Patents by Inventor Toyoharu Numata

Toyoharu Numata has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 10179779
    Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms of Polymorph Form I, Polymorph Form II, Polymorph Form III, Polymorph Form IV, Polymorph Form V, and Polymorph Form VI, and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: January 15, 2019
    Assignee: RaQualia Pharma Inc.
    Inventors: Toyoharu Numata, Hideyuki Aoyama, Kaori Muraji
  • Patent number: 9988370
    Abstract: Salts of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid are disclosed. More particularly, salt forms (HCl-salt, HBr-salt, p-toluenesulfonate salt and ethanedisulfonate salt) are disclosed. Furthermore, processes for the preparation of such salt forms, compositions containing such salt forms, and uses of such salt forms are disclosed. A method of treating disease conditions mediated by 5-HT4 receptor activity includes administering an effective amount of such salt forms to an animal, including a human, in need of such treatment.
    Type: Grant
    Filed: May 20, 2015
    Date of Patent: June 5, 2018
    Assignee: RaQualia Pharma Inc.
    Inventors: Toyoharu Numata, Masaki Sudo, Xufeng Sun
  • Publication number: 20170081318
    Abstract: Salts of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid are disclosed. More particularly, salt forms (HCl-salt, HBr-salt, p-toluenesulfonate salt and ethanedisulfonate salt) are disclosed. Furthermore, processes for the preparation of such salt forms, compositions containing such salt forms, and uses of such salt forms are disclosed. A method of treating disease conditions mediated by 5-HT4 receptor activity includes administering an effective amount of such salt forms to an animal, including a human, in need of such treatment.
    Type: Application
    Filed: May 20, 2015
    Publication date: March 23, 2017
    Applicant: RaQualia Pharma Inc.
    Inventors: Toyoharu Numata, Masaki Sudo, Xufeng Sun
  • Patent number: 9499543
    Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: November 22, 2016
    Assignee: RaQualia Pharma Inc.
    Inventors: Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi, Toyoharu Numata
  • Patent number: 9447096
    Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: September 20, 2016
    Assignee: RaQualia Pharma Inc.
    Inventors: Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi, Toyoharu Numata
  • Patent number: 9447066
    Abstract: This invention relates to salts and crystal forms of (S)-6-chloro-7-(1,1-dimethylethyl)-2-trifluoromethyl-2H-1-benzopyran-3-carboxylic acid, Compound A, which is cyclooxygenase-2 inhibitor. The present invention provides a salt of compound A, a crystal form thereof, a process for preparing the said salt and a pharmaceutical composition thereof and its use. The salts and/or co-crystals of Compound A of the present invention show good formulation properties such as high aqueous solubility, good intrinsic dissolution, good crystallinity, good thermal stability or low hygroscopicity.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: September 20, 2016
    Assignee: AskAt Inc.
    Inventors: Yoshiyuki Okumura, Yasuhiro Iwata, Toyoharu Numata, Masaki Sudo, Takako Okumura
  • Publication number: 20160083381
    Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.
    Type: Application
    Filed: May 28, 2014
    Publication date: March 24, 2016
    Applicant: RaQualia Pharma Inc.
    Inventors: Masaki SUDO, Kaoru SHIMADA, Hiroaki WAKABAYASHI, Toyoharu NUMATA
  • Publication number: 20150353520
    Abstract: This invention relates to salts and crystal forms of (S)-6-chloro-7-(1,1-dimethylethyl)-2-trifluoromethyl-2H-1-benzopyran-3-carboxylic acid, Compound A, which is cyclooxygenase-2 inhibitor. The present invention provides a salt of compound A, a crystal form thereof, a process for preparing the said salt and a pharmaceutical composition thereof and its use. The salts and/or co-crystals of Compound A of the present invention show good formulation properties such as high aqueous solubility, good intrinsic dissolution, good crystallinity, good thermal stability or low hygroscopicity.
    Type: Application
    Filed: January 6, 2014
    Publication date: December 10, 2015
    Applicant: AskAt Inc.
    Inventors: Yoshiyuki OKUMURA, Yasuhiro IWATA, Toyoharu NUMATA, Masaki SUDO, Takako OKUMURA
  • Patent number: 9187463
    Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: November 17, 2015
    Assignee: RAQUALIA PHARMA INC.
    Inventors: Toyoharu Numata, Hirohide Noguchi, Nobuaki Waizumi, Takashi Kojima
  • Publication number: 20150322055
    Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I, Polymorph Form II, Polymorph Form III, Polymorph Form IV, Polymorph Form V, and Polymorph Form VI), and to processes for the preparation of compositions containing and to uses of such polymorph forms.
    Type: Application
    Filed: November 21, 2013
    Publication date: November 12, 2015
    Applicant: RaQualia Pharma Inc.
    Inventors: Toyoharu Numata, Hideyuki Aoyama, Kaori Muraji
  • Publication number: 20140187583
    Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.
    Type: Application
    Filed: May 18, 2012
    Publication date: July 3, 2014
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Toyoharu Numata, Hirohide Noguchi, Nobuaki Waizumi, Takashi Kojima
  • Patent number: 7960407
    Abstract: The invention relates to the essentially pure ?/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the uses of, such crystal forms.
    Type: Grant
    Filed: March 1, 2006
    Date of Patent: June 14, 2011
    Assignee: Requalia Pharma Inc.
    Inventors: Naoaki Haruta, Tomoki Kato, Zheng Jane Li, Toyoharu Numata, Andrew Vincent Trask
  • Patent number: 7737163
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: June 15, 2010
    Assignee: Pfizer Inc.
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Patent number: 7705020
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: April 27, 2010
    Assignee: Pfizer Inc.
    Inventors: Koji Ando, Saturu Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Patent number: 7595329
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: September 29, 2009
    Assignee: Pfizer Inc
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Publication number: 20090018158
    Abstract: The invention relates to the essentially pure ?/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1 -yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the uses of, such crystal forms.
    Type: Application
    Filed: March 1, 2006
    Publication date: January 15, 2009
    Inventors: Naoaki Haruta, Tomoki Kato, Zheng Jane Li, Toyoharu Numata, Andrew Vincent Trask
  • Publication number: 20080108660
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Application
    Filed: January 9, 2008
    Publication date: May 8, 2008
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Publication number: 20050277672
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Application
    Filed: June 14, 2005
    Publication date: December 15, 2005
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Publication number: 20050277671
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Application
    Filed: June 14, 2005
    Publication date: December 15, 2005
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki
  • Publication number: 20050277673
    Abstract: This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
    Type: Application
    Filed: June 14, 2005
    Publication date: December 15, 2005
    Inventors: Koji Ando, Satoru Iguchi, Noriaki Murase, Yoshinori Murata, Toyoharu Numata, Hiroki Sone, Chikara Uchida, Tatsuo Ueki