Patents by Inventor Akiyoshi Kawai

Akiyoshi Kawai 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).

  • Publication number: 20180072708
    Abstract: An amyloid fibril formation inhibitor comprising a compound represented by the following general formulae (I) to (III): wherein Q is —C(?O)—; X is —C(?O)—, —NH—C(?O)—; Y is —(CH2)m—; Z is —(CH2)n—; R1, R2, and R3 are each independently a hydrogen atom, an alkyl group, a hydroxyalkyl group, an alkylaminoalkyl group; and R4 is an amino group, an alkylamino group or the like; or a pharmaceutically acceptable salt thereof or a solvate thereof.
    Type: Application
    Filed: March 25, 2016
    Publication date: March 15, 2018
    Inventors: Katsuhiko Yanagisawa, Akiyoshi Kawai
  • Patent number: 7479564
    Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.
    Type: Grant
    Filed: November 3, 2006
    Date of Patent: January 20, 2009
    Assignee: RaQualia Pharma Inc.
    Inventors: Kazunari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
  • Publication number: 20070155732
    Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.
    Type: Application
    Filed: November 3, 2006
    Publication date: July 5, 2007
    Inventors: Kazunari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
  • Patent number: 7141580
    Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5–12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5–6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5–12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl, etc.; Q2 is a 5–12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: November 28, 2006
    Assignee: Pfizer Inc.
    Inventors: Kazunari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
  • Patent number: 6949536
    Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: September 27, 2005
    Assignee: Pfizer, Inc.
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
  • Publication number: 20040181059
    Abstract: This invention provides a compound of the formula (I): 1
    Type: Application
    Filed: February 4, 2004
    Publication date: September 16, 2004
    Inventors: Kazunari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
  • Publication number: 20040157824
    Abstract: This invention provides a compound of the formula: 1
    Type: Application
    Filed: February 3, 2004
    Publication date: August 12, 2004
    Applicant: Pfizer Inc.
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
  • Publication number: 20040142976
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: January 6, 2004
    Publication date: July 22, 2004
    Applicant: Pfizer Inc.
    Inventors: Akiyoshi Kawai, Makoto Kawai
  • Patent number: 6727238
    Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 o
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: April 27, 2004
    Assignee: Pfizer Inc.
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
  • Patent number: 6710054
    Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N, and S, etc.; A is 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl; etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: March 23, 2004
    Assignee: Pfizer Inc
    Inventors: Kazunari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
  • Patent number: 6696470
    Abstract: A compound of the formula: and its pharmaceutically effective salts, wherein R1 and R2 are independently selected from the following: (a) hydrogen, halo, R5—, C2-6 alkenyl, C2-6 alkynyl, hydroxy-R5—, R5—O—R5—, or the like; (b) Ar—, Ar—R5—, Ar—C2-6 alkenyl, Ar—C2-6 alkynyl, Ar—O—, Ar—O—R5— or the like; (c) R5—C(O)—, —NO2, cyano, NH2—C(O)—, R5—NH—C(O)—, (R5)2—N—C(O)—, Ar—C(O)— or the like; and (d) R5—C(O)—NH—, Ar—C(O)—NH— or the like; wherein Ar is optionally substituted aryl or heteroaryl such as phenyl and pyridyl; and wherein R5 is optionally halo-substituted C1-6 alkyl; R3 is selected from the following: (e) cyano, formyl, tetrazolyl, triazolyl, imidazolyl, oxazolyl, thiazolyl, R5—C(O)—, C2-6 alkenyl-C(O)—, C2-6 alkynyl-C(O)—, R5—C(O)—R5—, or the
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: February 24, 2004
    Assignee: Pfizer Inc.
    Inventors: Akiyoshi Kawai, Makoto Kawai
  • Publication number: 20030225064
    Abstract: This invention provides a compound of the formula: 1
    Type: Application
    Filed: June 18, 2003
    Publication date: December 4, 2003
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
  • Patent number: 6608095
    Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: August 19, 2003
    Assignee: Pfizer Inc.
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
  • Patent number: 6506779
    Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, R4, R5, R6, X and Y are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: January 14, 2003
    Assignee: Pfizer Inc.
    Inventors: Hengmiao Cheng, Akiyoshi Kawai
  • Publication number: 20020107273
    Abstract: This invention provides a compound of the formula (I): 1
    Type: Application
    Filed: October 15, 2001
    Publication date: August 8, 2002
    Inventors: Kazunnari Nakao, Yoshiyuki Okumura, Miyako Matsumizu, Naomi Ueno, Yoshinobu Hashizume, Tomoki Kato, Akiyoshi Kawai, Yoriko Miyake, Seiji Nukui, Katsuhiro Shinjyo, Kana Taniguchi
  • Patent number: 6417202
    Abstract: The present invention provides a compound of the formula: and its pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5 and m are as defined in claim 1. The present invention also provides processes for the preparation thereof, the use thereof in treating cytokines mediated diseases and/or cell adhesion molecules (CAMs) mediated diseases and pharmaceutical compositions for use in such therapy.
    Type: Grant
    Filed: December 10, 1999
    Date of Patent: July 9, 2002
    Assignee: Pfizer Inc.
    Inventors: Akiyoshi Kawai, Makoto Kawai, Yoshinori Murata, Junji Takada, Minoru Sakakibara
  • Publication number: 20020049235
    Abstract: The present invention provides a compound of the formula: 1
    Type: Application
    Filed: December 10, 1999
    Publication date: April 25, 2002
    Inventors: AKIYOSHI KAWAI, MAKOTO KAWAI, YOSHINORI MURATA, JUNJI TAKADA, MINORU SAKAKIBARA
  • Publication number: 20020045654
    Abstract: This invention provides a compound of the formula: 1
    Type: Application
    Filed: April 24, 2001
    Publication date: April 18, 2002
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
  • Publication number: 20020022729
    Abstract: A compound of the formula: 1
    Type: Application
    Filed: July 30, 2001
    Publication date: February 21, 2002
    Inventors: Akiyoshi Kawai, Makoto Kawai
  • Patent number: 6294558
    Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: September 25, 2001
    Assignee: Pfizer Inc.
    Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura