Bicyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 544/47)
  • Patent number: 11059835
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: July 13, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • Patent number: 10662202
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
    Type: Grant
    Filed: November 6, 2018
    Date of Patent: May 26, 2020
    Assignee: Merck Sharp & Dohm Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • Patent number: 10125149
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a method for preparing a compound of formula (II), or a salt thereof, comprising the step of admixing, e.g., reacting, a compound of formula (III), or a salt thereof, with a nucleophile (Nuc) in the presence of reagents comprising: (a) a palladium source; and (b) a palladium-binding ligand, to form a compound of formula (II), or a salt thereof.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: November 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • Patent number: 10004750
    Abstract: The present invention provides an acid addition salt or a sodium salt of a compound represented by the formula (IA): or their hydrate or a stable crystalline solid thereof. The salt or the crystalline solid is extremely useful as an active ingredient for the production of a pharmaceutical product.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: June 26, 2018
    Assignee: Shionogi & Co., Ltd.
    Inventors: Fumihiko Matsubara, Takanori Kurita, Daiki Nagamatsu
  • Patent number: 9949982
    Abstract: The present invention relates to a stable pharmaceutical composition comprising a compound represented by formula (I), its pharmaceutically acceptable salt or a solvate thereof. The stable pharmaceutical composition can be prepared by comprising 1) a compound represented by formula (I), its pharmaceutically acceptable salt, or a solvate thereof, 2) one or more selected from the group consisting of alkali metal chlorides, alkaline earth metal chlorides, transition metal chlorides and magnesium chloride; and 3) sugar and/or a sugar alcohol.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: April 24, 2018
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hidenori Kawasaki, Natsuko Kojima, Atsushi Fujihira, Kanako Takahashi, Fumihiko Matsubara, Nao Matsuoka
  • Patent number: 9527866
    Abstract: The invention relates to processes for the production of intermediates for preparing 2-alkyl cephem compounds useful as antimicrobial drugs. The invention provides a process which comprises oxidating a compound of the formula (I) or a salt thereof to give a compound of the formula (II) or a salt thereof wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: December 27, 2016
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Katsuki Yokoo, Shinya Hisakawa, Kenji Yamawaki, Toshiaki Aoki, Yutaka Yokota, Masatoshi Takeo, Mikito Asai
  • Patent number: 9382278
    Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil via intermediates of Formulae (1), (3) or (4) of this process.
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: July 5, 2016
    Assignee: Sandoz AG
    Inventors: Peter Kremminger, Hubert Sturm
  • Publication number: 20150105548
    Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.
    Type: Application
    Filed: May 25, 2012
    Publication date: April 16, 2015
    Inventors: Allan Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
  • Publication number: 20150099719
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
  • Publication number: 20150094293
    Abstract: Novel solid forms of ceftolozane are described, as well as methods for the preparation and use of these solid forms.
    Type: Application
    Filed: May 28, 2014
    Publication date: April 2, 2015
    Applicant: CALIXA THERAPEUTICS, INC.
    Inventors: Valdas Jurkauskas, Nicole Miller Damour, Lisa Duong, You Seok Hwang, Kristos Adrian Moshos, Sanjay Mudur, Asli Ovat, Joseph Terracciano, Jason Woertink
  • Publication number: 20150073138
    Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to a intermediates of this process.
    Type: Application
    Filed: September 7, 2012
    Publication date: March 12, 2015
    Applicant: Sandoz AG
    Inventors: Peter Kremminger, Hubert Sturm
  • Publication number: 20150038497
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Application
    Filed: July 29, 2014
    Publication date: February 5, 2015
    Inventors: Richard T. LEWIS, Jennifer R. ALLEN, James BROWN, Angel GUZMAN-PEREZ, Zihao HUA, Ted JUDD, Qingyian LIU, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE
  • Publication number: 20150018342
    Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 15, 2015
    Applicant: SANOFI
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Patent number: 8933068
    Abstract: A diluted solution of ceftiofur sodium is intrathecally or ventricularly delivered to effectively treat bacterial meningitis while maintaining the patient's threshold and reducing the likelihood of seizure.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: January 13, 2015
    Assignee: NBR Pathfinder LLC
    Inventor: Robert B. Boyd
  • Patent number: 8895728
    Abstract: A novel process for purifying Cefmenoxime hydrochloride comprises: 1) adding a solvent wherein Cefmenoxime hydrochloride is insoluble at the temperature less than 30° C., filtering after vigorous stirring, washing the filter cake with a solvent wherein Cefmenoxime hydrochloride is insoluble at a temperature less 20° C., and drying; 2) placing the filter cake into ammonium hydroxide, controlling the pH value less than 9 with a gentle agitation to obtain Cefmenoxime acid solution in ammonium hydroxide, and then filtering out the precipitate; 3) adding hydrochloric acid at a concentration of 0.5-4 mol/L to Cefmenoxime acid solution in ammonium hydroxide slowly and controlling the temperature between 30-60° C. and the final pH between 0.5-3.0, and then cooling down to a minimum of 10° C. and standing still to allow crystallization, filtrating and vacuum drying.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: November 25, 2014
    Assignee: Hainan Lingkang Pharmaceutical Co., Ltd.
    Inventor: Linggang Tao
  • Publication number: 20140343032
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Buyu Kou, Gangqin Li, Xianfeng Lin, Haixia Liu, Hong Shen, Houguang Shi, Guolong Wu, Zhisen Zhang, Mingwei Zhou, Wei Zhu
  • Patent number: 8871927
    Abstract: A novel process for refining Ceftizoxime sodium compound, comprises the steps of: 1) dissolving crude Ceftizoxime sodium in water, and extracting with cyclohexane or ethyl acetate, followed by separating the organic phase containing impurities, producing an aqueous phase containing Ceftizoxime sodium; 2) adding ammonia or ammonium hydroxide into the above aqueous phase while stirring, followed by filtrating the precipitate, producing an aqueous filtrate containing Ceftizoxime sodium; 3) adding an alcoholic solvent in the aqueous solution and recrystallizing under controlled temperature, followed by centrifuging and washing the resultant crystals, producing the refined Ceftizoxime sodium after drying; and 4) optionally returning the mother liquid of the recrystallization process to step 3).
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: October 28, 2014
    Assignee: Hainan Lingkang Pharmaceutical Co., Ltd.
    Inventor: Linggang Tao
  • Patent number: 8801939
    Abstract: A method for increasing ozone concentration in a liquid can include: providing a gas having ozone; introducing the ozone-containing gas into a liquid, wherein the liquid and ozone combination has a temperature between about 0.8 and about 1.5 times the critical temperature of ozone; and increasing isothermally, the pressure of the ozone-containing gas above the liquid to about 0.3 to about 5 times the critical pressure of ozone so as to increase the ozone concentration in the liquid. The temperature is expressed in absolute units (Kelvin or Rankin). The method can be used for removing ozone from a gas or for purifying ozone. The liquid having a high ozone concentration can be used for ozonolysis of a substrate.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: August 12, 2014
    Assignees: University of Kansas, Archer Daniels Midland Company
    Inventors: Bala Subramaniam, Daryle Busch, Andrew M. Danby, Thomas P Binder
  • Publication number: 20140135318
    Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 23, 2012
    Publication date: May 15, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
  • Publication number: 20140121370
    Abstract: A novel process for purifying Cefmenoxime hydrochloride comprises: 1) adding a solvent wherein Cefmenoxime hydrochloride is insoluble at the temperature less than 30° C. filtering after vigorous stirring, washing the filter cake with a solvent wherein Cefmenoxime hydrochloride is insoluble at a temperature less 20° C., and drying; 2) placing the filter cake into ammonium hydroxide, controlling the pH value less than 9 with a gentle agitation to obtain Cefmenoxime acid solution in ammonium hydroxide, and then filtering out the precipitate; 3) adding hydrochloric acid at a concentration of 0.5-4 mol/L to Cefmenoxime acid solution in ammonium hydroxide slowly and controlling the temperature between 30-60° C. and the final pH between 0.5-3.0, and then cooling down to a minimum of 10° C. and standing still to allow crystallization, filtrating and vacuum drying.
    Type: Application
    Filed: August 11, 2011
    Publication date: May 1, 2014
    Applicant: Hainan Lingkang Pharmaceutical Co., Ltd.
    Inventor: Linggang Tao
  • Publication number: 20140121369
    Abstract: A novel process for refining Ceftizoxime sodium compound, comprises the steps of: 1) dissolving crude Ceftizoxime sodium in water, and extracting with cyclohexane or ethyl acetate, followed by separating the organic phase containing impurities, producing an aqueous phase containing Ceftizoxime sodium; 2) adding ammonia or ammonium hydroxide into the above aqueous phase while stirring, followed by filtrating the precipitate, producing an aqueous filtrate containing Ceftizoxime sodium; 3) adding an alcoholic solvent in the aqueous solution and recrystallizing under controlled temperature, followed by centrifuging and washing the resultant crystals, producing the refined Ceftizoxime sodium after drying; and 4) optionally returning the mother liquid of the recrystallization process to step 3).
    Type: Application
    Filed: August 11, 2011
    Publication date: May 1, 2014
    Applicant: HAINAN LINGKANG PHARMACEUTICAL CO., LTD.
    Inventor: Linggang Tao
  • Publication number: 20140107109
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Inventors: Richard T. LEWIS, Jennifer R. ALLEN, Yuan CHENG, Deborah CHOQUETTE, Oleg EPSTEIN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Zihao HUA, Randall W. HUNGATE, Jason Brooks HUMAN, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Ana Elena MINATTI, Philip OLIVIERI, Karina ROMERO, Shannon RUMFELT, Robert M. RZASA, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE, Qiufen XUE, Xiao ZHENG, Wenge ZHONG
  • Publication number: 20140031339
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: July 16, 2013
    Publication date: January 30, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael Jason BURKE, Thomas Martin KIRRANE, JR., Chuk Chui MAN, Daniel Richard MARSHALL, Anil Kumar PADYANA, Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Roger John SNOW, Ronald John SORCEK, Hidenori TAKAHASHI, Steven John TAYLOR, Michael Robert TURNER, Erick Richard Roush YOUNG, Qiang ZHANG, Yunlong ZHANG, Renee M. ZINDELL
  • Publication number: 20130338152
    Abstract: The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: March 8, 2012
    Publication date: December 19, 2013
    Applicants: IRM LLC, NOVARTIS AG
    Inventors: Bei Chen, Robin Alec Fairhurst, Songchun Jiang, Wenshuo Lu, Thomas H. Marsilje, III, Clive McCarthy, Pierre-Yves Michellys, Stefan Stutz
  • Patent number: 8425784
    Abstract: A method for increasing ozone concentration in a liquid can include: providing a gas having ozone; introducing the ozone-containing gas into a liquid, wherein the liquid and ozone combination has a temperature between about 0.8 and about 1.5 times the critical temperature of ozone; and increasing isothermally, the pressure of the ozone-containing gas above the liquid to about 0.3 to about 5 times the critical pressure of ozone so as to increase the ozone concentration in the liquid. The temperature is expressed in absolute units (Kelvin or Rankin). The method can be used for removing ozone from a gas or for purifying ozone. The liquid having a high ozone concentration can be used for ozonolysis of a substrate.
    Type: Grant
    Filed: November 4, 2008
    Date of Patent: April 23, 2013
    Assignees: University of Kansas, Archer Daniels Midland Company
    Inventors: Bala Subramaniam, Daryle Busch, Andrew M. Danby, Thomas P. Binder
  • Publication number: 20130040935
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.
    Type: Application
    Filed: February 8, 2011
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
  • Publication number: 20120323001
    Abstract: The present invention provides BACE inhibitors of Formula I: methods for their use, intermediates, and methods for their preparation.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 20, 2012
    Applicant: ELI LILLY AND COMPANY
    Inventors: James Edmund AUDIA, Chongsheng Eric SHI
  • Publication number: 20120322791
    Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.
    Type: Application
    Filed: January 18, 2011
    Publication date: December 20, 2012
    Inventors: M. Arshad Siddiqui, Yang Nan, Mehul F. Patel, Panduranga Adulla P. Reddy, Umar Faruk Mansoor, Zhaoyang Meng, Lalanthi Dilrukshi Vitharana, Lianyun Zhao, Amit K. Mandal, Duan Liu, Shuyi Tang, Andrew McRiner, David B. Belanger, Patrick J. Curran, Chaoyang Dai, Angie R. Angeles, Liping Yang, Matthew Hersh Daniels
  • Publication number: 20120309964
    Abstract: The present invention provides a cyclic amine compound represented by formula (I) (in formula (I), Cy1 and Cy2 independently represent a C6-10 aryl group or a heterocyclyl group; R1a to R5a independently represent a hydrogen atom or an unsubstituted or substituted C1-6 alkyl group; R10, R11, R20 and R21 independently represent an unsubstituted or substituted C1-6 alkyl group, an unsubstituted or substituted C1-6 alkoxy group, a halogen atom or the like; m, n, p, and r each represent an integer of 0 to 5; and Y represents an oxygen atom or the like) or salt thereof, and an acaricide including the same.
    Type: Application
    Filed: February 24, 2011
    Publication date: December 6, 2012
    Inventors: Isami Hamamoto, Keiji Koizumi, Masahiro Kawaguchi, Hisashi Tanigawa, Takehiko Nakamura, Tomomi Kobayashi
  • Publication number: 20120283237
    Abstract: The present invention provides novel cephalosporin derivatives of formula I, their analogues, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: April 30, 2012
    Publication date: November 8, 2012
    Applicant: PFIZER INC.
    Inventors: Brian A. Duclos, Edmund L. Ellsworth, Richard A. Ewin, Paul D. Johnson, Timothy A. Johnson, Graham M. Kyne, Susan M. K. Sheehan, Rajendran Vairagoundar
  • Publication number: 20120245154
    Abstract: The present invention relates to an agent for treating or preventing disease induced by production, secretion and/or deposition of amyloid ? protein, for example, a compound of formula (I), wherein, R1, R2a, R2b R3, R4a, R4b, ring A, and dashed line are described in this specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 8, 2010
    Publication date: September 27, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Kousuke Anan, Yukio Tada, Akihiro Hori, Moriyasu Masui
  • Patent number: 8193179
    Abstract: Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: June 5, 2012
    Assignee: Actelion Pharmaceuticals, Ltd
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Publication number: 20120094984
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Application
    Filed: December 21, 2011
    Publication date: April 19, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Publication number: 20120041194
    Abstract: The present invention provides nitrogen and sulfur-containing heterocycle compounds to be used as scaffolds and, in particular, nitrogen and sulfur-containing heterocycle compounds having a thiomorpholine core. The compounds herein described may be useful in treating diseases such as diabetes, obesity, cancer, cardiovascular, Alzheimer's, inflammatory, antidepressant, rheumatoid arthritis, multiple sclerosis, allergic rhinitis, asthma as well as viral and bacterial infections. The compounds herein described may also be useful in treating CNS disorders such as but not limited to Schizophrenia, Alzheimer's disease (AD).
    Type: Application
    Filed: August 29, 2009
    Publication date: February 16, 2012
    Applicant: Triad Multitech Pharmaceuticals, Inc.
    Inventor: Murty N. Armilli
  • Publication number: 20110136777
    Abstract: Polymorphs of Ceftiofur sodium as a crystalline product and a process for the preparation of polymorphs of crystalline Ceftiofur sodium of formula (I).
    Type: Application
    Filed: August 20, 2009
    Publication date: June 9, 2011
    Applicant: Orchid Chemicals and Pharmaceuticals Limited
    Inventors: Senthilkumar Udayampalayam Palanisamy, Sivakumar Balasubramanian, Manimaran Arasappan, Meenakshi Sundaram Soma Sundaram, Sureshkumar Kanagaraj, Mohan Singaravel
  • Publication number: 20100317850
    Abstract: Disclosed is a compound represented by General formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt, which has an inhibitory activity of the production of A? or a BACE1-inhibiting activity, and is therefore useful as a prophylactic or therapeutic agent for A?-induced neurodegenerative diseases typified by Alzheimer-type dementia. Wherein the ring A represents a C6-14 aryl group or the like; L represents —NReCO— [wherein Re represents a hydrogen atom or the like] or the like; the ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a single bond or the like; Z represents a C1-3 alkylene group or the like; R1 and R2 independently represent a hydrogen atom or the like; and R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen atom or the like.
    Type: Application
    Filed: January 16, 2009
    Publication date: December 16, 2010
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Patent number: 7785375
    Abstract: Disclosed is a method of dyeing keratin-containing fibers comprising treating the fiber with at least one compound of formula (1), wherein R1, R2, R3, R4 independently from each other are hydrogen; hydroxy; —S—H; —S—C1-C12alkyl; halogen; C1-C12alkyl or C1-C12alkoxy, which may be substituted by one or more C1-C5alkyl, C1-C5-alkoxy, hydroxy, —(CO)—H or —(CO)—C1-C5alkyl; —NR5R6; —NO2; —(CO)H or (CO)—C1-C5alkyl; C6-C12aryl, C6-C12aryl-C1-C4alkyl or C6-C12aryl-C1-C4alkoxy, wherein the aryl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, —(CO)—H or —(CO)—C1-C5alkyl; R5 and R6 independently from each other are hydrogen; hydroxy; C1-C12alkyl; hydroxy-C1-C12alkyl; —(CO)—H; —(CO)—C1-C5alkyl; phenyl or phenyl-C1-C5alkyl, wherein the phenyl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, halogen, —NH2, mono-C1-C5alkylamino, di-C1-C5alkylamino, —NO2, carboxy or hydroxy; and An is an anion.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: August 31, 2010
    Assignee: Ciba Specialty Chemicals Corp.
    Inventors: Victor Paul Eliu, Beate Fröhling, Dominique Kauffmann
  • Patent number: 7776791
    Abstract: The invention relates to novel N-heterocyclylphenyl-substituted cyclic ketoenols of the formula (I) in which CKE, W, X, Y and Z are as defined in the disclosure, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides. The invention further relates to selective herbicidal compositions comprising firstly the N-heterocyclylphenyl-substituted cyclic ketoenols and secondly a compound which improves crop plant tolerance.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: August 17, 2010
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Stefan Lehr, Klaus Kunz, Jörg Konze, Olga Malsam, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann, Wahed Ahmed Moradi, Guido Bojack, Thomas Auler, Martin Hills, Heinz Kehne
  • Publication number: 20100166839
    Abstract: Non-peptidic renin inhibitors nitroderivatives of general formula (I): A1-(Xa—ONO2)j ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.
    Type: Application
    Filed: March 1, 2007
    Publication date: July 1, 2010
    Applicant: Nicox S.A
    Inventors: Nicoletta Almirante, Stefano Biondi, Ennio Ongini
  • Publication number: 20100063277
    Abstract: Cobalt (II) complexes of porphyrins are effective catalysts for intramolecular nitrene insertion of C—H bonds with arylsulfonyl azides. The cobalt-catalyzed process can proceed efficiently under mild and neutral conditions in low catalyst loading without the need of other reagents or additives, generating nitrogen gas as the only byproduct.
    Type: Application
    Filed: May 5, 2008
    Publication date: March 11, 2010
    Inventors: X. Peter Zhang, Joshua V. Ruppel
  • Publication number: 20100047172
    Abstract: Provided herein are imaging methods for detecting, diagnosing and imaging pathogenic bacteria or a pathophysiological condition associated therewith using fluorescent, luminescent or colorimetric detection agents, e.g., fluorogenic substrates for bacterial enzymes, caged luciferins and fluorescent proteins, luciferases and enzymes expressed by recombinant bacteria. Signals emitted by the fluorescent, luminescent or colorimetric detection agents in the presence of the bacteria are compared to controls to detect and locate the pathogenic bacteria. Also provided is a method for screening therapeutic agents to treat the pathophysiological conditions by measuring fluorescence or luminescence emitted from the detection agents in the presence and absence of the potential therapeutic agent. In addition, a method for detecting a pathogenic bacteria via PET or SPECT imaging using a positron-emitting or gamma-emitting substrate for a beta-lactamase or other enzyme or protein of the pathogenic bacteria.
    Type: Application
    Filed: August 6, 2009
    Publication date: February 25, 2010
    Inventors: Jeffrey D. Cirillo, Jianghong Rao
  • Publication number: 20100040548
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: June 10, 2009
    Publication date: February 18, 2010
    Inventor: Chongxi Yu
  • Publication number: 20100004231
    Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
    Type: Application
    Filed: July 1, 2009
    Publication date: January 7, 2010
    Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
  • Publication number: 20090300855
    Abstract: Disclosed is a method of dyeing keratin-containing fibers comprising treating the fiber with at least one compound of formula (1), wherein R1, R2, R3, R4 independently from each other are hydrogen; hydroxy; —S—H; —S—C1-C12alkyl; halogen; C1-C12alkyl or C1-C12alkoxy, which may be substituted by one or more C1-C5alkyl, C1-C5-alkoxy, hydroxy, —(CO)—H or —(CO)—C1-C5alkyl; —NR5R6; —NO2; —(CO)H or (CO)—C1-C5alkyl; C6-C12aryl, C6-C12aryl-C1-C4alkyl or C6-C12aryl-C1-C4alkoxy, wherein the aryl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, —(CO)—H or —(CO)—C1-C5alkyl; R5 and R6 independently from each other are hydrogen; hydroxy; C1-C12alkyl; hydroxy-C1-C12alkyl; —(CO)—H; —(CO)—C1-C5alkyl; phenyl or phenyl-C1-C5alkyl, wherein the phenyl moiety may be substituted by one or more C1-C5alkyl, C1-C5alkoxy, halogen, —NH2, mono-C1-C5alkylamino, di-C1-C5alkylamino, —NO2, carboxy or hydroxy; and An is an anion.
    Type: Application
    Filed: June 21, 2006
    Publication date: December 10, 2009
    Inventors: Victor Paul Eliu, Beate Fröhling, Dominique Kauffmann
  • Patent number: 7579343
    Abstract: 1H-Pyrrolo-1,4-thiazines and a process for the preparation thereof are described. These compounds are useful as enzyme inhibitors in cells, particularly for medical uses.
    Type: Grant
    Filed: September 6, 2006
    Date of Patent: August 25, 2009
    Assignee: Board of Trustees of Michigan State University
    Inventors: Rawle Hollingsworth, Li Gao
  • Publication number: 20090209755
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Application
    Filed: January 16, 2009
    Publication date: August 20, 2009
    Inventors: Yuichi SUZUKI, Takafumi MOTOKI, Toshihiko KANEKO, Mamoru TAKAISHI, Tasuku ISHIDA, Yoichi KITA, Kunitoshi TAKEDA, Noboru YAMAMOTO, Afzal KHAN, Paschalis DIMOPOULOS
  • Publication number: 20090118498
    Abstract: A method for increasing ozone concentration in a liquid can include: providing a gas having ozone; introducing the ozone-containing gas into a liquid, wherein the liquid and ozone combination has a temperature between about 0.8 and about 1.5 times the critical temperature of ozone; and increasing isothermally, the pressure of the ozone-containing gas above the liquid to about 0.3 to about 5 times the critical pressure of ozone so as to increase the ozone concentration in the liquid. The temperature is expressed in absolute units (Kelvin or Rankin). The method can be used for removing ozone from a gas or for purifying ozone. The liquid having a high ozone concentration can be used for ozonolysis of a substrate.
    Type: Application
    Filed: November 4, 2008
    Publication date: May 7, 2009
    Inventors: Bala Subramaniam, Daryle Busch, Andrew M. Danby, Thomas P. Binder
  • Publication number: 20090113639
    Abstract: Disclosed are thiol dyes of formula (1), wherein R1 is hydrogen; C1-C12alkyl; or phenyl-C1-C4alkyl; X is C1-C12alkylene; C2-C12alkenylene; C5-C10cycloalkylene; C5-C10arylene; or C5-C10arylene-C1-C10alkylene; Y is the residue of an organic dye which corresponds to the formula (1a), wherein R2 is hydrogen; or C1-C5alkyl; R3 is a radical of formula (1a1): (1a2); or (1a3); or R2 and R3 together with the linking carbon atom 1C form a 6 to 10 membered carbocyclic ring which may optionally be a condensated aromatic system and may contain one or more than one hetero atom; and R4, R5 and R6 independently form each other are hydrogen, or C1-C5alkyl; Z is H; or a thio ester group of formula (1b), wherein A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and A is O; S; or N—R9; B is —OR7; —NR7R8, or —SR7; and R7, R8 and R9, independently from each other are hydrogen; C1-C12alkyl C6-C12aryl; or C6-C12aryl-C1-C12alkyl.
    Type: Application
    Filed: September 27, 2006
    Publication date: May 7, 2009
    Inventors: Victor Paul Eliu, Beate Frohling, Achim Buhrer
  • Publication number: 20090036433
    Abstract: Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials.
    Type: Application
    Filed: December 15, 2006
    Publication date: February 5, 2009
    Inventors: Nathalie Caileau, David Thomas Davies, Alan Joseph Hennessy, Graham Elgin Jones, Timothy James Miles, Neil David Pearson
  • Publication number: 20090012054
    Abstract: The present invention provides a compound of the formula [I]: wherein R1 is lower alkyl, etc. and R2 is hydrogen, etc., or R1 and R2 are bonded together to form lower alkylene; R3 is a group represented by wherein R6 and R7 are independently optionally protected amino, etc.; m and n are independently an integer of 0 to 6; R8 and R9 are independently optionally protected amino, etc., and q and r are independently an integer of 0 to 6, or R8 and R9, together with the adjacent alkylene(s) and the nitrogen atom, form saturated nitrogen-containing heterocycle optionally having substituent(s); R4 is lower alkyl, etc.; and R5 is amino, etc., or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 16, 2007
    Publication date: January 8, 2009
    Applicants: ASTELLAS PHARMA INC., WAKUNAGA PHARMACEUTICAL CO. LTD.
    Inventors: Toshio Yamanaka, Ayako Toda, Hidenori Ohki, Shinya Okuda, Kohji Kawabata, Kenji Murano, Kazuo Hatano, Shinobu Takeda, Toru Nakai, Masaru Oogaki, Satoshi Inoue, Keiji Misumi, Kenji Itoh