Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/476)
  • Patent number: 9969690
    Abstract: Cure accelerators for anaerobic curable compositions, such as adhesives and sealants, are provided, and which are defined with reference to the compounds shown in structure I where A is CH2 or benzyl, R is C1-10 alkyl, R? is H or C1-10 alkyl, or R and R? taken together may form a four to seven membered ring fused to the benzene ring, R? is optional, but when R? is present, R? is halogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, hydroxyalkenyl, alkoxy, amino, alkylene- or alkenylene-ether, alkylene (meth)acrylate, carbonyl, carboxyl, nitroso, sulfonate, hydroxyl or haloalkyl, and EWG is as shown, an electron withdrawing group, such as nitro, nitrile, carboxylate or trihaloalkyl.
    Type: Grant
    Filed: March 8, 2017
    Date of Patent: May 15, 2018
    Assignee: Henkel IP & Holding GmbH
    Inventor: Philip T. Klemarczyk
  • Patent number: 8940722
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: January 27, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Olaf Kinzel, Christoph Steeneck, Gerald Kleymann, Michael Albers, Thomas Hoffmann, Claus Kremoser, Sanja Perovic-Ottstadt, Thomas Schlüter
  • Patent number: 8933066
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: January 13, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Li-Qiang Sun, Paul Michael Scola
  • Patent number: 8859762
    Abstract: Chlorinated aromatic compounds are prepared by ultrasonicating a mixture of ICl and an aromatic compound.
    Type: Grant
    Filed: November 26, 2010
    Date of Patent: October 14, 2014
    Assignee: Peking University
    Inventors: Yu Wei, Xiangyun Wang
  • Patent number: 8809347
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: August 19, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
  • Patent number: 8809364
    Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: August 19, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
  • Patent number: 8754190
    Abstract: The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
    Type: Grant
    Filed: May 5, 2011
    Date of Patent: June 17, 2014
    Assignee: Prolynx LLC
    Inventors: Gary Ashley, Daniel V. Santi
  • Patent number: 8741943
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: June 3, 2014
    Assignee: Tobira Therapeutics, Inc.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
  • Publication number: 20130287687
    Abstract: The present disclosure relates to organic chemistry and in particular to a series of corticotropin releasing factor type-1 (CRF1) receptor ligand compounds and compositions, as well as methods of preparation and treatment.
    Type: Application
    Filed: April 30, 2013
    Publication date: October 31, 2013
    Inventor: EMORY UNIVERSITY
  • Publication number: 20130281468
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: June 14, 2013
    Publication date: October 24, 2013
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
  • Publication number: 20130280172
    Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. The cyanine compounds of Formula I are presented: wherein Q is a portion of a polymethine bridge: Also included are bioconjugates of the compounds of Formula I, methods of labeling biomolecules with the compounds, and methods of imaging.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 24, 2013
    Inventor: LI-COR, INC.
  • Publication number: 20130237686
    Abstract: The present application is directed to rapid and efficient synthesis of radiometal-labeled probes, pharmaceutical compositions comprising radiometal-labeled probes, and methods of using the radiometal-labeled probes. Such radiometal-labeled probes can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT), and therapy studies.
    Type: Application
    Filed: March 6, 2013
    Publication date: September 12, 2013
    Applicant: University of Southern California
    Inventors: Kai CHEN, Peter Stephen CONTI
  • Patent number: 8513433
    Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: August 20, 2013
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
  • Publication number: 20130123487
    Abstract: The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.
    Type: Application
    Filed: May 5, 2011
    Publication date: May 16, 2013
    Applicant: PROLYNX LLC
    Inventors: Gary Ashley, Daniel V. Santi
  • Publication number: 20130116407
    Abstract: The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
    Type: Application
    Filed: May 5, 2011
    Publication date: May 9, 2013
    Inventors: Gary Ashley, Daniel V. Santi
  • Patent number: 8362164
    Abstract: The embodiments of the invention relate to a multifunctional lithiated amine-containing compound comprising at least two molecules of lithiated amine in a molecule of the compound. In one embodiment, the compound has a formula where x is an integer of 1 or more, Q is (a) an element selected from the group consisting of O, S, N, P and Si or (b) an alkylene group having from 1 to 20 methylene groups, and R1 and R2 are the same or different and are selected from the group consisting of alkyls, cycloalkyls and aralkyls containing from 1 to 20 carbon atoms. In another embodiment, the compound comprises cyclic lithio amines and has a formula: where x is 1 or more, R3, R4 and R5 are the same or different and represent alkylene groups containing from 3 to 20 carbon atoms.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: January 29, 2013
    Assignee: Bridgestone Corporation
    Inventor: Yan Yan-Yong
  • Patent number: 8362058
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: January 29, 2013
    Assignee: Tobira Therapeutics, Inc.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
  • Publication number: 20120283284
    Abstract: The present invention relates to pharmaceutical technical field, to melonine bisindole compounds, pharmaceutical compositions thereof, and preparation methods thereof. Specifically, the present invention relates to melonine bisindole compounds of Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts thereof. The present invention further relates to method for preparing the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof, and the use of the melonine bisindole compounds of Formula I or pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of cancers.
    Type: Application
    Filed: November 4, 2010
    Publication date: November 8, 2012
    Applicant: Kunming Institute of Botany, The Chinese Academy of Sciences
    Inventors: Xiaodong Luo, Tao Feng, Yan Li, Yuanyuan Wang, Xianghai Cai, Yaping Liu
  • Publication number: 20120276051
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: July 9, 2012
    Publication date: November 1, 2012
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20120277422
    Abstract: Chlorinated aromatic compounds are prepared by ultrasonicating a mixture of ICl and an aromatic compound.
    Type: Application
    Filed: November 26, 2010
    Publication date: November 1, 2012
    Inventors: Yu Wei, Xiangyun Wang
  • Publication number: 20120238745
    Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Application
    Filed: January 9, 2012
    Publication date: September 20, 2012
    Applicant: AnaSpec Incorporated
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
  • Publication number: 20120232028
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Application
    Filed: May 21, 2012
    Publication date: September 13, 2012
    Applicant: Tobira Therapeutics, Inc.
    Inventors: Mitsuru SHIRAISHI, Masanori BABA, Katsuji AIKAWA, Naoyuki KANZAKI, Masaki SETO, Yuji IIZAWA
  • Publication number: 20120184533
    Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.
    Type: Application
    Filed: July 2, 2010
    Publication date: July 19, 2012
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
  • Patent number: 8188306
    Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: May 29, 2012
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Gang Shen
  • Patent number: 8183273
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: May 22, 2012
    Assignee: Tobira Therapeutics, Inc.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
  • Patent number: 8163790
    Abstract: Cocrystals of metronidazole are described herein. Such cocrystals are a cocrystal of metronidazole with gentisic acid and a cocrystal of metronidazole with gallic acid. Cocrystals of imipramine hydrochloride are also described. Such cocrystals are a cocrystal of imipramine hydrochloride with (+)-camphoric acid, a cocrystal of imipramine hydrochloride with fumaric acid, and a cocrystal of imipramine hydrochloride with 1-hydroxy-2-naphthoic acid.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: April 24, 2012
    Assignee: New Form Pharmaceuticals, Inc.
    Inventor: Scott Lawrence Childs
  • Publication number: 20120070409
    Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.
    Type: Application
    Filed: February 3, 2011
    Publication date: March 22, 2012
    Applicant: Japan Tobacco Inc.
    Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
  • Publication number: 20110305636
    Abstract: Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).
    Type: Application
    Filed: March 12, 2010
    Publication date: December 15, 2011
    Applicant: EMORY UNIVERSITY
    Inventors: Jeff Stehouwer, Mark Goodman, Clint Kilts, Charles Nemeroff
  • Publication number: 20110237567
    Abstract: This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
    Type: Application
    Filed: October 12, 2007
    Publication date: September 29, 2011
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Ranjender Kamboj
  • Publication number: 20110183986
    Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.
    Type: Application
    Filed: April 1, 2011
    Publication date: July 28, 2011
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
  • Patent number: 7968553
    Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: June 28, 2011
    Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
  • Patent number: 7964722
    Abstract: Compounds of Formula (1) are disclosed. Cb is a carbocyclic or heterocyclic group having an atom within the cyclic structure selected from C, N, Si, and Cr and singly bound to A. A is CR, COR, CSR, CNR2, CCN, CCONR2, CNO2, CNNAr, CX1, or N. Cr is a chromophore having a substantially planar cyclic structure. The compounds function as nanometer-scale rotary molecular motors powered and controlled by light energy. The design of the molecular motor devices is flexible so that the rotary direction, drive light wavelength, and other physical characteristics can be varied. The compounds can be chemically functionalized to allow it to be integrated into or attached to a variety of structures. The device can be used in applications where mechanical power, positional control, and information encoding are to be generated at the size scale of individual molecules.
    Type: Grant
    Filed: June 24, 2004
    Date of Patent: June 21, 2011
    Assignee: Board of Regents of the Nevada System of Higher Education, on behalf of the University of Nevada, Reno
    Inventors: Thomas W. Bell, Joseph I. Cline, Christine R. Cremo, Stephen L. Gillett, John H. Frederick
  • Publication number: 20110104287
    Abstract: Formulations of fenoldopam are disclosed for repeated administration or continued slow release administration, over prolonged periods of time or targeted slow and regulated delivery. The formulations include those formulations that increase the bioavailability of fenoldopam after oral intake, particularly lipid based nano dispersions and pronanodispersions and surfactant rich formulations. This may be accomplished by entrapment in nanoparticles or liposomal formulations or conjugation to a polymer or small molecule via a soft bond.
    Type: Application
    Filed: October 20, 2008
    Publication date: May 5, 2011
    Inventors: Mia Levite, Avi Domb
  • Publication number: 20110082130
    Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Application
    Filed: August 23, 2010
    Publication date: April 7, 2011
    Applicant: LIGAND PHARMACEUTICALS, INC.
    Inventors: Yang Gao, Bingsong Han, Yuelian Xu, Timothy M Caldwell, Linghong Xie
  • Publication number: 20100324266
    Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
    Type: Application
    Filed: June 9, 2010
    Publication date: December 23, 2010
    Applicant: Affymetrix, INC.
    Inventors: Anthony D. Barone, Glenn H. McGall
  • Patent number: 7842802
    Abstract: The present invention relates to novel vinorelbine derivatives. Pharmaceutical compositions containing these compounds as well as processes of preparation and processes of use for treatment of various conditions are also disclosed.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: November 30, 2010
    Assignee: Albany Molecular Research, Inc.
    Inventors: Ian L. Scott, Jeffrey M. Ralph, Matthew E. Voss
  • Publication number: 20100249106
    Abstract: Thiopheneprymidinone compounds useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.
    Type: Application
    Filed: June 8, 2010
    Publication date: September 30, 2010
    Applicant: SOLVAY PHARMACEUTICALS B.V.
    Inventors: Kristiina WAEHAELAE, Annamaria Lilienkampf, Sari Alho, Kaisa Huhtinen, Nina Johansson, Pasi Koskimies, Kimmo Vihko
  • Publication number: 20100234351
    Abstract: A compound of the formula: wherein ring A is a 7-membered or 8-membered nitrogen-containing ring optionally further substituted, ring B is an optionally substituted aryl group or an optionally substituted heteroaryl group, X1 is a group represented by —NR3—Y1—, —O—, —S—, —SO—, —SO2— or —CHR3— wherein R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 may be bonded to the carbon atom of ring B to form an optionally substituted ring structure, and Y1 is a bond or an optionally substituted alkylene, R1 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, the formula shows a single bond or a double bond, when R2 is —R2, R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, and when R2 is ?R2, R2 is an oxo group, an optionally substituted alkylidene group, or an optionally substituted imino group.
    Type: Application
    Filed: February 22, 2007
    Publication date: September 16, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masaki Seto, Tomohiro Ohashi
  • Publication number: 20100216988
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
    Type: Application
    Filed: December 22, 2009
    Publication date: August 26, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Omar RKYEK, Matthias URMANN, Nis HALLAND
  • Patent number: 7763691
    Abstract: Norbornene monomers with fluorene group and polymer material thereof are disclosed. The norbornene monomers with fluorene group are prepared by Diels-Alder reation. The Norbornene monomers containing fluorene groups are highly active for ring-opening-metathesis polymerization (ROMP), and the molecular weight and PDI value of the obtained polymers are controllable.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: July 27, 2010
    Assignee: National Taiwan University of Science & Technology
    Inventor: Der-Jang Liaw
  • Patent number: 7754709
    Abstract: Thiopheneprymidinone compounds useful in therapy, especially for use in the treatment and/or prevention of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: July 13, 2010
    Assignee: Solvay Pharmaceuticals BV
    Inventors: Kristiina Waehaelae, Annamaria Lilienkampf, Sari Alho, Kaisa Huhtinen, Nina Johansson, Pasi Koskimies, Kimmo Vihko
  • Publication number: 20100160291
    Abstract: This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
    Type: Application
    Filed: October 12, 2007
    Publication date: June 24, 2010
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Ranjender Kamboj
  • Patent number: 7741315
    Abstract: Tricyclic compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: June 22, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne, Richard C. A. Isaacs, Richard Pracitto
  • Publication number: 20100112090
    Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.
    Type: Application
    Filed: April 16, 2008
    Publication date: May 6, 2010
    Applicant: KISSEI PHARMACEUTICAL CO., LTD
    Inventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
  • Publication number: 20100113460
    Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 6, 2010
    Applicant: Givaudan SA
    Inventors: Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
  • Publication number: 20100076046
    Abstract: Compounds of the formula (I) wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.
    Type: Application
    Filed: December 19, 2007
    Publication date: March 25, 2010
    Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SPA
    Inventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
  • Patent number: 7662809
    Abstract: The present invention relates to tetracyclic indole compounds of formula (I); wherein R1, R2, R14, R15, A, Ar, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Grant
    Filed: October 25, 2005
    Date of Patent: February 16, 2010
    Assignee: Istituto di Richerche di Biologia Molecolare P Angeletti SpA
    Inventors: Caterina Ercolani, Joerg Habermann, Frank Narjes, Simona Ponzi, Michael Rowley, Ian Stansfield
  • Publication number: 20100016385
    Abstract: A process for formulating certain epothilones and analogs thereof for parenteral administration is provided wherein the pH of the formulation for administration can be controlled to enhance the stability and thus, potency of the epothilone, or analog thereof.
    Type: Application
    Filed: September 11, 2009
    Publication date: January 21, 2010
    Inventors: Thomas A. Haby, Uday S. Gogate, Vijay H. Naringrekar
  • Publication number: 20090270370
    Abstract: Certain fused pyrrole- and pyrazole-containing heterocyclic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: July 2, 2009
    Publication date: October 29, 2009
    Inventors: Nicholas I. Carruthers, Wenying Chai, Xiaohu Deng, Curt A. Dvorak, Annette K. Kwok, Jimmy T. Liang, Neelakandha Mani, Dale A. Rudolph, Victoria D. Wong
  • Patent number: 7605288
    Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: October 20, 2009
    Assignee: University of Kansas
    Inventors: Brian Blagg, Gang Shen, Randell C. Clevenger