Plural Double Bonds Between Ring Members Of The Hetero Ring Patents (Class 549/471)
  • Patent number: 7998968
    Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8?, or a salt thereof. For example, the compound may be substituted pyrimidines and pharmaceutical compositions of the formula (I) where X=—CR3; X1=—CR2 or —NR2; and X2=—CR5 or —NR5. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.
    Type: Grant
    Filed: November 25, 2009
    Date of Patent: August 16, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa, Koji Fuji
  • Publication number: 20110184058
    Abstract: The present invention describes the preparation of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one, a key intermediate in preparation of ramelteon. The present invention also describes further preceding intermediate compounds useful for the synthesis of 6,7-dihydro-1H-indeno[5,4-b]furan-8(2H)-one.
    Type: Application
    Filed: July 13, 2009
    Publication date: July 28, 2011
    Applicant: Lek Pharmaceuticals D.D.
    Inventor: Jerome Cluzeau
  • Patent number: 7981925
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: July 19, 2011
    Assignee: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 7956185
    Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 7, 2011
    Assignee: Abbott Laboratories
    Inventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
  • Patent number: 7906553
    Abstract: Described herein are compounds of Formula (I) having the structure: where A, J, R1, R4, Z and X are described herein; and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: March 15, 2011
    Assignee: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20110054175
    Abstract: Described herein are fluorinated organic compounds and methods of making fluorinated organic compounds, for example, using palladium complexes. Also described herein are compositions and kits containing compounds and palladium complexes described herein.
    Type: Application
    Filed: February 2, 2009
    Publication date: March 3, 2011
    Inventors: Tobias Ritter, Takeru Furuya, Hanns M. Kaiser
  • Publication number: 20100311582
    Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.
    Type: Application
    Filed: January 23, 2009
    Publication date: December 9, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
  • Patent number: 7829574
    Abstract: Substituted quinazoline compounds of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and X are defined herein. It also discloses a pharmaceutical composition containing one of these compounds.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: November 9, 2010
    Assignee: Hutchison MediPharma Enterprises Limited
    Inventors: Wei-Guo Su, Weihan Zhang, Xiaoqiang Yan, Yumin Cui, Yongxin Ren, Jifeng Duan
  • Patent number: 7790728
    Abstract: The present disclosure relates to a compound of formula (I) wherein: A is an optionally substituted monocyclic or polycyclic aryl or heteroaryl group; B is an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 are chosen from a hydrogen atom and specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety chosen from the moiety of formulae (IIa) and (IIb): or a pharmaceutically acceptable salt thereof, or a N-oxide thereof. The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.
    Type: Grant
    Filed: July 25, 2006
    Date of Patent: September 7, 2010
    Assignee: Laboratorios Almirall, S.A.
    Inventors: Bernat Vidal Juan, Christina Esteve Trias, Lidia Soca Pueyo, Paul Robert Eastwood
  • Patent number: 7700607
    Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: April 20, 2010
    Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
  • Patent number: 7678926
    Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: September 20, 2007
    Date of Patent: March 16, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • Patent number: 7652020
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: January 26, 2010
    Assignee: Schering Corporation
    Inventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, Jr., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
  • Patent number: 7638513
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: December 29, 2009
    Assignee: Schering Corporation
    Inventors: M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga A. Reddy, Vincent S. Madison
  • Patent number: 7534475
    Abstract: A new liquid crystal compound comprises two condensed and substituted rings. The ring preferably is a five-membered heterocyclic ring. The heterocyclic ring is preferably condensed with benzene ring or an aromatic six-membered heterocyclic ring. The benzene ring or the aromatic six-membered heterocyclic ring is preferably substituted with a group comprising a cyclic structure and a chain structure. The liquid crystal compound is advantageously used in preparation of a thin phase retarder, such as a wide-ranged ?/4 plate, which gives inverse wavelength distribution. The phase retarder can be easily produced according to a simple process by using the new liquid crystal compound.
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: May 19, 2009
    Assignee: Fujifilm Corporation
    Inventors: Hideyuki Nishikawa, Ryo Hamasaki, Atsuhiro Ohkawa
  • Publication number: 20090118323
    Abstract: The present invention provides antitumor compounds of the formula (I); and antitumor methods.
    Type: Application
    Filed: September 11, 2007
    Publication date: May 7, 2009
    Inventors: Mary Margaret Mader, Luisa Maria Martin-Cabrejas, Michael Enrico Richett
  • Publication number: 20090087409
    Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, al
    Type: Application
    Filed: November 26, 2008
    Publication date: April 2, 2009
    Applicant: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
  • Publication number: 20080293684
    Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: July 26, 2005
    Publication date: November 27, 2008
    Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
  • Patent number: 7456302
    Abstract: Taxan derivatives are produced efficiently and inexpensively, which are useful as oral-administrable antitumor compounds. A compound of formula (1) (wherein R1 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group; R2 is a hydroxyl group optionally having a protective group) is processed with an alkali metal permanganate to produce a compound of formula (2), which may be a starting material for oral-administrable antitumor compounds.
    Type: Grant
    Filed: April 27, 2005
    Date of Patent: November 25, 2008
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Akihiro Imura, Tatsuya Yamaguchi, Yoshihiro Takayanagi, Seishiro Uchida
  • Patent number: 7439374
    Abstract: The present invention provides compounds of Formula 1, wherein the variables Ar, A1, A2, A3, A4, R5, R6, R7, V, W, X, and Y are defined herein. Certain compounds of Formula 1 described herein possess potent antiviral activity. The invention also provides compounds of Formula 1 that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of Formula 1, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula 1 effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.
    Type: Grant
    Filed: January 5, 2005
    Date of Patent: October 21, 2008
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Andrew Thurkauf, Dawei Chen, Avinash Phadke, Shouming Li, Milind Deshpande
  • Patent number: 7435838
    Abstract: The present invention relates to the diol intermediate of citalopram useful for treatment of depression, which is the crystal of free base of 3-hydroxylmethyl-4-[1-(4-fluorophenyl)-1-hydroxyl-4-(dimethylamino)]butylbenzonitrile and the method of crystallization thereof. The present invention has disclosed the method to prepare pure citalopram and its purified salts through crystallization of the described base; the optical resolution method of citalopram diol intermediate, the method to prepare S-citalopram and its purified salts by crystals mentioned above. The present invention has also disclosed the method to prepare citalopram and its purified salts, S-citalopram and its purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the present invention, the quality and yield of the product can be significantly improved, and the production cost of the medicinal material can be reduced.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: October 14, 2008
    Assignee: Hangzhou Minsheng Pharmaceutical Co. Ltd.
    Inventors: Runan Mei, Dianwu Guo, Shulong Wang
  • Patent number: 7419986
    Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: September 2, 2008
    Assignee: Wyeth
    Inventors: Dahui Zhou, Gary Paul Stack
  • Patent number: 7417158
    Abstract: A method of treating a Mycobacterium tuberculosis infection in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of treating microbial infections, including infections from protozoan pathogens, such as Leishmania donovani, Trypanosoma brucei rhodesiense, a Trypanosoma cruzi, and Plasmodium falciparum, and fungal pathogens, such as Candida albicans, Aspergillus fumigatus, and Cryptococcus neoformans, in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of synthesizing novel cationic substituted benzofuran compounds and the novel compounds themselves.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: August 26, 2008
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Richard R. Tidwell, Karl Werbovetz, Scott Gary Franzblau, Svetlana Bakunova, Stanislav Bakunov
  • Patent number: 7390913
    Abstract: In the following, citalopram diol means 4-(4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl)-3-(hydroxymethyl)-benzonitrile, as free base and/or acid addition salt. The invention relates to a process for the preparation of racemic citalopram diol and/or R- or S-citalopram diol, comprising the separation of a non-racemic mixture of R- and S-citalopram diol with more than 50% of one of the enantiomers into a fraction being enriched with S- or R-citalopram diol and a fraction comprising RS-citalopram diol wherein the ratio of R-citalopram diol:S-citalopram diol is equal to 1:1 or closer to 1:1 than in the initial mixture.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: June 24, 2008
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Brian Christiansen, Robert Dancer, Rikke E. Humble
  • 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: 7348359
    Abstract: The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.
    Type: Grant
    Filed: March 14, 2002
    Date of Patent: March 25, 2008
    Assignees: Eli Lilly and Company, Ligand Pharmaceuticals
    Inventors: Kevin M. Gardinier, Douglas L. Gernert, Timothy A. Grese, David A. Neel, Christopher M. Mapes, Pierre-Yves Michellys, Marcus F. Boehm
  • Patent number: 7335666
    Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: February 26, 2008
    Assignee: Wyeth
    Inventors: Dahui Zhou, Gary Paul Stack
  • Patent number: 7312345
    Abstract: The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: December 25, 2007
    Assignee: ISP Investments Inc.
    Inventors: Arie Gutman, Gennadi Nisnevich, Lev Yudovitch
  • Patent number: 7256213
    Abstract: Taxanes having a methylcarbonate or ethylcarbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(13) side chain substituents.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: August 14, 2007
    Assignee: Florida State University Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7186849
    Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: June 25, 2003
    Date of Patent: March 6, 2007
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7173134
    Abstract: The present invention includes novel retinoid compounds that have selectivity as RXR agonists on one or more isoforms of RXR, currently, RXR?, RXR?, or RXR?. The present compounds, and pharmaceutical compositions incorporating these compounds, therefore, are effective in treating conditions mediated by RXRs. Among other physiological responses, the compounds of the present invention reduce blood glucose and maintain body weight, and, thus, are useful for the treatment of diabetes (NIDDIM) and obesity.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: February 6, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Curt Dale Haffner, Istvan Kaldor, Darryl Lynn McDougald, Aaron Bayne Miller
  • Patent number: 7157474
    Abstract: Compositions comprising a taxane having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 28, 2005
    Date of Patent: January 2, 2007
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7157491
    Abstract: This invention provides estrogen receptor modulators having the structure where R1–R5 are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 13, 2004
    Date of Patent: January 2, 2007
    Assignee: Wyeth
    Inventors: Richard Eric Mewshaw, Stephen Todd Cohn
  • Patent number: 7135479
    Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
    Type: Grant
    Filed: September 10, 2003
    Date of Patent: November 14, 2006
    Assignee: Wyeth
    Inventors: Dahui Zhou, Gary Paul Stack
  • Patent number: 7112686
    Abstract: The invention relates to a process for the preparation of racemic citalopram free base or an acid addition salt thereof and/or R- or S-citalopram as the free base or an acid addition salt thereof by separation of a mixture of R- and S-citalopram with more than 50% of one of the enantiomers into a fraction consisting of racemic citalopram and/or a fraction of S-citalopram or R-citalopram characterized in that i) citalopram is precipitated from a solvent as the free base or as an acid addition salt thereof; ii) the precipitate formed is separated from the mother liquor; iia) if the precipitate is crystalline it is optionally recrystallised one or more times to form racemic citalopram, and then optionally converted into an acid addition salt thereof; iib) if the precipitate is not crystalline, steps i) and ii) are optionally repeated until a crystalline precipitate is obtained and the crystalline precipitate is recrystallised one or more times to form racemic citalopram, and then optionally converted into an aci
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: September 26, 2006
    Assignee: H. Lundbeck A/S
    Inventors: Rikke E. Humble, Troels V. Christensen, Michael H. Rock, Ole Nielsen, Hans Petersen, Robert Dancer
  • Patent number: 7078541
    Abstract: Certain benzofuran derivatives are useful in the treatment of certain ischemic or inflammatory conditions, as well as neuroinflammation, neurodegeneration or degenerative diseases in which mitochondrial dysfunction leads to tissue degeneration. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
    Type: Grant
    Filed: September 17, 2003
    Date of Patent: July 18, 2006
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Sekhar Boddupalli, Gail Walkinshaw, Bing Wang
  • Patent number: 7056946
    Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: November 24, 2003
    Date of Patent: June 6, 2006
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7008636
    Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: May 11, 2004
    Date of Patent: March 7, 2006
    Assignee: Wyeth
    Inventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
  • Patent number: 6992104
    Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: January 31, 2006
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6936638
    Abstract: Compounds which have utility in the treatment of conditions associated with altered mitochondrial function. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
    Type: Grant
    Filed: December 19, 2003
    Date of Patent: August 30, 2005
    Assignees: Migenix Corp., Pfizer Inc.
    Inventors: Soumitra S. Ghosh, Yazhong Pei, Xiao-Qing Tang, Spiros J. Liras, Michael K. Ahlijanian
  • Patent number: 6911469
    Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2??(I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: June 28, 2005
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Tsuyoshi Mizutani, Teruo Oku, Noritsugu Yamasaki, Osamu Onomura, Masahiro Nishikawa, Takahiro Hiramura, Takafumi Imoto
  • Patent number: 6906088
    Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: June 14, 2005
    Assignee: FSU Research Foundation, Inc.
    Inventors: Robert A. Holton, Weishuo Fang
  • Patent number: 6884821
    Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: April 26, 2005
    Assignee: Eisai Co., Ltd.
    Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
  • Patent number: 6878706
    Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: April 12, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals Inc.
    Inventors: Thomas A. Gilmore, Eugene Richard Hickey, Weimin Liu, Peter Allen Nemoto, Denice M. Spero
  • Patent number: 6872837
    Abstract: Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: March 29, 2005
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6864379
    Abstract: Methods for manufacture of citalopram through stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans are disclosed.
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: March 8, 2005
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Haleh Ahmadian
  • Patent number: 6861444
    Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: March 1, 2005
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
  • Patent number: 6828448
    Abstract: The invention relates to 2-butyl-5-(methanesulfonamido)benzofuran, its preparation and its use. This compound is a synthesis intermediate, in particular for the preparation of dronedarone.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: December 7, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Noël Fino, Corinne Leroy
  • Patent number: 6787565
    Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2  (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: September 7, 2004
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada, Tsuyoshi Mizutani, Teruo Oku, Noritsugu Yamasaki, Osamu Onomura, Masahiro Nishikawa, Takahiro Hiramura, Takafumi Imoto
  • Patent number: 6780879
    Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: August 24, 2004
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6767920
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration, a wavy line represents the &agr; configuration or the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2; provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents may
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: July 27, 2004
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner