Spiro Patents (Class 546/15)
  • Patent number: 8207184
    Abstract: A condensation compound of a fluorinated cyclopentane ring and an aromatic ring, which is useful, for example, for electronic materials, and a process for producing the same are provided. For instance, according to Scheme 1 below, a compound (68) containing a condensed structure formed of a hexafluorocyclopentane ring and an aromatic ring is synthesized. The aromatic ring is not limited to a thiophene ring but can be any ring and any substituent can be used. Thus a compound containing a condensed ring structure formed of a hexafluorocyclopentane ring and an aromatic ring, particularly, for instance, a thiophene ring, which was impossible to produce conventionally, can be produced easily with high yield. The compound of the present invention is particularly suitable to be applied to, for example, electronic materials or semiconductors.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: June 26, 2012
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Yutaka Ie, Yoshio Aso
  • Publication number: 20120157448
    Abstract: The invention provides novel tricyclic compounds of Formula I? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
    Type: Application
    Filed: November 22, 2011
    Publication date: June 21, 2012
    Inventors: Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Andrew T. Metcalf, Brad Newhouse, Tony P. Tang, Allen A. Thomas, Michael Siu, Malcolm Huestis, Matthew Volgraf
  • Publication number: 20120149698
    Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: November 21, 2008
    Publication date: June 14, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
  • Publication number: 20120149703
    Abstract: A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].
    Type: Application
    Filed: February 15, 2012
    Publication date: June 14, 2012
    Inventors: Makoto Jitsuoka, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20120145974
    Abstract: A chromene compound which contains a skeleton represented by the following formula (1) and has high color optical density at the time of exposure, double peak characteristic, little initial coloration, a practical fading speed and durability. (wherein R1 is an electron donor group having a Hammett constant of less than 0, the ring including X is a hetero ring formed together with the 7-position and 8-position carbon atoms, and X is an oxygen atom, sulfur atom or group represented by ?NR2 directly bonded to the 7-position carbon atom.
    Type: Application
    Filed: June 22, 2010
    Publication date: June 14, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka, Kazuhiro Teranishi
  • Publication number: 20120149686
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Application
    Filed: April 6, 2010
    Publication date: June 14, 2012
    Applicant: University Health Networks
    Inventors: Peter B. Sampson, Yong liu, Sze-Wan Le, Brian T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
  • Patent number: 8198290
    Abstract: The present invention provides for compounds of Formula I and II: wherein y, X, Y, Z, R1, and R2 have any of the values defined there for in the specification. The compounds of formula I are useful as reagents in the isolation and the assay of PQQ dependent enzymes. Also provided are compositions comprising compounds of Formula I and II.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: June 12, 2012
    Assignee: Berry and Associates, Inc.
    Inventor: John C. Hodges
  • Publication number: 20120129846
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 5, 2009
    Publication date: May 24, 2012
    Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
  • Publication number: 20120122899
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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: Application
    Filed: November 10, 2011
    Publication date: May 17, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Heather E. Stevenson, Cheng Wang, C. Blair Zartman
  • Publication number: 20120121651
    Abstract: Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, and prodrugs thereof, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
    Type: Application
    Filed: January 26, 2012
    Publication date: May 17, 2012
    Inventors: David S. Hays, Michael E. Danielson, John F. Gerster, Shri Niwas, Ryan B. Prince, Tushar A. Kshirsagar, Philip D. Heppner, William H. Moser, Joan T. Moseman, Matthew R. Radmer, Maureen A. Kavanagh, Sarah A. Strong, Jason D. Bonk
  • Publication number: 20120122900
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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: Application
    Filed: November 10, 2011
    Publication date: May 17, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
  • Publication number: 20120122911
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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: Application
    Filed: November 10, 2011
    Publication date: May 17, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley
  • Publication number: 20120122136
    Abstract: Provided is a compound comprising the structure: (SIG)-(SI-MOD)m. In this compound, SIG is a signaling molecule, SI is a self-immolative structure bound to SIG such that SIG has a reduced signal relative to the signal of SIG without SI, MOD is a moiety bound to SI that is subject to modification by an activator, and m is an integer from 1 to about 10. With this compound, when MOD is modified by an activator, SI is destabilized and self-cleaved from SIG such that SIG generates an increased signal. Also provided is a method of determining whether a sample comprises an activator, using the above-described compound. Additionally provided is a method of determining whether a cell comprises a nitroreductase using the above-described compound where nitroreductase is the activator. Further provided is a method of determining whether a mammalian cell is hypoxic using the above-described compound where nitroreductase is the activator.
    Type: Application
    Filed: November 16, 2010
    Publication date: May 17, 2012
    Applicant: ENZO LIFE SCIENCES, INC., C/O ENZO BIOCHEM, INC.
    Inventors: Maciej Szczepanik, Irina V. Lebedeva, Yuejun Xiang, Praveen Pande, Wayne Forrest Patton
  • Publication number: 20120121934
    Abstract: A photochromic chromene compound which develops a color of a neutral tint, has high color optical density, a high fading speed and high durability, and has an indeno(2,1-f)naphtho(1,2-b)pyran structure represented by the following formula as the basic skeleton, wherein a sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group is bonded to the 6-position and/or 7-position carbon atom(s).
    Type: Application
    Filed: August 4, 2010
    Publication date: May 17, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi
  • Publication number: 20120115841
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Application
    Filed: May 17, 2010
    Publication date: May 10, 2012
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20120115882
    Abstract: A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: July 15, 2010
    Publication date: May 10, 2012
    Inventors: Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20120115895
    Abstract: The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases. The compounds according to Formula (I) are suitable as modulators of CRTH2. The invention provides Spiro derivatives according to Formula (I) and related formulae that are useful in the treatment and/or prevention of diseases selected from allergic diseases such as allergic asthma, allergic rhinitis, allergic conjunctivitis, and inflammatory dermatoses such as atopic dermatitis, contact hypersensitivity, allergic contact dermatitis, chronic urticaria/chronic idiopathic/autoimmune urticaria, drag-induced exanthems (e.g., toxic epidermal necrolysis or Lyell's syndrome/Stevens-Johnson syndrome/drug hypersensitivity syndrome), photodermatosis or polymorphous light emption (e.g.
    Type: Application
    Filed: July 14, 2010
    Publication date: May 10, 2012
    Applicant: Merck Serono S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Tania Grippi-Vallotton
  • Patent number: 8173810
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: May 8, 2012
    Assignee: Amgen Inc.
    Inventors: Wenge Zhong, Stephen Hitchcock, Vinod F. Patel, Michael Croghan, Thomas Dineen, Daniel Horne, Matthew Kaller, Charles Kreiman, Patricia Lopez, Holger Monenschein, Thomas Nguyen, Lewis Pennington, Qiufen Xue, Bryant Yang, Yuan Cheng
  • Patent number: 8173655
    Abstract: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 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: Grant
    Filed: April 11, 2008
    Date of Patent: May 8, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump
  • Publication number: 20120108618
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X 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 for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: April 22, 2010
    Publication date: May 3, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Lars Van Der Veen, Darryl Mcconnell, Siegfried Schneider, Matthias Grauert, Andreas Schoop, Tobias Wunberg
  • Publication number: 20120101092
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Application
    Filed: December 23, 2011
    Publication date: April 26, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
  • Patent number: 8163752
    Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 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: Grant
    Filed: June 3, 2008
    Date of Patent: April 24, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Ian Bell, Craig A. Stump
  • Patent number: 8163909
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I or Formula II wherein R1a, R1b, R1c, B, R3, R4, R5 and W of Formula I, and R1a, R1b, R1c, R2, R2a, R3, R4, R5, A1, A2, A3, A4, W, X, Z, m and n of Formula II are defined herein. The invention also provides compounds of Formula III, sub-Formulas II-A-II-D, sub-Formulas III-A-III-D and Formula IV. The invention further includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: April 24, 2012
    Assignee: Amgen Inc.
    Inventors: Wenge Zhong, Stephen Hitchcock, Vinod F. Patel, Michael Croghan, Thomas Dineen, Scott Harried, Daniel Horne, Ted Judd, Matthew Kaller, Charles Kreiman, Patricia Lopez, Holger Monenschein, Thomas Nguyen, Matthew Weiss, Qiufen Xue, Bryant Yang
  • Patent number: 8163766
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: April 24, 2012
    Assignee: Amgen Inc.
    Inventors: Wenge Zhong, Stephen A. Hitchcock, Vinod F. Patel, Yuan Cheng, Michael Croghan, Randall W. Hungate, Daniel La, Patricia Lopez, Matthew K. Kaller, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Lewis Pennington, Matthew Weiss, Ted Judd, Russell Graceffa, Qiufen Xue, Charles Kreiman, Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Scott Harried, Craig Masse, Bryant Yang
  • Patent number: 8158791
    Abstract: A compound of the following formula (I) or its pharmaceutically-acceptable salt is provided: [wherein X, Y, Z and W each independently represent a methine group or a nitrogen atom, provided that a case where all of X, Y, Z and W are methine group; A represents —O— or the like, B represents —C(O)— or the like, D represent —(CH2)m2-, —O— or the like, and m2 represents 0 or 1; Q represents a methine group or a nitrogen atom; and R represents a group represented by the following formula (II-1) (wherein R6, R7 and R8 independently represent a lower alkyl group or the like].
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: April 17, 2012
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20120083476
    Abstract: Certain heteroaryl-substituted spirocyclic diamine urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).
    Type: Application
    Filed: June 4, 2010
    Publication date: April 5, 2012
    Applicant: Janssen Pharmaceutica NV
    Inventors: J. Guy Breitenbucher, John M. Keith, William M. Jone
  • Publication number: 20120083607
    Abstract: Provided are processes for the synthesis of amino analogues from ketone starting materials.
    Type: Application
    Filed: July 1, 2011
    Publication date: April 5, 2012
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Brian c. Austad, Adilah Bahadoor, Jitendra D. Belani, Somarajannair Janardanannair, Charles W. Johannes, Gregg F. Keaney, Priscilla L. White, Sheldon L. Wallerstein
  • Publication number: 20120083501
    Abstract: The invention provides novel tricyclic compounds of Formula I? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
    Type: Application
    Filed: September 23, 2011
    Publication date: April 5, 2012
    Inventors: Kevin W. Hunt, Tony P. Tang, Allen A. Thomas
  • Publication number: 20120083488
    Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).
    Type: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
  • Patent number: 8148390
    Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, 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 is involved.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: April 3, 2012
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Craig A. Stump, Ian M. Bell, Harold G. Selnick
  • Patent number: 8143266
    Abstract: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, X, R4, G1, G2, G3 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: Grant
    Filed: April 11, 2008
    Date of Patent: March 27, 2012
    Assignee: Merck, Sharp & Dohme Corp
    Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump
  • Publication number: 20120071459
    Abstract: 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: Application
    Filed: June 2, 2010
    Publication date: March 22, 2012
    Inventors: Siegfried Benjamin Christensen, IV, Donghui Qin, Shuhul Chen, Shi Lu
  • Publication number: 20120071499
    Abstract: There are provided compounds of the formula wherein X, Y, R1, R1?, R2, R2?, R3, R4, R5 and R6 are as described herein and enantiomers or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: August 18, 2011
    Publication date: March 22, 2012
    Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Jing Zhang, Zhuming Zhang
  • Publication number: 20120065188
    Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.
    Type: Application
    Filed: November 22, 2011
    Publication date: March 15, 2012
    Inventors: Steven Joseph Brickner, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
  • Publication number: 20120065400
    Abstract: Provided herein is a process for the transfer-hydrogenation of ketone analogs of members of the jervine type of Veratrum alkaloids, such as cyclopamine. Also provided herein are novel ruthenium transfer-hydrogenation catalysts.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 15, 2012
    Applicant: INFINITY PHARMACEUTICALS, INC.
    Inventors: Daniel G. Genov, Brian C. Austad, Brian H. White
  • Publication number: 20120065399
    Abstract: Provided herein is a process for the transfer-hydrogenation of ketone analogs of members of the jervine type of Veratrum alkaloids, such as cyclopamine. Also provided herein are novel ruthenium transfer-hydrogenation catalysts.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 15, 2012
    Applicant: INFINITY PHARMACEUTICALS, INC.
    Inventors: Daniel G. Genov, Brian C. Austad, Brian H. White
  • Publication number: 20120065195
    Abstract: The invention provides novel spirotetrahydronaphthalene compounds of Formula ? that inhibit ?-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
    Type: Application
    Filed: March 31, 2011
    Publication date: March 15, 2012
    Inventors: Christopher T. Clark, Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Michael Siu, Allen A. Thomas, Matthew Volgraf
  • Publication number: 20120065218
    Abstract: The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.
    Type: Application
    Filed: June 24, 2011
    Publication date: March 15, 2012
    Inventors: Alfredo C. Castro, Michael J. Grogan, Martin R. Tremblay
  • Patent number: 8134017
    Abstract: A compound represented by the following formula (1) or (2):
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: March 13, 2012
    Assignee: Riken
    Inventors: Shinichiro Kamino, Shuichi Enomoto
  • Publication number: 20120059015
    Abstract: The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed.
    Type: Application
    Filed: July 11, 2011
    Publication date: March 8, 2012
    Applicant: Recordati Ireland Ltd.
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Luciano Guarneri, Davide Graziani, Carlo De Toma, Katia Dimitrova Karamfilova
  • Publication number: 20120053197
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
    Type: Application
    Filed: February 17, 2011
    Publication date: March 1, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger WAGNER, Daniela BERTA, Klaus FUCHS, Riccardo GIOVANNINI, Dieter Wolfgang HAMPRECHT, Ingo KONETZKI, Ruediger STREICHER, Thomas TRIESELMANN
  • Publication number: 20120052096
    Abstract: SOAT-1 inhibitors of general formula (I) and cosmetic and pharmaceutical compositions containing such a compound are described.
    Type: Application
    Filed: February 26, 2010
    Publication date: March 1, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Laurence Dumais, Cédric Poinsard, Thibaud Portal
  • Publication number: 20120046304
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
    Type: Application
    Filed: February 17, 2011
    Publication date: February 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Holger WAGNER, Daniela BERTA, Klaus FUCHS, Riccardo GIOVANNINI, Dieter Wolfgang HAMPRECHT, Ingo KONETZKI, Ruediger STREICHER, Thomas TRIESELMANN
  • Publication number: 20120046306
    Abstract: There are provided compounds of the general formula wherein A, B, V, W, R1, R2, R3, R3, and R4, are as described herein and enantiomers and pharmaceutically acceptable salts thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: July 12, 2011
    Publication date: February 23, 2012
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Prabha Saba Karnachi, Jin-Jun Liu, Sung-Sau So, Jing Zhang, Zhuming Zhang
  • Publication number: 20120046464
    Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, X, n and G have the meanings given above as insecticides and/or acaricides and/or fungicides.
    Type: Application
    Filed: January 14, 2010
    Publication date: February 23, 2012
    Applicant: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Reiner Fischer, Stefan Lehr, Jürgen Benting, Arnd Voerste
  • Publication number: 20120046267
    Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
    Type: Application
    Filed: February 11, 2011
    Publication date: February 23, 2012
    Inventors: Keith R. Hornberger, Dan M. Berger, Xin Chen, Andrew P. Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Lifu Ma, Mark J. Mulvihill, Bijoy Panicker, Kam W. Siu, Arno G. Steinig, James G. Tarrant, Jing Wang, Qinghua Weng, Rajaram Sangem, Ramesh C. Gupta
  • Patent number: 8119816
    Abstract: The present invention provides a blue laser light-absorbent substance, which is suitably used in organic photo conductor, laser optical data carrier or organic light-emitting diodes. The blue laser light-absorbent substance includes a merocyanine compound of the general formula (1) wherein n is an integer of from 0 to 3; R1 is unsubstituted or phenyl-, halogen-, ester-, siliy-substituted linear or branched alkyl group having 1 to 6 carbon atoms; R2 is unsubstituted or substituted phenyl, benzyl or naphthyl; N and R1R2 together represent aromatic-fused N-containing heterocyclic group (NR1R2); Y1 is unsubstituted or substituted alkoxy group having 1 to 8 carbon atoms; Y2 is cyano, nitro, halogen or carboxylate; or O and Y1Y2 together represent epoxy or N-containing heterocyclic hydrocarbonyl ketone (OY1Y2).
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: February 21, 2012
    Assignee: Taiwan Fluoro Technology Co., Ltd.
    Inventors: Fu-Shing Wang, Kuang-Mei Hsu
  • Publication number: 20120040972
    Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
    Type: Application
    Filed: October 25, 2011
    Publication date: February 16, 2012
    Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Publication number: 20120041011
    Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 16, 2012
    Applicant: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR-JOSHI, Suresh Mahadev KADAM
  • Publication number: 20120040942
    Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
    Type: Application
    Filed: February 24, 2010
    Publication date: February 16, 2012
    Applicant: RESPIRATORIUS AB
    Inventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence