The Polycyclo Ring System Is Bicyclo-carbocyclic Patents (Class 546/205)
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Publication number: 20120088746Abstract: Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: May 10, 2007Publication date: April 12, 2012Applicants: PFIZER INC., RENOVIS, INC.Inventors: Yuji Shishido, Kazunari Nakao, Satoshi Nagayama, Hirotaka Tanaka, Matthew Alexander James Duncton, Matthew Cox, John Kincaid, Kiran Sahasrabudhe, Maria de Los Angeles Estiarte-Martinez
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Patent number: 8153658Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: GrantFiled: November 14, 2007Date of Patent: April 10, 2012Assignee: Astellas Pharma, Inc.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
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Patent number: 8152861Abstract: The present invention relates to a) a non-oxidative coloring agent for keratin fibers, in particular human hair, comprising at least one dye according to formula (I) or (II), b) an oxidative coloring agent for keratin fibers, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide), at least one oxidative dye precursor and at least one dye according to formula (I) or (II), and c) a lightening agent for keratin fibers, in particular human hair, which comprises at least one oxidizing agent (e.g. hydrogen peroxide) and at least one dye according to formula (I) or (II), with R4 being a cationic group.Type: GrantFiled: June 3, 2011Date of Patent: April 10, 2012Assignee: The Procter & Gamble CompanyInventors: Markus Speckbacher, Jessica Chassot, Hans-Jürgen Braun
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Patent number: 8148422Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: December 15, 2009Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, James J. McNally
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Patent number: 8124783Abstract: Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates.Type: GrantFiled: December 30, 2004Date of Patent: February 28, 2012Assignee: Jubilant Organosys LimitedInventors: Shailendra Kumar Dubey, Amit Kumar Sharma, Beena S. Rani, Soumendu Paul, Rajesh Kumar Thaper, Dubey Sushil Kumar, Jag Mohan Khanna
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Publication number: 20120041001Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: Janssen Pharmaceutica, NVInventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
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Patent number: 8114880Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives 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 atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: GrantFiled: October 22, 2007Date of Patent: February 14, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Joannes Theodorus Maria Linders, Libuse Jaroskova, Marcel Viellevoye, Leo Jacobus Jozef Backx, Didier Jean-Claude Berthelot, Guuske Frederike Busscher
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Publication number: 20120022039Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.Type: ApplicationFiled: February 12, 2010Publication date: January 26, 2012Applicant: SANOFIInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
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Publication number: 20120015943Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmacuticals, Inc.Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
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Publication number: 20120015942Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20110319416Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-E, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.Type: ApplicationFiled: January 28, 2010Publication date: December 29, 2011Applicant: EMORY UNIVERSITYInventors: Stephen F. Traynelis, Dennis C. Liotta, Cara Mosley, Timothy M. Acker, Sommer Zimmerman
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Publication number: 20110311466Abstract: 4-(azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.Type: ApplicationFiled: December 2, 2009Publication date: December 22, 2011Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Jean-Guy Boiteau, Karine Bouquet, Sandrine Talano, Corinne Millois Barbuis
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Publication number: 20110301197Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X, Y and Q are each as defined in the description, and agrochemically active salts thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: May 16, 2011Publication date: December 8, 2011Applicant: Bayer CropScience AGInventors: Pierre CRISTAU, Sebastian HOFFMANN, Joachim KLUTH, Thomas SEITZ, Tomoki TSUCHIYA, Pierre WASNAIRE, Jürgen BENTING, Ulrike WACHENDORFF-NEUMANN
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Patent number: 8063070Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.Type: GrantFiled: May 4, 2010Date of Patent: November 22, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Publication number: 20110275670Abstract: The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: June 4, 2009Publication date: November 10, 2011Inventors: Emma Chapman, Michael Higginbottom, Anne Viet-Anh Horgan (nee Nguyen), Iain Simpson
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Publication number: 20110269747Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: ApplicationFiled: July 13, 2011Publication date: November 3, 2011Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Patent number: 8044048Abstract: Derivatives of sulindac are provided along with pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: GrantFiled: January 4, 2007Date of Patent: October 25, 2011Assignee: Southern Research InstituteInventors: Gary Piazza, Robert Reynolds
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Publication number: 20110237553Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: March 16, 2011Publication date: September 29, 2011Applicant: ABBOTT LABORATORIESInventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
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Publication number: 20110218217Abstract: This invention relates to novel piperidine-4-propionamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: August 25, 2009Publication date: September 8, 2011Applicant: NEUROSEARCH A/SInventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
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Patent number: 7994328Abstract: The present invention relates to an improved process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride of Formula I.Type: GrantFiled: February 8, 2007Date of Patent: August 9, 2011Assignee: Aurobindo Pharma Ltd.Inventors: Mahesh Nagarimadugu, Arun Kumar Gupta, Ramesh Dandala, Sivakumaran Meenakshisunderam
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Publication number: 20110178096Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.Type: ApplicationFiled: March 29, 2011Publication date: July 21, 2011Applicant: ABBOTT LABORATORIESInventors: Dawn M. George, Lu X. Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
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Publication number: 20110172202Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.Type: ApplicationFiled: November 15, 2010Publication date: July 14, 2011Inventors: Esther Martinborough, Marcus F. Boehm, Adam Richard Yeager, Junko Tamiya, Liming Huang, Enugurthi Brahmachary, Manisha Moorjani, Gregg Alan Timony, Jennifer L. Brooks, Robert Peach, Fiona Lorraine Scott, Michael Allen Hanson
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Patent number: 7977339Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.Type: GrantFiled: August 3, 2010Date of Patent: July 12, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20110152290Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, 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: ApplicationFiled: November 4, 2010Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK -
Publication number: 20110144108Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: ApplicationFiled: January 17, 2011Publication date: June 16, 2011Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec
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Patent number: 7960369Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.Type: GrantFiled: November 6, 2003Date of Patent: June 14, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Kohji Fukatsu, Shinobu Sasaki, Shuji Hinuma, Yasuaki Ito, Nobuhiro Suzuki, Masataka Harada, Tsuneo Yasuma
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Patent number: 7960412Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; ??(I-1) formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R? represents 1 to 4 independent hydrogen atoms and the like; and R? represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.Type: GrantFiled: August 20, 2009Date of Patent: June 14, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Shinichi Hamaoka, Noritaka Kitazawa, Kazumasa Nara, Atsushi Sasaki, Atsushi Kamada, Tadashi Okabe
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Publication number: 20110086880Abstract: This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: December 16, 2010Publication date: April 14, 2011Inventors: Dan PETERS, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Jørgen Scheel-Krüger, Birgitte L. Eriksen
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Patent number: 7902191Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.Type: GrantFiled: February 22, 2005Date of Patent: March 8, 2011Assignee: Eli Lilly and CompanyInventors: Lisa Selsam Beavers, Robert Alan Gadski, Philip Arthur Hipskind, Cynthia Darshini Jesudason, Karen Lynn Lobb, Richard Todd Pickard, Craig William Lindsley
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Publication number: 20110053980Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: July 4, 2008Publication date: March 3, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover
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Publication number: 20110046179Abstract: This invention relates to novel piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: August 29, 2007Publication date: February 24, 2011Inventors: Birgitte L. Eriksen, Dan Peters, Bjarne H. Dahl, Elsebet Østergaard Nielsen, John Paul Redrobe
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Publication number: 20110039888Abstract: The present invention relates, generally, to asymmetric ?-functionalization and to asymmetric ?,?-bisfunctionalization of ketones and aldehydes and, in particular, to chiral auxiliaries suitable for use in effecting such functionalizations and to methods of using same.Type: ApplicationFiled: April 21, 2009Publication date: February 17, 2011Inventors: Don M. Coltart, Daniel Lim
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Publication number: 20110028515Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.Type: ApplicationFiled: July 23, 2010Publication date: February 3, 2011Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
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Patent number: 7879881Abstract: The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.Type: GrantFiled: August 30, 2007Date of Patent: February 1, 2011Assignee: Janssen Pharmaceutica NVInventors: Bart De Corte, William A. Kinney, Bruce E. Maryanoff, Shyamali Ghosh, Li Liu
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Patent number: 7880007Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: November 29, 2005Date of Patent: February 1, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dennis J. Hurley, Daniele M. Bergeron, Ioana Drutu, Miguel Garcia-Guzman Blanco, Lewis R. Makings, Akiko Nakatani, Gabriel Raffai, Alina Silina
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Patent number: 7858629Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.Type: GrantFiled: April 10, 2007Date of Patent: December 28, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
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Publication number: 20100286152Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof,Type: ApplicationFiled: June 5, 2008Publication date: November 11, 2010Applicant: Glaxo Group LimitedInventors: Giovanni Bernasconi, Steven Mark Bromidge, Andrew James Carpenter, Lucilla D'Adamo, Romano Di Fabio, Sebastien Guery, Francesca Pavone, Alfonso Pozzan, Marilisa Rinaldi, Fabio Maria Sabbatini, Yves St-Denis
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Publication number: 20100256144Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: ApplicationFiled: June 26, 2008Publication date: October 7, 2010Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Adreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Publication number: 20100240679Abstract: Compounds of the present invention having the formula exhibit inhibitory activity on the natural enzyme renin. Thus, compounds of formula (I) may be employed for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: May 28, 2010Publication date: September 23, 2010Inventors: Richard Sedrani, Juergen Klaus Maibaum, Werner Breitenstein, Holger Sellner, Claus Ehrhardt, Nils Ostermann
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Patent number: 7799824Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.Type: GrantFiled: June 22, 2005Date of Patent: September 21, 2010Assignee: OraPharma, Inc.Inventors: Bharat Lagu, Michael Wachter
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Publication number: 20100234424Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.Type: ApplicationFiled: May 20, 2010Publication date: September 16, 2010Applicant: SANOFI-AVENTISInventors: Gihad DARGAZANLI, Genevieve ESTENNE-BOUHTOU, Pascale MAGAT
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Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-2-yl]methylpiperidine and hydrochloride
Patent number: 7795438Abstract: Processes for preparing 1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-yl]methylpiperidine (donepezil), which is useful as an intermediate for medicines, and for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride (donepezil hydrochloride), which is useful as a medicine. The process for donepezil hydrochloride production comprises catalytically hydrogenating the compound represented by the structural formula (III) [1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-ylidene]methylpiperidine] with a Raney nickel catalyst under mild conditions and subsequently treating it with hydrochloric acid. Thus, impurities are further diminished. The operations are simple and the process is suitable for industrial production.Type: GrantFiled: April 27, 2005Date of Patent: September 14, 2010Assignee: Eisai R&D Management Co., LtdInventors: Akio Imai, Hiroshi Nishimura -
Patent number: 7795265Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.Type: GrantFiled: April 10, 2007Date of Patent: September 14, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
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Patent number: 7790753Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.Type: GrantFiled: April 17, 2006Date of Patent: September 7, 2010Assignee: sanofi-aventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Corinne Veronique
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Patent number: 7790750Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(?O)—R9, or -Alk-Y—C(?O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each indepenType: GrantFiled: October 20, 2006Date of Patent: September 7, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul René Marie André Bosmans, Michel Anna Jozef De Cleyn, Michel Surkyn
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Patent number: 7772251Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.Type: GrantFiled: May 17, 2004Date of Patent: August 10, 2010Assignee: The Medicines Company (Leipzig) GmbHInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
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Patent number: 7772399Abstract: The present invention provides a novel process for the preparation of amorphous form of donepezil hydrochloride.Type: GrantFiled: April 2, 2003Date of Patent: August 10, 2010Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Attunuri Narasa Reddy
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Publication number: 20100197662Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.Type: ApplicationFiled: June 6, 2006Publication date: August 5, 2010Applicant: Shionogi & Co., Ltd.Inventors: Tomoyuki Ogawa, Noriyuki Kurose, Satoru Tanaka, Koichi Nishi
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Patent number: RE42412Abstract: The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.Type: GrantFiled: December 21, 2007Date of Patent: May 31, 2011Assignee: ARYx Therapeutics, Inc.Inventors: Pascal Druzgala, Peter G. Milner, Jurg Pfister, Cyrus Becker