Double Bonded Divalent Chalcogen Containing Patents (Class 544/52)
  • Patent number: 9604944
    Abstract: The present invention provides arylpiperazine derivatives having Formula 1a as shown below, which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression,
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: March 28, 2017
    Assignee: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Patent number: 9246239
    Abstract: A crimped terminal for automobiles includes an aluminum electric wire, a connecting terminal made from a copper-based material, and a resin-coated portion. The connecting terminal is crimped onto an end of the wire and includes a crimped member, a crimped portion where the terminal is crimped onto the wire, and the resin-coated portion disposed on the crimped portion, wherein the resin-coated portion is disposed on the crimped portion while an entire periphery of the crimped portion is coated with the resin-coated portion.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: January 26, 2016
    Assignees: AUTONETWORKS TECHNOLOGIES, LTD., SUMITOMO WIRING SYSTEMS, LTD., SUMITOMO ELECTRIC INDUSTRIES, LTD.
    Inventors: Akiko Inoue, Takehiro Hosokawa, Yasuyuki Otsuka, Fumitoshi Imasato, Tetsuya Nakamura, Shigeyuki Tanaka, Yutaka Takata, Yoshiaki Yamano, Kazunari Sakura, Naoya Nishimura, Takaaki Ito
  • Patent number: 9242945
    Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, Ar, and n are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: January 26, 2016
    Assignee: TEMPLE UNIVERSITY—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 8999976
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
    Type: Grant
    Filed: December 9, 2013
    Date of Patent: April 7, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Dennis Hurley, Lev T. D. Fanning, Peter D. J. Grootenhuis, Martyn Botfield, Fredrick Van Goor
  • Publication number: 20150080373
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Patent number: 8980883
    Abstract: The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: March 17, 2015
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Publication number: 20150072975
    Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
  • Publication number: 20150065492
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Application
    Filed: June 10, 2014
    Publication date: March 5, 2015
    Inventors: Peter Dragovich, Douglas E. Murphy
  • Publication number: 20150065487
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Publication number: 20150051188
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1a represents H or carboxy and R1b represents H, or R1a and R1b represent together either the group *—C(O)—NH—S—# or the group *—C(OH)?N—S—# wherein “*” represents the point of attachment of R1a and “#” represents the point of attachment of R1b; R2 represents H, (C1-C3)alkyl, hydroxy-(C1-C3)alkyl, benzyl or (C3-C5)cycloalkyl; R3 represents H or halogen; U represents N or CR4; wherein R4 is H or (C1-C3)alkoxy; A represents CH, B represents NH and m represents 1 or 2 and n represents 1 or 2; or A represents N, B is absent, m represents 2 and n represents 2; Y represents CH or N; and Q represents O or S; and salts of such compounds.
    Type: Application
    Filed: November 7, 2012
    Publication date: February 19, 2015
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Publication number: 20150031685
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 29, 2015
    Applicant: Dr. Reeddy's Laboratories Ltd.
    Inventors: Pradip Kumar Sasmal, Chintakunta Vamseekrishna, Vijay Potluri, Ashok Tehim, Yonghua Gai, Hang Zhang
  • Patent number: 8940271
    Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: January 27, 2015
    Assignee: Abbott Laboratories
    Inventors: Mark C. Heit, Antonio M. Benitz, Dennis F. Steadman, David M. Petrick
  • Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20150005294
    Abstract: The invention provides novel substituted azaheterocyclic compounds compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.
    Type: Application
    Filed: January 10, 2013
    Publication date: January 1, 2015
    Applicants: CANCER RESEARCH TECHNOLOGY LIMITED, MERCK PATENT GMBH
    Inventors: Kai Schiemann, Frank Stieber, Christina Esdar
  • Publication number: 20140364414
    Abstract: Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: December 11, 2014
    Applicant: JANSSEN PHARMACEUTICA, NV
    Inventors: Mark R. Player, Sanath K. Meegalla, Carl R. Illig, Jinsheng Chen, Kenneth J. Wilson, Yu-Kai Lee, Daniel J. Parks, Hui Huang, Sharmila Patel, Tianbao Lu
  • Publication number: 20140343277
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Application
    Filed: June 25, 2014
    Publication date: November 20, 2014
    Inventors: Shinichi TAIRA, Kunio OSHIMA, Takashi OSHIYAMA, Yasuhiro MENJO, Yasuo KOGA, Hokuto YAMABE, Sunao NAKAYAMA, Kenji TSUJIMAE, Toshiyuki ONOGAWA, Kuninori TAI, Motohiro ITOTANI
  • Publication number: 20140309218
    Abstract: The invention relates to antibacterial compounds of formula I wherein G and K are as defined in the description; and salts of such compounds.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 16, 2014
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Publication number: 20140235625
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using such CFTR modulators.
    Type: Application
    Filed: December 9, 2013
    Publication date: August 21, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Dennis Hurley, Lev T.D. Fanning, Peter D.J. Grootenhuis, Martyn Botfield, Fredrick Van Goor
  • Publication number: 20140235855
    Abstract: Compounds of formula (I), wherein A1 represents —O—, —S— or —CH2—; A2 represents —CH2— or —O—; A3 represents C3-C8-cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, —C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; m is 0 or 1; n is 1; the —(CH2)n— group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.
    Type: Application
    Filed: June 11, 2012
    Publication date: August 21, 2014
    Inventors: Berangere Gaucher, Franck Hubert Danel, Tong Xie, Lin Xu
  • Publication number: 20140221348
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: March 17, 2014
    Publication date: August 7, 2014
    Applicant: Basilea Pharmaceutica AG
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8765940
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: July 1, 2014
    Assignee: Amgen Inc.
    Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
  • Publication number: 20140179675
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140171425
    Abstract: The invention relates to antibacterial compounds of formula (I), wherein R1 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; R2 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy or pyrrolidin-1-yl; R3 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy, vinyl or 2-methoxycarbonyvinyl or R2 and R3 together with the two carbon atoms which bear them form a phenyl ring; R4 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; and R5 is H, (C1-C3)alkyl or cyclopropyl, or R4 and R5 form together a —CH2CH2CH2— group; A is the divalent group —CH2—, —CH2CH2—, #—CH(OH)CH2—*, #—CH2N(R6)—* and —CH2NHCH2—, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: June 19, 2014
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Publication number: 20140163016
    Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
    Type: Application
    Filed: December 11, 2013
    Publication date: June 12, 2014
    Applicant: NeurAxon, Inc.
    Inventors: Jailall RAMNAUTH, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
  • Publication number: 20140142093
    Abstract: The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CR6 or N; R0 is H or, if “----” is a bond, may also be alkoxy; R1 is cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH2, NH or NH9; R2 is H, alkylcarbonyl or CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2, wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the s
    Type: Application
    Filed: December 4, 2013
    Publication date: May 22, 2014
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Christian HUBSCHWERLEN, Daniel RITZ, Georg RUEEDI, Jean-Philippe SURIVET, Cornelia ZUMBRUNN-ACKLIN
  • Patent number: 8723017
    Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: May 13, 2014
    Assignee: BASF SE
    Inventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
  • Patent number: 8716280
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Grant
    Filed: January 21, 2010
    Date of Patent: May 6, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Patent number: 8703721
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Publication number: 20140086941
    Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, Ar, and n are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicants: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI, TEMPLE UNIVERSITY - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Publication number: 20140080770
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 17, 2013
    Publication date: March 20, 2014
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
  • Publication number: 20140080788
    Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.
    Type: Application
    Filed: April 27, 2012
    Publication date: March 20, 2014
    Inventors: Jeffrey A. Robl, Jun Li, Lawrence J. Kennedy, Steven J. Walker, Haixia Wang, William N. Washburn, Saleem Ahmad, Khehyong Ngu
  • Patent number: 8658639
    Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: February 25, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd
    Inventors: Satoshi Suetsugu, Nobuhisa Fukuda, Yoshio Nakai, Takashi Takada, Yohei Ikuma, Hiroyuki Nakahira
  • Publication number: 20140031346
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is CR3, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Application
    Filed: September 30, 2013
    Publication date: January 30, 2014
    Applicant: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich
  • Publication number: 20130338151
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Publication number: 20130324524
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: August 7, 2013
    Publication date: December 5, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8507478
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; U and V each independently are CH or N; is a bond or is absent; W is CH or N or, when is absent, W is CH2 or NH, with the proviso that U, V and W are not all N; A is a bond or CH2; R2 is H or, provided A is CH2, may also be OH; m and n each independently are 0 or 1; D is CH2 or a bond; G represents a phenyl group substituted once or twice in the meta and/or para position(s) by substituents selected from alkyl, (C1-C3)alkoxy and halogen, or G is a group G1 or G2 wherein Z1, Z2 and Z3 may each represent CH or N; X is N or CH and Q is O or S; it being understood that if m and n each are 0, then A is CH2; and salts of such compounds.
    Type: Grant
    Filed: October 9, 2009
    Date of Patent: August 13, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Patent number: 8492111
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: July 23, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
  • Patent number: 8461154
    Abstract: The present invention provides arylpiperazine derivatives having Formula I which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: June 11, 2013
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Patent number: 8389511
    Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, being useful as a renin inhibitor. [wherein R1a is halogen, etc.; R1m is H, etc.; G1 is —N(R1b)—, etc.; G2 is —CO—, etc.; G3 is —C(R1c)(R1d)—, etc.; G4 is oxygen, etc.; R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are independently the same or different, H, etc.; R3 is H, optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are independently the same or different, and a group: -A-B (said A is single bond, etc., and said B is H, etc.), etc.; and n is 1, etc.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: March 5, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Hiroyuki Nakahira, Yohei Ikuma, Nobuhisa Fukuda, Kozo Yoshida, Hidenori Kimura, Satoshi Suetsugu, Akira Fusano, Kiyoto Sawamura, Junya Ikeda, Yoshio Nakai
  • Publication number: 20130035327
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: October 8, 2012
    Publication date: February 7, 2013
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 8349826
    Abstract: The invention relates to compounds of Formula (I) wherein U, V, W, R1, R1b, A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: January 8, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Patent number: 8349828
    Abstract: The invention relates to antibacterial compounds of formula I wherein n is 0 or 1; R1 represents H or F; U represents CH2 or, provided n is 1, O or NH; “-----” is a bond or is absent; V represents CH or N when “-----” is a bond, or CH2 or NH when “-----” is absent; W represents CH or N; A represents —(CH2)p—NH—(CH2)q— wherein p is 1 and q is 1 or 2 or, provided U represents CH2 and n is 1, p may also be 0 and q is then 2; G represents one of the groups 1 wherein Z represents N or CH and Q represents O or S; and Z0, Z1 and Z2 each represent CH, or Z0 and Z1 each represent CH and Z2 represents N, or Z0 represents CH, Z1 represents N and Z2 represents CH or N, or Z0 represents N and Z1 and Z2 each represent CH; and to salts of such compounds.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: January 8, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • Publication number: 20120329775
    Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: June 4, 2012
    Publication date: December 27, 2012
    Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
  • Publication number: 20120309751
    Abstract: New tertiary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are also active against Candida species such as Candida Albicans and Candida Glabrata.
    Type: Application
    Filed: December 28, 2010
    Publication date: December 6, 2012
    Applicant: POLICHEM SA
    Inventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
  • Publication number: 20120270863
    Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
    Type: Application
    Filed: October 21, 2010
    Publication date: October 25, 2012
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Publication number: 20120245345
    Abstract: Compound of formula (I): wherein A1 represents —O—, —S— or —N—R3; A2 represents —CH2—, —O—, —N—R4, —C(?O)— or —CH(O—R4)—; A3 represents C3-C8cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, C2-C4alkenylene, >C?O or a group selected from —C2H4NH—, —C2H4O—, and —C2H4S— being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is un-substituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which sub
    Type: Application
    Filed: December 17, 2010
    Publication date: September 27, 2012
    Applicant: BASILEA PHARMACEUTICA AG
    Inventors: Bérangère Gaucher, Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin Xu
  • Publication number: 20120220574
    Abstract: The present invention provides arylpiperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
    Type: Application
    Filed: May 7, 2012
    Publication date: August 30, 2012
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey