The Chalcogen Or The Acyclic Nitrogen Is Bonded Directly To The Six Membered Hetero Ring Patents (Class 546/292)
  • Patent number: 10759756
    Abstract: Disclosed are small molecule antagonists of ?4?7 integrin, and methods of using them to treat a number of specific diseases or conditions.
    Type: Grant
    Filed: April 12, 2019
    Date of Patent: September 1, 2020
    Assignee: 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
  • Patent number: 10343999
    Abstract: 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: Grant
    Filed: November 8, 2016
    Date of Patent: July 9, 2019
    Assignee: Galderma Research & Development
    Inventors: Jean-Guy Boiteau, Sebastien Daver, Nicolas Rodeville
  • Publication number: 20150133301
    Abstract: 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: Application
    Filed: April 29, 2014
    Publication date: May 14, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventors: 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
  • Patent number: 9018206
    Abstract: 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: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150105432
    Abstract: 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: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Takashi NAKAGAWA, Makoto SAKAMOTO, Kazuya YAMAGUCHI, Yuki TERAUCHI, Masamichi SHIRAKURA, Yasuo HARADA, Yutaka KOJIMA, Takumi SUMIDA
  • Patent number: 8865908
    Abstract: 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: Grant
    Filed: July 30, 2010
    Date of Patent: October 21, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
  • Publication number: 20140234245
    Abstract: 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: Application
    Filed: November 5, 2012
    Publication date: August 21, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Publication number: 20140213616
    Abstract: 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: Application
    Filed: January 29, 2014
    Publication date: July 31, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Publication number: 20140018326
    Abstract: 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: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
  • Publication number: 20130317020
    Abstract: 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: Application
    Filed: August 2, 2013
    Publication date: November 28, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
  • Patent number: 8563763
    Abstract: 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: Grant
    Filed: March 14, 2012
    Date of Patent: October 22, 2013
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Fraser Ferguson Fleming, Bhaskar Reddy Pitta
  • Publication number: 20130237702
    Abstract: 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: Application
    Filed: August 31, 2012
    Publication date: September 12, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masayuki SUGIKI, Toru OKAMATSU, Tetsuo YANO, Shinya TANIGUCHI
  • Patent number: 8524896
    Abstract: 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: Grant
    Filed: March 2, 2009
    Date of Patent: September 3, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
  • Publication number: 20130190325
    Abstract: 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: Application
    Filed: June 21, 2011
    Publication date: July 25, 2013
    Applicant: ITEK VENTURES PTY LTD
    Inventors: Shudong Wang, Osama Chahrour, Tiangong Lu, Anran Hu
  • Publication number: 20130150367
    Abstract: 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: Application
    Filed: September 12, 2012
    Publication date: June 13, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Patent number: 8455501
    Abstract: 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: Grant
    Filed: September 10, 2012
    Date of Patent: June 4, 2013
    Assignee: Hoffmann-La Roche Inc
    Inventors: Uwe Grether, Stephan Roever
  • Publication number: 20130065911
    Abstract: 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: Application
    Filed: September 10, 2012
    Publication date: March 14, 2013
    Inventors: Uwe Grether, Stephan Roever
  • Publication number: 20130065907
    Abstract: 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: Application
    Filed: September 11, 2012
    Publication date: March 14, 2013
    Inventors: Stephan Roever, Uwe Grether
  • Publication number: 20120258947
    Abstract: 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: Application
    Filed: April 18, 2012
    Publication date: October 11, 2012
    Applicant: Grunenthal GmbH
    Inventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
  • Publication number: 20120232049
    Abstract: 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: Application
    Filed: February 22, 2008
    Publication date: September 13, 2012
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Hiroshi Obaishi, Takayuki Nakagawa, Tomohiro Matsushima, Setsuo Funasaka, Shuji Shirotori, Keiko Takahashi
  • Publication number: 20120177634
    Abstract: This disclosure concerns novel demethylpenclomedine analogs. Also disclosed are pharmaceutical compositions and methods for using such compositions to treat hyperproliferative disorders.
    Type: Application
    Filed: February 22, 2012
    Publication date: July 12, 2012
    Inventor: Lee Roy Morgan
  • Publication number: 20120071513
    Abstract: 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: Application
    Filed: November 28, 2011
    Publication date: March 22, 2012
    Applicant: COMPASS PHARMACEUTICALS LLC
    Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
  • Patent number: 8101639
    Abstract: 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: Grant
    Filed: October 12, 2009
    Date of Patent: January 24, 2012
    Assignee: Array BioPharma Inc.
    Inventors: Allison L. Marlow, Eli M. Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong-Woon Yang, James Blake
  • Publication number: 20110319437
    Abstract: 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: Application
    Filed: August 31, 2011
    Publication date: December 29, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Shigeyuki ITOH, Atsushi IWATA
  • Publication number: 20110245210
    Abstract: 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: Application
    Filed: June 3, 2011
    Publication date: October 6, 2011
    Inventors: Nigel H. Greig, Harold Holloway, Arnold Brossi, Xiaoxiang Zhu, Tony Giordano, Qian-sheng Yu, William D. Figg
  • Publication number: 20110200535
    Abstract: 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: Application
    Filed: August 5, 2009
    Publication date: August 18, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Lutz Lehmann, Andrea Thiele, Tobias Heinrich, Sonja Vollmer
  • Publication number: 20110118470
    Abstract: 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: Application
    Filed: January 7, 2011
    Publication date: May 19, 2011
    Inventors: 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
  • Publication number: 20110082295
    Abstract: 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: Application
    Filed: May 27, 2009
    Publication date: April 7, 2011
    Applicants: Tokyo Institute of Technology, Kyoto University
    Inventors: Hachiro Sugimoto, Takashi Takahashi, Ichiro Hijikuro, Michiaki Okuda
  • Patent number: 7820827
    Abstract: 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: Grant
    Filed: September 1, 2005
    Date of Patent: October 26, 2010
    Assignee: Adolor Corporation
    Inventors: Bertrand Le Bourdonnec, Roland E. Dolle
  • Patent number: 7732616
    Abstract: 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: Grant
    Filed: May 17, 2006
    Date of Patent: June 8, 2010
    Assignee: Array BioPharma Inc.
    Inventors: Allison L. Marlow, Eli M. Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20090324569
    Abstract: 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: Application
    Filed: November 20, 2008
    Publication date: December 31, 2009
    Applicant: DECODE GENETICS EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Publication number: 20090137814
    Abstract: 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: Application
    Filed: November 27, 2007
    Publication date: May 28, 2009
    Inventors: Hasan Dindi, James Arnold Schultz
  • Patent number: 7468382
    Abstract: 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: Grant
    Filed: March 27, 2006
    Date of Patent: December 23, 2008
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Steven Richard Brunette, Jin Mi Kim, Rene′ Marc Lemieux, Matt Aaron Tschantz
  • Patent number: 7456315
    Abstract: 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: Grant
    Filed: February 26, 2004
    Date of Patent: November 25, 2008
    Assignee: Intrexon Corporation
    Inventors: Robert Eugene Hormann, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Publication number: 20080045546
    Abstract: 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: Application
    Filed: October 2, 2004
    Publication date: February 21, 2008
    Inventors: 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
  • Patent number: 7304161
    Abstract: 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: Grant
    Filed: February 9, 2004
    Date of Patent: December 4, 2007
    Assignee: Intrexon Corporation
    Inventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
  • Patent number: 7300991
    Abstract: 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: Grant
    Filed: March 21, 2003
    Date of Patent: November 27, 2007
    Assignee: Hitachi, Ltd.
    Inventors: Shin Nishimura, Akira Satou, Takefumi Okumura, Makoto Morishima, Hitoshi Yamamoto, Norikazu Ueyama
  • Patent number: 7279470
    Abstract: 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: Grant
    Filed: December 13, 2002
    Date of Patent: October 9, 2007
    Assignee: Novo Nordisk A/S
    Inventors: Soren Ebdrup, Johannes Cornelis de Jong, Poul Jacobsen, Holger Claus Hansen, Per Vedso
  • Patent number: 7273867
    Abstract: 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 disorders
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: September 25, 2007
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
  • Patent number: 6992192
    Abstract: Compounds of the general structural formula (I), and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: January 31, 2006
    Assignee: Lilly Icos LLC.
    Inventors: Jason S. Sawyer, Mark W. Orme
  • Patent number: 6949539
    Abstract: 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: Grant
    Filed: June 1, 2001
    Date of Patent: September 27, 2005
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Mark Furber
  • Patent number: 6815556
    Abstract: A compound according to formula one that is useful as a fungicide is provided. Additionally, processes to make and use same are provided.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: November 9, 2004
    Assignee: Dow AgroSciences LLC
    Inventors: 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
  • Patent number: 6727265
    Abstract: 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: Grant
    Filed: April 15, 2003
    Date of Patent: April 27, 2004
    Assignee: Parker Hughes Institute
    Inventors: Fatih M. Uckun, Taracad K. Venkatachalam
  • Patent number: 6713492
    Abstract: 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: Grant
    Filed: May 24, 2001
    Date of Patent: March 30, 2004
    Assignees: Daiichi Radioisotope Laboratories, Ltd., Yamagata Public Corporation for the Development of Industry
    Inventors: Osamu Itoh, Heitaro Obara, Hidekatsu Yokoyama, Masaaki Aoyama
  • Patent number: 6667327
    Abstract: 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: Grant
    Filed: January 14, 2003
    Date of Patent: December 23, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
  • Publication number: 20030158233
    Abstract: 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: Application
    Filed: December 20, 2002
    Publication date: August 21, 2003
    Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans,
  • Patent number: 6608204
    Abstract: 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: Grant
    Filed: December 13, 1994
    Date of Patent: August 19, 2003
    Assignee: Corvas International, Inc.
    Inventor: Susan Yoshiko Tamura
  • Patent number: 6603044
    Abstract: 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: Grant
    Filed: November 29, 1999
    Date of Patent: August 5, 2003
    Assignee: 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
  • Patent number: 6452008
    Abstract: 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: Grant
    Filed: May 14, 2001
    Date of Patent: September 17, 2002
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Masami Muraoka, Koji Morishita, Nagisa Aida, Masashi Tanaka, Masatoshi Yuri, Naohito Ohashi
  • Publication number: 20020061887
    Abstract: The present invention relates to compounds of the formula I 1
    Type: Application
    Filed: November 28, 2001
    Publication date: May 23, 2002
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Ursula Schindler, Karl Schonafinger, Hartmut Strobel