The Polycyclo Ring System Is Tricyclo-carbocyclic Patents (Class 546/203)
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Patent number: 11886113Abstract: The present invention provides an actinic ray-sensitive or radiation-sensitive resin composition with which a pattern having an excellent pattern collapse suppressing property and excellent LWR performance can be obtained. In addition, the present invention also provides a resist film, a pattern forming method, and a method for manufacturing an electronic device, each regarding the actinic ray-sensitive or radiation-sensitive resin composition. The actinic ray-sensitive or radiation-sensitive resin composition of the present invention includes a resin whose solubility in a developer is changed by the action of an acid, a photoacid generator represented by General Formula (b1), and a solvent, in which the photoacid generator represented by General Formula (b1) is a compound that generates an acid having a pka of 1.Type: GrantFiled: August 26, 2020Date of Patent: January 30, 2024Assignee: FUJIFILM CorporationInventors: Keita Kato, Michihiro Shirakawa, Akiyoshi Goto, Takashi Kawashima, Masafumi Kojima
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Patent number: 8957212Abstract: 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, brancType: GrantFiled: December 1, 2009Date of Patent: February 17, 2015Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Ayako Kuramoto, Motoshige Sumino, Nobuhiko Sakai
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Patent number: 8946682Abstract: 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: GrantFiled: September 30, 2010Date of Patent: February 3, 2015Assignee: Council of Scientific & Industrial ResearchInventors: Atul Goel, Sumit Chaurasia, Vijay Kumar, Sundar Manoharan, R. S. Anand
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Publication number: 20150004544Abstract: 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: ApplicationFiled: September 15, 2014Publication date: January 1, 2015Applicant: JSR CORPORATIONInventor: Hayato NAMAI
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Publication number: 20140371207Abstract: 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: ApplicationFiled: December 13, 2013Publication date: December 18, 2014Applicants: 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
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Patent number: 8889716Abstract: 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: GrantFiled: May 7, 2012Date of Patent: November 18, 2014Assignee: CHDI Foundation, Inc.Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
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Patent number: 8822679Abstract: 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: GrantFiled: June 22, 2012Date of Patent: September 2, 2014Assignee: California Institute of TechnologyInventors: Brian M Stoltz, Scott C. Virgil, David E White, Taiga Yurino, Yiyang Liu, Douglas C Behenna, Douglas Duquette, Christian Eidamshaus
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Patent number: 8822692Abstract: 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: GrantFiled: July 26, 2013Date of Patent: September 2, 2014Assignee: Sigma-Tau Industrie Farmaceutiche Riunite, S.p.A.Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
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Publication number: 20140213578Abstract: 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: ApplicationFiled: August 16, 2012Publication date: July 31, 2014Applicant: MT. SINAI SCHOOL OF MEDICINEInventors: Michael Ohlmeyer, Goutham Narla, Neil Dhawan, David Kastrinsky
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Publication number: 20140178374Abstract: 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: ApplicationFiled: August 17, 2012Publication date: June 26, 2014Applicants: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, EMORY UNIVERSITYInventors: Xingming Deng, Jia Zhou, Chunyong Ding
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Patent number: 8716312Abstract: 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: GrantFiled: November 17, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme CorporationInventors: 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
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Publication number: 20130310423Abstract: 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: ApplicationFiled: July 26, 2013Publication date: November 21, 2013Applicant: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
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Publication number: 20130310558Abstract: 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: ApplicationFiled: March 15, 2013Publication date: November 21, 2013Inventor: Key M. Brummond
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Patent number: 8586611Abstract: 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: GrantFiled: July 26, 2006Date of Patent: November 19, 2013Assignee: E. I. du Pont de Nemours and CompanyInventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renee Marie Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
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Patent number: 8377968Abstract: 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: GrantFiled: April 8, 2009Date of Patent: February 19, 2013Assignee: Zalicus Pharmaceuticals, Ltd.Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, Mike Grimwood, Jason Tan, Yuanxi Zhou
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Publication number: 20130012701Abstract: 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: ApplicationFiled: June 22, 2012Publication date: January 10, 2013Applicant: California Institute of TechnologyInventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
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Patent number: 8334305Abstract: 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: GrantFiled: February 19, 2008Date of Patent: December 18, 2012Assignee: High Point Pharmaceuticals, LLCInventor: Soren Ebdrup
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Publication number: 20120302539Abstract: 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: ApplicationFiled: May 7, 2012Publication date: November 29, 2012Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
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Publication number: 20120285538Abstract: 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: ApplicationFiled: July 12, 2011Publication date: November 15, 2012Applicant: EVERLIGHT USA, INC.Inventors: Wei-Cheng Tang, Szu-Yu Lin
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Patent number: 8278329Abstract: 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: GrantFiled: October 26, 2007Date of Patent: October 2, 2012Assignee: 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
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Patent number: 8278321Abstract: 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: GrantFiled: December 22, 2009Date of Patent: October 2, 2012Assignee: Washington UniversityInventor: David B. Haslam
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Patent number: 8188288Abstract: 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: GrantFiled: November 22, 2006Date of Patent: May 29, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
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Patent number: 8106191Abstract: 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: GrantFiled: June 13, 2003Date of Patent: January 31, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
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Publication number: 20110269747Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: ApplicationFiled: July 13, 2011Publication date: November 3, 2011Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Publication number: 20110269736Abstract: 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: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
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Publication number: 20110233048Abstract: 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, brancType: ApplicationFiled: December 1, 2009Publication date: September 29, 2011Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.Inventors: Ayako Kuramoto, Motoshige Sumino, Nobuhiko Sakai
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Publication number: 20110210315Abstract: 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: ApplicationFiled: September 30, 2010Publication date: September 1, 2011Inventors: Atul GOEL, Sumit CHAURASIA, Vijay KUMAR, Sundar MANOHARAN, R.S. ANAND
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Patent number: 7985759Abstract: 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: GrantFiled: March 30, 2007Date of Patent: July 26, 2011Assignee: Matrix Laboratories Ltd.Inventors: Gopalan Balasubramanian, Ravi Dhamjewar, Rasheed Mohammed, Sreedhara Swamy Keshavapura Hosamane, Ishtiyaque Ahmad
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Publication number: 20110039853Abstract: 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: ApplicationFiled: February 19, 2008Publication date: February 17, 2011Inventor: Soren Ebdrup
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Publication number: 20100331366Abstract: 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: ApplicationFiled: February 19, 2008Publication date: December 30, 2010Applicant: High Point Pharmaceuticals ,LLCInventor: Soren Ebdrup
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Publication number: 20100292215Abstract: 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: ApplicationFiled: March 27, 2007Publication date: November 18, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20100222387Abstract: 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: ApplicationFiled: June 21, 2006Publication date: September 2, 2010Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhi-Qiang Yang
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Patent number: 7772251Abstract: 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: GrantFiled: May 17, 2004Date of Patent: August 10, 2010Assignee: The Medicines Company (Leipzig) GmbHInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
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Publication number: 20100191475Abstract: 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: ApplicationFiled: March 4, 2010Publication date: July 29, 2010Inventors: Scott Perschke, Ming Liu
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Publication number: 20090325932Abstract: 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: ApplicationFiled: June 28, 2007Publication date: December 31, 2009Inventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20090281081Abstract: 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: ApplicationFiled: May 6, 2009Publication date: November 12, 2009Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
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Publication number: 20090227631Abstract: 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: ApplicationFiled: November 22, 2006Publication date: September 10, 2009Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
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Patent number: 7432284Abstract: 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: GrantFiled: September 15, 2003Date of Patent: October 7, 2008Assignee: Merck & Co., Inc.Inventors: Dann LeRoy Parker, Robert R. Wilkening, Dongfang Meng, Ronald W. Ratcliffe
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Publication number: 20080207908Abstract: Disclosed are processes for the synthesis of piperidinyl-substituted urea compounds. This invention further relates to novel intermediates prepared during this synthesis.Type: ApplicationFiled: January 28, 2008Publication date: August 28, 2008Inventor: Richard D. Gless
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Publication number: 20080176838Abstract: 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: ApplicationFiled: June 8, 2005Publication date: July 24, 2008Applicant: SANTHERA PHARMACEUTICALS (DEUTSCHLAND) AGInventors: Paul John Edwards, Silvia Cerezo-Galvez, Achim Feurer, Oliver Hill, Meinolf Thiemann, Victor Giulio Matassa, Sonja Nordhoff, Meritxell Lopez-Canet
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Patent number: 7365196Abstract: 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: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: 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
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Patent number: 7351720Abstract: 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: GrantFiled: June 10, 2004Date of Patent: April 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Soo S. Ko, George V. Delucca
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Process for the preparation of 10,11-dihydro-5h-dibenzo[a,d]cyclohept-5-enes and derivatives thereof
Patent number: 7282587Abstract: 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: GrantFiled: March 15, 2000Date of Patent: October 16, 2007Assignee: Robalo, S.L.Inventor: William Paul Jackson -
Patent number: 7250519Abstract: 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: GrantFiled: October 25, 2002Date of Patent: July 31, 2007Assignee: Merck Patent GmbHInventors: Philipp Stössel, Hubert Spreitzer, Heinrich Becker
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Patent number: 7164025Abstract: 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: GrantFiled: August 10, 2001Date of Patent: January 16, 2007Assignee: Celltech Pharma Europe LimitedInventors: Marianne Langston, Hooshang Shahriari Zavareh
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Patent number: 7053071Abstract: 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: GrantFiled: December 2, 2002Date of Patent: May 30, 2006Assignee: The Burnham InstituteInventors: Marcia Dawson, Joseph A. Fontana, Xiao-kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs
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Patent number: 6969724Abstract: 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 C1-6alkylType: GrantFiled: December 19, 2002Date of Patent: November 29, 2005Assignee: SmithKline Beecham-SpAInventors: Daniela Barlocco, Giorgio Cignarella, Giuseppe Arnaldo Maria Giardina, Mario Grugni, Silvano Ronzoni
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Patent number: 6800636Abstract: 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: GrantFiled: December 20, 2001Date of Patent: October 5, 2004Assignee: Schering CorporationInventors: 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
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Publication number: 20040180884Abstract: The present invention discloses a dibenzocycloheptene compound represented by the formula (I): 1Type: ApplicationFiled: December 23, 2003Publication date: September 16, 2004Inventors: Yoshiaki Kuroki, Hitoshi Ueno, Tetsushi Katsube, Tetsuo Kawaguchi, Eiji Okanari, Ichiro Tanaka, Masayuki Tanaka, Masahiko Hagihara
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Patent number: RE42700Abstract: 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: GrantFiled: July 25, 2008Date of Patent: September 13, 2011Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State UniversityInventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs