Spiro Patents (Class 548/216)
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Patent number: 11569466Abstract: A novel light-emitting element is provided. A light-emitting element with a long lifetime is provided. A light-emitting element with high emission efficiency is provided. In the light-emitting element, an EL layer includes a hole-injection layer, a first hole-transport layer, a second hole-transport layer, a third hole-transport layer, a light-emitting layer, a first electron-transport layer, and a second electron-transport layer in this order; the hole-injection layer includes an organic acceptor; the LUMO level of the host material is higher than that of the first electron-transport layer; the LUMO level of the second electron-transport layer is higher than that of the first electron-transport layer; the host material is a substance including a condensed aromatic ring skeleton; and the first and second electron-transport layers each include a substance having a heteroaromatic ring skeleton.Type: GrantFiled: August 15, 2019Date of Patent: January 31, 2023Inventors: Satoshi Seo, Tsunenori Suzuki, Yusuke Takita, Naoaki Hashimoto
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Patent number: 9611232Abstract: 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: GrantFiled: April 29, 2015Date of Patent: April 4, 2017Assignee: Hoffmann-La Roche Inc.Inventors: Luke Green, Haiyan Wang
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Patent number: 9242973Abstract: 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: GrantFiled: January 22, 2015Date of Patent: January 26, 2016Assignee: COMENTIS, INC.Inventors: Ryosuke Munakata, Makoto Inoue, Hiroaki Tominaga, Shingo Yamasaki, Yasuhiro Shiina, Kiyohiro Samizu, Hisao Hamaguchi, Lin Hong
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Patent number: 9035054Abstract: 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: GrantFiled: October 30, 2013Date of Patent: May 19, 2015Assignee: UNIVERSITE D'AIX-MARSEILLEInventors: Oliver Ouari, Hakim Karoui, Francois Le Moigne, Paul Tordo, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
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Publication number: 20150119376Abstract: 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: ApplicationFiled: April 12, 2012Publication date: April 30, 2015Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
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Publication number: 20150099734Abstract: 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: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
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Publication number: 20150099730Abstract: 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: ApplicationFiled: September 6, 2013Publication date: April 9, 2015Applicant: Janssen Pharmaceutica, NVInventor: Peter J. Connolly
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Patent number: 8975415Abstract: 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: GrantFiled: February 27, 2014Date of Patent: March 10, 2015Assignee: CoMentis, Inc.Inventors: Ryosuke Munakata, Makoto Inoue, Hiroaki Tominaga, Shingo Yamasaki, Yasuhiro Shina, Kiyohiro Samizu, Hisao Hamaguchi, Lin Hong
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Publication number: 20150051407Abstract: 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: ApplicationFiled: March 25, 2013Publication date: February 19, 2015Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Taraneh Farida, Berndt Maiwald, Martin Littmann, Winfried Etzel
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Patent number: 8927585Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: GrantFiled: June 15, 2012Date of Patent: January 6, 2015Assignee: GlaxoSmithKline Intellectual Property (NO.2) LimitedInventors: Carl Brooks, Mui Cheung, Krista B. Goodman, Marlys Hammond
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Publication number: 20140357655Abstract: 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: ApplicationFiled: January 15, 2013Publication date: December 4, 2014Inventors: Olaf Panknin, Stefan Bäurle, Sven Ring, Wolfgang Schwede, Wilhelm Bone, Katrin Nowak-Reppel, Eckhard Bender, Reinhard Nubbemeyer, Mark Jean Gnoth
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Publication number: 20140350253Abstract: 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: ApplicationFiled: December 26, 2012Publication date: November 27, 2014Applicant: The Regents Of The University Of CaliforniaInventors: 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
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Patent number: 8883782Abstract: 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: GrantFiled: March 14, 2011Date of Patent: November 11, 2014Assignee: 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
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Patent number: 8834749Abstract: 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: GrantFiled: July 22, 2013Date of Patent: September 16, 2014Assignee: 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
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Patent number: 8785631Abstract: 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: GrantFiled: January 10, 2007Date of Patent: July 22, 2014Assignee: Seikagaku CorporationInventors: Tsuneo Koji, Hisatomo Kunii, Nobuo Kobayashi
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Patent number: 8778938Abstract: 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: GrantFiled: June 3, 2011Date of Patent: July 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Publication number: 20140179695Abstract: 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: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
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Patent number: 8729077Abstract: 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: GrantFiled: November 19, 2009Date of Patent: May 20, 2014Assignee: GlaxoSmithKline LLCInventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Don Roberts, Wieslaw Kazmierski, Richard Grimes
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Publication number: 20140135369Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: ApplicationFiled: June 15, 2012Publication date: May 15, 2014Applicant: GlaxoSmith Kline,LLCInventors: Carl Brooks, Mui Cheung, Krista B. Goodman, Marlys Hammond
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Publication number: 20140121206Abstract: 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: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: GlaxoSmithKliine, LLCInventors: 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
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Publication number: 20140113916Abstract: The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: ApplicationFiled: June 15, 2012Publication date: April 24, 2014Applicant: GlaxoSmithKLine, LLCInventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
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Patent number: 8648193Abstract: 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: GrantFiled: May 29, 2009Date of Patent: February 11, 2014Assignee: Universite d'Aix MarseilleInventors: Olivier Ouari, Hakim Karoui, Francois Le Moigne, Paul Tordo, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
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Publication number: 20140031335Abstract: 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: ApplicationFiled: April 12, 2012Publication date: January 30, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: SeoHee Lee, Jung Taek Oh, JaeKwang Lee, JaeWon Lee, Suyeal Bae, Nina Ha, Sera Lee
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Patent number: 8586609Abstract: 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: GrantFiled: July 29, 2010Date of Patent: November 19, 2013Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Petra Lennig
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Patent number: 8563714Abstract: 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: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20130252962Abstract: 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: ApplicationFiled: March 6, 2013Publication date: September 26, 2013Inventors: 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
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Publication number: 20130231377Abstract: 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: ApplicationFiled: August 2, 2011Publication date: September 5, 2013Applicants: Oregon State UniversityInventor: Taifo Mahmud
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Patent number: 8476274Abstract: 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: GrantFiled: October 18, 2012Date of Patent: July 2, 2013Assignee: 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
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Publication number: 20130131042Abstract: 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: ApplicationFiled: August 12, 2011Publication date: May 23, 2013Applicant: 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
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Publication number: 20130123217Abstract: 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: ApplicationFiled: December 13, 2012Publication date: May 16, 2013Applicant: NEUMEDICSInventor: Neumedics
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Publication number: 20130109710Abstract: The spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereofType: ApplicationFiled: September 14, 2012Publication date: May 2, 2013Applicant: JAPAN TOBACCO INC.Inventors: Takashi Shimada, Hiroshi Ueno, Kazuhiro Tsutsumi, Kouichi Aoyagi, Tomoyuki Manabe, Shin-Ya Sasaki, Susumu Katoh
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Publication number: 20130102604Abstract: 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: ApplicationFiled: December 10, 2012Publication date: April 25, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130079271Abstract: 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: ApplicationFiled: September 22, 2010Publication date: March 28, 2013Inventors: 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
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Publication number: 20130045914Abstract: 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: ApplicationFiled: October 18, 2012Publication date: February 21, 2013Applicant: Merck Sharp & Dohme CorpInventor: Merck Sharp & Dohme Corp.
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Patent number: 8324213Abstract: 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: GrantFiled: October 6, 2009Date of Patent: December 4, 2012Assignee: 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
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Publication number: 20120295897Abstract: 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: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: 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
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Publication number: 20120277259Abstract: 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: ApplicationFiled: July 10, 2012Publication date: November 1, 2012Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR-JOSHI, Suresh Mahadev KADAM
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Publication number: 20120270071Abstract: 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: ApplicationFiled: July 21, 2010Publication date: October 25, 2012Inventors: Toshiaki Takahashi, Junji Takenaka
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Publication number: 20120245191Abstract: 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: ApplicationFiled: March 19, 2012Publication date: September 27, 2012Inventors: Daniel Hunziker, Werner Neidhart
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Patent number: 8211932Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: September 10, 2010Date of Patent: July 3, 2012Assignee: Novartis AGInventors: 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
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Publication number: 20120165331Abstract: 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: ApplicationFiled: December 19, 2011Publication date: June 28, 2012Inventors: Sangamesh BADIGER, Dirk BEHNKE, Claudia BETSCHART, Vinod CHAUDHARI, Simona COTESTA, Samuel HINTERMANN, Andreas LERCHNER, Fatma LIMAM, Silvio OFNER, Chetan PANDIT, Jürgen WAGNER
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Publication number: 20120157448Abstract: 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: ApplicationFiled: November 22, 2011Publication date: June 21, 2012Inventors: 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
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Publication number: 20120129830Abstract: 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: ApplicationFiled: May 11, 2010Publication date: May 24, 2012Applicant: SANOFIInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
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Patent number: 8168797Abstract: 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: GrantFiled: November 25, 2008Date of Patent: May 1, 2012Assignee: Korea Institute of Science and TechnologyInventors: Chang Hyun Oh, Jung Hyuck Cho
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Patent number: 8138182Abstract: 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: GrantFiled: September 24, 2009Date of Patent: March 20, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
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Publication number: 20120065195Abstract: 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: ApplicationFiled: March 31, 2011Publication date: March 15, 2012Inventors: Christopher T. Clark, Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Nicholas C. Kallan, Michael Siu, Allen A. Thomas, Matthew Volgraf
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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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Publication number: 20110300104Abstract: 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: ApplicationFiled: June 3, 2011Publication date: December 8, 2011Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Publication number: 20110251207Abstract: 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: ApplicationFiled: October 6, 2009Publication date: October 13, 2011Applicant: 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
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Patent number: 8022250Abstract: 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: GrantFiled: December 24, 2009Date of Patent: September 20, 2011Assignee: Chiesi Farmaceutici S.p.A.Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti