Chalcogen Bonded Directly To The Tricyclo-carbocyclic Ring System Patents (Class 546/204)
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Patent number: 8822692
    Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: September 2, 2014
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite, S.p.A.
    Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
  • Patent number: 8785468
    Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: July 22, 2014
    Assignee: Amgen Inc.
    Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, XianYun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
  • Publication number: 20130274240
    Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
    Type: Application
    Filed: November 5, 2012
    Publication date: October 17, 2013
    Inventor: JAPAN TOBACCO INC.
  • Publication number: 20130244994
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: February 15, 2013
    Publication date: September 19, 2013
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
  • Patent number: 8530465
    Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: September 10, 2013
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Publication number: 20130090476
    Abstract: Thiazolylpiperidine derivatives of the formula (I), in which the symbols A, G, Y, n, R1, R2, R3, R4 and R5 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Application
    Filed: September 5, 2012
    Publication date: April 11, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Pierre CRISTAU, Nicola Rahn, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Jurgen Benting
  • Publication number: 20130090477
    Abstract: Thiazolylpiperidine derivatives of the formula (I), in which the symbols A, G, Y, n, R1, R2, R3, R4 and R5 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Application
    Filed: September 5, 2012
    Publication date: April 11, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Pierre CRISTAU, Nicola RAHN, Tomoki TSUCHIYA, Ulrike WACHENDORFF-NEUMANN, Jürgen BENTING
  • Publication number: 20130053571
    Abstract: A process for the preparation of 14-O—[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl)acetyl]mutilins of formula feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O—[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: NABRIVA THERAPEUTICS AG
    Inventor: NABRIVA THERAPEUTICS AG
  • Patent number: 8362020
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: January 29, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
  • Patent number: 8304415
    Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: November 6, 2012
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Patent number: 8093391
    Abstract: This invention relates to an improved and scalable process for the preparation of substantially pure palonosetron and its acid addition salts, in particular hydrochloride (I) which comprises of, (a) converting intermediate (IIa) as such or as its freebase (II) to a crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) via hydrogenation under pressure with an appropriately chosen hydrogenation catalyst in an suitable organic solvent. (b) making the resulting crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) substantially free from (II) or (IIa) via halogenation reaction.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: January 10, 2012
    Assignee: Sterling Biotech Research Center
    Inventors: Sugata Chatterjee, Ajay Singh Rawat, Anil V. Pawar, Jetti Rajanikanth, Penigandla Venkateswarlu
  • Publication number: 20110184022
    Abstract: Compounds of formula (I), which are 14-O-{[(optionally substituted hydroxy)cyclohexyl)sulfanyl]acetyl}mutilins further substituted at the cyclohexyl group by an acylated amino group, salts and solvates thereof, pharmaceutical compositions comprising such compounds and their use as a pharmaceutical, e.g. for the treatment of diseases mediated by microbes and for the treatment of inflammation where microbese are mediating said inflammation.
    Type: Application
    Filed: August 17, 2009
    Publication date: July 28, 2011
    Applicant: NABRIVA THERAPEUTICS AG
    Inventors: Rosemarie Mang, Werner Heilmayer
  • Publication number: 20110172270
    Abstract: 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1 that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.
    Type: Application
    Filed: January 6, 2011
    Publication date: July 14, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE S.A
    Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
  • Publication number: 20110124856
    Abstract: An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.
    Type: Application
    Filed: July 31, 2009
    Publication date: May 26, 2011
    Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Taizo Ito, Koji Kunimasu, Kazuhito Furukawa
  • Publication number: 20110053943
    Abstract: This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: June 1, 2010
    Publication date: March 3, 2011
    Inventors: David A. Claremon, Colin M. Tice, Linghang Zhuang, Katerina Leftheris, Yuanjie Ye, Suresh B. Singh
  • Patent number: 7888510
    Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: February 15, 2011
    Assignee: Laboratorios del Dr. Esteve S.A.
    Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
  • Publication number: 20100249075
    Abstract: The present invention relates to novel tetralin ER-? agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-? mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis.
    Type: Application
    Filed: February 10, 2006
    Publication date: September 30, 2010
    Applicant: ELI LILLY AND COMPANY
    Inventors: Venkatesh Krishnan, Julian Stanley Kroin, Bryan Hurst Norman, Elizabeth Marie Thomas
  • Patent number: 7772251
    Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.
    Type: Grant
    Filed: May 17, 2004
    Date of Patent: August 10, 2010
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
  • Publication number: 20100197734
    Abstract: A compound of formula (I) or of formula (II) wherein X is oxygen or sulfur, and Y is a residue of pipecolic acid or a residue of an amino acid, preferably a naturally occurring amino acid.
    Type: Application
    Filed: July 11, 2008
    Publication date: August 5, 2010
    Applicant: NABRIVA THERAPEUTICS AG
    Inventors: Klaus Thirring, Werner Heilmayer
  • Publication number: 20100160266
    Abstract: A pleuromutilin in the form of a salt with salicylic acid, azelaic acid, sebacic acid or 2-[(2,6-dichlorophenyl)amino]benzeneacetic acid.
    Type: Application
    Filed: June 14, 2006
    Publication date: June 24, 2010
    Applicant: NABRIVA THERAPEUTICS FORSCHUNGS GMBH
    Inventor: Gerd Ascher
  • Publication number: 20100099703
    Abstract: The present invention relates to phenylamino-substituted piperidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.
    Type: Application
    Filed: October 31, 2007
    Publication date: April 22, 2010
    Inventors: Mónica Garcia-López, Josep Mas-Prio, Antonio Torrens-Jover
  • Publication number: 20090253748
    Abstract: A process for the preparation of 14-O-[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl) acetyl]mutilins of formula (I) feasible for large-scale production of high purity products, and wherein the carbon atom at the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, and a new crystalline form of 14-O-[(N-3-methyl-2-(R)-amino-butyryl-piperidine-3(S)-yl)sulfanyl)acetyl]mutilin-hydrochloride.
    Type: Application
    Filed: October 3, 2007
    Publication date: October 8, 2009
    Applicant: NABRIVA THERAPEUTICS AG
    Inventors: Ingolf Macher, Andreas Berger, Martin De Cristoforo
  • Patent number: 7579364
    Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: August 25, 2009
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Gabriele Fontana
  • Publication number: 20090209584
    Abstract: A compound of formula (I) wherein R and R2 and the attached nitrogen atom form pyrrolidinyl or piperidinyl. R1 is a group of formula (II). R3 and R?3 are hydrogen, deuterium or halogen. R4, R5 and R10 are independently of each other hydrogen or alkyl. R6, R7 and R8 are hydrogen or deuterium. R9 is amino, alkyl, aryl, heterocyclyl or mercapto. If X is oxygen, R9 is additionally hydrogen; R?10 is alkyl, X is sulphur, oxygen, NR10, or N+(R?10)2; Y is sulphur or oxygen, and m is 0, 1 or 2, with the proviso that, when R and R2 and the attached nitrogen atom form piperidinyl, m is O, Y is S and Y is attached in position 3 of the piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S)-configuration which is useful as antimicrobial, antibacterial.
    Type: Application
    Filed: April 7, 2009
    Publication date: August 20, 2009
    Applicant: Nabriva Therapeutics Forschungs AG
    Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
  • Publication number: 20080287499
    Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.
    Type: Application
    Filed: June 19, 2008
    Publication date: November 20, 2008
    Applicant: INDENA S.P.A.
    Inventors: Ezio Bombardelli, Gabriele Fontana
  • Publication number: 20080261985
    Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Application
    Filed: November 16, 2007
    Publication date: October 23, 2008
    Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
  • Patent number: 7432284
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: September 15, 2003
    Date of Patent: October 7, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Robert R. Wilkening, Dongfang Meng, Ronald W. Ratcliffe
  • Publication number: 20080119516
    Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrom, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man. Said object was achieved by providing 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1.
    Type: Application
    Filed: July 29, 2004
    Publication date: May 22, 2008
    Applicant: LABORATORIOS DEL DR. ESTEVE S.A.
    Inventors: Antoni Torrens Jover, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany
  • Publication number: 20080027107
    Abstract: Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (Rs)2 in which R° is a C1l12 alkanediyl and each R5 is H or optionally substituted C14 alkyl, and a group of formula (11) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C14 alkyl; R9 is selected from H, C14 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1.6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C16 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives.
    Type: Application
    Filed: December 22, 2004
    Publication date: January 31, 2008
    Inventors: Laurence Hylton Patterson, Klaus Pors, Paul Henry Teesdale-Spittle
  • Patent number: 7320985
    Abstract: A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an aqueous solution containing a stabilized arylcarboxylic acid. According to the stabilization method of the present invention, arylcarboxylic acid and pharmacologically acceptable salts thereof, particularly pranoprofen, can be stabilized at every temperature range, particularly at lower temperatures, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: January 22, 2008
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventor: Shirou Sawa
  • Patent number: 7314875
    Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: January 1, 2008
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John A. Gruner, Rabindranath Tripathy
  • Patent number: 7087599
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: August 8, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
  • Patent number: 7052863
    Abstract: An alizarin-based chromogenic substrate, a composition containing the substrate, and its use to detect the presence of an enzymatic activity are disclosed. The substrate is particularly applicable in the field of biological diagnosis.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: May 30, 2006
    Assignee: Biomerieux S. A.
    Inventors: Lyle Armstrong, Arthur James
  • Publication number: 20040162432
    Abstract: The invention relates to substituted octahydrophenanthrene compounds of general formula (I), to a method for their production, to medicaments containing these compounds and to the use of said compounds for producing medicaments.
    Type: Application
    Filed: February 13, 2004
    Publication date: August 19, 2004
    Inventors: Helmut Buschmann, Werner Englberger, Michael Przewosny, Hans Schick, Birgitta Henkel, Michael Sattlegger
  • Publication number: 20040129178
    Abstract: A light resistant colorant is obtained by coupling a dye or a pigment with a light resistant material. A light resistant colorant-containing composition has no additional light stabilizer. Therefore, side effects caused by the addition of a light stabilizer, such as precipitate generation, may be prevented. Furthermore, substrates to which the composition is applied preserve excellent light resistance for a long term.
    Type: Application
    Filed: September 29, 2003
    Publication date: July 8, 2004
    Applicant: SAMSUNG Electronics Co., Ltd.
    Inventors: Yeon-Kyoung Jung, Seung-min Ryu
  • Publication number: 20040102482
    Abstract: A compound of formula (I) wherein R and R2 together with the nitrogen atom to which they are attached form pyrrolidinyl or piperidinyl, R1 is a group of formula (II) R3 and R′3 are hydrogen, deuterium or halogen, R4, R5 and R10 are independently of each other hydrogen or alkyl, R6, R7 and R8 are hydrogen or deuterium; R9 is amino, alkyl, aryl, heterocyclyl or mercapto; and, if X is oxygen, R9 is additionally hydrogen; R′10 is alkyl, X is sulphur, oxygen, NR10, or N+(R′10)2; Y is sulphur or oxygen, and m is 0, 1 or 2; with the proviso that, when R and R2 together with the nitrogen atom to which they are attached form piperidinyl, m is O, Y is S and Y is attached in position 3 of said piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S) -configuration which is e.g. useful as antimicrobial, antibacterial.
    Type: Application
    Filed: March 10, 2003
    Publication date: May 27, 2004
    Inventors: Gerd Ascher, Heinz Berner, Johannes Hildebrandt
  • Publication number: 20040014741
    Abstract: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.
    Type: Application
    Filed: October 26, 2001
    Publication date: January 22, 2004
    Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
  • Publication number: 20030208073
    Abstract: The invention relates to novel substituted N-aryl nitrogen-containing heterocyclic compounds of the general formula (I) 1
    Type: Application
    Filed: January 29, 2003
    Publication date: November 6, 2003
    Inventors: Karl-Heinz Linker, Kurt Findeisen, Otto Schallner, Andreas Lender, Hans-Joachim Santel, Markus Dollinger, Akihiko Yanagi, Toshio Goto
  • Publication number: 20030166925
    Abstract: The present invention provides a novel compound having a superior acetylcholinesterase inhibitory action.
    Type: Application
    Filed: November 25, 2002
    Publication date: September 4, 2003
    Inventors: Yoichi Iimura, Takashi Kosasa
  • Publication number: 20030114674
    Abstract: 1 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infections.
    Type: Application
    Filed: October 4, 2002
    Publication date: June 19, 2003
    Inventors: Gerald Brooks, Eric Hunt, Steven Howard
  • Patent number: 6569849
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Y, Z, A, R1, R2, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: May 27, 2003
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh Jorgensen, Rolf Hohlweg, Peter Madsen, Knud Erik Andersen, Svend Treppendahl, Uffe Bang Olsen, Zdenek Polivka, Alexandra Silhankova, Karel Sindelar, Vladimir Valenta, Tomas Kalisz
  • Publication number: 20030082667
    Abstract: The invention concerns a novel chromogenic substrate based on Alizarin. The invention also concerns the uses to which this substrate can be put, and a formulation containing such a substrate.
    Type: Application
    Filed: June 3, 2002
    Publication date: May 1, 2003
    Inventors: Lyle Armstrong, Arthur James
  • Publication number: 20030027840
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Application
    Filed: February 14, 2001
    Publication date: February 6, 2003
    Inventors: Dann LeRoy Parker, Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
  • Publication number: 20030008316
    Abstract: There is disclosed a compound of formula (I) wherein each of X1 and X2 are independently NH—A—NR1R2, and wherein A is A C2-8 alkylene and R1 and R2 are independently selected from hydrogen, C1-4 alkyl, C2-4 hydroxy-alkyl and C2-4 aminoalkyl, or R1 and R2 together form a C2-6 alkylene group which with the nitrogen atom to which R1 and R2 are attached forms a heterocyclic ring, or an N-oxide derivative thereof, and wherein the compound (I) or its N-oxide derivative is optionally in the form of an acid salt derived from an organic or inorganic acid. Also disclosed is a method of its production and its uses, including its use in analyzing a cell or biological material and detecting the emitted fluorescence signal.
    Type: Application
    Filed: August 12, 2002
    Publication date: January 9, 2003
    Applicant: BIOSTATUS LIMITED
    Inventors: Paul James Smith, Laurence Hylton Patterson
  • Patent number: 6441244
    Abstract: The invention relates to new compounds of the formula (I) in which R is phenyl, C1-4alkyl-, C1-4alkoxy- or halogen-substituted phenyl, naphthyl or an aromatic ring containing heteroatoms; X is O or S; R1 and R2 are each a methyl radical or R1 and R2 together are a C4-8alkylene radical; Y is hydroxyl, C1-12alkoxy, C1-4alkylamino, di-C1-4alkylamino or a piperidine or morpholine ring that is attached by its nitrogen atom; to a process for preparing them and to their use as photoinitiators and/or photosensitizers.
    Type: Grant
    Filed: July 12, 2001
    Date of Patent: August 27, 2002
    Assignee: Clariant Finance (BVI) Limited
    Inventors: Lajos Avar, René Bär, Victor Sanahuja
  • Publication number: 20020107235
    Abstract: The present invention provides non-steroidal compounds of Formula I, and prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.
    Type: Application
    Filed: October 26, 2001
    Publication date: August 8, 2002
    Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
  • Publication number: 20020099214
    Abstract: There is provided a compound of formula I, 1
    Type: Application
    Filed: March 27, 2002
    Publication date: July 25, 2002
    Applicant: Pfizer Inc.
    Inventors: Stephen Paul Gibson, Ivan Tommasini, David Morris Gethin, Richard Edward Armer
  • Patent number: 6288123
    Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: September 11, 2001
    Assignee: Cambridge NeuroSciences, Inc.
    Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
  • Patent number: RE38257
    Abstract: A piperidine compound of the formula (I): wherein A is a fused aromatic ring; R is hydrogen, chloro or methoxy; X is (CH2)n, which may be substituted, in which n is 0 or an integer of 1 to 10, —CH≡CH—, —C≡C—, —O—, —S—, —NH—, —N(COCH3)—, —N(COOC2H5)—, —N(CHO)—, —N(CH3)—, —CO—, —SO—, or —SO2—; Y is —CH≡CH—, —CH2CH2—, —CH2CO—, —O—, —S—, —NH—, —OCH2—, —SCH2—, —NHCH2—, —CH(OH)CH2— or —CH(OH)CH(OH)—; and Q is substituted or unsubstituted n-hexyl, carboxypropyl, ethoxycarbonylpropyl, cyanopropyl, cyclohexyl, phenyl, indanyl, naphthyl, tetrahydronaphthyl, benzocycloheptyl, piperidinyl, tetrahydroisoquinolinyl, indolyl, pyrolyl, furyl, thienyl, thiazolyl, oxazolyl or N-methylpyrolyl, wherein any one or more of t
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: September 23, 2003
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yoshikatsu Koyama, Hideki Domoto, Akira Kamimura