The Chalcogen Or The Acyclic Nitrogen Is Bonded Directly To The Six Membered Hetero Ring Patents (Class 546/292)
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Patent number: 10759756Abstract: Disclosed are small molecule antagonists of ?4?7 integrin, and methods of using them to treat a number of specific diseases or conditions.Type: GrantFiled: April 12, 2019Date of Patent: September 1, 2020Assignee: Morphic Therapeutic, Inc.Inventors: Matthew G. Bursavich, Dawn M. Troast, Bryce A. Harrison, Blaise S. Lippa, Bruce N. Rogers, Kyle D. Konze, Aleksey I. Gerasyuto, Tyler Day, Fu-Yang Lin, Kristopher N. Hahn, Mats A. Svensson, Byungchan Kim, Cheng Zhong, Alexey A. Lugovskoy, Brian Sosa
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Patent number: 10343999Abstract: The present invention relates to a novel process for preparing enantiomerically pure compounds of N-(pyrid-4-yl)-2-hydroxyalkylamide type corresponding to the general formula (C) below: and also to processes for preparing the reaction intermediates used in this synthesis, said intermediates having the general formulae (A) and (B) below:Type: GrantFiled: November 8, 2016Date of Patent: July 9, 2019Assignee: Galderma Research & DevelopmentInventors: Jean-Guy Boiteau, Sebastien Daver, Nicolas Rodeville
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Publication number: 20150133301Abstract: 3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di-tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: April 29, 2014Publication date: May 14, 2015Applicant: DOW AGROSCIENCES LLCInventors: Jeffrey B. Epp, Christian T. Lowe, James M. Renga, Paul R. Schmitzer, Joseph D. Eckelbarger, Katherine A. Guenthenspberger, Thomas L. Siddall, Carla N. Yerkes, Lindsey G. Fischer, Natalie C. Giampietro, Jeremy Kister, Joshua Roth
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Patent number: 9018206Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: September 12, 2012Date of Patent: April 28, 2015Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150105432Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group or it lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Inventors: Takashi NAKAGAWA, Makoto SAKAMOTO, Kazuya YAMAGUCHI, Yuki TERAUCHI, Masamichi SHIRAKURA, Yasuo HARADA, Yutaka KOJIMA, Takumi SUMIDA
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Patent number: 8865908Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)Type: GrantFiled: July 30, 2010Date of Patent: October 21, 2014Assignee: Bayer Cropscience AGInventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
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Publication number: 20140234245Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.Type: ApplicationFiled: November 5, 2012Publication date: August 21, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Cédric Poinsard
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Publication number: 20140213616Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.Type: ApplicationFiled: January 29, 2014Publication date: July 31, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
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Publication number: 20140018326Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 27, 2011Publication date: January 16, 2014Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
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Publication number: 20130317020Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 2, 2013Publication date: November 28, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Patent number: 8563763Abstract: The present invention relates to isonitrile compounds, methods of synthesis, and uses in a variety of fields. In one aspect, the present invention includes sulfinyl methyl isonitriles and methods for their preparation. In another aspect, the present invention includes the use of sulfinyl methyl isonitriles to prepare various other isonitrile compounds and derivatives thereof. In yet another aspect, the present invention includes a relatively simple and routine synthesis of sulfinyl methyl isonitrile compounds, other isonitrile compounds and derivatives thereof.Type: GrantFiled: March 14, 2012Date of Patent: October 22, 2013Assignee: Duquesne University of the Holy GhostInventors: Fraser Ferguson Fleming, Bhaskar Reddy Pitta
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Publication number: 20130237702Abstract: A composition containing a compound represented by General Formula (I) below (see the definition in the specification for the symbols in the formula) or a salt thereof has an excellent CaSR agonistic effect and provides a pharmaceutical agent, a CaSR agonistic agent, a prophylactic or therapeutic agent for a disease that can be ameliorated through CaSR activation as well as seasonings and an agent for imparting kokumi.Type: ApplicationFiled: August 31, 2012Publication date: September 12, 2013Applicant: AJINOMOTO CO., INC.Inventors: Masayuki SUGIKI, Toru OKAMATSU, Tetsuo YANO, Shinya TANIGUCHI
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Patent number: 8524896Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.Type: GrantFiled: March 2, 2009Date of Patent: September 3, 2013Assignee: Syngenta Crop Protection LLCInventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
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Publication number: 20130190325Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X.Type: ApplicationFiled: June 21, 2011Publication date: July 25, 2013Applicant: ITEK VENTURES PTY LTDInventors: Shudong Wang, Osama Chahrour, Tiangong Lu, Anran Hu
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Publication number: 20130150367Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: September 12, 2012Publication date: June 13, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Patent number: 8455501Abstract: The present invention relates to compounds of the formula wherein R1 to R3 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: GrantFiled: September 10, 2012Date of Patent: June 4, 2013Assignee: Hoffmann-La Roche IncInventors: Uwe Grether, Stephan Roever
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Publication number: 20130065911Abstract: The present invention relates to compounds of the formula wherein R1 to R3 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 10, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Stephan Roever
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Publication number: 20130065907Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Stephan Roever, Uwe Grether
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Publication number: 20120232049Abstract: A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen.Type: ApplicationFiled: February 22, 2008Publication date: September 13, 2012Applicant: Eisai R&D Management Co., Ltd.Inventors: Hiroshi Obaishi, Takayuki Nakagawa, Tomohiro Matsushima, Setsuo Funasaka, Shuji Shirotori, Keiko Takahashi
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Publication number: 20120177634Abstract: This disclosure concerns novel demethylpenclomedine analogs. Also disclosed are pharmaceutical compositions and methods for using such compositions to treat hyperproliferative disorders.Type: ApplicationFiled: February 22, 2012Publication date: July 12, 2012Inventor: Lee Roy Morgan
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Publication number: 20120071513Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: November 28, 2011Publication date: March 22, 2012Applicant: COMPASS PHARMACEUTICALS LLCInventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
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Patent number: 8101639Abstract: Disclosed are compounds of the Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: October 12, 2009Date of Patent: January 24, 2012Assignee: Array BioPharma Inc.Inventors: Allison L. Marlow, Eli M. Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong-Woon Yang, James Blake
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Publication number: 20110319437Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: August 31, 2011Publication date: December 29, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Shigeyuki ITOH, Atsushi IWATA
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Publication number: 20110245210Abstract: Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-?) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.Type: ApplicationFiled: June 3, 2011Publication date: October 6, 2011Inventors: Nigel H. Greig, Harold Holloway, Arnold Brossi, Xiaoxiang Zhu, Tony Giordano, Qian-sheng Yu, William D. Figg
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Publication number: 20110200535Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for therapy and diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: August 5, 2009Publication date: August 18, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lutz Lehmann, Andrea Thiele, Tobias Heinrich, Sonja Vollmer
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Publication number: 20110118470Abstract: Compounds represented by the following general formula: wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—), Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.), salts thereof or hydrates of the foregoing.Type: ApplicationFiled: January 7, 2011Publication date: May 19, 2011Inventors: Yasuhiro FUNAHASHI, Akihiko Tsuruoka, Masayuki Matsukura, Toru Haneda, Yoshio Fukuda, Junichi Kamata, Keiko Takahashi, Tomohiro Matsushima, Kazuki Miyazaki, Ken-ichi Nomoto, Tatsuo Watanabe, Hiroshi Obaishi, Atsumi Yamaguchi, Sachi Suzuki, Katsuji Nakamura, Fusayo Mimura, Yuji Yamamoto, Junji Matsui, Kenji Matsui, Takako Yoshiba, Yasuyuki Suzuki, Itaru Arimoto
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Publication number: 20110082295Abstract: To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH?CH.Type: ApplicationFiled: May 27, 2009Publication date: April 7, 2011Applicants: Tokyo Institute of Technology, Kyoto UniversityInventors: Hachiro Sugimoto, Takashi Takahashi, Ichiro Hijikuro, Michiaki Okuda
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Patent number: 7820827Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.Type: GrantFiled: September 1, 2005Date of Patent: October 26, 2010Assignee: Adolor CorporationInventors: Bertrand Le Bourdonnec, Roland E. Dolle
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Patent number: 7732616Abstract: Disclosed are compounds of the Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: May 17, 2006Date of Patent: June 8, 2010Assignee: Array BioPharma Inc.Inventors: Allison L. Marlow, Eli M. Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Publication number: 20090324569Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: November 20, 2008Publication date: December 31, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Publication number: 20090137814Abstract: A process for the preparation of diaminodinitropyridine or diaminodinitrobenzene by contacting an aminopyridine or aminobenzene with oleum and nitric acid, wherein the improvement comprises adding at least about 1% molar excess of nitric acid, based upon the aminopyridine or aminobenzene, with stirring for at least two hours to form first the intermediate sulfonic acid, and then diaminodinitropyridine or diaminodinitrobenzene, and use of such products in the preparation of rigid rod polymers is disclosed.Type: ApplicationFiled: November 27, 2007Publication date: May 28, 2009Inventors: Hasan Dindi, James Arnold Schultz
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Patent number: 7468382Abstract: Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: March 27, 2006Date of Patent: December 23, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Steven Richard Brunette, Jin Mi Kim, Rene′ Marc Lemieux, Matt Aaron Tschantz
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Patent number: 7456315Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: GrantFiled: February 26, 2004Date of Patent: November 25, 2008Assignee: Intrexon CorporationInventors: Robert Eugene Hormann, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20080045546Abstract: This invention relates to tetrahydro-naphthalene and urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene and urea derivatives of the present invention have vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).Type: ApplicationFiled: October 2, 2004Publication date: February 21, 2008Inventors: Axel Bouchon, Nicole Diedrichs, Achim Hermann, Klemens Lustig, Heinrich Meier, Josef Pemerstorfer, Elke Reissmuller, Muneto Mogi, Takeshi Yura, Hiroshi Fujishima, Masanori Seki, Yuji Koriyama, Kayo Yasoshima, Keiko Misawa, Masaomi Tajimi, Noriyuki Yammoto, Klaus Urbahns, Fumihiko Hayashi, Yasuhiro Tsukimi, Jang Gupta
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Patent number: 7304161Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: GrantFiled: February 9, 2004Date of Patent: December 4, 2007Assignee: Intrexon CorporationInventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
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Patent number: 7300991Abstract: The disclosure discloses a polymer represented by the general formula, wherein Rp is a residue of a polymer of a compound having a polymerizable unsaturated bond, Q is an organic residue of n+1 valences and connected directly or through another group to Rp by means of a single bond, Mk+ is a cation of k valence, Z is an organic function group capable of forming an ionic bond with cation Mk+ or an organic function group having a coordination capability with Mk+, and m, n and k are integers of one or more. The disclosure also discloses an intermediate of the polymer mentioned above.Type: GrantFiled: March 21, 2003Date of Patent: November 27, 2007Assignee: Hitachi, Ltd.Inventors: Shin Nishimura, Akira Satou, Takefumi Okumura, Makoto Morishima, Hitoshi Yamamoto, Norikazu Ueyama
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Patent number: 7279470Abstract: Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may be useful in the treatment and/or prevention of medical disorders where a decreased activity of hormone-sensitive lipase is desirable.Type: GrantFiled: December 13, 2002Date of Patent: October 9, 2007Assignee: Novo Nordisk A/SInventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
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Patent number: 7273867Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disordersType: GrantFiled: December 5, 2001Date of Patent: September 25, 2007Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
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Patent number: 6992192Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: May 2, 2002Date of Patent: January 31, 2006Assignee: Lilly Icos LLC.Inventors: Jason S. Sawyer, Mark W. Orme
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Patent number: 6949539Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: GrantFiled: June 1, 2001Date of Patent: September 27, 2005Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Mark Furber
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Patent number: 6815556Abstract: A compound according to formula one that is useful as a fungicide is provided. Additionally, processes to make and use same are provided.Type: GrantFiled: June 9, 2003Date of Patent: November 9, 2004Assignee: Dow AgroSciences LLCInventors: Carla Jean Rasmussen Klittich, Jeannie Rachel Cetusic, Marilene Tenguan Iamauti, Irene Mae Morrison, Michael Thomas Sullenberger, William Chi-Leung Lo, Ann Marie Buysse, Brent Jeffrey Rieder, John Todd Mathieson, Monica Britt Olson, Michael John Ricks
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Patent number: 6727265Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.Type: GrantFiled: April 15, 2003Date of Patent: April 27, 2004Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Venkatachalam
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Patent number: 6713492Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.Type: GrantFiled: May 24, 2001Date of Patent: March 30, 2004Assignees: Daiichi Radioisotope Laboratories, Ltd., Yamagata Public Corporation for the Development of IndustryInventors: Osamu Itoh, Heitaro Obara, Hidekatsu Yokoyama, Masaaki Aoyama
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Patent number: 6667327Abstract: Disclosed are pyridine amido derivatives of the formula wherein X, Y, and R1 to R6 are as defined herein. These compounds are selective MAO-B inhibitors and are useful in treating diseases such as, for example, Alzheimer's and senile dementia. Also disclosed are pharmaceutical compositions containing such compounds and a method of preparing such compounds.Type: GrantFiled: January 14, 2003Date of Patent: December 23, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Publication number: 20030158233Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: December 20, 2002Publication date: August 21, 2003Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans,
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Patent number: 6608204Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: December 13, 1994Date of Patent: August 19, 2003Assignee: Corvas International, Inc.Inventor: Susan Yoshiko Tamura
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Patent number: 6603044Abstract: The present invention provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.Type: GrantFiled: November 29, 1999Date of Patent: August 5, 2003Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
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Patent number: 6452008Abstract: A process for preparing a pyridone derivative (4), which comprises reacting the compound (1) with a hypochlorite or a hypobromite or with lead tetraacetate to give the compound (2), and reacting the compound (2) with the compound (3). Said process is preferably especially from the standpoint of safety. wherein R1 is hydrogen, alkyl, substituted alkyl, etc.; Y1 is hydrogen, alky, substituted alky, etc.; Y2 and Y3 are indenpently hydrogen, halogen, etc.; and L is alkyl, substituted alkyl, etc.Type: GrantFiled: May 14, 2001Date of Patent: September 17, 2002Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Masami Muraoka, Koji Morishita, Nagisa Aida, Masashi Tanaka, Masatoshi Yuri, Naohito Ohashi
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Publication number: 20020061887Abstract: The present invention relates to compounds of the formula I 1Type: ApplicationFiled: November 28, 2001Publication date: May 23, 2002Applicant: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schonafinger, Hartmut Strobel