Patents by Inventor Nakao Kojima
Nakao Kojima 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: 6416979Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).Type: GrantFiled: September 8, 2000Date of Patent: July 9, 2002Assignee: Pfizer Inc.Inventors: Hideo Hirai, Katsuomi Ichikawa, Nakao Kojima, Hiroyuki Nishida, Kunio Satake, Nobuji Yoshikawa
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Patent number: 6391616Abstract: This invention provides terpenoid lactone compounds, and processes for producing the terpenoid lactone compounds, which comprise cultivating Oidiodedron griseum FERM BP-5778 and then isolating the terpenoid lactone compounds from the fermentation broth. The present invention also provides a pharmaceutical composition comprising the terpenoid lactone compound, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.Type: GrantFiled: June 16, 2000Date of Patent: May 21, 2002Assignee: Pfizer Inc.Inventors: Hiroyuki Nishida, Masaya Ikunaka, Nobuji Yoshikawa, Katsuomi Ichikawa, Nakao Kojima
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Patent number: 6225339Abstract: This invention provides terpenoid lactone compounds, and processes for producing the terpenoid lactone compounds, which comprise cultivating Oidiodedron griseum FERM BP-5778 and then isolating the terpenoid lactone compounds from the fermentation broth. The present invention also provides a pharmaceutical composition comprising the terpenoid lactone compound, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.Type: GrantFiled: January 15, 1999Date of Patent: May 1, 2001Assignee: Pfizer Inc.Inventors: Hiroyuki Nishida, Masaya Ikunaka, Nobuji Yoshikawa, Katsuomi Ichikawa, Nakao Kojima
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Patent number: 6221899Abstract: This invention provides terpenoid lactone compounds, and processes for producing the terpenoid lactone compounds, which comprise cultivating Oidiodedron griseum FERM BP-5778 and then isolating the terpenoid lactone compounds from the fermentation broth. The present invention also provides a pharmaceutical composition comprising the teipenoid lactone compound, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.Type: GrantFiled: June 16, 2000Date of Patent: April 24, 2001Assignee: Pfizer Inc.Inventors: Hiroyuki Nishida, Masaya Ikunaka, Nobuji Yoshikawa, Katsuomi Ichikawa, Nakao Kojima
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Patent number: 6194442Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are independently H, C2-C6 acyl or halo-substituted benzoyl; and R3 is —C(O)O—C1-C6 alkyl, C(O)OH, CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R2 is acetyl and R3 is methoxycarbonyl, R1 is not H; and that when R3 is CN, CONH2, CONHCH3, CON(CH3)2, 1-methyltetrazole or 2-methyltetrazole, R1 and R2 are H. The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like. The present invention further relates to a process for producing the compounds of the formula (I).Type: GrantFiled: December 14, 1999Date of Patent: February 27, 2001Assignee: Pfizer IncInventors: Hideo Hirai, Katsuomi Ichikawa, Nakao Kojima, Hiroyuki Nishida, Kunio Satake, Nobuji Yoshikawa
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Patent number: 6187568Abstract: This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocylic lactone compound from the fermentation broth. The compounds produced by this process include a compound of the following formula: The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.Type: GrantFiled: August 20, 1999Date of Patent: February 13, 2001Assignee: Pfizer IncInventors: Hiroyuki Nishida, Yuji Yamauchi, Taisuke Inagaki, Yasuhiro Kojima, Nakao Kojima
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Patent number: 6034107Abstract: The present invention provides novel 5-substituted picolinic acid compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are independently H, C.sub.2 -C.sub.6 acyl or halo-substituted benzoyl; and R.sup.3 is --C(O)O--C.sub.1 -C.sub.6 alkyl, C(O)OH, CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, with the proviso that when R.sub.2 is acetyl and R.sup.3 is methoxycarbonyl, R.sup.1 is not H; and that when R.sup.3 is CN, CONH.sub.2, CONHCH.sub.3, CON(CH.sub.3).sub.2, 1-methyltetrazole or 2-methyltetrazole, R.sup.1 and R.sup.2 are H.The present invention also relates to a pharmaceutical composition comprising compound of the present invention, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.The present invention further relates to a process for producing the compounds of the formula (I).Type: GrantFiled: October 26, 1998Date of Patent: March 7, 2000Assignee: Pfizer Inc.Inventors: Hideo Hirai, Katsuomi Ichikawa, Nakao Kojima, Hiroyuki Nishida, Kunio Satake, Nobuji Yoshikawa
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Patent number: 6001998Abstract: This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocyclic lactone compound from the fermentation broth. The compounds produced by this process include a compound of formula (I). The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.Type: GrantFiled: October 27, 1997Date of Patent: December 14, 1999Assignee: Pfizer IncInventors: Hiroyuki Nishida, Yuji Yamauchi, Taisuke Inagaki, Yasuhiro Kojima, Nakao Kojima
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Patent number: 5942619Abstract: This invention provides processes for producing quinolone compounds which comprise cultivating Amycoa sp. FERM BP-4785, and then isolating quinolone compounds from the fermentation broth. The compounds produced by these processes include compounds of formula (I) wherein R.sup.1 is H, R.sup.2 is (a) and R.sup.3 is CH.sub.3 ; R.sup.1 is CH.sub.3, R.sup.2 is (a) and R.sup.3 is CH.sub.3 ; or R.sup.1 is CH.sub.3, R.sup.2 is (b) and R.sup.3 is CH.sub.3 ; and the like. The present invention also relates to a pharmaceutical composition comprising the same, which is useful in the treatment of diseases, disorders and adverse conditions caused by Helicobacter pylori and is particularly useful in the treatment of gastroduodenal disorders, diseases and adverse conditions caused thereby.Type: GrantFiled: April 24, 1998Date of Patent: August 24, 1999Assignee: Pfizer Inc.Inventors: Koenraad A. Dekker, Liang H. Huang, Taisuke Inagaki, Nakao Kojima, Yasuhiro Kojima, Yuji Yamauchi
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Patent number: 5885959Abstract: This invention provides processes for producing novel cyclic peptide compounds, which comprise cultivating Ctenomyces serratus FERM BP-5731 and then isolating the cyclic peptide compounds from the fermentation broth. The compounds produced by these processes include a cyclic peptide compound of the following formula (I): ##STR1## The present invention also relates to a pharmaceutical composition comprising the same, which is useful in the treatment of severe pain, detoxication of narcotics dependency or acute narcotics intoxication or the like.Type: GrantFiled: December 3, 1997Date of Patent: March 23, 1999Assignee: Pfizer Inc.Inventors: Hideo Hirai, Nakao Kojima, Hiroyuki Nishida, Toshiyuki Saito, Nobuji Yoshikawa
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Patent number: 5861518Abstract: This invention provides processes for producing phthalide compounds which comprise cultivating Phanerochaete avelutina FERM BP-4787 and then isolating phthalide compounds from the fermentation broth.Type: GrantFiled: October 31, 1997Date of Patent: January 19, 1999Inventors: Koenraad A. Dekker, Yuji Yamauchi, Taisuke Inagaki, Shinichi Sakemi, Nakao Kojima
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Patent number: 5801023Abstract: This invention provides compounds of the following chemical formula or their pharmaceutically-acceptable salts: ##STR1## wherein R is hydrogen or chloro. Also, the present invention provides a process for the production of the compound of formula I, which comprises cultivating a microorganism having the identifying characteristics of Aspergillus fischeri var. thermomutatis ATCC 18618 or the like, and then isolating the compound of formula I from the fermentation broth. The pyrrolobenzoxazine compounds of formula I of this invention have broad antiparasitic activity, and thus are useful as antiparasitic agents, especially as anthelmintics.Type: GrantFiled: November 29, 1996Date of Patent: September 1, 1998Assignee: Pfizer Inc.Inventors: Yasuhiro Kojima, Yuji Yamauchi, Nakao Kojima, Bernard F. Bishop
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Patent number: 5674732Abstract: The present invention provides a novel culture which belongs to Actinoplanes (Actinoplanes sp. FERM BP-3832). This culture is capable of producing rapamycin more than ten times efficiently than the cultures which have been reported (e.g., Streptomyces hygroscopicus ATCC 29253). The present invention provides a process for the production of rapamycin which comprises cultivating Actinoplanes sp. FERM BP-3832 and thereafter isolating rapamycin from the fermentation mixture.Type: GrantFiled: October 26, 1994Date of Patent: October 7, 1997Assignee: Pfizer Inc.Inventors: Hiroyuki Nishida, Tatsuo Sakakibara, Yuji Yamauchi, Taisuke Inagaki, Yasuhiro Kojima, Nakao Kojima
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Streptomyces braegensis strain and its cultivation in a process for producing C.sub.9 -desoxo-FK-520
Patent number: 5494820Abstract: A compound of the formula ##STR1## is a novel immunosuppressant agent prepared by fermenting Steptomyces braeaensis subsp. pulcherrimus, ATCC 55150, or another compound of the formula I producing strain and extracting the compound of the formula I from the fermentation medium. The compound is useful in treating transplant rejection and autoimmune diseases.Type: GrantFiled: January 24, 1994Date of Patent: February 27, 1996Assignee: Pfizer Inc.Inventors: Walter P. Cullen, Mark A. Guadliana, Liang H. Huang, Keiji Kaneda, Nakao Kojima, Gloria Kostek, Satoshi Nishiyama, Yuji Yamauchi, Yasuhiro Kojima