Terrell, Colin Tice, Tritin Tran, Zhenrong Xu, Jing Yuan, Jing Zhang, Wei Zhao
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Publication number: 20100075987Abstract: Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: December 10, 2007Publication date: March 25, 2010Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang, Ralph T. Mosley
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Publication number: 20100075986Abstract: The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.Type: ApplicationFiled: November 30, 2009Publication date: March 25, 2010Applicant: SANOFI-AVENTISInventors: Philippe R. BOVY, Roberto CECCHI, Tiziano CROCI, Olivier VENIER
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Publication number: 20100063081Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: June 29, 2006Publication date: March 11, 2010Inventor: Stuart Edward Bradly
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Patent number: 7662964Abstract: The present invention is related to a process for the preparation of [1,4?]bipiperidinyl-1?-carbonyl chloride or its hydrochloride using methylene chloride as a solvent in the reaction of 4-piperidinopiperidine with phosgene and the removing the reaction solvent by using an additional distillation solvent to raise the distillation temperature.Type: GrantFiled: February 6, 2006Date of Patent: February 16, 2010Assignee: Fermion OyInventor: Ilpo Laitinen
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Publication number: 20100016288Abstract: Compounds with ?7 nicotinic acetylcholine receptor (?7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.Type: ApplicationFiled: July 15, 2008Publication date: January 21, 2010Inventors: Hendrick BOTHMANN, Renza Roncarati, Jolanda Micco, Arianna Nencini, Chiara Ghiron
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SELECTED CGRP ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS
Publication number: 20100004228Abstract: The present invention relates to the CGRP antagonists of general formula I wherein R1, R2, R3 and R4 are as defined in claim 1, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates thereof, the mixtures thereof and the salts thereof and the hydrates of the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, as well as those compounds of general formula I wherein one or more hydrogen atoms are replaced by deuterium, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: ApplicationFiled: June 17, 2009Publication date: January 7, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Georg MUELLER, Klaus RUDOLF, Philipp LUSTENBERGER, Gerhard SCHAENZLE, Marco SANTAGOSTINO, Dirk STENKAMP, Kirsten ARNDT, Henri DOODS -
Patent number: 7635700Abstract: Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: September 26, 2007Date of Patent: December 22, 2009Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Publication number: 20090306042Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 10, 2008Publication date: December 10, 2009Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
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Patent number: 7612101Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.Type: GrantFiled: April 24, 2006Date of Patent: November 3, 2009Assignee: Allergan, Inc.Inventors: June Chen, Simon Pettit, Hans Fliri
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Patent number: 7608617Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: GrantFiled: June 22, 2007Date of Patent: October 27, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Silvia Gatti McArthur, Cornelia Hertel, Matthias Heinrich Nettekoven, Jean-Marc Plancher, Susanne Raab, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Franz Schuler
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Patent number: 7608629Abstract: The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.Type: GrantFiled: April 14, 2004Date of Patent: October 27, 2009Assignee: Eli Lilly and CompanyInventors: Maria-Jesus Blanco-Pillado, Dana Rae Benesh, Sandra Ann Filla, Kevin John Hudziak, Brian Michael Mathes, Daniel Timothy Kohlman, Bai-Ping Ying, Deyi Zhang, Yao-Chang Xu