-
公开(公告)号:US08536197B2
公开(公告)日:2013-09-17
申请号:US12811004
申请日:2008-12-26
申请人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
发明人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
IPC分类号: C07D417/04 , C07D401/12 , A61K31/4164 , A61K31/4178
CPC分类号: C07D487/04 , C07D233/66 , C07D233/90 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/06 , C07D487/12 , C07D495/04 , C07D495/16 , C07D498/04 , C07D513/04 , C07D519/00
摘要: An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.
摘要翻译: 具有新的作用机理,细胞毒性低,在水中溶解度高的抗生素化合物,有效抑制DNA促旋酶GyrB和拓扑异构酶IV ParE亚基,具有抗菌活性。
-
公开(公告)号:US06337403B1
公开(公告)日:2002-01-08
申请号:US09872744
申请日:2001-06-01
申请人: Toshiyuki Konosu , Sadao Oida , Makoto Mori , Takuya Uchida , Satoshi Ohya , Akihiko Nakagawa
发明人: Toshiyuki Konosu , Sadao Oida , Makoto Mori , Takuya Uchida , Satoshi Ohya , Akihiko Nakagawa
IPC分类号: A61K314196
CPC分类号: C07D231/12 , C07C255/56 , C07D233/56 , C07D249/08
摘要: Compounds of the following formula (I) and pharmaceutically acceptable esters and salts thereof: Ar is a phenyl group which may optionally be substituted by from 1 to 3 substituents selected from the group consisting of halogen atoms and trifluoromethyl groups. The compounds (and pharmaceutically acceptable esters and salts thereof) have excellent antifungal activity.
摘要翻译: 下式(I)的化合物及其药学上可接受的酯和盐:Ar是可任选被1至3个选自卤原子和三氟甲基的取代基取代的苯基。 化合物(及其药学上可接受的酯和盐)具有优异的抗真菌活性。
-
公开(公告)号:US5393769A
公开(公告)日:1995-02-28
申请号:US24827
申请日:1993-03-01
申请人: Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
发明人: Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
IPC分类号: C07D249/08 , C07D401/12 , C07D521/00 , A61K31/41
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08
摘要: Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; R.sup.1 is alkyl; R.sup.2 is substituted alkyl or substituted cycloalkyl; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.
摘要翻译: 式(I)化合物:其中:Ar为任选取代的苯基; R1是烷基; R2是取代的烷基或取代的环烷基; 且n为0,1或2; 及其药学上可接受的盐和酯具有有价值的抗真菌性质,并可用于药物和兽医治疗。 还提供了制备这些化合物的方法。
-
公开(公告)号:US06306880B1
公开(公告)日:2001-10-23
申请号:US09241370
申请日:1999-02-01
申请人: Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
发明人: Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
IPC分类号: C07D40112
CPC分类号: C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08
摘要: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted; Ar2 represents a phenyl group which may be substituted; R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represnet a hydrogen atom or an unsubstituted or halo substituted alkyl; n represnets 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic, not including 1,3-dioxan-5-yl. The compound of the present invention exhibits an excellent antifungal activity.
摘要翻译: 具有下式的三唑化合物:其中Ar 1表示可被取代的苯基; Ar2表示可以被取代的苯基; R 0表示氢原子或低级烷基; R1代表低级烷基; R2至R5各自代表氢原子或未取代或卤代取代的烷基; n表示0到2; p表示0或1; q,r和s各自表示0〜2; A代表4-至7-元碳环或4-至7-元杂环,不包括1,3-二恶烷-5-基。 本发明的化合物显示出优异的抗真菌活性。
-
公开(公告)号:US5489606A
公开(公告)日:1996-02-06
申请号:US316082
申请日:1994-09-30
申请人: Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
发明人: Sadao Oida , Takeo Miyaoka , Yawara Tajima , Toshiyuki Konosu , Noriko Takeda , Hiroshi Yasuda
IPC分类号: C07D249/08 , C07D401/12 , C07D521/00 , A01N43/653
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08
摘要: Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; is R.sup.1 is alkyl; R.sup.2 is substituted alkyl, substituted cycloalkyl R.sup.2 or optionally substituted heterocyclic; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.
摘要翻译: 式(I)化合物:其中:Ar为任选取代的苯基; R1是烷基; R2是取代的烷基,取代的环烷基R2或任选取代的杂环; 且n为0,1或2; 及其药学上可接受的盐和酯具有有价值的抗真菌性质,并可用于药物和兽医治疗。 还提供了制备这些化合物的方法。
-
公开(公告)号:US07829580B2
公开(公告)日:2010-11-09
申请号:US11442429
申请日:2006-05-26
IPC分类号: A61K31/445 , C07D211/54
CPC分类号: C07D211/72 , C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要: A compound having the general formula (I) wherein R1 represents C1-C6 alkyl, etc., R2 represents hydrogen, C2-C7 alkanoyl, C7-C11 arylcarbonyl, the formula R4—(CH2)l—, etc., R3 represents C6-C10 aryl, etc., X1, X2, X3, X4 and X5 each independently represents hydrogen, halogen, etc., and n represents an integer of 0 to 2, pharmacologically acceptable salts thereof or prodrugs thereof. They have excellent inhibition of platelet activation, etc. and are useful as a prophylactic or therapeutic agents for diseases related to thrombus or embolus formation.
摘要翻译: 具有通式(I)的化合物,其中R1表示C1-C6烷基等,R2表示氢,C2-C7烷酰基,C7-C11芳基羰基,式R4-(CH2)-1-等,R3表示C6 -C 10芳基等,X 1,X 2,X 3,X 4和X 5各自独立地表示氢,卤素等,n表示0〜2的整数,其药理学上可接受的盐或其前药。 它们具有优异的血小板活化抑制等,并且可用作与血栓或栓塞形成有关的疾病的预防或治疗剂。
-
公开(公告)号:US5977152A
公开(公告)日:1999-11-02
申请号:US944304
申请日:1997-10-06
申请人: Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
发明人: Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
IPC分类号: A01N43/653 , A61K31/4196 , C07D249/08 , C07D401/12 , C07D409/12 , C07D521/00 , A61K31/41
CPC分类号: C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08
摘要: A triazole compound having the formula: ##STR1## wherein Ar.sup.1 represents an optionally substituted phenyl, Ar.sup.2 represents an optionally substituted phenyl, R.sup.0 represents a hydrogen atom or a lower alkyl; R.sup.1 represents a lower alkyl; R.sup.2 to R.sup.5 represent a hydrogen atom or an unsubstituted or halo substituted alkyl, n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; and A represents a 1,3-dioxan-5-yl. The triazole compound of the present invention exhibits an excellent antifungal activity.
摘要翻译: 具有下式的三唑化合物:其中Ar 1表示任选取代的苯基,Ar 2表示任选取代的苯基,R 0表示氢原子或低级烷基; R1代表低级烷基; R 2至R 5表示氢原子或未取代或卤素取代的烷基,n表示0至2; p表示0或1; q,r和s各自表示0〜2; A代表1,3-二恶烷-5-基。 本发明的三唑化合物表现出优异的抗真菌活性。
-
公开(公告)号:US06391903B1
公开(公告)日:2002-05-21
申请号:US09656154
申请日:2000-09-06
申请人: Toshiyuki Konosu , Sadao Oida , Makoto Mori , Takuya Uchida , Satoshi Ohya , Akihiko Nakagawa
发明人: Toshiyuki Konosu , Sadao Oida , Makoto Mori , Takuya Uchida , Satoshi Ohya , Akihiko Nakagawa
IPC分类号: A61K314196
CPC分类号: C07D231/12 , C07C255/56 , C07D233/56 , C07D249/08
摘要: Compounds of the following formula (I) and pharmaceutically acceptable esters and salts thereof: Ar is a phenyl group which may optionally be substituted by from 1 to 3 substituents selected from the group consisting of halogen atoms and trifluoromethyl groups. Said compounds (and pharmaceutically acceptable esters and salts thereof) have excellent antifungal activity.
摘要翻译: 下式(I)的化合物及其药学上可接受的酯和盐:Ar是可任选被1至3个选自卤原子和三氟甲基的取代基取代的苯基。 所述化合物(及其药学上可接受的酯和盐)具有优异的抗真菌活性。
-
公开(公告)号:US06300357B1
公开(公告)日:2001-10-09
申请号:US09241369
申请日:1999-02-01
申请人: Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
发明人: Sadao Oida , Teruo Tanaka , Yawara Tajima , Toshiyuki Konosu , Atsushi Somada , Takeo Miyaoka , Hiroshi Yasuda
IPC分类号: C07D24908
CPC分类号: C07D231/12 , A01N43/653 , C07D233/56 , C07D249/08
摘要: A triazole compound having the formula: wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represent a hydrogen atom or an unsubstituted or halo substituted alkyl; n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic group. The compound of the present invention exhibits an excellent antifungal activity.
摘要翻译: 具有下式的三唑化合物:其中Ar1表示可被取代的苯基,Ar2表示可被取代的杂环基,R0表示氢原子或低级烷基; R1代表低级烷基; R 2至R 5各自表示氢原子或未取代或卤素取代的烷基; n表示0〜2; p表示0或1; q,r和s各自表示0〜2; A表示4-至7-元碳环或4-至7-元杂环基。 本发明的化合物显示出优异的抗真菌活性。
-
公开(公告)号:US20100311966A1
公开(公告)日:2010-12-09
申请号:US12811004
申请日:2008-12-26
申请人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
发明人: Tsuyoshi Soneda , Hiroshi Takeshita , Yoshiko Kagoshima , Yuko Yamamoto , Takafumi Hosokawa , Toshiyuki Konosu , Nobuhisa Masuda , Takuya Uchida , Issei Achiwa , Junichi Kuroyanagi , Tetsunori Fujisawa , Aki Yokomizo , Tetsuji Noguchi
IPC分类号: C07D498/04 , C07D277/56 , C07D513/04 , C07D233/90 , C07D403/12 , C07D495/04 , C07D495/16
CPC分类号: C07D487/04 , C07D233/66 , C07D233/90 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/06 , C07D487/12 , C07D495/04 , C07D495/16 , C07D498/04 , C07D513/04 , C07D519/00
摘要: An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.
摘要翻译: 具有新的作用机理,细胞毒性低,在水中溶解度高的抗生素化合物,有效抑制DNA促旋酶GyrB和拓扑异构酶IV ParE亚基,具有抗菌活性。
-
-
-
-
-
-
-
-
-