Both Rings Which Form The Spiro Are Hetero Rings Patents (Class 548/409)
  • Patent number: 9302120
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: April 5, 2016
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Yujun Zhao, Wei Sun
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Patent number: 8980877
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: March 17, 2015
    Assignee: DAC S.R.L.
    Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
  • Publication number: 20150031691
    Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 29, 2015
    Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
  • Patent number: 8921576
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 30, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Patent number: 8877796
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: November 4, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
  • Publication number: 20140288045
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Publication number: 20140288042
    Abstract: This invention relates to compounds of Formula I having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R represents a fused bicyclic or spirocyclic aliphatic diamine and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 25, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato, Esther Y. Kim
  • Publication number: 20140288091
    Abstract: Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Application
    Filed: October 10, 2012
    Publication date: September 25, 2014
    Applicants: ASTRAZENECA AB, ASTRAZENECA AB
    Inventors: Anna Minidis, Fredrik Rahm, Jenny Viklund
  • Publication number: 20140256712
    Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 11, 2014
    Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.
    Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
  • Patent number: 8778925
    Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
    Type: Grant
    Filed: October 6, 2009
    Date of Patent: July 15, 2014
    Assignee: Cancer Research Technology Ltd.
    Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
  • Publication number: 20140187467
    Abstract: A dioxirane-containing compound has a first substituent that is an alkyl, polyalkoxy, aryl, heteroaryl, or heterocyclyl group, and a second substituent that is an electron withdrawing group, and where the first and second substituents can optionally join to form a cycloalkyl or heterocyclyl group. The dioxirane-containing compound can be used as an oxidant, surfactant, and/or an ionic liquid.
    Type: Application
    Filed: July 20, 2012
    Publication date: July 3, 2014
    Inventor: Kraig ANDERSON
  • Publication number: 20140147412
    Abstract: Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
    Type: Application
    Filed: July 9, 2012
    Publication date: May 29, 2014
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Jiancun Zhang, Yingjun Zhang, Hongming Xie, Qingyun Ren, Huichao Luo, Tianzhu Yu, Yumei Tan
  • Patent number: 8735385
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • Patent number: 8729063
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Patent number: 8697739
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: April 15, 2014
    Assignee: Novartis AG
    Inventors: David Weninger Barnes, Gregory Raymond Bebernitz, Kevin Clairmont, Scott Louis Cohen, Robert Edson Damon, Robert Francis Day, Stephanie Kay Dodd, Christoph Gaul, Hatice Belgin Gulgeze Efthymiou, Monish Jain, Rajeshri Ganesh Karki, Louise Clare Kirman, Kai Lin, Justin Yik Ching Mao, Tajesh Jayprakash Patel, Brian Kenneth Raymer, Liansheng Su
  • Patent number: 8686020
    Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher Hamblett, Joey L. Methot, Thomas Miller, David L. Sloman, Matthew G. Stanton, Paul Tempest, Anna A. Zabierek
  • Patent number: 8685958
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: April 1, 2014
    Assignee: AstraZeneca AB
    Inventor: Lars Anders Mikael Johansson
  • Patent number: 8680132
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: March 25, 2014
    Assignees: The Regents of the University of Michigan, Ascenta Licensing Corporation, Sanofi
    Inventors: Shaomeng Wang, Wei Sun
  • Patent number: 8664213
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: are useful as HIV attachment inhibitors.
    Type: Grant
    Filed: August 28, 2012
    Date of Patent: March 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, David R. Langley, John F. Kadow, Nicholas A. Meanwell
  • Patent number: 8608988
    Abstract: The present invention provides a curable, organic polymeric photochromic composition comprising: a photochromic amount of at least one photochromic material; a polymeric polyol having carbonate groups along its backbone and having a number average molecular weight greater than 5000 g/mole; and a curing agent having reactive functional groups capable of reacting with hydroxyl groups on the polymeric polyol. After curing and after the Photochromic Performance Test the composition demonstrates a T1/2 fade rate of less than 200 seconds. Also provided is a photochromic article comprising a rigid substrate and a photochromic organic polymeric coating applied to a surface of the substrate. The photochromic organic polymeric coating comprises the composition described above.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: December 17, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Steven E. Bowles, Cynthia Kutchko, Paul H. Lamers, Jason R. Lewis, David E. Sartori, Robert W. Walters, Feng Wang
  • Patent number: 8580161
    Abstract: Photochromic materials that are useful for a variety of applications, including for making various unit functions of fluidic devices, particularly microfluidic devices, such as microchannels, valves and gates, using spiropyran materials, such as a polymeric composition comprising a spiropyran. In certain disclosed embodiments the spiropyran is admixed with a polymeric material. For example, the spiropyran may be intercalated into a polyalkylene or polyalkylene phthalate. The spiropyran also may be polymerized with at least one additional monomer to form a heteropolymer, such as by polymerization with styrene, styrene derivatives, acrylate and acrylate derivatives. The spiropyran compositions can be used to make, for example, a photoactuatable valve, a fluidic channel, etc. The valve may be associated with a microchannel, including photochromic microchannel. In certain disclosed embodiments, the valve, at least one microchannel, or both, are re-patternable by light exposure.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: November 12, 2013
    Assignee: State of Oregon acting by and through the State Board of Higher Education on behalf of Oregon State University
    Inventors: Vincent Thomas Remcho, Jintana Nammoonnoy, Myra Koesdjojo
  • Publication number: 20130296554
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: March 13, 2013
    Publication date: November 7, 2013
    Inventors: Ny Sin, Zheng Liu, Jacob Swidorski, Sing-Yuen Sit, Jie Chen, Yan Chen, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Patent number: 8575208
    Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: November 5, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc Farmer, Randy Scott Bethiel, Dylan Jacobs, Robert B. Perni, John Maxwell, Kevin Cottrell, Summer Halas
  • Publication number: 20130196973
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. 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: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Publication number: 20130196998
    Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)a
    Type: Application
    Filed: July 8, 2011
    Publication date: August 1, 2013
    Applicant: AbbVie B.V.
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme
  • Publication number: 20130190288
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130184250
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Application
    Filed: July 13, 2012
    Publication date: July 18, 2013
    Applicant: ASTRAZENECA AB
    Inventor: Lars Anders Mikael Johansson
  • Publication number: 20130116230
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 9, 2013
    Applicant: INCYTE CORPORATION
    Inventor: Incyte Corporation
  • Publication number: 20130096277
    Abstract: A process for preparing enantioselectively a compound of formula I-1a or I-1b: over a compound of formulas I-2-I-7:
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130065877
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Application
    Filed: November 6, 2012
    Publication date: March 14, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130053377
    Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: February 23, 2011
    Publication date: February 28, 2013
    Applicant: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh Singh, Yajun Zheng
  • Patent number: 8287776
    Abstract: The present invention relates to a photochromic ink, the process for its preparation which is based on a spiropyran powder obtainable by melting, cooling and crushing, and to a new form of a spiropyran obtainable thereby. Said process to prepare a photochromic ink comprises the steps of a) heating and melting the spiropyran at a temperature below 250 C, b) cooling the melt to obtain a solidified spiropyran, c) crushing the solidified spiropyran to obtain a powder, d) optionally adding the powder to a binder providing the basis for the photochromic ink.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: October 16, 2012
    Assignee: BASF SE
    Inventors: Marc Maurer, Max Hügin, Thomas Raimann, Leonhard Feiler, Bruno Inderbitzin, André Fuchs
  • Patent number: 8288431
    Abstract: There is provided a compound of the formula wherein X, Y, W, R1, R2 and R3 are as described herein. The compounds have activity as anticancer agents.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: October 16, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jin-Jun Liu, Jing Zhang, Zhuming Zhang
  • Publication number: 20120258949
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: October 11, 2012
    Applicant: DAC S.r.I.
    Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
  • Patent number: 8222288
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: July 17, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Dongguang Qin, Jianyong Chen, Shanghai Yu
  • Patent number: 8217051
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, R1, R2 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: July 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jing Zhang, Zhuming Zhang
  • Publication number: 20120157432
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: August 17, 2010
    Publication date: June 21, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent j. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
  • Patent number: 8134017
    Abstract: A compound represented by the following formula (1) or (2):
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: March 13, 2012
    Assignee: Riken
    Inventors: Shinichiro Kamino, Shuichi Enomoto
  • Publication number: 20120027796
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).
    Type: Application
    Filed: November 10, 2009
    Publication date: February 2, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, David Butler, Jayaprakash K. Narayanannair, Muthusamy Jayaraman, Laxmab Eltepu
  • Patent number: 8088931
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: January 3, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
  • Publication number: 20110297898
    Abstract: The present invention relates to a photochromic ink, the process for its preparation which is based on a spiropyran powder obtainable by melting, cooling and crushing, and to a new form of a spiropyran obtainable thereby. Said process to prepare a photochromic ink comprises the steps of a) heating and melting the spiropyran at a temperature below 250 C, b) cooling the melt to obtain a solidified spiropyran, c) crushing the solidified spiropyran to obtain a powder, d) optionally adding the powder to a binder providing the basis for the photochromic ink.
    Type: Application
    Filed: December 23, 2009
    Publication date: December 8, 2011
    Applicant: BASF SE
    Inventors: Marc Maurer, Max Hügin, Thomas Raimann, Leonhard Feiler, Bruno Inderbitzin, André Fuchs
  • Publication number: 20110287549
    Abstract: The present invention relates to photochromic spiropyrans as active ingredients of Time-Temperature Indicators (TTIs), and to new spiropyrans per se. More particularly, the invention provides TTIs on the base of photochromic spiropyrans comprising alkylsulfanyl/arylsulfanyl substituents in the phenyl ring of the benzopyrane moiety.
    Type: Application
    Filed: February 9, 2010
    Publication date: November 24, 2011
    Applicant: FRESHPOINT HOLDINGS SA
    Inventors: Husein Salman, Elena Tenetov
  • Publication number: 20110272644
    Abstract: Photochromic materials that are useful for a variety of applications, including for making various unit functions of fluidic devices, particularly microfluidic devices, such as microchannels, valves and gates, using spiropyran materials, such as a polymeric composition comprising a spiropyran. In certain disclosed embodiments the spiropyran is admixed with a polymeric material. For example, the spiropyran may be intercalated into a polyalkylene or polyalkylene phthalate. The spiropyran also may be polymerized with at least one additional monomer to form a heteropolymer, such as by polymerization with styrene, styrene derivatives, acrylate and acrylate derivatives. The spiropyran compositions can be used to make, for example, a photoactuatable valve, a fluidic channel, etc. The valve may be associated with a microchannel, including photochromic microchannel. In certain disclosed embodiments, the valve, at least one microchannel, or both, are re-patternable by light exposure.
    Type: Application
    Filed: May 4, 2011
    Publication date: November 10, 2011
    Inventors: Vincent Thomas Remcho, Jintana Nammoonnoy, Myra Koesdjojo
  • Publication number: 20110269242
    Abstract: The present invention relates to time-temperature indicator (TTI) systems comprising indolenin based spiropyrans containing a cyclohexyl residue of formula (I), a method of manufacturing the time temperature indicator system, and a method of determining the time temperature history of perishable goods using the system. Moreover, the invention relates to a matrix selected from a printing ink or printing ink concentrate, paint, varnish, label, packaging material, and polymeric material comprising the system.
    Type: Application
    Filed: December 30, 2009
    Publication date: November 3, 2011
    Applicant: BASF SE
    Inventors: Hans Reichert, Max Hügin, Mathias Düggeli, Leonhard Feiler
  • Patent number: 8039503
    Abstract: The present invention provides novel tricyclic spiro-oxathiine naphthoquinone derivatives, a synthetic method for making the derivatives, and the use of the derivatives to induce cell death and/or to inhibit proliferation of cancer or precancerous cells. The naphthoquinone derivatives of the present invention are related to the compound known as ?-lapachone (3,4-dihydro-2,2-dimethyl-2H-naphtho(1,2-b)pyran-5,6-dione).
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: October 18, 2011
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed M. Ali, David Vensel, Chiang J. Li
  • Publication number: 20110237794
    Abstract: The present invention relates to spiro compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states such as cancers associated with protein tyrosine kinases, especially epidermal growth factor (EGF) and vascular endothelial growth factor (VEGF), to their method of use as medicaments and to their method of use in the manufacture of medicaments for use in the production of inhibition of tyrosine kinase reducing effects in warm-blooded animals such as humans.
    Type: Application
    Filed: June 1, 2011
    Publication date: September 29, 2011
    Inventor: GUOQING PAUL CHEN
  • Publication number: 20110166297
    Abstract: Molecularly imprinted smart polymers (MISPs) are provided herein, as well as novel monomers for preparing MISPs, and processes for preparing MISPs. The MISPs can be used applications such as, for example, detecting/absorbing or isolating biological and non-biological agents. The MISPs described herein comprise responsive monomeric units which undergo a physico-chemical change (e.g., a bond formation or cleavage) in response to an external change, such that the MISP selectively binds to a target molecule and releases a bound target molecule in response to the external change.
    Type: Application
    Filed: September 9, 2009
    Publication date: July 7, 2011
    Applicant: Sailo Nanotechnologies Ltd.
    Inventors: Flavio Grynszpan, Eran Partouche, Vladimir Shkoulev, Alex Aizikovich, Sharon Gazal, Rachel Nakash-Ozeri, Isaac Zigelboim
  • Publication number: 20110150757
    Abstract: The present invention relates to compounds of Formula (I), below, (wherein R1, R2, R3, R27, R28, R29, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
    Type: Application
    Filed: October 16, 2008
    Publication date: June 23, 2011
    Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana, Angie R. Angeles
  • Publication number: 20110139059
    Abstract: The present invention relates to time-temperature indicator (TTI) systems comprising indolenin based spiropyrans containing a N-acetylamido or N-acetylester side chain, especially to a time temperature indicator comprising at least one spiropyran indicator of formula (I) Wherein R1 is hydrogen, —C1-C18 alkoxy, —C1-C18 alkylthio, —C1-C18 alkyl-SO—, —C1-C18 alkyl-SO2—, phenylthio, phenyl, halogen, —C1-C18 alkylthio, —C1-C18 alkyl-SO—, —C1-C18 alkyl-SO2—, phenylthio, phenyl, halogen, —C1-C18 alkyl or —NO2; R2 is hydrogen or —C1-C18 alkoxy; R3 is NO2 or halogen; R4 is hydrogen, —C1-C18 alkoxy or halogen; R5 is hydrogen, halogen, —C1-C18 alkoxy, —COOH, —COO—C1-C18alkyl, —CF3 or phenyl; R6 is hydrogen or R6 and R7 form together a phenyl ring; R7 is hydrogen; Ra is hydrogen or —C1-C6 alkyl; Rb is hydrogen or —C1-C6 alkyl, or together with Ra form a 5-6 membered ring; Y is —CH2—COO—R8 or —CH2—CO—N(R10)—R9; or CH2—CO—N(R10)-L-N(R10) CO—CH2— or Y is —CH2—CO—O-L?-O—CO—CH2— wherein R8 is hydrogen, C3-C18alkyl or R8 is et
    Type: Application
    Filed: May 11, 2009
    Publication date: June 16, 2011
    Applicant: BASF SE
    Inventors: Leonhard Feiler, Thomas Raimann