The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/142)
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Publication number: 20150105552Abstract: 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: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
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Publication number: 20150064624Abstract: 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 substitutedType: ApplicationFiled: May 6, 2013Publication date: March 5, 2015Applicant: BASF SEInventors: Yuichi Nishimae, Hisatoshi Kura, Kazuhiko Kunimoto, Ryuhei Yamagami, Keita Tanaka
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Publication number: 20150065498Abstract: 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: ApplicationFiled: May 11, 2012Publication date: March 5, 2015Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
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Publication number: 20140315889Abstract: 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: ApplicationFiled: October 26, 2012Publication date: October 23, 2014Applicant: 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
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Patent number: 8815840Abstract: 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: GrantFiled: December 17, 2009Date of Patent: August 26, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
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Patent number: 8765738Abstract: 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: GrantFiled: October 5, 2009Date of Patent: July 1, 2014Assignee: Incuron, LLCInventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
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Patent number: 8691352Abstract: 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: GrantFiled: August 10, 2010Date of Patent: April 8, 2014Assignee: FUJIFILM CorporationInventor: Masaomi Makino
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Publication number: 20130188270Abstract: 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 cType: ApplicationFiled: October 4, 2011Publication date: July 25, 2013Applicant: BASF SEInventors: Yuichi Nishimae, Hisatoshi Kura, Kazuhiko Kunimoto, Ryuhei Yamagami, Keita Tanaka
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Patent number: 8415347Abstract: 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: GrantFiled: August 5, 2010Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica, NVInventors: 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
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Publication number: 20130030166Abstract: 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: ApplicationFiled: July 24, 2012Publication date: January 31, 2013Inventors: Alexei Vorobiev, Eugeny A. Lukhtanov
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Publication number: 20120252740Abstract: 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: ApplicationFiled: July 2, 2010Publication date: October 4, 2012Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
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Publication number: 20120176571Abstract: 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: ApplicationFiled: August 10, 2010Publication date: July 12, 2012Applicant: FUJIFILM CORPORATIONInventor: Masaomi Makino
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Publication number: 20120101092Abstract: 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: ApplicationFiled: December 23, 2011Publication date: April 26, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
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Publication number: 20120083488Abstract: 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: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: 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
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Publication number: 20120058988Abstract: 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: ApplicationFiled: December 17, 2009Publication date: March 8, 2012Inventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
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Publication number: 20120058996Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: November 9, 2011Publication date: March 8, 2012Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Publication number: 20110305661Abstract: 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: ApplicationFiled: October 5, 2009Publication date: December 15, 2011Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
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Patent number: 8076348Abstract: [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: GrantFiled: August 7, 2006Date of Patent: December 13, 2011Assignee: Astellas Pharma Inc.Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada
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Publication number: 20110267714Abstract: 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: ApplicationFiled: January 12, 2010Publication date: November 3, 2011Applicant: FUJIFILM CORPORATIONInventors: Masaomi Makino, Tomotaka Tsuchimura
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Publication number: 20110190493Abstract: 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: ApplicationFiled: February 25, 2011Publication date: August 4, 2011Applicant: Bayer CropScience AGInventors: 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
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Publication number: 20110182850Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: ApplicationFiled: April 7, 2010Publication date: July 28, 2011Inventors: Trixi BRANDL, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
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Patent number: 7951801Abstract: 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: GrantFiled: April 8, 2005Date of Patent: May 31, 2011Assignee: 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
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Publication number: 20110105490Abstract: 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: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Stephen C. Yabut, Hong Ye, Cailin Chen
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Publication number: 20110065703Abstract: 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: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Publication number: 20110059959Abstract: 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: ApplicationFiled: November 18, 2010Publication date: March 10, 2011Applicant: CEPHALON, INC.Inventors: Sankar Chatterjee, James L. Diebold, Derek Dunn, Robert L. Hudkins, Reddeppareddy Dandu, Gregory J. Wells, Allison L. Zulli
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Publication number: 20100331325Abstract: 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: ApplicationFiled: August 5, 2010Publication date: December 30, 2010Inventors: 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
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Publication number: 20100331324Abstract: 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: ApplicationFiled: June 26, 2008Publication date: December 30, 2010Inventors: Derek J. Norris, Ashvinikumar V. Gavai, James Aaron Balog, Joel F. Austin, Weifang Shan, Yufen Zhao, Andrew James Nation, Wen-Ching Han
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Publication number: 20100324017Abstract: 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: ApplicationFiled: February 6, 2008Publication date: December 23, 2010Inventors: Isao Kinoyama, Satoshi Miyamoto, Hiroaki Hoshii, Takehiro Miyazaki, Mayako Yamazaki
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Patent number: 7807672Abstract: 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: GrantFiled: February 13, 2007Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: 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
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Publication number: 20100168096Abstract: [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: ApplicationFiled: August 7, 2006Publication date: July 1, 2010Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada
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Publication number: 20100160303Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: December 17, 2009Publication date: June 24, 2010Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Patent number: 7741343Abstract: 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: GrantFiled: October 30, 2007Date of Patent: June 22, 2010Assignee: Merck Patent GmbHInventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
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Publication number: 20100137294Abstract: 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: ApplicationFiled: November 15, 2007Publication date: June 3, 2010Applicants: GENETIC TECHNOLOGIES LIMITED, MEAT & LIVESTOCK AUTRALIA LIMITEDInventors: Robin Beat Gasser, Adam McCluskey
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Patent number: 7629338Abstract: 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: GrantFiled: May 7, 2007Date of Patent: December 8, 2009Assignee: Merck & Co., Inc.Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
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Publication number: 20090075996Abstract: 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: ApplicationFiled: July 14, 2006Publication date: March 19, 2009Applicant: Irm LLCInventors: Phillip B. Alper, Thomas Marsilje, Arnab Chatterjee, Wenshuo Lu, Daniel Mutnick, Michael Roberts, Yun He
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Publication number: 20090075997Abstract: The present application describes deuterium-enriched satavaptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 15, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090048219Abstract: 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: ApplicationFiled: May 23, 2006Publication date: February 19, 2009Applicant: NITROMED INC.Inventor: David S. Garvey
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Publication number: 20090042866Abstract: 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: ApplicationFiled: November 23, 2005Publication date: February 12, 2009Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20090036441Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.Type: ApplicationFiled: December 22, 2005Publication date: February 5, 2009Applicant: Cell Therapeutics Europe S.R.L.Inventors: Mario Grugni, Mara Cassin, Gennaro Colella, Sergio De Munari, Gianluca Pardi, Paolo Pavesi
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Publication number: 20090023721Abstract: 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: ApplicationFiled: May 24, 2006Publication date: January 22, 2009Inventors: 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
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Publication number: 20080269212Abstract: 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: ApplicationFiled: December 28, 2006Publication date: October 30, 2008Applicant: The Scripps Research InstituteInventors: Congxin Liang, Yangbo Feng
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Publication number: 20080255117Abstract: 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: ApplicationFiled: February 29, 2008Publication date: October 16, 2008Inventors: Lars WORTMANN, Bernd Menzenbach, Marcus Koppitz, Dirk Kosemund, Hans Peter Muhn, Anna Schrey, Ronald Kuehne, Thomas Frenzel, Florian Peter Liesener
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Publication number: 20080153817Abstract: Compounds of formula (I): are useful in the treatment of diseases associated with deposition of ?-amyloid in the brain.Type: ApplicationFiled: July 29, 2004Publication date: June 26, 2008Inventors: Dirk Beher, Michela Bettati, Graham David Checksfield, Ian Churcher, Victoria Alexandra Doughty, Paul Joseph Oakley, Abdul Quddus, Martin Richard Teall, Jonathan David Wrigley
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Patent number: 7348425Abstract: 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: GrantFiled: February 3, 2006Date of Patent: March 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7291633Abstract: 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 hyperactivityType: GrantFiled: April 5, 2002Date of Patent: November 6, 2007Assignee: Merck Patent GmbHInventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
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Patent number: 7262215Abstract: 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: GrantFiled: December 4, 2002Date of Patent: August 28, 2007Assignee: NAD AGInventors: 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
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Patent number: 7153848Abstract: 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: GrantFiled: July 14, 2005Date of Patent: December 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7151100Abstract: 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: GrantFiled: August 9, 2000Date of Patent: December 19, 2006Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Lorenzo M. Leoni, Howard B. Cottam
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Patent number: 7087600Abstract: 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: GrantFiled: May 31, 2002Date of Patent: August 8, 2006Assignee: Medarex, Inc.Inventors: Howard P. Ng, Danny P. C. McGee, Guoxian Wu, Jimmie Moore, Zhihong Li, Sanjeev Gangwar, Oliver L. Saunders, Irina Astafieva
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Patent number: RE41252Abstract: 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: GrantFiled: May 23, 2008Date of Patent: April 20, 2010Assignee: 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