Patents by Inventor Toshihito Kumagai
Toshihito Kumagai 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).
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Patent number: 6600038Abstract: Carbamoyl tetrahydropyridine derivatives represented by the formula: [in the formula, R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C5 alkyl group, or the like; Y1-Y2 represents (R4)C═C(R5), (R6)C═N, N═N, (R7)N—CO, or N═C(R8); X1, X2, and X3 are identical or different, and each represents a hydrogen atom, a halogen atom, or the like; R3, R4, R5, and R6 are identical or different, and each represents a hydrogen atom or an alkyl group; R7 represents a hydrogen atom, a C1-C5 alkyl group, or the like; and R8 represents a hydrogen atom or a carbamoyl group] or a pharmaceutically acceptable salt thereof, and intermediates for the preparation thereof are provided. The derivatives described above are effective for diseases which are believed to involve CRF.Type: GrantFiled: August 30, 2001Date of Patent: July 29, 2003Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Kazuyuki Tomisawa
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Publication number: 20030134902Abstract: The present invention relates to 2-amino-6-fluorobicyclo[3.1.Type: ApplicationFiled: December 6, 2002Publication date: July 17, 2003Inventors: Atsuro Nakazato, Toshihito Kumagai, Kosuke Kanuma, Kazunari Sakagami
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Patent number: 6500958Abstract: The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.Type: GrantFiled: June 24, 2002Date of Patent: December 31, 2002Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Patent number: 6479674Abstract: The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.Type: GrantFiled: September 24, 2001Date of Patent: November 12, 2002Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Publication number: 20020156283Abstract: The present invention provides an arylpiperidine derivative of the formula (I) or a pharmaceutically acceptable salt thereof, which has antipsychotic effect: 1Type: ApplicationFiled: April 12, 2002Publication date: October 24, 2002Inventors: Masashi Nagamine, Makoto Gotoh, Masanori Yoshida, Atsuro Nakazato, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa
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Publication number: 20020156299Abstract: The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids.Type: ApplicationFiled: June 24, 2002Publication date: October 24, 2002Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Patent number: 6407121Abstract: The present invention provides an arylpiperidine derivative of the formula (I) or a pharmaceutically acceptable salt thereof, which has antipsychotic effect: wherein D is a carbon atom or a nitrogen atom, E is a CH group or a nitrogen atom, G is an oxygen atom, a sulfur atom, a nitrogen atom or an NH group, Y1 is a hydrogen atom or a halogen atom, n is an integer of 1 to 4, and R1 is a group represented by any of the formulas (i) to (iv) defined in the specification.Type: GrantFiled: September 13, 2000Date of Patent: June 18, 2002Assignees: Nihon Nohyaku Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Masashi Nagamine, Makoto Gotoh, Masanori Yoshida, Atsuro Nakazato, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa
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Patent number: 6392086Abstract: The present inventions relate to a (1S,5R,6S)- or (1SR, 5RS, 6SR)-3-fluoro-2-oxobicyclo[3.1.0]hex-3-ene-6-carboxylic acid derivative represented by Formula (1): [in the formula, R represents OR1 or NR1R2, wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a (C3-C6 cycloalkyl) (C1-C6 alkyl) group, an aryl group, an aryl (C1-C6 alkyl) group, a (C1-C6 alkoxy) (C1-C6 alkyl) group, a C1-C6 hydroxyalkyl group, a (C1-C6 alkylthio) (C1-C6 alkyl) group, or a C1-C6 mercaptoalkyl group], and a process for producing the same, and a process for efficiently producing a fluorine-containing amino acid compound acting on group 2 metabotropic glutamate receptors, which has treatment effects or prevention effects on psychiatric diseases or neurological diseases, characterized by hydrogenating the derivative, and subsequently, subjecting it to hydantoination or aminocyanidation, followed by hydrolysis.Type: GrantFiled: June 7, 2001Date of Patent: May 21, 2002Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa, Hisanako Ito, Takeo Taguchi
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Patent number: 6380384Abstract: A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom; or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 10, 2001Date of Patent: April 30, 2002Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
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Publication number: 20020049323Abstract: A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: 1Type: ApplicationFiled: April 10, 2001Publication date: April 25, 2002Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
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Patent number: 6333428Abstract: The present invention provides fluorobicyclo[3.1.0]hexane derivatives represented by the formula [wherein R1 and R2 are the same or different and each represents a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a C3-8 cycloalkyl-C1-5 alkyl group: Y1 and Y2 are the same or different and each represents a hydrogen atom, a C1-10 alkylthio group, a C3-8 cycloalkylthio group, a C3-8 cycloalkyl-C1-5 alkylthio group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or one represents a hydrogen atom and the other represents a hydroxyl group, a C1-5 alkoxy group, a C3-8 cycloalkoxy group or a C3-8 cycloalkyl-C1-5 alkoxy group; or Y1 and Y2 together represent an oxygen atom or —X(CH2)nX— (X represents an oxygen atom or a sulfur atom: N is 2 or 3)], pharmaceutically acceptable salts thereof, or hydrates thereof.Type: GrantFiled: February 22, 2001Date of Patent: December 25, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Patent number: 6329525Abstract: A 1,2-dihydro-2-oxoquinoline derivative represented by the formula: wherein Ar is a pyridyl group or a group represented by the formula: (wherein X3 and X4 are the same or different, and are each a hydrogen atom, a halogen atom, a C1-5 alkyl group, a C1-5 alkoxy group, a hydroxyl group or a trifluoromethyl group), Y is a nitrogen atom, CH or C(OH), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom, or X1 and X2 taken together form an alkylenedioxy group, and n is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 1, 2000Date of Patent: December 11, 2001Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
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Patent number: 6316498Abstract: Fluorine-containing amino acid derivatives represented general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein X1 represents hydrogen or fluorine; and R1 and R2 are the same or different and each represents hydrogen or lower C1-10 alkyl. These compounds are useful as drugs, in particular, group 2 metabotropic glutamate receptor agonists for treating and preventing psychiatric disorders such as schizophrenia, anxiety and associated diseases, depression, bipolar disturbance and epilepsy, and neurological diseases such as drug addiction, cognition disorder, Alzheimer's disease, Huntington's chorea, Parkinson's disease, motility disturbance associating muscular stiffness, cerebral ischemia, cerebral insufficiency, spinal cord lesion and head disturbance.Type: GrantFiled: July 27, 2000Date of Patent: November 13, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
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Patent number: 6291467Abstract: An aromaheterocyclic derivative represented by the formula: wherein Z is a group represented by the following formula: wherein Ar1 is a phenyl group or a phenyl group substituted with a halogen atom or an alkyl group of 1 to 5 carbon atoms, R2 is an alkyl group of 1 to 5 carbon atoms, Y is a hydrogen atom, a mercapto group, an alkylthio group of 1 to 5 carbon atoms, an amino group or an amino group substituted with one or two alkyl groups having 1 to 5 carbon atoms, Ar2 is a phenyl group of one or two substituents selected from the group consisting of a halogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms, a hydroxyl group and a trifluoromethyl group, or a phenyl group, B1-B2 is CH—CO or C═C(R1) (wherein R1 is a hydrogen atom or an alkyl group of 1 to 5 carbon atoms), and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof, which is a dopamine D4 receptor antagonist compound having an antipsychotic actioType: GrantFiled: September 15, 2000Date of Patent: September 18, 2001Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co. Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
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Patent number: 6281355Abstract: A nitrogen-containing tetracyclic compound represented by the formula: wherein Y1—Y2—Y3 is N—C═N or a group represented by the formula: C═C—NR3 (wherein R3 is a hydrogen atom, a C1-5 alkyl group or a nitrogen-containing C2-10 alkyl group), Y4 is S, SO, SO2, CH2 or a group represented by the formula: NR4 (wherein R4 is a C1-5 alkanoyl group or a C1-5 alkyl group), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom, and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 1, 2000Date of Patent: August 28, 2001Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Kuniaki Kondoh, Masanori Yoshida
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Patent number: 6187781Abstract: A 4-tetrahydropyridylpyrimidine compound represented by formula (I): wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, and a trifluoromethyl group, a phenyl group, a thienyl group or a furanyl group; R1 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms; R2 represents an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, an alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms; and X1, X2, and X3, which may be the same or different, each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, an alkylthio group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 orType: GrantFiled: September 21, 1999Date of Patent: February 13, 2001Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Taketoshi Okubo, Izumi Aibe, Hideo Tanaka, Shigeyuki Chaki, Shigeru Okuyama, Kazuyuki Tomisawa
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Patent number: 6166033Abstract: This invention provides a 2-carbonylthiazole derivative represented by formula (I): ##STR1## wherein each of Ar.sup.1 and Ar.sup.2 represents a phenyl group or a substituted phenyl group; R.sup.1 represents an alkoxy group having 1 to 5 carbon atoms, a hydroxyl group or an amino group; Y.sup.1 --Y.sup.2 represents CH--CO or C.dbd.CR.sup.2, wherein R.sup.2 represents a hydrogen atom or an alkyl group having 1 to 5 carbon atoms; and n is an integer of from 1 to 4, or a pharmaceutically acceptable salt thereof. The disclosed compounds are useful as drugs for preventing and treating dopamine D receptor-related morbid states such as schizophrenia and problematic behavior caused by cerebrovascular accidents and senile dementia and do not induce extrapyramidal disorders as side effects.Type: GrantFiled: November 5, 1999Date of Patent: December 26, 2000Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Masanori Yoshida
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Patent number: 5990151Abstract: The present invention relates to an optically active, substituted phenylalkylamine derivative represented by Formula [1]: ##STR1## wherein A is a substituted or non-substituted phenyl or thienyl; X.sup.1 is hydrogen, halogen, hydroxyl or a substituted or non-substituted C.sub.1-5 alkoxy; R.sup.1 and R.sup.2 are equally or differently hydrogen, C.sub.1-7 alkyl, C.sub.3-7 alkenyl or C.sub.3-7 alkynyl; R.sup.3 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl or C.sub.2-10 alkynyl; n is an integer from 2 to 5; and m is an integer from 1 to 4,or a pharmaceutically acceptable salt thereof, and pharmaceutical use of such compound or salt. The compound of the invention is excellent in sigma 1 receptor antagonism and useful for treating schizophrenia, depression, anxiety, cerebrovascular diseases/senile troublesome behaviors, and cognitive dysfunctions and motor dysfunctions such as Alzheimer's disease, Parkinson's disease and Huntington's disease which are neurodegenerative diseases.Type: GrantFiled: May 15, 1998Date of Patent: November 23, 1999Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Tomoki Miyazawa, Koumei Ohta, Yutaka Kawashima, Katsuo Hatayama, deceased