The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/142)
  • 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: 20150065498
    Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: March 5, 2015
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
  • Publication number: 20150064624
    Abstract: Oxime ester compounds of the formula I, II, III, IV or V, wherein Z is for example (formula A); Z1 for is NO2, unsubstituted or substituted C7-C20aroyl or unsubstituted or substituted C4-C20heteroaroyl; provided that at least one Z1 is other than NO2; Z2 is for example unsubstituted or substituted C7-C20aroyl; R1, R2, R3, R4, R5 and R6 for example are hydrogen, halogen, or unsubstituted or substituted C1-C20alkyl, unsubstituted or substituted C6-C20aryl, or unsubstituted or substituted C4-C20heteroaryl; R9, R10, R11, R12 and R13 for example are hydrogen, halogen, OR16, unsubstituted or substituted C1-C20alkyl; provided that R9 and R13 are neither hydrogen nor fluorine; R14 is for example unsubstituted or substituted C6-C20aryl or C3-C20heteroaryl Q is for example C6-C20arylene or C3-C20heteroarylene; Q1 is —C1-C20alkylene-CO—; Q2 is naphthoylene; Q3 is for example phenylene; L is for example O-alkylene-O—; R15 is for example hydrogen or C1-C20alkyl; R20 is for example hydrogen, or unsubstituted or substituted
    Type: Application
    Filed: May 6, 2013
    Publication date: March 5, 2015
    Applicant: BASF SE
    Inventors: Yuichi Nishimae, Hisatoshi Kura, Kazuhiko Kunimoto, Ryuhei Yamagami, Keita Tanaka
  • Publication number: 20140315889
    Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 23, 2014
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
  • Patent number: 8815840
    Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: August 26, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
  • Patent number: 8765738
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: July 1, 2014
    Assignee: Incuron, LLC
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • Patent number: 8691352
    Abstract: Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R3 and R4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R3 and R4 may form a ring with each other; and X represents OR5, SR6, or NR17R18. The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.
    Type: Grant
    Filed: August 10, 2010
    Date of Patent: April 8, 2014
    Assignee: FUJIFILM Corporation
    Inventor: Masaomi Makino
  • Publication number: 20130188270
    Abstract: Compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 for example independently of each other are hydro-gen, C1-C20alkyl, (II), COR16 or NO2, provided that at least one pair of R1 and R2, R2 and R3, R3 and R4, R5 and R6, R6 and R7, or R7 and R8 is (III); R9, R10, R11 and R12 for example independently of each other are hydrogen, C1-C20alkyl which optionally substituted; or R9, R10, R11, and R12 independently of each other are unsubstituted or substituted phenyl; X is CO or a direct bond; R13 is for example C1-C20alkyl which optionally is substituted, C2-C12alkenyl, C4-C8cycloalkenyl, C2-C12alkinyl, C3-C10-cycloalkyl, phenyl or naphthyl both of which are optionally substituted; R14 is for example hydrogen, C3-C8cycloalkyl, C2-C5alkenyl, C1-C20alkoxy, C1-C20alkyl, phenyl or naphthyl; R15 is for example C6-C20aryl or C5-C20heteroaryl; R16 is for example C6-C20aryl which is unsubstituted or substituted by one or more C1-C20alkoxy or C1-C20alkyl; are in particular suitable as photoinitiators for c
    Type: Application
    Filed: October 4, 2011
    Publication date: July 25, 2013
    Applicant: BASF SE
    Inventors: Yuichi Nishimae, Hisatoshi Kura, Kazuhiko Kunimoto, Ryuhei Yamagami, Keita Tanaka
  • Patent number: 8415347
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: April 9, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
  • Publication number: 20130030166
    Abstract: Minor groove binder phosphoramidites having unique structures have been synthesized according to particular methods. These minor groove binder phosphoramidites are useful in the preparation of oligonucleotide conjugates, particularly those for use as probes and primers.
    Type: Application
    Filed: July 24, 2012
    Publication date: January 31, 2013
    Inventors: Alexei Vorobiev, Eugeny A. Lukhtanov
  • Publication number: 20120252740
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.
    Type: Application
    Filed: July 2, 2010
    Publication date: October 4, 2012
    Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
  • Publication number: 20120176571
    Abstract: Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R3 and R4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R3 and R4 may form a ring with each other; and X represents OR5, SR6, or NR17R18. The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.
    Type: Application
    Filed: August 10, 2010
    Publication date: July 12, 2012
    Applicant: FUJIFILM CORPORATION
    Inventor: Masaomi Makino
  • Publication number: 20120101092
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Application
    Filed: December 23, 2011
    Publication date: April 26, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
  • Publication number: 20120083488
    Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).
    Type: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
  • Publication number: 20120058996
    Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.
    Type: Application
    Filed: November 9, 2011
    Publication date: March 8, 2012
    Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
  • Publication number: 20120058988
    Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
    Type: Application
    Filed: December 17, 2009
    Publication date: March 8, 2012
    Inventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
  • Publication number: 20110305661
    Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
    Type: Application
    Filed: October 5, 2009
    Publication date: December 15, 2011
    Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
  • Patent number: 8076348
    Abstract: [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: December 13, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada
  • Publication number: 20110267714
    Abstract: Provided is a photopolymerizable composition that is highly sensitive to light having wavelengths of 365 nm and 405 nm, and is capable of forming a curable film that can suppress deterioration in physical properties of the film due to heat-aging. The photopolymerizable composition include: (A) an oxime polymerization initiator which includes a condensed ring formed by containing two or more rings selected from an aromatic ring and a heterocyclic ring, and a cyclic structure which is connected to the condensed ring, the cyclic structure containing a carbonyl group and having an oxime group directly connected to the carbonyl group; and (B) a polymerizable compound.
    Type: Application
    Filed: January 12, 2010
    Publication date: November 3, 2011
    Applicant: FUJIFILM CORPORATION
    Inventors: Masaomi Makino, Tomotaka Tsuchimura
  • Publication number: 20110190493
    Abstract: The invention relates to novel spiroketal-substituted cyclic ketoenols of the formula (I) in which A, B, Q1, Q2, D, G, W, X, Y, and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, spiroketal-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound.
    Type: Application
    Filed: February 25, 2011
    Publication date: August 4, 2011
    Applicant: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Udo Reckmann, Christian Arnold, Thomas Auler, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger, Erich Sanwald
  • Publication number: 20110182850
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Application
    Filed: April 7, 2010
    Publication date: July 28, 2011
    Inventors: Trixi BRANDL, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
  • Patent number: 7951801
    Abstract: This invention provides beta-carboline compounds of formula III-A-aa: wherein Q, G, R1, R2, R3, and R6b are as described in the specification. The compounds are useful for treating diseases such as inflammatory diseases and cancer.
    Type: Grant
    Filed: April 8, 2005
    Date of Patent: May 31, 2011
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Prakash Raman, Jeremy D. Little, Paul E. Fleming, Dominic Reynolds, Geraldine C. B. Harriman
  • Publication number: 20110105490
    Abstract: The present invention is directed to novel 2,3-dihydro-1H-isoindol-1-imine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the thrombin PAR-1 receptor antagonists.
    Type: Application
    Filed: October 28, 2010
    Publication date: May 5, 2011
    Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Stephen C. Yabut, Hong Ye, Cailin Chen
  • Publication number: 20110065703
    Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.
    Type: Application
    Filed: March 12, 2008
    Publication date: March 17, 2011
    Inventor: Jay Jie-Qiang Wu
  • Publication number: 20110059959
    Abstract: The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.
    Type: Application
    Filed: November 18, 2010
    Publication date: March 10, 2011
    Applicant: CEPHALON, INC.
    Inventors: Sankar Chatterjee, James L. Diebold, Derek Dunn, Robert L. Hudkins, Reddeppareddy Dandu, Gregory J. Wells, Allison L. Zulli
  • Publication number: 20100331325
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: August 5, 2010
    Publication date: December 30, 2010
    Inventors: José Maria CID-NÚÑEZ, Antonius Adrianus Hendrikus Petrus MEGENS, Andrés Avelino TRABANCO-SUÁREZ, Mohamed KOUKNI, Georges Joseph Cornelius HOORNAERT, Frans Josef Cornelius COMPERNOLLE, Tomasz KOZLECKI, Hua MAO, Sushil Chandra JHA, Francisco Javier FERNÁNDEZ-GADEA
  • Publication number: 20100331324
    Abstract: Disclosed are fused heterocyclic compounds of Formula (I) or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: June 26, 2008
    Publication date: December 30, 2010
    Inventors: Derek J. Norris, Ashvinikumar V. Gavai, James Aaron Balog, Joel F. Austin, Weifang Shan, Yufen Zhao, Andrew James Nation, Wen-Ching Han
  • Publication number: 20100324017
    Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT5A receptor modulating action. It was confirmed that a compound characterized by a structure that a tricyclic hetero ring having a pyrrole ring at the center and guanidine are bonded via a carbonyl group has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based thereon, and thus, it was found that the compound can be an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder, particularly for memory-related functional disorders such as cognitive impairments including dementia and schizophrenia, thereby completing the present invention.
    Type: Application
    Filed: February 6, 2008
    Publication date: December 23, 2010
    Inventors: Isao Kinoyama, Satoshi Miyamoto, Hiroaki Hoshii, Takehiro Miyazaki, Mayako Yamazaki
  • Patent number: 7807672
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: October 5, 2010
    Assignee: Schering Corporation
    Inventors: Yongqi Deng, Gerald W. Shipps, Jr., Alan Cooper, Yang Nan, Tong Wang, M. Arshad Siddiqui, Hugh Zhu, Robert Sun, Joseph M. Kelly, Ronald Doll, Jagdish Desai, James J-S Wang, Youhao Dong, Vincent Madison, Li Xiao, Alan Hruza, Neng-Yang Shih
  • Publication number: 20100168096
    Abstract: [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
    Type: Application
    Filed: August 7, 2006
    Publication date: July 1, 2010
    Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada
  • Publication number: 20100160303
    Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.
    Type: Application
    Filed: December 17, 2009
    Publication date: June 24, 2010
    Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
  • Patent number: 7741343
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: June 22, 2010
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
  • Publication number: 20100137294
    Abstract: The present application discloses the Tv-stp-1 serine/threonine phosphatase gene from Trichostrongylus vitrinus, and compounds that are useful as invertebrate control agents.
    Type: Application
    Filed: November 15, 2007
    Publication date: June 3, 2010
    Applicants: GENETIC TECHNOLOGIES LIMITED, MEAT & LIVESTOCK AUTRALIA LIMITED
    Inventors: Robin Beat Gasser, Adam McCluskey
  • Patent number: 7629338
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Grant
    Filed: May 7, 2007
    Date of Patent: December 8, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
  • Publication number: 20090075996
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
    Type: Application
    Filed: July 14, 2006
    Publication date: March 19, 2009
    Applicant: Irm LLC
    Inventors: Phillip B. Alper, Thomas Marsilje, Arnab Chatterjee, Wenshuo Lu, Daniel Mutnick, Michael Roberts, Yun He
  • Publication number: 20090075997
    Abstract: The present application describes deuterium-enriched satavaptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 15, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20090048219
    Abstract: The invention describes novel organic nitric oxide enhancing salts of nonsteroidal antiinflammatory drugs (NSAIDs) and novel compositions comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one organic nitric oxide enhancing salt of an NSAID, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent.
    Type: Application
    Filed: May 23, 2006
    Publication date: February 19, 2009
    Applicant: NITROMED INC.
    Inventor: David S. Garvey
  • Publication number: 20090042866
    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: Application
    Filed: November 23, 2005
    Publication date: February 12, 2009
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Publication number: 20090036441
    Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.
    Type: Application
    Filed: December 22, 2005
    Publication date: February 5, 2009
    Applicant: Cell Therapeutics Europe S.R.L.
    Inventors: Mario Grugni, Mara Cassin, Gennaro Colella, Sergio De Munari, Gianluca Pardi, Paolo Pavesi
  • Publication number: 20090023721
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: May 24, 2006
    Publication date: January 22, 2009
    Inventors: Antonius Adrianus Hendrikus Petrus Megens, Andres Avelino Trabanco-Suarez, Jose Maria Cid-Nunez, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernandez-Gadea, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki
  • Publication number: 20080269212
    Abstract: Amino acid derivatives of pyrrolyl-indolinones and their amide or ester derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
    Type: Application
    Filed: December 28, 2006
    Publication date: October 30, 2008
    Applicant: The Scripps Research Institute
    Inventors: Congxin Liang, Yangbo Feng
  • Publication number: 20080255117
    Abstract: The present invention relates to sulfonyltryptophanols of the general formula I, in which Q, X, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH receptor antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
    Type: Application
    Filed: February 29, 2008
    Publication date: October 16, 2008
    Inventors: Lars WORTMANN, Bernd Menzenbach, Marcus Koppitz, Dirk Kosemund, Hans Peter Muhn, Anna Schrey, Ronald Kuehne, Thomas Frenzel, Florian Peter Liesener
  • Publication number: 20080153817
    Abstract: Compounds of formula (I): are useful in the treatment of diseases associated with deposition of ?-amyloid in the brain.
    Type: Application
    Filed: July 29, 2004
    Publication date: June 26, 2008
    Inventors: Dirk Beher, Michela Bettati, Graham David Checksfield, Ian Churcher, Victoria Alexandra Doughty, Paul Joseph Oakley, Abdul Quddus, Martin Richard Teall, Jonathan David Wrigley
  • Patent number: 7348425
    Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Grant
    Filed: February 3, 2006
    Date of Patent: March 25, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
  • Patent number: 7291633
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: November 6, 2007
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
  • Patent number: 7262215
    Abstract: This invention relates to N-carbacycle monosubstituted indolocarbazole compounds. Furthermore, this invention relates to medicaments comprising N-carbacycle monosubstituted indolocarbazoles compounds and the use of such compounds for treating non-insulin dependent diabetes mellitus, acute stroke and other neurotraumatic injuries, for treating diabetes mellitus, as a chemotherapeutic for the treatment of various malignant diseases, for treating diseases caused by malfunctioning of specific signaling pathways, and for treating neurodegenerative diseases such as for example Alzheimer's disease.
    Type: Grant
    Filed: December 4, 2002
    Date of Patent: August 28, 2007
    Assignee: NAD AG
    Inventors: Heidi Sahagun-Krause, Olivier Thillaye Du Boullay, Valerie Thillaye Du Boullay, Laura Casiraghi, Hans-Wolfgang Klafki, Pierfausto Seneci, Tobias Braxmeier, Silvia Müller, Wolfgang Fr{hacek over (o)}hner, Barbara Monse, Sandra Gordon, Hanno M. Roder
  • Patent number: 7153848
    Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
    Type: Grant
    Filed: July 14, 2005
    Date of Patent: December 26, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
  • Patent number: 7151100
    Abstract: The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
    Type: Grant
    Filed: August 9, 2000
    Date of Patent: December 19, 2006
    Assignee: The Regents of the University of California
    Inventors: Dennis A. Carson, Lorenzo M. Leoni, Howard B. Cottam
  • Patent number: 7087600
    Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: August 8, 2006
    Assignee: Medarex, Inc.
    Inventors: Howard P. Ng, Danny P. C. McGee, Guoxian Wu, Jimmie Moore, Zhihong Li, Sanjeev Gangwar, Oliver L. Saunders, Irina Astafieva
  • Patent number: RE41252
    Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: April 20, 2010
    Assignee: Medarex, Inc.
    Inventors: Howard P. Ng, Danny P. C. McGee, Guoxian Wu, Jimmie Moore, Zhi-Hong Li, Sanjeev Gangwar, Oliver L. Saunder, Irina Astafieva, Valeri Martichonok