Spiro Patents (Class 548/216)
  • Patent number: 9611232
    Abstract: The invention provides compounds having the general formula I wherein n, R1, R2a, R2b, R3a and R3b are as herein defined, composition comprising the compounds and methods of using the compounds.
    Type: Grant
    Filed: April 29, 2015
    Date of Patent: April 4, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Haiyan Wang
  • Patent number: 9242973
    Abstract: The present invention provides a hydrate of N-[(4S)-2-amino-2?,2?-dimethyldispiro[1,3-oxazole-4,4?-chromene-3?,3?-oxetan]-6?-yl]-5-chloropyridine-2-carboxamide which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: January 26, 2016
    Assignee: COMENTIS, INC.
    Inventors: Ryosuke Munakata, Makoto Inoue, Hiroaki Tominaga, Shingo Yamasaki, Yasuhiro Shiina, Kiyohiro Samizu, Hisao Hamaguchi, Lin Hong
  • Patent number: 9035054
    Abstract: The present invention relates to the field of organic chemistry and in particular to organic free radicals used as polarizing agents in the technique of Dynamic Nuclear Polarization (DNP), which involves transferring the polarization of electron spins to the nuclei of a compound whose Nuclear Magnetic Resonance (NMR) is being observed. It concerns Dinitroxide-type Biradical polarizing agents characterized by a rigid linkage between the aminoxyl groups of said nitroxide units. This particular structure enables, at low temperatures and high fields, optimal transfer of polarization and optimal enhancement of NMR/MAS signals of the polarized nuclei of the compound studied.
    Type: Grant
    Filed: October 30, 2013
    Date of Patent: May 19, 2015
    Assignee: UNIVERSITE D'AIX-MARSEILLE
    Inventors: Oliver Ouari, Hakim Karoui, Francois Le Moigne, Paul Tordo, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
  • Publication number: 20150119376
    Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
    Type: Application
    Filed: April 12, 2012
    Publication date: April 30, 2015
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Publication number: 20150099734
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
  • Patent number: 8975415
    Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: March 10, 2015
    Assignee: CoMentis, Inc.
    Inventors: Ryosuke Munakata, Makoto Inoue, Hiroaki Tominaga, Shingo Yamasaki, Yasuhiro Shina, Kiyohiro Samizu, Hisao Hamaguchi, Lin Hong
  • Publication number: 20150051407
    Abstract: The present invention relates to a novel process for preparing cis-alkoxy-substituted spirocyclic phenylacetylamino acid esters and cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives, and also to novel intermediates and starting materials which are produced and/or used in the process according to the invention.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 19, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Taraneh Farida, Berndt Maiwald, Martin Littmann, Winfried Etzel
  • Patent number: 8927585
    Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: January 6, 2015
    Assignee: GlaxoSmithKline Intellectual Property (NO.2) Limited
    Inventors: Carl Brooks, Mui Cheung, Krista B. Goodman, Marlys Hammond
  • Publication number: 20140357655
    Abstract: Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
    Type: Application
    Filed: January 15, 2013
    Publication date: December 4, 2014
    Inventors: Olaf Panknin, Stefan Bäurle, Sven Ring, Wolfgang Schwede, Wilhelm Bone, Katrin Nowak-Reppel, Eckhard Bender, Reinhard Nubbemeyer, Mark Jean Gnoth
  • Publication number: 20140350253
    Abstract: The discovery of distinct modes of asymmetric catalysis has the potential to rapidly advance chemists' ability to build enantioenriched molecules. As an example, the use of chiral cation salts as phase-transfer catalysts for anionic reagents has enabled a vast set of enantioselective transformations. A largely overlooked analogous mechanism wherein a chiral anionic catalyst brings a cationic species into solution is itself a powerful method. The concept is broadly applicable to a number of different reaction pathways, including to the enantioselective fluorocyclization of olefins, and dearomatization of aromatic systems with a cationic electrophile-transferring (e.g., fluorinating) agent and a chiral phosphate catalyst. The reactions proceed in high yield and stereoselectivity. The compounds and methods of the invention are of particular value, especially considering the scarcity of alternative approaches.
    Type: Application
    Filed: December 26, 2012
    Publication date: November 27, 2014
    Applicant: The Regents Of The University Of California
    Inventors: Vivek Rauniyar, Aaron D. Lackner, Gregory L. Hamilton, F. Dean Toste, Robert J. Phipps, Hunter Shunatona, Natalja Frueh, Yiming Wang, Jeffrey Wu, Jigar Patel, Takashi Honjo
  • Patent number: 8883782
    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 other related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X and Y of Formula I 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, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: November 11, 2014
    Assignee: Amgen Inc.
    Inventors: Yuan Cheng, Ryan White, Albert Amegadzie, James Brown, Alan C. Cheng, Erin F. Dimauro, Thomas Dineen, Oleg Epstein, Vijay Keshav Gore, Jason Brooks Human, Ted Judd, Charles Kreiman, Qingyian Liu, Patricia Lopez, Vu Van Ma, Isaac Marx, Ana Minatti, Hanh Nho Nguyen, Nick A. Paras, Vinod F. Patel, Wenyuan Qian, Matthew Weiss, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
  • Patent number: 8834749
    Abstract: Disclosed are a photosensitive resin composition including (A) a binder resin including a cardo-based resin including a repeating unit represented by the following Chemical Formula 1, (B) a photopolymerizable monomer, (C) a photopolymerization initiator, (D) a colorant and (E) a solvent, and a light blocking layer using the same. In the above Chemical Formula 1, each substituent is the same as defined in the detailed description.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: September 16, 2014
    Assignee: Cheil Industries Inc.
    Inventors: Hyun-Moo Choi, Chang-Min Lee, Ji-Hye Kim, Kyung-Won Ahn, A-Rum Yu, Jae-Bum Yim, Hwan-Sung Cheon, Ju-Ho Jung
  • Patent number: 8785631
    Abstract: Novel raw material compounds are provided that are useful for producing novel cycloalkane carboxamide derivatives having cathepsin K inhibitory action. An oxazolone derivative represented by formula (I): [wherein, R1 represents a substituted or unsubstituted alkyl group, substituted or unsubstituted alkenyl group, substituted or unsubstituted alkynyl group, substituted phenyl group, substituted or unsubstituted naphthyl group or substituted or unsubstituted heterocyclic group, and ring A represents a saturated cyclic alkylidene group having 6 to 7 carbon atoms].
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: July 22, 2014
    Assignee: Seikagaku Corporation
    Inventors: Tsuneo Koji, Hisatomo Kunii, Nobuo Kobayashi
  • Patent number: 8778938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
  • Publication number: 20140179695
    Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.
    Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
  • Patent number: 8729077
    Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: May 20, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Don Roberts, Wieslaw Kazmierski, Richard Grimes
  • Publication number: 20140135369
    Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 15, 2014
    Applicant: GlaxoSmith Kline,LLC
    Inventors: Carl Brooks, Mui Cheung, Krista B. Goodman, Marlys Hammond
  • Publication number: 20140121206
    Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: GlaxoSmithKliine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • Publication number: 20140113916
    Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 24, 2014
    Applicant: GlaxoSmithKLine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • Patent number: 8648193
    Abstract: The present invention relates to the field of organic chemistry and in particular to organic free radicals used as polarizing agents in the technique of Dynamic Nuclear Polarization (DNP), which involves transferring the polarization of electron spins to the nuclei of a compound whose Nuclear Magnetic Resonance (NMR) is being observed. It concerns dinitroxide-type biradical polarizing agents characterized by a rigid linkage between the nitroxide units that enables optimal orientation and distance to be maintained between the aminoxyl groups of said nitroxide units. This particular structure enables, at low temperatures and high fields, optimal transfer of polarization and optimal enhancement of NMR/MAS signals of the polarized nuclei of the compound studied.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: February 11, 2014
    Assignee: Universite d'Aix Marseille
    Inventors: Olivier Ouari, Hakim Karoui, Francois Le Moigne, Paul Tordo, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
  • Publication number: 20140031335
    Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
    Type: Application
    Filed: April 12, 2012
    Publication date: January 30, 2014
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: SeoHee Lee, Jung Taek Oh, JaeKwang Lee, JaeWon Lee, Suyeal Bae, Nina Ha, Sera Lee
  • Patent number: 8586609
    Abstract: The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: November 19, 2013
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
  • Patent number: 8563714
    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: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20130252962
    Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: March 6, 2013
    Publication date: September 26, 2013
    Inventors: Mikhail CHAFEEV, Sultan CHOWDHURY, Lauren FRASER, Jianmin FU, Jonathan LANGILLE, Shifeng LIU, Jianyu SUN, Shaoyi SUN, Serguei SVIRIDOV, Mark WOOD, Alla Yurevna ZENOVA, Qi JIA, Jean-Jacques Alexandre CADIEUX, Simon J. GAUTHIER, Amy Frances DOUGLAS, Tom HSIEH, Nagasree CHAKKA, Zoran CIKOJEVIC
  • Publication number: 20130231377
    Abstract: Disclosed are pactamycin analogs, pharmaceutical compositions including the analogs, and methods of using the analogs, such as to inhibit tumor growth or a pathogenic infection such as a bacterial or parasitic infection. The pactamycin analogs have a general formula where R1 is H, lower aliphatic, amide, acyl, or aminoacyl; R2 is —C(O)NR8R9 where R8 and R9 independently are hydrogen or lower aliphatic, or R1 and R2 together form a cyclic structure; R3 and R4 independently are hydrogen, hydroxyl, or lower aliphatic, or R2 and R3 together form a cyclic structure; R5 is hydrogen or acyl; R6 and R7 independently are hydrogen, hydroxyl, halogen, lower aliphatic, or amino.
    Type: Application
    Filed: August 2, 2011
    Publication date: September 5, 2013
    Applicants: Oregon State University
    Inventor: Taifo Mahmud
  • Patent number: 8476274
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: July 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Publication number: 20130131042
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype 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: Application
    Filed: August 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu
  • Publication number: 20130123217
    Abstract: The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.
    Type: Application
    Filed: December 13, 2012
    Publication date: May 16, 2013
    Applicant: NEUMEDICS
    Inventor: Neumedics
  • Publication number: 20130109710
    Abstract: The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof
    Type: Application
    Filed: September 14, 2012
    Publication date: May 2, 2013
    Applicant: JAPAN TOBACCO INC.
    Inventors: Takashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
  • Publication number: 20130102604
    Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.
    Type: Application
    Filed: December 10, 2012
    Publication date: April 25, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130079271
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: September 22, 2010
    Publication date: March 28, 2013
    Inventors: Kevin D. McCormick, Ning Shao, Younong Yu, Xianhai Huang, Manuel De Lera Ruiz, Anandan Palani, Junying Zheng, Christopher W. Boyce, Robert G. Aslanian, Jianhua Chao
  • Publication number: 20130045914
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: October 18, 2012
    Publication date: February 21, 2013
    Applicant: Merck Sharp & Dohme Corp
    Inventor: Merck Sharp & Dohme Corp.
  • Patent number: 8324213
    Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: October 6, 2009
    Date of Patent: December 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Youngong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Publication number: 20120295897
    Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: July 25, 2012
    Publication date: November 22, 2012
    Applicant: Xenon Pharmaceuticals Inc.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
  • Publication number: 20120277259
    Abstract: The present invention relates to substituted benzofused derivatives, which can be 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 10, 2012
    Publication date: November 1, 2012
    Applicant: Glenmark Pharmaceuticals S.A.
    Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR-JOSHI, Suresh Mahadev KADAM
  • Publication number: 20120270071
    Abstract: A chromene compound having a skeleton represented by the following formula (1) and exhibiting double peak characteristic: wherein Z is a group represented by any one of the following formulas: n is an integer of 1 to 3, when n is 2 or 3, Z? s may be the same or different, with the proviso that when n is 1, Z cannot be —CH2—, and when n is 2 or 3, Z's cannot be —CH2— at the same time; R1 is an electron absorbing group having a Hammett constant ?p of more than 0, with the proviso that when there are a plurality of R1's, R1's may be the same or different; and X and Y are each independently an oxygen atom or ?NR2, with the proviso that X and Y cannot be oxygen atoms at the same time.
    Type: Application
    Filed: July 21, 2010
    Publication date: October 25, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka
  • Publication number: 20120245191
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: March 19, 2012
    Publication date: September 27, 2012
    Inventors: Daniel Hunziker, Werner Neidhart
  • Patent number: 8211932
    Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: July 3, 2012
    Assignee: Novartis AG
    Inventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
  • Publication number: 20120165331
    Abstract: The invention relates to compounds of the formula I A-D-C(R1)2—B??(I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: December 19, 2011
    Publication date: June 28, 2012
    Inventors: Sangamesh BADIGER, Dirk BEHNKE, Claudia BETSCHART, Vinod CHAUDHARI, Simona COTESTA, Samuel HINTERMANN, Andreas LERCHNER, Fatma LIMAM, Silvio OFNER, Chetan PANDIT, Jürgen WAGNER
  • 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: 20120129830
    Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3, provided that m+n?7 and that o+p?7; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.
    Type: Application
    Filed: May 11, 2010
    Publication date: May 24, 2012
    Applicant: SANOFI
    Inventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
  • Patent number: 8168797
    Abstract: Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including Haemophilus influenza and Coagulase negative staphylococci and resistant bacteria including vancomycin-resistant enterococci (VRE), the pharmaceutical composition is useful as an antibiotic (wherein, R is as defined in the specification).
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: May 1, 2012
    Assignee: Korea Institute of Science and Technology
    Inventors: Chang Hyun Oh, Jung Hyuck Cho
  • Patent number: 8138182
    Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 20, 2012
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
  • 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: 20120015933
    Abstract: 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: Application
    Filed: September 29, 2011
    Publication date: January 19, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Manfred SCHUDOK, Michael WAGNER, Armin BAUER, Anna KOHLMANN
  • Publication number: 20110300104
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: June 3, 2011
    Publication date: December 8, 2011
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
  • Publication number: 20110251207
    Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: October 6, 2009
    Publication date: October 13, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Adandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Patent number: 8022250
    Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.
    Type: Grant
    Filed: December 24, 2009
    Date of Patent: September 20, 2011
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
  • Publication number: 20110224211
    Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.
    Type: Application
    Filed: November 19, 2009
    Publication date: September 15, 2011
    Inventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Ron Roberts, Wieslaw Kazmierski, Richard Grimes