The Five-membered Hetero Ring Shares Ring Carbons With Two Carbocyclic Rings (e.g., Tetrahydrocarbazoles, Etc.) Patents (Class 548/439)
  • Patent number: 10000454
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: June 19, 2018
    Assignee: Merck Sharp & Dohme
    Inventors: Tesfaye Biftu, Purakkattle Biju, Timothy A. Blizzard, Zhengxia Chen, Matthew J. Clements, Mingxiang Cui, Jessica L. Frie, William K. Hagmann, Bin Hu, Hubert Josien, Anilkumar G. Nair, Christopher W. Plummer, Cheng Zhu
  • Patent number: 9745266
    Abstract: The present invention relates to indoline alkaloid compounds. In particular, indoline alkaloid compounds of the invention have antibacterial activity and/or are capable of resensitizing the susceptibility of methicillin-resistant S. aureus to a ?-lactam antibiotic. The present invention also relates to a method for producing and using the same.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: August 29, 2017
    Assignee: The Regents of the University of Colorado
    Inventors: Xiang Wang, Jessica Podoll, Le Chang
  • Publication number: 20150105552
    Abstract: This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
  • Publication number: 20150105564
    Abstract: An organic light-emitting device having a light-emitting layer containing a compound represented by the general formula below has a high light emission efficiency. In the general formula, at least one of R1 to R5 represents a cyano group, at least one of R1 to R5 represents a 9-carbazolyl group, a 1,2,3,4-tetrahydro-9-carbazolyl group, a 1-indolyl group or a diarylamino group, and the balance of R1 to R5 represents a hydrogen atom or a substituent.
    Type: Application
    Filed: April 8, 2013
    Publication date: April 16, 2015
    Inventors: Chihaya Adachi, Hiroki Uoyama, Hiroko Nomura, Kenichi Goushi, Takuma Yasuda, Ryosuke Kondo, Katsuyuki Shizu, Hajime Nakanotani, Jyunichi Nishide
  • Publication number: 20150057326
    Abstract: A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: Trustees of Dartmouth College
    Inventor: Jimmy Wu
  • Patent number: 8946444
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: February 3, 2015
    Assignee: PTC Therapeutics, Inc.
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Publication number: 20140371461
    Abstract: The present invention provides a process for effectively producing an N-(hetero)arylazole with high yield, which is useful as a medical or agrochemical product, an organic photoconductor material, an organic electroluminescent element material, or the like. The present invention relates to a process for producing an N-(hetero)arylazole, which includes reacting a (hetero)aryl (pseudo)halide with an NH-azole in the presence of: a catalyst including a palladium compound and a coordination compound; and a basic magnesium compound.
    Type: Application
    Filed: August 31, 2012
    Publication date: December 18, 2014
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Yuji Nakayama, Tohru Kobayashi
  • Patent number: 8912199
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: December 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Patent number: 8853419
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: October 7, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Khulman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
  • Publication number: 20140038987
    Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 6, 2014
    Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
  • Patent number: 8637860
    Abstract: A photoelectric conversion device comprising a transparent electrically conductive film, a photoelectric conversion film and an electrically conductive film in this order, wherein the photoelectric conversion film comprises a photoelectric conversion layer, and an electron blocking layer, wherein the electron blocking layer contains a compound represented by the specific formula.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: January 28, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Kimiatsu Nomura, Eiji Fukuzaki, Tetsuro Mitsui
  • Patent number: 8598181
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: December 3, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Patent number: 8580841
    Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia): and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: November 12, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M Jones, Daniel J Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V Moody, Xiuwen Zhu, Scott Stirn
  • Patent number: 8558007
    Abstract: A polymer and an organic light-emitting device including the polymer are provided, wherein the polymer comprises a polymeric unit represented by the Formula: In which variables are as defined herein.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: October 15, 2013
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Hye-yeon Yang, Won-jae Joo, Jhun-mo Son, Ho-suk Kang
  • Publication number: 20130175509
    Abstract: Embodiments of the present invention are directed to a condensed-cyclic compound and an OLED including the same.
    Type: Application
    Filed: November 19, 2012
    Publication date: July 11, 2013
    Applicants: SFC CO., LTD., SAMSUNG DISPLAY CO., LTD.
    Inventors: SAMSUNG DISPLAY CO., LTD., SFC CO., LTD.
  • Patent number: 8383831
    Abstract: The dye for a dye-sensitized solar cell, which dye is a compound classified into melocyanine dyes and has a structure in which an electron donor unit and an electron acceptor unit are connected with conjugated double bonds, provided by this invention, has excellent photoelectric conversion efficiency and excellent durability, and according to this invention, there can be provided a semiconductor electrode sensitized by the dye and a dye-sensitized solar cell using the semiconductor electrode.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: February 26, 2013
    Assignee: Mitsubishi Paper Mills Limited
    Inventors: Masakazu Takata, Koichi Sumioka, Takaaki Kozai
  • Patent number: 8378339
    Abstract: A photoelectric conversion device comprising a transparent electrically conductive film, a photoelectric conversion film and an electrically conductive film in this order, wherein the photoelectric conversion film comprises a photoelectric conversion layer, and an electron blocking layer, wherein the electron blocking layer contains a compound represented by the specific formula.
    Type: Grant
    Filed: September 8, 2010
    Date of Patent: February 19, 2013
    Assignee: FUJIFILM Corporation
    Inventors: Kimiatsu Nomura, Eiji Fukuzaki, Tetsuro Mitsui
  • Publication number: 20130041007
    Abstract: This invention provides compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and or salts thereof, pharmaceutical compositions comprising a compound of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type II diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and intermediates useful in the preparation of same.
    Type: Application
    Filed: February 4, 2011
    Publication date: February 14, 2013
    Inventor: Chris P. Miller
  • Publication number: 20120295947
    Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).
    Type: Application
    Filed: January 27, 2011
    Publication date: November 22, 2012
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Khulman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
  • Patent number: 8273716
    Abstract: The invention relates to methods of treatment or prophylaxis of physiological and/or pathological conditions with at least one LHRH antagonist, in particular at least one peptidomimetic LHRH antagonist such that the at least one LHRH antagonist is administered in a dose, which does not cause chemical (hormonal) castration.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: September 25, 2012
    Assignee: Spectrum Pharmaceuticals, Inc.
    Inventor: Juergen Engel
  • Publication number: 20120104370
    Abstract: A carbazole compound in which the 2-position of a dibenzofuran skeleton or a dibenzothiophene skeleton is bonded to the 3-position of a carbazole skeleton and nitrogen of the carbazolyl group is bonded to the 9- or 10-position of an anthracene skeleton directly or via a phenylene group was able to be synthesized. It was found out that the carbazole compound has an excellent carrier-transport property, favorable film quality, and a wide band gap, and can be suitably used as a light-emitting element material and an organic semiconductor material.
    Type: Application
    Filed: October 27, 2011
    Publication date: May 3, 2012
    Inventors: Hiroki Suzuki, Harue Osaka, Tsunenori Suzuki
  • Patent number: 8143303
    Abstract: Carbazole derivatives of formula (I), useful in treatment of a CNS disorders related to or affected by the 5-HT6 receptor are described. The pharmacological profile of these compounds includes high affinity binding with 5-HT6 receptor along with good selectivity towards the receptor. Stereoisomers, the salts, methods of preparation and medicines containing the carbazole derivatives are also described.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: March 27, 2012
    Assignee: Suven Life Sciences Limited
    Inventors: Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Vikas Shreekrishna Shirsath, Jagadish Babu Konda, Santosh Vishwakarma, Venkateswarlu Jasti
  • Patent number: 8143304
    Abstract: The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: March 27, 2012
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Heinz Fretz, Julien Pothier, Philippe Risch
  • Publication number: 20120052427
    Abstract: [Problems] To provide a novel compound having a high carrier mobility and is useful as a charge transporting agent which not only makes it possible to stably form a photosensitive layer without precipitating crystals or without developing pinholes when the photosensitive layer is being formed but also makes it possible to form an organic photosensitive material for electrophotography of a high sensitivity and a low residual potential. [Means for Solution] An indole derivative represented by the following general formula (1), wherein R1 and R2 are alkyl groups, k is an integer of 0 to 3, j is an integer of 0 to 4, a ring Z is a 5- to 6-membered ring and is, specifically, a cyclopentane ring, and X1 and X2 are hydrocarbon groups having at least one ethylenically unsaturated bond.
    Type: Application
    Filed: July 21, 2010
    Publication date: March 1, 2012
    Applicant: HODOGAYA CHEMICAL CO., LTD.
    Inventors: Shigetaka Numazawa, Katsumi Abe, Kiyotaka Ihara, Takehiro Nakajima, Makoto Koike
  • Publication number: 20110280808
    Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
    Type: Application
    Filed: April 18, 2011
    Publication date: November 17, 2011
    Applicant: AC Immune, S.A.
    Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
  • Publication number: 20110155241
    Abstract: The dye for a dye-sensitized solar cell, which dye is a compound classified into melocyanine dyes and has a structure in which an electron donor unit and an electron acceptor unit are connected with conjugated double bonds, provided by this invention, has excellent photoelectric conversion efficiency and excellent durability, and according to this invention, there can be provided a semiconductor electrode sensitized by the dye and a dye-sensitized solar cell using the semiconductor electrode.
    Type: Application
    Filed: August 5, 2009
    Publication date: June 30, 2011
    Inventors: Masakazu Takata, Koichi Sumioka, Takaaki Kozai
  • Publication number: 20110132439
    Abstract: Amorphous fullerene derivatives and their use in organic electronic devices that include the fullerene derivative as the electron acceptor component in the device's active layer.
    Type: Application
    Filed: November 2, 2010
    Publication date: June 9, 2011
    Applicant: University of Washington Center for Commercialization
    Inventors: Alex Kwan-yue Jen, Yong Zhang, Hin-Lap Yip
  • Publication number: 20110130409
    Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
    Type: Application
    Filed: July 22, 2009
    Publication date: June 2, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
  • Publication number: 20110118326
    Abstract: The present invention relates to the compound of the formula: to pharmaceutical compositions comprising the compound of Formula (I); and to methods for treating or preventing hypogonadism, osteoporosis, osteopenia, sarcopenia, cachexia, muscle atrophy, sexual dysfunction or erectile dysfunction, comprising administering to a patient in need thereof an effective amount of the compound of Formula (I).
    Type: Application
    Filed: November 10, 2010
    Publication date: May 19, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan
  • Patent number: 7935722
    Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of formula (I).
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: May 3, 2011
    Assignee: Eli Lilly and Company
    Inventors: Kevin Robert Fales, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews, David Andrew Neel, Edward C R Smith
  • Patent number: 7906546
    Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: March 15, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
  • Patent number: 7902196
    Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: March 8, 2011
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Seth B. Herzon, Jeremy Earle Wulff, Romain Siegrist, Jakub Svenda, Matthew Allen Zajac
  • Publication number: 20110039855
    Abstract: The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 14, 2009
    Publication date: February 17, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Euibong Jemes Kim
  • Patent number: 7880019
    Abstract: It is an object to provide a noble anthracene derivative, a light emitting element with a high luminous efficiency, and further a light emitting element with a long lifetime. It is another object to provide a light emitting device and electronic device with a long lifetime by using the light emitting element. An anthracene derivative represented by General Formula (1) is provided. Since the anthracene derivative represented by General Formula (1) has a high luminous efficiency, when the anthracene derivative is used for a light emitting element, the light emitting element can have a high luminous efficiency. Further, when the anthracene derivative represented by General Formula (1) is used for a light emitting element, the light emitting element can have a long lifetime.
    Type: Grant
    Filed: September 24, 2007
    Date of Patent: February 1, 2011
    Assignee: Semiconductor Energy laboratory Co., Ltd.
    Inventors: Masakazu Egawa, Harue Osaka, Sachiko Kawakami, Satoko Shitagaki
  • 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
  • Publication number: 20100137270
    Abstract: A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2.
    Type: Application
    Filed: November 29, 2007
    Publication date: June 3, 2010
    Applicant: Hunter-Fleming Limited
    Inventor: Ernst Wülfert
  • Patent number: 7705163
    Abstract: A process for the preparation of carvedilol of formula (I) (I) either in enantiomeric substantially pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers. The above process is characterised in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium.
    Type: Grant
    Filed: May 19, 2005
    Date of Patent: April 27, 2010
    Assignee: Cipla Limited
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
  • Patent number: 7696356
    Abstract: The present invention provides a rapid, high-yielding process for preparing 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one from 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one without using a secondary amine as a catalyst, and without using glacial acetic acid as a solvent. The present invention further provides a rapid, high-yielding process for preparing ondansetron from 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one without using alumina as a catalyst.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: April 13, 2010
    Assignee: Taro Pharmaceutical Industries Limited
    Inventors: Daniella Gutman, Rosa Cyjon
  • Publication number: 20100022550
    Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of formula (I).
    Type: Application
    Filed: June 21, 2006
    Publication date: January 28, 2010
    Applicant: CELLECTIS
    Inventors: Kevin Robert Fales, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews, David Andrew Neel, Edward C.R. Smith
  • Patent number: 7629379
    Abstract: The invention relates to new compounds of formula (1) wherein R is hydrogen or a linear or branched C1-40alkyl; where X is O, S, or NR1 where R1 is a hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2-40 alkynyl group, an aryl, a heteroaryl or C1-40 alkylaryl or alkylheteroaryl group and where one or both of C and D is OR2, SR2, NR3R4 where R2, R3 and R4 are each independently hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2-40 alkynyl group, an aryl or C1-40 alkylaryl group or a linear or branched C1-40 alkyl NR5R6 chain where R5 and R6 are each independently hydrogen, a linear or branched C1-40 alkyl; or an optionally complex metal ion Mn+/n wherein n is an integer from 1 to 8; or where one or both of C and D are amino acids or nucleic acids attached via either N, O or S; and wherein m is an integer from 1 to 8; and wherein either: I) A is a known aryl or heteroaryl fluorescent group and B is hydrogen, a linear or branched C1-40 alkyl, C2-40 alkenyl or C2- 40 alkynyl group, an ar
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: December 8, 2009
    Assignee: Queen Mary & Westfield College
    Inventors: John Robert Howe Wilson, Alice Caroline Sullivan, Siud Pui Man, Lesley Robson
  • Patent number: 7622494
    Abstract: The present invention relates to compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: November 24, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Sharon Davis Boggs, John G Catalano, Kristjan S Gudmundsson, Leah D'Aurora Richardson, Paul Richard Sebahar
  • Patent number: 7615640
    Abstract: Disclosed are an organic dye having a specific structure, a photoelectric conversion material containing the dye, a semiconductor electrode formed of a substrate having an electrically conductive surface, a semiconductor layer coated on the electrically conductive surface and the above dye adsorbed on the surface, and a photoelectric conversion device to which the above dye is applied. The present invention uses the above dye and can therefore provide a photoelectric conversion device excellent in photoelectric conversion efficiency, and the photoelectric conversion device is suitable for use in a solar cell or the like.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: November 10, 2009
    Assignee: Mitsubishi PaperMillsLtd.
    Inventors: Tamotsu Horiuchi, Hidetoshi Miura
  • Patent number: 7576118
    Abstract: The present invention provides an asymmetric hydrogenation process for the preparation of chiral cycloalkanoindole DP receptor antagonists in high enantiomeric excess.
    Type: Grant
    Filed: April 1, 2005
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: David M. Tellers, Guy R. Humphrey
  • Publication number: 20090143581
    Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.
    Type: Application
    Filed: March 17, 2006
    Publication date: June 4, 2009
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Andrew G. Myers, Seth B. Herzon, Jeremy Earle Wulff, Romain Siegrist, Jakub Svenda, Matthew Alan Zajac
  • Patent number: 7482471
    Abstract: The present invention provides a process for preparation of 1-[9H-carbazol-4-yloxy]-3-[{2-(2-(methoxy)phenoxy)-ethyl}-amino]-propan-2-ol,a compound of formula 1 in racemic form or in the form of optically active R or S enantiomer or its pharmaceutically acceptable salt, comprising, reacting 4-(oxiranylmethoxy)-9H-carbazole, a compound of formula (2) or the R or S enantiomer thereof with a compound of formula (5), wherein R1 is benzyl or substituted benzyl group, in an aprotic organic solvent in presence of a catalyst to obtain a compound of formula (6), or the R or S enantiomer thereof, wherein R1 is as defined above. The resultant compound of formula (6) is subjected to debenzylation reaction by catalytic hydrogenation to obtain the compound of formula (1), if desired converting the resultant compound of formula (1) to a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: January 27, 2009
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Vijay Chhangamal Chhabada, Rajeev Budhdev Rehani, Rajamannar Thennati
  • Publication number: 20090017330
    Abstract: A material for organic electroluminescence devices of the invention which is for use in combination with at least one phosphorescent metal complex has a specific heterocyclic structure. The material for organic electroluminescence devices is used as a host material or a hole transporting material. An organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers which is interposed between the anode and cathode, in which at least one layer of the organic thin film layer contains the material for organic electroluminescence devices, has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and shows a long lifetime.
    Type: Application
    Filed: November 21, 2007
    Publication date: January 15, 2009
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
  • Patent number: 7468442
    Abstract: The present invention provides a cost-effective, industrially feasible process for the manufacture of crystalline Carvedilol Form-II using novel Carvedilol salts comprising a step of reacting 4-(2,3-epoxy propoxy)carbazole (II) with 2-(2-methoxy phenoxy)ethyl amine (III) followed by acidification with mineral acid in presence of an organic solvent to yield acid addition salts, treatment of the said salts with base(s) in presence of organic solvent(s), water and isolation from the organic solvent(s) followed by crystallization from ethyl acetate.
    Type: Grant
    Filed: April 16, 2004
    Date of Patent: December 23, 2008
    Assignee: Matrix Laboratories Ltd.
    Inventors: Gorantla Seeta Ramanjaneyulu, Indukuri Venkata Sunil Kumar, Ketavarapu Narasimha Rao, Jammula Vera Venkata Krishna Kishore
  • Patent number: 7442808
    Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: October 28, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Min Ge, Jiafang He, Fiona Wai Yu Lau, Gui-Bai Liang, Songnian Lin, Weiguo Liu, Shawn P. Walsh, Lihu Yang
  • Patent number: 7419997
    Abstract: The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: September 2, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Sharon Davis Boggs, Kristjan S Gudmundsson
  • Publication number: 20080152950
    Abstract: An anthracene derivative and an organic electroluminescent device using the same are provided. More specifically, provided are an anthracene derivative represented by Formula 1: wherein each R1 is aryl; and each R2 is independently C6-C20 aryl or C3-C19 heteroaryl, which are unsubstituted or substituted with one or more substituents selected from the group consisting of C1-C10 alkyl, C1-C10 alkoxy, cyano, C1-C10 alkylamino, C1-C10 alkylsilyl, halogen, C6-C10 aryl, C6-C10 aryloxy, C6-C10 arylamino, C6-C10 arylsilyl, C3-C19 heteroaryl and hydrogen; and an organic electroluminescent device using the same. The present invention can provide an organic electroluminescent device having excellent power and luminance efficiencies in conjunction with a long service life.
    Type: Application
    Filed: November 30, 2007
    Publication date: June 26, 2008
    Applicant: SFC CO., LTD.
    Inventors: Jong-Tae JE, Sug-Kwang Hwang, Sung-Hoon Kim, Seung-Hyuck Choi, Seon-Keun Yoo