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1. 发明授权

US5885959A Cyclic peptide compounds and their production process 失效
标题翻译：环肽化合物及其制备方法
公开(公告)号：US5885959A
公开(公告)日：1999-03-23
申请号：US999627
申请日：1997-12-03
申请人： Hideo Hirai , Nakao Kojima , Hiroyuki Nishida , Toshiyuki Saito , Nobuji Yoshikawa
发明人： Hideo Hirai , Nakao Kojima , Hiroyuki Nishida , Toshiyuki Saito , Nobuji Yoshikawa
IPC分类号： C12P21/04 , A61K38/00 , A61P25/04 , A61P25/30 , A61P39/02 , C07K5/12 , C12P21/02 , C12R1/645 , A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00
CPC分类号： C07K5/126 , C12P21/02 , A61K38/00
摘要： 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.
摘要翻译：本发明提供了生产新型环肽化合物的方法，其包括培养C ivating atus ERM FERM BP-5731，然后从发酵液中分离出环状肽化合物。通过这些方法制备的化合物包括下式（I）的环肽化合物：（I）本发明还涉及包含其的药物组合物，其可用于治疗严重疼痛，解毒麻醉品依赖或急性毒品中毒等。

2. 发明授权

US06194442B1 5-substituted picolinic acid compounds and their method of use 失效
标题翻译： 5-取代吡啶甲酸化合物及其使用方法
公开(公告)号：US06194442B1
公开(公告)日：2001-02-27
申请号：US09460483
申请日：1999-12-14
申请人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
发明人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
IPC分类号： A61K3144
CPC分类号： A61K31/44 , Y02A50/411
摘要： 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).
摘要翻译：本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R3为CN，CONH2，CONHCH3，CON（CH3）2,1-甲基四唑或2-甲基四唑时，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，其有用在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。

3. 发明授权

US06416979B1 5-substituted picolinic acid compounds production by Marasmiellus sp 失效
标题翻译：由马拉斯马司属（Malasmiellus sp。）生产的5-取代吡啶甲酸化合物
公开(公告)号：US06416979B1
公开(公告)日：2002-07-09
申请号：US09657730
申请日：2000-09-08
申请人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
发明人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
IPC分类号： C12P1712
CPC分类号： A61K31/44
摘要： 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).
摘要翻译：本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R3为CN，CONH2，CONHCH3，CON（CH3）2,1-甲基四唑或2-甲基四唑时，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，其有用在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。

4. 发明授权

US6034107A 5-Substituted picolinic acid compounds and their production process 失效
标题翻译： 5-取代的吡啶甲酸化合物及其制备方法
公开(公告)号：US6034107A
公开(公告)日：2000-03-07
申请号：US178949
申请日：1998-10-26
申请人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
发明人： Hideo Hirai , Katsuomi Ichikawa , Nakao Kojima , Hiroyuki Nishida , Kunio Satake , Nobuji Yoshikawa
IPC分类号： C07D213/78 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61P11/00 , A61P19/00 , A61P19/02 , A61P29/00 , A61P43/00 , C07D213/79 , C07D213/81 , C07D213/84 , C07D401/04 , C12N1/14 , C12P17/12 , C12P17/16 , C12R1/645
CPC分类号： C07D213/79 , C07D213/81 , C07D213/84 , C07D401/04 , C12P17/12
摘要： 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).
摘要翻译：本发明提供式（I）的新的5-取代的吡啶甲酸化合物或其药学上可接受的盐：其中R 1和R 2独立地为H，C 2 -C 6酰基或卤素取代的苯甲酰基; 并且R 3是-C（O）O-C 1 -C 6烷基，C（O）OH，CN，CONH 2，CONHCH 3，CON（CH 3）2,1-甲基四唑或2-甲基四唑，条件是当R 2是乙酰基和 R3是甲氧基羰基，R1不是H; 当R 3为CN时，CONH 2，CONHCH 3，CON（CH 3）2，1-甲基四唑或2-甲基四唑，R 1和R 2为H.本发明还涉及含有本发明化合物的药物组合物，在治疗IL-1和TNF介导的疾病等中。本发明还涉及制备式（I）化合物的方法。

5. 发明授权

US06221899B1 Terpenoid lactone compounds and their production process 失效
标题翻译：萜类内酯化合物及其制备方法
公开(公告)号：US06221899B1
公开(公告)日：2001-04-24
申请号：US09596728
申请日：2000-06-16
申请人： Hiroyuki Nishida , Masaya Ikunaka , Nobuji Yoshikawa , Katsuomi Ichikawa , Nakao Kojima
发明人： Hiroyuki Nishida , Masaya Ikunaka , Nobuji Yoshikawa , Katsuomi Ichikawa , Nakao Kojima
IPC分类号： A61K3135
CPC分类号： A61K31/4741 , A61K31/365 , A61K31/366 , Y02A50/411
摘要： 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.
摘要翻译：本发明提供萜类内酯化合物，以及萜类内酯化合物的制备方法，其包括培育Oidiodedron griseum FERM BP-5778，然后从发酵液中分离萜类内酯化合物。本发明还提供了一种药物组合物，其包含可用于治疗IL-1和TNF介导的疾病等的脯氨酸内酯化合物。

6. 发明授权

US06391616B1 Oidiodendron strain for the production of terpenoid lactone compounds 失效
标题翻译：用于生产萜类内酯化合物的Oidiodendron菌株
公开(公告)号：US06391616B1
公开(公告)日：2002-05-21
申请号：US09596140
申请日：2000-06-16
申请人： Hiroyuki Nishida , Masaya Ikunaka , Nobuji Yoshikawa , Katsuomi Ichikawa , Nakao Kojima
发明人： Hiroyuki Nishida , Masaya Ikunaka , Nobuji Yoshikawa , Katsuomi Ichikawa , Nakao Kojima
IPC分类号： C12N114
CPC分类号： C07D307/92 , A61K31/365 , A61K31/366 , A61K31/4741 , C07D311/92 , C07D491/06 , C07D493/06 , Y02A50/411
摘要： 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.
摘要翻译：本发明提供萜类内酯化合物，以及萜类内酯化合物的制备方法，其包括培育Oidiodedron griseum FERM BP-5778，然后从发酵液中分离萜类内酯化合物。本发明还提供了包含萜类内酯化合物的药物组合物，其可用于治疗IL-1和TNF介导的疾病等。

7. 发明授权

US06225339B1 Terpenoid lactone compounds and their production process 失效
标题翻译：萜类内酯化合物及其制备方法
公开(公告)号：US06225339B1
公开(公告)日：2001-05-01
申请号：US09232080
申请日：1999-01-15
申请人： Hiroyuki Nishida , Masaya Ikunaka , Nobuji Yoshikawa , Katsuomi Ichikawa , Nakao Kojima
发明人： Hiroyuki Nishida , Masaya Ikunaka , Nobuji Yoshikawa , Katsuomi Ichikawa , Nakao Kojima
IPC分类号： A61K3135
CPC分类号： C07D307/92 , A61K31/365 , A61K31/366 , A61K31/4741 , C07D311/92 , C07D491/06 , C07D493/06 , Y02A50/411
摘要： 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.
摘要翻译：本发明提供萜类内酯化合物，以及萜类内酯化合物的制备方法，其包括培育Oidiodedron griseum FERM BP-5778，然后从发酵液中分离萜类内酯化合物。本发明还提供了包含萜类内酯化合物的药物组合物，其可用于治疗IL-1和TNF介导的疾病等。

8. 发明授权

US06277860B1 Furopyridine antibacterials 失效
标题翻译：呋喃西林抗菌剂
公开(公告)号：US06277860B1
公开(公告)日：2001-08-21
申请号：US09430763
申请日：1999-10-29
申请人： Yutaka Sugie , Akemi Sugiura , Nobuji Yoshikawa , Susan J. I Truesdell , John W. Wong
发明人： Yutaka Sugie , Akemi Sugiura , Nobuji Yoshikawa , Susan J. I Truesdell , John W. Wong
IPC分类号： A61K31436
CPC分类号： C07D491/04 , C07D491/14
摘要： This invention provides a compound of formula (I): or pharmaceutically acceptable salts thereof, wherein X1 and X2 are C or N, respectively; R1 and R2 are independently phenyl optionally substituted with a hydroxy group with proviso that X1 and X2 are not simultaneously C or N, when X1 is N, R1 is absent, and when X2 is N, R2 is absent; R3 is methyl or hydroxymethyl; R4 is formyl, hydroxymethyl or hydroxy C3-6 alkenyl; R5 is hydroxy, C3-6 alkenyl or hydroxy C3-6 alkenyl; or R4 and R5, together with the carbon atoms in the furopyridine ring to which they are attached, may form the following ring (to be fused with the furopyridine ring): with the proviso that when R3 is methyl and R5 is 2-buten-2-yl, X2 is not N. These compounds and pharmaceutical compositions containing such compounds are useful for treating infectious diseases caused by bacteria.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中X 1和X 2分别是C或N; R1和R2独立地为羟基取代的苯基，条件是X1和X2不同时为C或N，当X1为N时，R1不存在，当X2为N时，R2为不; R3是甲基或羟甲基; R4是甲酰基，羟甲基或羟基C 3-6烯基; R5是羟基，C3-6烯基或羟基C3-6烯基; 或R 4和R 5与它们所连接的呋喃啶环中的碳原子一起形成以下环（与呋喃啶环稠合）：条件是当R 3为甲基且R 5为2-丁烯基时， 2-这些化合物和含有这些化合物的药物组合物可用于治疗由细菌引起的感染性疾病。

9. 发明授权

US4871667A Process for preparing muconic acid 失效
标题翻译：制备粘康酸的方法
公开(公告)号：US4871667A
公开(公告)日：1989-10-03
申请号：US800027
申请日：1985-11-20
申请人： Yukio Imada , Nobuji Yoshikawa , Sumiko Mizuno , Takashi Mikawa
发明人： Yukio Imada , Nobuji Yoshikawa , Sumiko Mizuno , Takashi Mikawa
IPC分类号： C12P7/44
CPC分类号： C12P7/44 , Y10S435/83 , Y10S435/84 , Y10S435/843
摘要： Muconic acid is obtained from the culture of strains of Arthrobacter sp. mutant strains, strains belonging to Corynebacterium acetoacidophilum, Corynebacterium lilium, genus Brevibacterium or genus Microbacterium.
摘要翻译：粘液酸从节杆菌属菌株的培养物中获得。突变菌株，属于乙酰乙酸棒状杆菌，棒状杆菌属，短杆菌属或微杆菌属的菌株。

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