The Spiro Includes The Six-membered Hetero Ring Patents (Class 546/16)
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Publication number: 20120071459Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.Type: ApplicationFiled: June 2, 2010Publication date: March 22, 2012Inventors: Siegfried Benjamin Christensen, IV, Donghui Qin, Shuhul Chen, Shi Lu
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Patent number: 8138357Abstract: Therefore the present invention relates specifically to the compounds of general formula (I), in which R1 and R2, which may be identical or different, are selected from the group comprising H, —CnH2n-1, a linear or branched alkyl group having from 1 to 6 carbon atoms, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is selected from —CO—CH3, —NHOH, —OH, —OR6 in which R6 is a linear or branched alkyl group having from 1 to 6 carbon atoms; R4 is selected from H, a linear or branched alkyl group having from 1 to 6 carbon atoms, phenyl, benzyl, —CF3 or —CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O. and use thereof in the medical field.Type: GrantFiled: July 24, 2006Date of Patent: March 20, 2012Assignee: Giuliani International LimitedInventors: Giancarlo Naccari, Sergio Baroni
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Patent number: 8138197Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nType: GrantFiled: January 8, 2008Date of Patent: March 20, 2012Assignees: MSD K.K., Merck Sharp & Dohme Corp.Inventors: Tomoharu Iino, Hideki Jona, Hideki Kurihara, Masayuki Nakamura, Kenji Niiyama, Jun Shibata, Tadashi Shimamura, Hitomi Watanabe, Takeru Yamakawa, Lihu Yang
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Patent number: 8138206Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.Type: GrantFiled: May 29, 2006Date of Patent: March 20, 2012Assignee: MSD. K.K.Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
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Patent number: 8129529Abstract: Novel energy transfer dyes which can be used with shorter wavelength light sources are provided. These dyes include a donor dye with an absorption maxima at a wavelength between about 250 to 450 nm and an acceptor dye which is capable of absorbing energy emitted from the donor dye. One of the energy transfer dyes has a donor dye which is a member of a class of dyes having a coumarin or pyrene ring structure and an acceptor dye which is capable of absorbing energy emitted from the donor dye, wherein the donor dye has an absorption maxima between about 250 and 450 nm and the acceptor dye has an emission maxima at a wavelength greater than about 500 nm.Type: GrantFiled: December 2, 2010Date of Patent: March 6, 2012Assignee: Applied Biosystems, LLCInventor: Linda G. Lee
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Patent number: 8119805Abstract: Substituted disulfonamide compounds corresponding to formula I: In which R1, R2, R3, R4a, R4b, R5a, R5b, R8, R9a, R9b, R10, R11, a, b, s, t and A have defined meanings, pharmaceutical compositions containing one or more such compounds, processes for preparing such compounds, and a method of using such compounds for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin receptor 1 (BR1).Type: GrantFiled: November 6, 2009Date of Patent: February 21, 2012Assignee: Gruenenthal GmbHInventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Sabine Hees, Tieno Germann, Michael Franz-Martin Engels
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Publication number: 20120041013Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) for the treatment of diabetes, metabolic syndrome and obesity.Type: ApplicationFiled: August 8, 2011Publication date: February 16, 2012Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Publication number: 20120041012Abstract: Substituted spirocyclic amines of structural formula I are selective antagonists of the somatostatin sub-type receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.Type: ApplicationFiled: May 6, 2010Publication date: February 16, 2012Inventors: Susan D. Aster, Joseph L. Duffy, Gui-Bai Liang, Patrick Shao, Feng Ye
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Publication number: 20120040959Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicant: Achillion Pharmaceuticals, Inc.Inventors: Barton James Bradbury, Jason Allan Wiles, Qiuping Wang, Akhiro Hashimoto, Edlaine Lucien, Godwin Clarence Gilroy Pais, Milind Deshpande, Michael John Pucci, Ha Young Kim
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Publication number: 20120035201Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1 are useful as pesticides.Type: ApplicationFiled: March 30, 2010Publication date: February 9, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Michel Muehlebach, Ottmar Franz Hueter
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Patent number: 8110581Abstract: 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: October 16, 2008Date of Patent: February 7, 2012Assignee: Incyte CorporationInventors: Wenqing Yao, Chunhong He, David M. Burns, Jincong Zhuo, Meizhong Xu, Colin Zhang, Ding-Quan Qian, Brian Metcalf
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Patent number: 8110684Abstract: A method of combating and controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I) wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; and R1, R3, R2 and R8 are defined organic, groups, p is 0, 1, 2, 3 or 4 or salts or N-oxides thereof; novel compounds and composition's containing them are also provided.Type: GrantFiled: January 19, 2007Date of Patent: February 7, 2012Assignee: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Jerome Cassayre, Louis-Pierre Molleyres, Peter Maienfisch
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Publication number: 20120015970Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: July 12, 2011Publication date: January 19, 2012Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Publication number: 20120015933Abstract: The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.Type: ApplicationFiled: September 29, 2011Publication date: January 19, 2012Applicant: SANOFI-AVENTISInventors: Manfred SCHUDOK, Michael WAGNER, Armin BAUER, Anna KOHLMANN
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Patent number: 8097634Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and A are as described herein, compositions including the compounds and methods of using the compounds. The compounds inhibit hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, and obesity.Type: GrantFiled: April 8, 2011Date of Patent: January 17, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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Publication number: 20120010193Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.Type: ApplicationFiled: March 8, 2010Publication date: January 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
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Publication number: 20120010186Abstract: Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: March 18, 2010Publication date: January 12, 2012Applicant: MERCK FROSST CANADA LTD.Inventors: Nicolas Lachance, Serge Leger, Renata M. Oballa, David Powell, Geoffrey K. Tranmer, Evelyn Martins, Yves Gareau
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Publication number: 20120010228Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.Type: ApplicationFiled: June 17, 2011Publication date: January 12, 2012Inventors: Gary W. Luehr, Arathi Sundaram, Priyadarshini Jaishankar, Philip W. Payne, Pascal Druzgala
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Publication number: 20120004196Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: May 4, 2011Publication date: January 5, 2012Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Patent number: 8088368Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: May 12, 2010Date of Patent: January 3, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Scott E. Lazerwith, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, William J. Watkins, Lianhong Xu
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Publication number: 20110319381Abstract: The invention relates to a compound of the general formula (I) in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, NR8R9 group; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl group or a trifluoromethyl group; R4 is an optionally substituted 5-member heterocyclic compound; the compound being in the form of a base or acid addition salt. The invention also relates to the therapeutic use thereof.Type: ApplicationFiled: February 4, 2010Publication date: December 29, 2011Applicant: SANOFIInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Publication number: 20110312939Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20110306604Abstract: Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 receptors are involved.Type: ApplicationFiled: August 14, 2009Publication date: December 15, 2011Inventors: Michael R. Wood, Ian M. Bell, June J. Kim, Harold G. Selnick, Craig A. Stump
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Publication number: 20110301031Abstract: A compound of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: December 9, 2009Publication date: December 8, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Michel Muehlebach, Thomas Pitterna, Jérôme Yves Cassayre, Andrew Edmunds, Camilla Corsi, Myriem El Qacemi, Roger Graham Hall, André Jeanguenat, André Stoller, Christopher Richard Ayles Godfrey, Jürgen Harry Schaetzer, Olivier Loiseleur, Peter Maienfisch, Neil Brian Carter
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Publication number: 20110294785Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.Type: ApplicationFiled: August 21, 2009Publication date: December 1, 2011Applicant: The Trustees of the University of PennsylvaniaInventors: William F. DeGrado, Jun Wang
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Publication number: 20110294777Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.Type: ApplicationFiled: January 15, 2009Publication date: December 1, 2011Inventors: Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Sookhee Ha, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, Michael Shevlin
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Publication number: 20110288111Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.Type: ApplicationFiled: August 21, 2009Publication date: November 24, 2011Applicant: The Trustees of the University of PennsylvaniaInventors: William F. DeGrado, Jun Wang
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Publication number: 20110288068Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.Type: ApplicationFiled: July 18, 2011Publication date: November 24, 2011Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
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Patent number: 8063042Abstract: The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y, R3, R4, R5, R6, R7, R8, R9, R10, m and n are as herein defined, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.Type: GrantFiled: July 10, 2008Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin
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Publication number: 20110281903Abstract: There are disclosed bicyclic heterocyclic spiro compounds; pharmaceutical compositions comprising these compounds; and methods for the treatment in a mammal of diseases and conditions which are susceptible to modulation of the M1 muscarinic receptor, including Alzheimer's disease, insulin resistance syndrome and type 2 diabetes. Other embodiments are also disclosed.Type: ApplicationFiled: January 26, 2010Publication date: November 17, 2011Inventors: Abraham Fisher, Nira Bar-Ner, Victoria Nachum
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Publication number: 20110275595Abstract: The present invention relates to compounds defined by formula I wherein the groups R1, Y1 to Y4, V, W, and X are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: October 22, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
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Patent number: 8049012Abstract: This invention relates to novel 3-aza-spiro[5.5]undecane 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: GrantFiled: June 28, 2006Date of Patent: November 1, 2011Assignee: Neurosearch A/SInventors: Birgitte L. Eriksen, Dan Peters, Elsebet Ostergaard Nielsen, John Paul Redrobe
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Publication number: 20110257212Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and A are as described herein, compositions including the compounds and methods of using the compounds. The compounds inhibit hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, and obesity.Type: ApplicationFiled: April 8, 2011Publication date: October 20, 2011Inventors: Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
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SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF
Publication number: 20110257213Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor are disclosed.Type: ApplicationFiled: June 2, 2011Publication date: October 20, 2011Applicant: SANOFIInventors: Zhongli GAO, Daniel HALL, Ryan HARTUNG -
Patent number: 8039480Abstract: The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.Type: GrantFiled: November 25, 2008Date of Patent: October 18, 2011Assignee: Sanofi-AventisInventors: Manfred Schudok, Michael Wagner, Armin Bauer, Anna Kohlmann
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Publication number: 20110251225Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.Type: ApplicationFiled: June 2, 2011Publication date: October 13, 2011Applicant: SANOFIInventors: Zhongli GAO, Ryan HARTUNG, David STEFANY
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Publication number: 20110245240Abstract: Compounds of Formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, A8, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y and Z are as described herein) useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 receptors are involved.Type: ApplicationFiled: September 30, 2009Publication date: October 6, 2011Inventors: Donnette D. Staas, Ian M. Bell, Michael R. Wood
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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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Patent number: 8026365Abstract: This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: April 29, 2008Date of Patent: September 27, 2011Assignee: Hoffman-La Roche Inc.Inventors: Andreas Christ, Rainer Martin, Peter Mohr
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Publication number: 20110230493Abstract: Provided herein are 1-oxa-8-azaspiro[4.5]decane-8-carboxamide compounds of formula I wherein Ar1, Ar2, R1, R2, R3 and R4 are as defined herein and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.Type: ApplicationFiled: November 9, 2009Publication date: September 22, 2011Inventors: Scott Allen Long, Marvin Jay Meyers, Matthew James Pelc, Barbara Ann Schweitzer, Lijuan Jane Wang, Atli Thorarensen
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Publication number: 20110230419Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, that bind to Inhibitor of Apoptosis Proteins (IAPs). The compounds of the invention may be used as diagnostic and therapeutic agents in the treatment of proliferative diseases, such as cancer, for promoting apoptosis in proliferating cells, and for sensitizing cells to inducers of apoptosis. The present invention furthermore provides a polymeric compound of formulas (VI) or (VII), comprising either at least two monomeric units of compounds of formula (I), or at least one monomeric unit of a compound of formula (I) and an entity E. The present invention further relates to pharmaceutical compositions comprising said compounds of formulas (I), (VI), and (VII) and the use of said compounds in medicine.Type: ApplicationFiled: June 16, 2009Publication date: September 22, 2011Applicant: Nuevolution A/SInventors: Mikkel Dybro Lundorf, Kim Birkebaek Jenson, Sanne Schrøder Glad, Alek Haahr Gouliaev, Anette Holtmann, Michael Anders Godskesen
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Publication number: 20110230351Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the spiroheterocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular spiroheterocyclically substituted tetramic acid derivatives through the addition of ammonium or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or acaricides and/or fungicides and/or for preventing unwanted vegetation.Type: ApplicationFiled: February 10, 2011Publication date: September 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Arnd Voerste, Isolde Häuser-Hahn, Stefan Lehr, Elmar Gatzweiler, Ulrich Görgens, Ines Heinemann
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Publication number: 20110230461Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.Type: ApplicationFiled: March 16, 2011Publication date: September 22, 2011Inventors: Samit K. Bhattacharya, Kimberly O. Cameron, Dilinie P. Fernando, Kim F. McClure, Daniel W. Kung, Allyn T. Londregan, Suvi T. M. Simila
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Publication number: 20110230660Abstract: The present invention relates to a method comprising the step of contacting a protected N,N-bis(2-X-ethyl)amine with a (2-fluorophenyl)acetonitrile in the presence of a water-soluble phase transfer reagent, concentrated aqueous base, and an immiscible organic solvent, and under such conditions to form a 4-(2-fluorophenyl)-4-piperidinecarbonitrile in at least a 70% yield, wherein X is a leaving group. The 4-(2-fluorophenyl)-4-piperidinecarbonitrile is useful in preparing spiroindolines, which can be used as precursors of compounds that are modulators of CCR2 receptor.Type: ApplicationFiled: December 3, 2009Publication date: September 22, 2011Inventors: Stacie Calad, Brian Daniel Doan
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Publication number: 20110224137Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).Type: ApplicationFiled: November 17, 2009Publication date: September 15, 2011Inventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Publication number: 20110224230Abstract: Compounds of formula (I): wherein variables B, G1, G2, G3, G4, Ea, Eb, Ec, A1, A2, A3, A4, R6 and 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: September 10, 2009Publication date: September 15, 2011Inventor: Craig A. Stump
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Publication number: 20110224231Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: November 12, 2009Publication date: September 15, 2011Applicant: Pfizer Inc.Inventors: Michael A. Brodney, Ivan V. Efremov, Christopher J. Helal, Brian T. O'Neill
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Publication number: 20110224187Abstract: The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: October 14, 2009Publication date: September 15, 2011Inventors: Anandan Palani, Michael Y. Berlin, Aslanian G. Robert, Vaccaro M. Henry, Chan Tin-Yau, Xiao Dong, Degrado Sylvia, Rao U. Ashwin, Chen Xiao, Lee Yoon Joo, Sofolarides J. Michael, Shao Ning, Huang R. Ying, Liu Zhidan, Wang Li Yuan, Pu Haiyan
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Publication number: 20110207699Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 9, 2010Publication date: August 25, 2011Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd N. Soltwedel, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Clarence J. Maring, Michael D. Tufano, David A. Betebenner, Todd W. Rockway, Dachun Liu, John K. Pratt, Michael J. Lavin, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Publication number: 20110207730Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.Type: ApplicationFiled: December 16, 2010Publication date: August 25, 2011Applicant: Cardiome Pharma Corp.Inventors: Allen I. Bain, Gregory N. Beatch, Cindy J. Longley, Bertrand M.C. Plouvier, Tao Sheng, Michael J.A. Walker, Richard A. Wall, Sandro L. Yong, Jeff Jiqun Zhu, Alexander B. Zolotoy