Chalcogen Bonded Directly To Chalcogen Patents (Class 546/294)
  • Patent number: 10085985
    Abstract: The present invention provides for compounds of formula (I) wherein Y1, Y2, R1, R2, R3, A1, A2, A3, and A4, have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: October 2, 2018
    Assignee: AbbVie Inc.
    Inventors: Andrew Bogdan, Warren M. Kati, Keith F. McDaniel, Chang H. Park, George S. Sheppard, Le Wang
  • Patent number: 9487485
    Abstract: An object of the present invention is to provide a production method of an intermediate used in the production method of a sulfonylpyrrole compound useful as a pharmaceutical product. The present invention relates to a method of producing sulfonylpyrrole compound (VI) by reacting a pyridine-3-sulfonic acid compound with phosphorus pentachloride in a solvent of chlorobenzene or trifluoromethylbenzene to give a pyridine-3-sulfonyl chloride compound, reacting the compound without isolation with compound (III) to give compound (IV), and subjecting the compound (IV) to a reductive amination reaction. wherein R2 is a hydrocarbon group etc. and R3 and R4 are each a hydrogen atom etc., wherein R1 is an optionally substituted pyridin-3-yl group, and the other symbols are as defined above, wherein R5 is an alkyl group and the other symbols are as defined above.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: November 8, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventor: Keisuke Majima
  • Patent number: 9115150
    Abstract: Provided are a camptothecin compound containing 7-membered lactone ring, as shown in general formula I, and pharmaceutically acceptable salt thereof, as well as the preparation method and use thereof. In general formula I, R1 is H, a C1˜C3 alkyl, acetyl or propionyl; R2 is H, a C1˜C6 alkyl, a C3˜C6 cycloalkyl, piperidyl; or a C1˜C6 alkyl substituted by an amino; R3 is H, a C1˜C3 alkyl, or a C1˜C6 alkyl substituted by an amino; R4 is H, a hydroxyl, or a C1˜C6 alkoxy; R5 is H, or a C1˜C6 alkoxyl; or R4 and R5 are linked to each other to form —OCH2O— or —OCH2CH2O—. The compound has good anti-tumor activity, and can be clinically used via oral administration, intravenous injection, and intramuscular injection, among others.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: August 25, 2015
    Assignees: EAST CHINA NORMAL UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, NANJING LUYESIKE PHARMACEUTICAL CO., LTD.
    Inventors: Wei Lv, Shanbao Yu, Yu Luo, Yi Chen, Jian Ding
  • Publication number: 20150141468
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing metabolic disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be also used to the treatment of diabetes, lipid peroxidation, hypertriglyceridemia, metabolic disorders, free radical generated due to reactive oxygen and carbonyl groups, ionizing radiation, advanced glycation end products, kidney disease, renal complications and kidney stone disease.
    Type: Application
    Filed: February 1, 2013
    Publication date: May 21, 2015
    Applicant: Mahesh KANDULA
    Inventor: Mahesh Kandula
  • Patent number: 8969561
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: March 3, 2015
    Assignee: Dipharma Francis S.r.l.
    Inventors: Emanuele Attolino, Alessandro Lombardo, Simone Tambini
  • Publication number: 20150057316
    Abstract: The present description relates to compounds of Formula I (A+ X?), a diastereoisomer, an enantiomer, or a mixture thereof, pharmaceutical composition comprising same and uses thereof for gastrointestinal endoscopic and medical imaging applications, and for the treatment of visceral pain: Where R1 and R2 are as defined herein
    Type: Application
    Filed: March 11, 2013
    Publication date: February 26, 2015
    Inventors: Jean-Francois Meunier, Cheuk Kun Lau, Daniel Guay, Gregory Bydlinski, Nadejda Spassova, Louis-David Cantin, Maxime Ranger
  • Publication number: 20150025242
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 22, 2015
    Applicant: DIPHARMA FRANCIS S.r.l.
    Inventors: Emanuele ATTOLINO, Alessandro LOMBARDO, Simone TAMBINI
  • Publication number: 20140360395
    Abstract: A color-forming composition contains (A) a radical generator, (B) a compound represented by the following formula (1) and (C) a binder polymer: wherein, in the formula (1), R1 represents a group which reacts with a radical generated from the radical generator (A) to be released and forms a dye after the release, and T represents a nitrogen-containing hetero ring.
    Type: Application
    Filed: August 22, 2014
    Publication date: December 11, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Koki NAKAMURA, Akio MIZUNO, Shota SUZUKI
  • Patent number: 8884016
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: November 11, 2014
    Assignee: Dipharma Francis S.r.l.
    Inventor: Chiara Vladiskovic
  • Publication number: 20140275536
    Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.
    Type: Application
    Filed: December 22, 2010
    Publication date: September 18, 2014
    Applicant: Galderma Research & Development
    Inventor: Cédric Poinsard
  • Publication number: 20140272601
    Abstract: Salts with formula X?M+ wherein M+ is Li, Na, K, an ammonium, a phosphonium, an imidazolium, a pyridinium, or a pyrazolium and X? is an anion formed from covalent linking of two negative moieties to a positive onium-type core are provided. Also provided are electrolytes and batteries produced from these salts.
    Type: Application
    Filed: November 16, 2012
    Publication date: September 18, 2014
    Inventors: Erlendur Jónsson, Michel Bernard Armand, Jens Patrik Johansson
  • Patent number: 8829003
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilizing or immobilizable derivative thereof; wherein: any one or two of X.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: September 9, 2014
    Assignee: Changzhou Le Sun Pharmaceuticals Limited
    Inventors: Shudong Wang, Osama Chahrour, Tiangong Lu, Anran Hu
  • Publication number: 20140235565
    Abstract: The present invention provides N-alkylthio ?-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 21, 2014
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: EDWARD TUROS, KEVIN D. REVELL
  • Publication number: 20140221337
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.
    Type: Application
    Filed: February 6, 2014
    Publication date: August 7, 2014
    Applicant: Xention Limited
    Inventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
  • Publication number: 20140200239
    Abstract: The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III.
    Type: Application
    Filed: August 3, 2012
    Publication date: July 17, 2014
    Applicant: National Taiwan University
    Inventors: Chung-Wai Shiau, Kuen-Feng Chen
  • Publication number: 20140135502
    Abstract: Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert the resulting products to substantially a single salt form.
    Type: Application
    Filed: October 3, 2013
    Publication date: May 15, 2014
    Applicant: IMMUNOGEN, INC.
    Inventors: Wei Li, Robert Yongxin Zhao
  • Publication number: 20140058107
    Abstract: Process for the preparation of apixaban and intermediates useful for the preparation thereof.
    Type: Application
    Filed: June 7, 2012
    Publication date: February 27, 2014
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Chiara Vladiskovic, Emanuele Attolino, Alessandro Lombardo, Simone Tambini
  • Publication number: 20140057919
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Application
    Filed: October 31, 2013
    Publication date: February 27, 2014
    Applicant: Pfizer Inc.
    Inventors: Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
  • Patent number: 8598213
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: December 3, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20130231486
    Abstract: Disclosed herein are novel compounds which are useful as intermediates for producing substituted sulfoxide compounds and a process for producing the same. Further disclosed is a process for producing the substituted sulfoxide compounds used as pharmacologically active agents, employing the novel intermediates of the present invention.
    Type: Application
    Filed: April 11, 2013
    Publication date: September 5, 2013
    Applicant: Matrix Laboratories Limited
    Inventors: Saswata LAHIRI, Lakshmana Rao VADALI, Swamy SAIDUGARI, Verra Narayana BANDLAMUDI, Parameshwar MAKAM, Seshadri Rao MANUKONDA, Debashish DATTA
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20130203790
    Abstract: Novel sulphur-containing compounds and pharmaceutically acceptable salts thereof are disclosed, which have utility as anti-proliferative agents against mammalian cells. The invention provides a method for synthesizing the sulphur-containing compounds.
    Type: Application
    Filed: July 9, 2012
    Publication date: August 8, 2013
    Applicant: 221076 ONTARIO INC.
    Inventors: Dheeraj RAJAN, Mark Otto BAERLOCHER
  • Publication number: 20130197059
    Abstract: The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.
    Type: Application
    Filed: January 24, 2013
    Publication date: August 1, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • 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: 20130158271
    Abstract: Bivalent linkers to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.
    Type: Application
    Filed: September 11, 2012
    Publication date: June 20, 2013
    Inventors: Iontcho Radoslavov VLAHOV, Christopher Paul LEAMON, Apparao SATYAM, Stephen J. HOWARD
  • Publication number: 20130102639
    Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.
    Type: Application
    Filed: September 13, 2012
    Publication date: April 25, 2013
    Applicant: The Regents of the University of California
    Inventors: Ohyun Kwon, Fuyuhiko Tamanoi, Hannah Fiji, Masaru Watanabe
  • Patent number: 8367065
    Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: February 5, 2013
    Assignee: Enzon Pharmaceuticals, Inc.
    Inventors: Hong Zhao, Prasanna Reddy, Maria Belen Rubio
  • Publication number: 20130012530
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Patent number: 8338610
    Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: December 25, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Daniel Kuzmich, Pingrong Liu, Hossein Razavi
  • Patent number: 8334286
    Abstract: The invention refers to compounds of general formula (I) wherein the R groups are, independently, H, C1-6alkyl, aryl, CF3; Y is CH2, C?O; X is bond, C?O, SO2, or C?N—CN; m is 0, 1; n is 0, 1; A is a heterocycle, or a phenyl group optionally substituted as defined in the specification. The compounds are active on chronic pain conditions of different origin; they can be administered alone or with other drugs. Most of these compounds are new. The invention include a process to prepare said compounds, and pharmaceutical compositions suitable for their administration to a patient.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: December 18, 2012
    Assignee: Neurotune AG
    Inventors: Carla Ghelardini, Marisa Martinelli, Carlo Parini, Silvano Ronzoni
  • Patent number: 8314240
    Abstract: [Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: November 20, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Hideki Kubota, Issei Tsukamoto, Kazunori Kamijo, Koji Kato, Yuta Fukuda, Hidenori Azami
  • Patent number: 8299262
    Abstract: The present invention relates to novel pyridylmethyl-sulfonamide compounds of formula (I) where: n is 0 to 4; m is 0 to 4; R1 is halogen, CN, NO2, OH, SH, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc.; and/or two radicals R1 together form a fused ring; R2 is H, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C8-cycloalkyl, C1-C4-alkyl-C3-C8-cycloalkyl or benzyl; R3 is halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Y is —O—, C1-C4-alkanediyl, —O—CH2—, —CH2—O—, —C(NORn)—, —S—, —S(?O)—, —S(?O)2— or —N(Rn)—; and the N-oxides, and salts thereof and their use for combating phytopathogenic harmful fungi, and also to compositions and seed comprising at least one such compound.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: October 30, 2012
    Assignee: BASF SE
    Inventors: Wassilios Grammenos, Jan Klaas Lohmann, Thomas Grote, Jochen Dietz, Bernd Mueller, Michael Puhl, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Joachim Rheinheimer
  • Publication number: 20120259124
    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: Application
    Filed: March 14, 2012
    Publication date: October 11, 2012
    Applicant: Duquesne University of the Holy Ghost
    Inventors: FRASER FERGUSON FLEMING, Bhaskar Reddy Pitta
  • Publication number: 20120258985
    Abstract: Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, S—S is a disulfide group attached to an sp3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 11, 2012
    Applicant: Nektar Therapeutics
    Inventors: Antoni Kozlowski, Samuel McManus
  • Patent number: 8227490
    Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: July 24, 2012
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
  • Publication number: 20120165537
    Abstract: Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert the resulting products to substantially a single salt form.
    Type: Application
    Filed: December 8, 2011
    Publication date: June 28, 2012
    Applicant: IMMUNOGEN, INC.
    Inventors: Wei LI, Robert Yongxin ZHAO
  • Publication number: 20120149653
    Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 14, 2012
    Inventors: Alexander Chucholowski, Alisher Khasanov, Gregory Parker, Tong Zhu
  • Patent number: 8198314
    Abstract: The present invention provides indole derivatives that antagonize prostaglandin D2, and that can be used to treat inflammatory diseases mediated by prostaglandin D2.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: June 12, 2012
    Assignee: Oxagen Limited
    Inventors: David Middlemiss, Mark Richard Ashton, Edward Andrew Boyd, Frederick Arthur Brookfield, Michael George Hunter, Mark Whittaker, Chris Palmer, Eric R. Pettipher
  • Publication number: 20120136158
    Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.
    Type: Application
    Filed: February 8, 2012
    Publication date: May 31, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas COOK, Darren DiSALVO, Daniel Robert FANDRICK, Christian HARCKEN, Daniel KUZMICH, Thomas Wai-Ho LEE, Pingrong LIU, John LORD, Can MAO, Jochen NEU, Brian Christopher RAUDENBUSH, Hossein RAZAVI, Jonathan Timothy REEVES, Jinhua J. SONG, Alan David SWINAMER, Zhulin TAN
  • Publication number: 20120095012
    Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
    Type: Application
    Filed: December 30, 2009
    Publication date: April 19, 2012
    Applicant: Elara Pharmaceuticals GmbH
    Inventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen
  • Publication number: 20120035370
    Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.
    Type: Application
    Filed: October 14, 2011
    Publication date: February 9, 2012
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas COOK, Darren DiSALVO, Daniel Robert FANDRICK, Christian HARCKEN, Daniel KUZMICH, Thomas Wai-Ho LEE, Pingrong LIU, John LORD, Can MAO, Jochen NEU, Brian Christopher RAUDENBUSH, Hossein RAZAVI, Jonathan Timothy REEVES, Jinhua J. SONG, Alan David SWINAMER, Zhulin TAN
  • Publication number: 20120014997
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: September 26, 2011
    Publication date: January 19, 2012
    Inventors: Solomon Ungashe, J.J. Wright, Andrew Pennell, Zheng Wei, Anita Melikan
  • Publication number: 20110313168
    Abstract: The invention relates to a method for preparing an activated ester of the formula (I), where R is a (C1-C6) alkyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, and ALK is a (C1-C6) alkylene group, said method consisting of reacting the dicyclohexylamine P1 salt and the disuccinimidyl carbonate (DSC) in a solvent in which the dicyclohexylamine salt of the N-hydroxysuccinimide P2 is precipitated. The invention also relates to products of the formula P1.
    Type: Application
    Filed: December 15, 2009
    Publication date: December 22, 2011
    Applicant: SANOFI
    Inventor: Antony Bigot
  • Publication number: 20110237791
    Abstract: A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.
    Type: Application
    Filed: April 6, 2011
    Publication date: September 29, 2011
    Applicants: TAISHO PHARMACEUTICAL CO., LTD, NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Takanori KAWAGUCHI, Kengo WATATANI, Keiko FUSEGI, Masahiro BOHNO, Hajime ASANUMA, Shoichi KURODA, Yudai IMAI, Tomomichi CHONAN, Nagaaki SATO, Shigeru TOKITA, Shigetada SASAKO, Takumi OKADA, Keishi HAYASHI, Shin ITOH, Noriko SAITO, Rui JIBIKI, Seishi ISHIYAMA, Hirofumi OTA
  • Publication number: 20110230452
    Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Application
    Filed: September 23, 2010
    Publication date: September 22, 2011
    Inventor: Irving Sucholeiki
  • Publication number: 20110190227
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists Of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: July 2, 2009
    Publication date: August 4, 2011
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns, Jeffrey Roger Roppe
  • Patent number: 7981909
    Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: July 19, 2011
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
  • Publication number: 20110137042
    Abstract: Disclosed are processes for preparing compounds of formula (I): the compounds are useful as intermediates for preparing indazole and azaindazole substituted compounds.
    Type: Application
    Filed: December 1, 2010
    Publication date: June 9, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Hossein RAZAVI, Jonathan Timothy REEVES, Sonia RODRIGUEZ
  • Publication number: 20110112151
    Abstract: There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH?CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other than
    Type: Application
    Filed: February 25, 2009
    Publication date: May 12, 2011
    Inventors: Nigel Vicker, Xiangdong Su, Fabienne Pradaux-Caggiano, Barry Victor Lioyd Potter