Patents Assigned to Shionogi & Co., Ltd.
  • Substituted polycyclic carbamoyl pyridone derivative prodrug
    Patent number: 10202379
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: August 14, 2017
    Date of Patent: February 12, 2019
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Chika Takahashi, Hidenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa
  • Fused pyrazole derivative having autotaxin inhibitory activity
    Patent number: 10189843
    Abstract: The present invention provides a compound of formula (1), wherein R1, R2, R3, R4a, R4b, R5a and R5b are as defined in the description, which has an autotaxin inhibitory activity, a pharmaceutical composition comprising the compound as an active ingredient, and a method of prevention or treatment of a disease involving autotaxin, which is characterized by administering the compound.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: January 29, 2019
    Assignees: THE UNIVERSITY OF TOKYO, TOHOKU UNIVERSITY, SHIONOGI & CO., LTD.
    Inventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Mitsuyasu Kawaguchi, Osamu Nureki, Ryuichiro Ishitani, Hiroshi Nishimasu, Junken Aoki, Chiaki Fujikoshi, Manabu Katou, Masahide Odan, Nobuyuki Tanaka, Yusuke Tateno, Junji Yamane
  • Pyrimidinone derivative having autotaxin-inhibitory activity
    Patent number: 10183949
    Abstract: A compound according to any one of formula (Ia) to (Ic), or its pharmaceutically acceptable salt: wherein R1, R2, R3, R4a, R4c, R5 are as defined in the description.
    Type: Grant
    Filed: February 24, 2017
    Date of Patent: January 22, 2019
    Assignees: THE UNIVERSITY OF TOKYO, TOHOKU UNIVERSITY, SHIONOGI & CO., LTD.
    Inventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Mitsuyasu Kawaguchi, Osamu Nureki, Ryuichiro Ishitani, Hiroshi Nishimasu, Junken Aoki, Nobuyuki Tanaka, Yasuhiko Kanda, Yoshiyuki Kioi, Yusuke Tateno, Shiro Kida, Junji Yamane
  • 2 substituted cephem compounds
    Patent number: 10174053
    Abstract: The compounds of the subject invention are related to 2-substituted cephem compounds, which have a wide antimicrobial spectrum, in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: January 8, 2019
    Assignees: Glaxo Group Limited, Shionogi and Co., Ltd.
    Inventors: Toshiaki Aoki, Hiroki Kusano, Xiangmin Liao, Neil David Pearson, Israil Pendrak, Jun Sato, Reema K. Thalji, Kenji Yamawaki, Katsuki Yokoo
  • PROCESS AND INTERMEDIATES FOR PREPARATION OF THIAZINE DERIVATIVES
    Publication number: 20190002420
    Abstract: The present invention provides a process for preparation of the compound of formula (VI), wherein each symbol is as defined in the specification, without using any intermediate compound showing mutagenicity. The process comprises salt formation of the intermediate compound of formula (I) with acid to enable optical resolution to isolate the intermediate compound of formula (II) in a stereo-selective manner.
    Type: Application
    Filed: December 22, 2016
    Publication date: January 3, 2019
    Applicant: Shionogi & Co., Ltd.
    Inventors: Naohiro ONODERA, Kouichi NOGUCHI, Shigeru ANDO, Daiki NAGAMATSU, Kenichi ISHIBASHI, Shunsuke OCHI, Aiko HASEGAWA, Katsuo ODA
  • Heterocycle and carbocycle derivatives having TrkA inhibitory activity
    Patent number: 10160727
    Abstract: The present invention relates to a compound represented by Formula (I): wherein -L- is —C(?X)—, or the like, —Z— is —NR5—, or the like, —ZA— is —NR5A—, or the like, —W— is —C(R8R9)n-, —WA— is —C(R3R4)m-, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: December 25, 2018
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenichiroh Nakamura, Takatsugu Inoue
  • HIV REPLICATION INHIBITOR
    Publication number: 20180362543
    Abstract: The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent. wherein ring A is substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle; R1 is substituted or unsubstituted alkyl etc.; R2 is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R3 is substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl; R4 is a hydrogen atom etc.; R6 is substituted or unsubstituted alkyl etc.
    Type: Application
    Filed: August 23, 2018
    Publication date: December 20, 2018
    Applicant: Shionogi & Co., Ltd.
    Inventors: Kenji TOMITA, Yoshiyuki TAODA, Tsutomu IWAKI, Takashi KAWASUJI, Toshiyuki AKIYAMA, Shuichi SUGIYAMA, Yoshinori TAMURA, Masafumi IWATSU
  • NON-AROMATIC HETEROCYCLIC DERIVATIVE HAVING MGAT2 INHIBITORY ACTIVITY
    Publication number: 20180353492
    Abstract: The present invention relates to a compound represented by Formula (I): wherein X is, for example, C(?O); Z is, for example, C(?O); L is, for example, a single bond; A is, for example, aromatic carbocycle; R is, for example, R6 or B; R2 is, for example, hydrogen; R3 is, for example, substituted or unsubstituted alkyl; R4a is, for example, hydrogen; R4b is, for example, hydrogen; R5 is, for example, halogen; R6 is, for example, halogen; R7a is, for example, hydrogen; R7b is, for example, hydrogen; R8 is, for example, hydrogen; R9 is, for example, hydrogen; m is 0 to 5; n is 0 to 5; and p is 1 to 6, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.
    Type: Application
    Filed: December 21, 2016
    Publication date: December 13, 2018
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yuji NISHIURA, Kana KURAHASHI, Naoki OHYABU, Yoshikazu SASAKI
  • Alkylene derivatives
    Patent number: 10150728
    Abstract: The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound. A compound of formula (I): wherein R1 is substituted or unsubstituted fused aromatic heterocyclyl etc., ring A is substituted or unsubstituted non-aromatic carbocycle etc., -L1- is —O—(CR6R7)m- etc., -L2- is —O—(CR6R7)n- etc., each R6 and R7 are independently hydrogen, halogen etc., R2 is substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is substituted or unsubstituted alkylcarbonyl etc.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: December 11, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Naotake Kobayashi, Kentarou Asahi, Yutaka Tomida, Masahide Ohdan, Masataka Fumoto, Yoshikazu Sasaki, Kana Kurahashi, Takatsugu Inoue, Tomomi Urabe, Yuji Nishiura, Masafumi Iwatsu, Keisuke Miyazaki, Naoki Ohyabu, Toshihiro Wada, Manabu Katou
  • Heterocyclic derivative having AMPK-activating activity
    Patent number: 10123994
    Abstract: A compound of formula: or its pharmaceutically acceptable salt. L is NR2R3, SR7, SO2R8, alkyl, or alkenyl; R2 is hydrogen, alkyl, alkenyl, or alkynyl; R3 is hydrogen, alkyl, alkenyl, alkynyl; R7 is hydrogen, alkyl, alkenyl, or alkynyl; R8 is hydrogen, alkyl, alkenyl, or alkynyl, provided that R8 is not unsubstituted methyl or trifluoromethyl; Y is alkyl, alkenyl, alkynyl, aryl, provided that Y is not unsubstituted methyl or unsubstituted ethyl; Z is —CR6?, or —N?; R1 is hydrogen, or alkyl; R4, R5 and R6 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, alkyl, alkenyl, or alkynyl.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: November 13, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Eiichi Kojima, Yu Hinata, Toshihiro Wada
  • Crystalline methyl (4R,12aS)-7-(benzyloxy)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylate
    Patent number: 10125147
    Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: November 13, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yukihito Sumino, Moriyasu Masui, Daisuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
  • Crystalline methyl (4R,12aS)-7-(benzyloxy)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1?,2?:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylate
    Patent number: 10125146
    Abstract: A crystalline methyl (4R,12aS)-7-(benzyloxy)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1?,2?:4,5] pyrazino[2,1-b][1,3]oxazine-9-carboxylate of the formula (U2):
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: November 13, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yukihito Sumino, Moriyasu Masui, Daisuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
  • Azabenzimidazole derivative having AMPK-activating activity
    Patent number: 10093670
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen, or substituted or unsubstituted alkyl, R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or the like, with the proviso that R1, R2 and R3 are not simultaneously hydrogen, X is a single bond, —S—, —O—, —NR5—, —C(?O)— or the like, R5 is hydrogen, or substituted or unsubstituted alkyl, Y is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl or the like.
    Type: Grant
    Filed: December 27, 2016
    Date of Patent: October 9, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Eiichi Kojima, Keisuke Tonogaki, Nobuyuki Tanaka, Manabu Katou, Akira Ino, Masafumi Iwatsu, Masahiko Fujioka, Yu Hinata, Naoki Ohyabu
  • Pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity
    Patent number: 10085973
    Abstract: The present inventor has found out that the following criteria enable to ensure an effect for increasing the platelet count while preventing an excessive increase in the platelet count; “when the platelet count has increased by a certain amount and reached to a sufficient level of the platelet count during administration of a pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity, administration of the pharmaceutical composition is discontinued thereafter”.
    Type: Grant
    Filed: July 14, 2016
    Date of Patent: October 2, 2018
    Assignee: Shionogi & Co., Ltd.
    Inventors: Takeshi Kano, Takahiro Fukuhara, Takayuki Katsube
  • Pharmaceutical composition for treating chronic kidney disease
    Patent number: 10087449
    Abstract: This invention is related to a therapeutic agent for treating chronic kidney disease comprising a substance which inhibits the enzymatic activity of NNMT or suppresses NNMT gene expression, or a method for screening a therapeutic agent for treating chronic kidney disease which targets the NNMT enzyme or NNMT gene.
    Type: Grant
    Filed: April 6, 2015
    Date of Patent: October 2, 2018
    Assignees: SHIONOGI & CO., LTD., KEIO UNIVERSITY
    Inventors: Takashi Ono, Katsutoshi Yamada, Norito Yoshimura, Toshihiro Shinosaki, Yoshinari Gahara, Hiroshi Itoh, Shu Wakino, Takeshi Kanda, Kazuhiro Hasegawa, Motoaki Komatsu
  • POLYCYCLIC PYRIDONE DERIVATIVE HAVING INTEGRASE INHIBITORY ACTIVITY
    Publication number: 20180265525
    Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Application
    Filed: May 24, 2018
    Publication date: September 20, 2018
    Applicant: Shionogi & Co., Ltd.
    Inventors: Tomokazu YOSHINAGA, Kouhei NODU
  • NUCLEIC ACID DERIVATIVE HAVING IMMUNOSTIMULATORY ACTIVITY
    Publication number: 20180264105
    Abstract: The purpose of the present invention is to provide double-stranded oligonucleotides comprising the CpG oligonucleotide mentioned below, as a nucleic acid derivative having an immunostimulatory activity. An adjuvant comprising a double-stranded oligonucleotide, wherein a first strand is a CpG oligonucleotide consisting of 8 to 50 nucleotides, a second strand is an oligonucleotide consisting of 8 to 60 nucleotides and comprising a sequence capable of hybridizing with the first strand, and a lipid binds to the second strand through a linker.
    Type: Application
    Filed: February 28, 2018
    Publication date: September 20, 2018
    Applicant: Shionogi & Co., Ltd.
    Inventors: Akira KUGIMIYA, Tetsuya TANINO, Mitsuaki SEKIGUCHI, Yasunori MITSUOKA, Norikazu KURODA, Jun NAKAMURA
  • Aminotriazine derivative and pharmaceutical composition comprising the same
    Patent number: 10065941
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic activity. A compound of Formula (I): wherein Ra and Rb, and Rd and Re are taken together to form oxo or the like; R4a and R4b are hydrogen or the like; n is 1 or the like; R2 is aryl or the like; s and s? is 0 or the like; R9 and R9? are halogen or the like; R20a and R20b are hydrogen, alkyl or the like; u is 1 to 4; R13 is hydrogen or the like, or its pharmaceutically acceptable salt.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: September 4, 2018
    Assignee: SHIONOGI & CO., LTD.
    Inventor: Hiroyuki Kai
  • SALTS OF QUINAZOLINE DERIVATIVE OR CRYSTALS THEREOF, AND THE PROCESS FOR PRODUCING THEREOF
    Publication number: 20180215744
    Abstract: Crystals of a quinazoline derivative are provided. The present invention relates to an acid addition salt of a compound represented by Formula (I): a pharmaceutical composition containing it, and the like.
    Type: Application
    Filed: July 28, 2016
    Publication date: August 2, 2018
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yukio TADA, Yuusuke TAMURA, Shuji YONEZAWA, Kenichi ISHIBASHI, Yuki MURAKAMI
  • TRICYCLIC COMPOUND HAVING SULFINYL OR SULFONYL
    Publication number: 20180186814
    Abstract: The present invention provides a compound exhibiting a strong antimicrobial spectrum against various bacteria, including gram-negative bacteria, or a pharmaceutical composition having an antimicrobial activity carbapenem-resistant bacteria. Provided is a compound represented by formula (I), an ester thereof or a pharmaceutically acceptable salt thereof, or a hydrate thereof. (I) (in the formula, —W— is —S(?O)— or S(?O)2—, -T- is CR4AR4B— or —CR5A—R5B—CR6A—R6B—, each of R2A and R2B is independently a hydrogen atom, etc., or R2A and R2B together form a substituted or unsubstituted methylidene, etc., R3 is a hydrogran atom, etc., R11 is a carboxyl, etc., and each of R7A and R7B is independently a hydrogen atom, etc.
    Type: Application
    Filed: June 30, 2016
    Publication date: July 5, 2018
    Applicant: Shionogi & Co., Ltd.
    Inventors: Kenji YAMAWAKI, Hiroki KUSANO