The Polycyclo Ring System Is Tricyclo-carbocyclic Patents (Class 546/203)
  • Patent number: 8957212
    Abstract: There is intended to provide the novel compounds which generate a base easily when irradiated with long wavelength light (active energy rays), a photobase generator containing the compounds and a photobase generation method, and the present invention relates to the compounds represented by the general formula [1], a photobase generator containing the compounds and a photobase generation method: (wherein, Ar represents any of groups with specific structures selected from the group consisting of an anthracenyl group, an anthraquinonyl group and a pyrenyl group; R1 and R2 each independently represent a hydrogen atom or a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, or represent ones which can form an alicyclic ring containing nitrogen atom(s) or an aromatic ring containing nitrogen atom(s) together with a nitrogen atom to which they are bound, which the rings having 3 to 8 carbon atoms which may have a substituent, R3 and R4 each independently represent a hydrogen atom, a linear, branc
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: February 17, 2015
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Ayako Kuramoto, Motoshige Sumino, Nobuhiko Sakai
  • Patent number: 8946682
    Abstract: The present invention relates to novel donor-acceptor fluorene compounds, which can be used as for the fabrication of electroluminescent devices, and a process of preparing said novel compounds. More particularly, the present invention relates to amine donor and nitrile/ester acceptor fluorenes, fluorenones their ?-conjugated systems and related compounds, processes for preparing the said compounds including oxidation of fluorenes to corresponding fluorenones and their use in preparing organic electronic devices such as organic light emitting diodes (OLEDs), photovoltaic/solar cell, Field effect transistors and other useful electroluminescent devices. The compounds are prepared by reacting 2H-pyran-2-ones in isolated or rigid conformations with cyclic ketones containing methylene carbonyl moiety in the presence of a base in an organic solvent.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 3, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Atul Goel, Sumit Chaurasia, Vijay Kumar, Sundar Manoharan, R. S. Anand
  • Publication number: 20150004544
    Abstract: A photoresist composition containing: a polymer including an acid-labile group; a radiation-sensitive acid generator; and an acid diffusion control agent that contains a compound represented by a formula (1). In the formula (1), R1, R2 and R3 each independently represent a hydrogen atom or a monovalent hydrocarbon group having 1 to 10 carbon atoms. A represents a group having a valency of n that is obtained by combining: a hydrogen atom, a linear hydrocarbon group having 1 to 30 carbon atoms, an alicyclic hydrocarbon group having 3 to 30 carbon atoms or a combination thereof; —O—, —CO—, —COO—, —SO2O—, —NRSO2—, —NRSO2O—, —NRCO— or a combination thereof; and n nitrogen atoms as a binding site to the carbonyl group in the formula (1), in which a sum of atomic masses of the atoms constituting A is no less than 120. n is an integer of 1 to 4.
    Type: Application
    Filed: September 15, 2014
    Publication date: January 1, 2015
    Applicant: JSR CORPORATION
    Inventor: Hayato NAMAI
  • Publication number: 20140371207
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: December 13, 2013
    Publication date: December 18, 2014
    Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Patent number: 8822692
    Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: September 2, 2014
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite, S.p.A.
    Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
  • Patent number: 8822679
    Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: September 2, 2014
    Assignee: California Institute of Technology
    Inventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
  • Publication number: 20140213578
    Abstract: Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 31, 2014
    Applicant: MT. SINAI SCHOOL OF MEDICINE
    Inventors: Michael Ohlmeyer, Goutham Narla, Neil Dhawan, David Kastrinsky
  • Publication number: 20140178374
    Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
    Type: Application
    Filed: August 17, 2012
    Publication date: June 26, 2014
    Applicants: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, EMORY UNIVERSITY
    Inventors: Xingming Deng, Jia Zhou, Chunyong Ding
  • Patent number: 8716312
    Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: May 6, 2014
    Assignee: Merck Sharp & Dohme Corporation
    Inventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
  • Publication number: 20130310558
    Abstract: Methods for the synthesis and use of functionalized, substituted naphthalenes are described. The functionalized, substituted naphthalenes display useful properties including liquid crystals and fluorescence properties, such as solvatochromatic fluorescence, with high quantum yields, Stoke's shift, and show emission maxima that are significantly red-shifted.
    Type: Application
    Filed: March 15, 2013
    Publication date: November 21, 2013
    Inventor: Key M. Brummond
  • Publication number: 20130310423
    Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.
    Type: Application
    Filed: July 26, 2013
    Publication date: November 21, 2013
    Applicant: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
  • Patent number: 8586611
    Abstract: This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, (1) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula (1) where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: November 19, 2013
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renee Marie Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
  • Patent number: 8377968
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: February 19, 2013
    Assignee: Zalicus Pharmaceuticals, Ltd.
    Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, Mike Grimwood, Jason Tan, Yuanxi Zhou
  • Publication number: 20130012701
    Abstract: A compound useful as a building block for the manufacture of various compounds is represented by Formula A or D. In Formula A and D, z is 0 or 1; Q is a heteroatom; R1 through R11 and Ra through Rf are each independently hydrogen, a substituted or unsubstituted hydrocarbyl group, a substituted or unsubstituted heteroatom containing hydrocarbyl group, or a functional group; d, e and f are each independently 0 or greater; each of A, B and D is independently a carbon atom or a heteroatom; and two or more of R1 though R11, Ra through Rf and Y optionally combine to form a ring. In some embodiments, R8 and R9 combine to form a carbonyl group. In some embodiments, R2 and Y combine to form a ring with the Q atom. In some embodiments, the ring includes at least one double bond.
    Type: Application
    Filed: June 22, 2012
    Publication date: January 10, 2013
    Applicant: California Institute of Technology
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Patent number: 8334305
    Abstract: Novel substituted amide inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: December 18, 2012
    Assignee: High Point Pharmaceuticals, LLC
    Inventor: Soren Ebdrup
  • Publication number: 20120302539
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 29, 2012
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
  • Publication number: 20120285538
    Abstract: The present invention provides a dye compound of formula (I) or a salt thereof and a dye-sensitized solar cell using the dye compound: wherein R1 and R2 are, independently, H, C1-C12alkoxy or a halogen; and D1 and D2 are, independently, C1-C12alkyl, or D1, D2 and N form one of The dye compound is applicable to a dye-sensitized solar cell for increasing photoelectric efficiency of the dye-sensitized solar cell.
    Type: Application
    Filed: July 12, 2011
    Publication date: November 15, 2012
    Applicant: EVERLIGHT USA, INC.
    Inventors: Wei-Cheng Tang, Szu-Yu Lin
  • Patent number: 8278329
    Abstract: The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc. comprising the compound represented by the following general formula (1) or its analogue to a patient in need of such treatment: wherein, A represents CH?CH, etc., a, b, c and d represents CH etc., R1, R2, R3, R4, R5 and R6 represents H etc., V—W represents C?C, etc., n represents 0 to 3, Y1 represents O etc., B represents —(CH2)vCHR21 wherein v is 0 to 3, R21 represents H, a lower alkyl group or the like, etc., G represents —CO—, a covalent bond, etc., m is 0 to 6, R7 and R8 represents H, a lower alkyl group, —COR18a, —COOR20 wherein R18a and R20 each represents a lower alkyl group or the like, etc.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: October 2, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takashi Yamamoto, Seiji Niwa, Kayo Otani, Seiji Ohno, Hajime Koganei, Satoshi Iwayama, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Shinichi Fujita, Keiko Moki
  • Patent number: 8278321
    Abstract: The present disclosure characterizes the activity of Golgicide A (GCA), as a potent, specific and reversible small molecule inhibitor of Golgi BFA resistance factor 1 (GBF1) function. A mutant GBF1 gene that is resistant to GCA is also described. Methods of using GCA and the GCA-resistant GBF1 gene are described including methods for modulating GBF1 activity for research and therapeutic purposes. Also described are compositions incorporating a GCA-resistant GBF1.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: October 2, 2012
    Assignee: Washington University
    Inventor: David B. Haslam
  • Patent number: 8188288
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: May 29, 2012
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
  • Patent number: 8106191
    Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: January 31, 2012
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
  • Publication number: 20110269747
    Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.
    Type: Application
    Filed: July 13, 2011
    Publication date: November 3, 2011
    Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
  • Publication number: 20110269736
    Abstract: The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.
    Type: Application
    Filed: July 24, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
  • Publication number: 20110233048
    Abstract: There is intended to provide the novel compounds which generate a base easily when irradiated with long wavelength light (active energy rays), a photobase generator containing the compounds and a photobase generation method, and the present invention relates to the compounds represented by the general formula [1], a photobase generator containing the compounds and a photobase generation method: (wherein, Ar represents any of groups with specific structures selected from the group consisting of an anthracenyl group, an anthraquinonyl group and a pyrenyl group; R1 and R2 each independently represent a hydrogen atom or a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, or represent ones which can form an alicyclic ring containing nitrogen atom(s) or an aromatic ring containing nitrogen atom(s) together with a nitrogen atom to which they are bound, which the rings having 3 to 8 carbon atoms which may have a substituent, R3 and R4 each independently represent a hydrogen atom, a linear, branc
    Type: Application
    Filed: December 1, 2009
    Publication date: September 29, 2011
    Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.
    Inventors: Ayako Kuramoto, Motoshige Sumino, Nobuhiko Sakai
  • Publication number: 20110210315
    Abstract: The present invention relates to novel donor-acceptor fluorene compounds, which can be used as for the fabrication of electroluminescent devices, and a process of preparing said novel compounds. More particularly, the present invention relates to amine donor and nitrile/ester acceptor fluorenes, fluorenones their ?-conjugated systems and related compounds, processes for preparing the said compounds including oxidation of fluorenes to corresponding fluorenones and their use in preparing organic electronic devices such as organic light emitting diodes (OLEDs), photovoltaic/solar cell, Field effect transistors and other useful electroluminescent devices. The compounds are prepared by reacting 2H-pyran-2-ones in isolated or rigid conformations with cyclic ketones containing methylene carbonyl moiety in the presence of a base in an organic solvent.
    Type: Application
    Filed: September 30, 2010
    Publication date: September 1, 2011
    Inventors: Atul GOEL, Sumit CHAURASIA, Vijay KUMAR, Sundar MANOHARAN, R.S. ANAND
  • Patent number: 7985759
    Abstract: The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined. The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: July 26, 2011
    Assignee: Matrix Laboratories Ltd.
    Inventors: Gopalan Balasubramanian, Ravi Dhamjewar, Rasheed Mohammed, Sreedhara Swamy Keshavapura Hosamane, Ishtiyaque Ahmad
  • Publication number: 20110039853
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: February 19, 2008
    Publication date: February 17, 2011
    Inventor: Soren Ebdrup
  • Publication number: 20100331366
    Abstract: Novel substituted amide inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: February 19, 2008
    Publication date: December 30, 2010
    Applicant: High Point Pharmaceuticals ,LLC
    Inventor: Soren Ebdrup
  • Publication number: 20100292215
    Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
    Type: Application
    Filed: March 27, 2007
    Publication date: November 18, 2010
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Soren Ebdrup, Henrik Sune Andersen
  • Publication number: 20100222387
    Abstract: The present invention is directed to 3-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Application
    Filed: June 21, 2006
    Publication date: September 2, 2010
    Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhi-Qiang Yang
  • Patent number: 7772251
    Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.
    Type: Grant
    Filed: May 17, 2004
    Date of Patent: August 10, 2010
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
  • Publication number: 20100191475
    Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.
    Type: Application
    Filed: March 4, 2010
    Publication date: July 29, 2010
    Inventors: Scott Perschke, Ming Liu
  • Publication number: 20090325932
    Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11 ?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g the metabolic syndrome.
    Type: Application
    Filed: June 28, 2007
    Publication date: December 31, 2009
    Inventors: Soren Ebdrup, Henrik Sune Andersen
  • Publication number: 20090281081
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: May 6, 2009
    Publication date: November 12, 2009
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Publication number: 20090227631
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Application
    Filed: November 22, 2006
    Publication date: September 10, 2009
    Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
  • Patent number: 7432284
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: September 15, 2003
    Date of Patent: October 7, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Robert R. Wilkening, Dongfang Meng, Ronald W. Ratcliffe
  • Publication number: 20080207908
    Abstract: Disclosed are processes for the synthesis of piperidinyl-substituted urea compounds. This invention further relates to novel intermediates prepared during this synthesis.
    Type: Application
    Filed: January 28, 2008
    Publication date: August 28, 2008
    Inventor: Richard D. Gless
  • Publication number: 20080176838
    Abstract: The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.
    Type: Application
    Filed: June 8, 2005
    Publication date: July 24, 2008
    Applicant: SANTHERA PHARMACEUTICALS (DEUTSCHLAND) AG
    Inventors: Paul John Edwards, Silvia Cerezo-Galvez, Achim Feurer, Oliver Hill, Meinolf Thiemann, Victor Giulio Matassa, Sonja Nordhoff, Meritxell Lopez-Canet
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7351720
    Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: April 1, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Soo S. Ko, George V. Delucca
  • Patent number: 7282587
    Abstract: A process for preparing 10,11-dihydro-5H-dibenzo[a,d]cyclohept-5-enes (e.g. loratadine) by reacting a dibenzozuberone with an aliphatic ketone in the presence of low valent titanium.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: October 16, 2007
    Assignee: Robalo, S.L.
    Inventor: William Paul Jackson
  • Patent number: 7250519
    Abstract: The invention relates to a method for the production of tertiary amines by reaction of secondary amines with aromatics or heteroaromatics in the presence of a base, a nickel or palladium compound and one or several phosphines, dialkoxy-, and/or diaryloxyphosphines in an inert solvent. Aromatic or heteroaromatics of this type play an important role in industry as reagents or intermediates for pharmaceuticals and agrochemicals and in diverse fine and electronics chemicals, above all in the rapidly growing field of organic semi-conductors, in particular in organic or polymeric light diodes, organic solar cells and organic ICs.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: July 31, 2007
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stössel, Hubert Spreitzer, Heinrich Becker
  • Patent number: 7164025
    Abstract: The present invention pertains to a process for obtaining a single enantiomer, d or l, of threo-methylphenidate, comprising resolution of a mixture of the enantiomers; racemisation of the unwanted enantiomer, to give a mixture of all four stereoisomers; and separation of the erythro stereoisomers, to leave the same mixture of enantiomers for resolution.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: January 16, 2007
    Assignee: Celltech Pharma Europe Limited
    Inventors: Marianne Langston, Hooshang Shahriari Zavareh
  • Patent number: 7053071
    Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: May 30, 2006
    Assignee: The Burnham Institute
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
  • Patent number: 6969724
    Abstract: Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: wherein X and Y are selected independently from hydrogen and aryl, which aryl is unsubstituted or substituted one or more times by hydroxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aryl, heterocyclyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkoxy, C1-6alkyl, C1-6alkoxy or halo, which alkyl or alkoxy groups are unsubstituted or substituted one or more times by halo; m and n are independently 0 to 3, provided that m and n are not both 0; A represents a single bond or is —(CRpa Rpb)p— wherein p is 1-3 and Rpa and Rpb are selected independently from hydrogen, C1-6alkyl, C1-6alkoxy and halo, which alkyl or alkoxy groups are independently substituted one or more times by halo; B represents a C4-8 saturated or unsaturated ring, which ring is unsubstituted or substituted one or more times by C1-6alkyl, C1-6alkoxy, aryl, aryloxy, hydroxy, oxo, halo, amino, C1-6alkylamino, di(C1-6 alkyl)amino, and C1-6alkylamido, which C1-6alkyl
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: November 29, 2005
    Assignee: SmithKline Beecham-SpA
    Inventors: Daniela Barlocco, Giorgio Cignarella, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Silvano Ronzoni
  • Patent number: 6800636
    Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: October 5, 2004
    Assignee: Schering Corporation
    Inventors: Timothy Guzi, Dinanath F. Rane, Alan K. Mallams, Alan B. Cooper, Ronald J. Doll, Viyyoor M. Girijavallabhan, Arthur G. Taveras, Corey Strickland, Joseph M. Kelly, Jianping Chao
  • Publication number: 20040180884
    Abstract: The present invention discloses a dibenzocycloheptene compound represented by the formula (I): 1
    Type: Application
    Filed: December 23, 2003
    Publication date: September 16, 2004
    Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Ichiro Tanaka, Masayuki Tanaka, Masahiko Hagihara
  • Publication number: 20040152689
    Abstract: 4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed.
    Type: Application
    Filed: November 13, 2003
    Publication date: August 5, 2004
    Applicant: Euro-Celtique, S.A.
    Inventor: Zhengming Chen
  • Patent number: RE42700
    Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: September 13, 2011
    Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State University
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs