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1. 发明专利

IL189677D0 PROCESS FOR PREPARING NITROGENOUS AROMATIC RING COMPOUNDS 未知
公开(公告)号：IL189677D0
公开(公告)日：2008-06-05
申请号：IL18967708
申请日：2008-02-21
申请人： YASUHIRO FUNAHASHI , AKIHIKO TSURUOKA , MASAYUKI MATSUKURA , TORU HANEDA , YOSHIO FUKUDA , JUNICHI KAMATA , KEIKO TAKAHASHI , TOMOHIRO MATSUSHIMA , KAZUKI MIYAZAKI , KEN ICHI NOMOTO , TATSUO WATANABE , HIROSHI OBAISHI , ATSUMI YAMAGUCHI , SACHI SUZUKI , KATSUJI NAKAMURA , FUSAYO MIMURA , YUJI YAMAMOTO , JUNJI MATSUI , KENJI MATSUI , TAKAKO YOSHIBA , YASUYUKI SUZUKI , ITARU ARIMOTO , EISAI R&D MAN CO LTD , EISAI CO LTD
IPC分类号： C07D213/74 , A61K20060101 , A61K31/4355 , A61K31/437 , A61K31/4375 , A61K31/4409 , A61K31/4418 , A61K31/4439 , A61K31/4545 , A61K31/455 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/505 , A61K31/519 , A61K31/5377 , A61P20060101 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07D20100101 , C07D207/34 , C07D213/26 , C07D213/68 , C07D213/73 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/18 , C07D215/22 , C07D215/233 , C07D215/36 , C07D215/38 , C07D215/48 , C07D239/34 , C07D239/42 , C07D239/46 , C07D239/88 , C07D249/04 , C07D261/14 , C07D277/48 , C07D307/68 , C07D319/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： The present invention concerns a process for preparing a compound represented by the following general formula (a- or a pharmacologically acceptable salt or hydrate thereof, which comprises reacting a compound repr with a compound represented by the following general formula (a-4) : wherein the residues R 1 , R 2 , R sa1 - R sa3 , R 300 , R 301 and Z are as defined in the claims.

2. 发明授权

US08183264B2 Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same 有权
标题翻译：被杂芳基环取代的吡啶衍生物，及含有它们的抗真菌剂
公开(公告)号：US08183264B2
公开(公告)日：2012-05-22
申请号：US12442293
申请日：2007-09-20
申请人： Masayuki Matsukura , Satoshi Inoue , Keigo Tanaka , Norio Murai , Shuji Shirotori
发明人： Masayuki Matsukura , Satoshi Inoue , Keigo Tanaka , Norio Murai , Shuji Shirotori
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/04
摘要： The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability. The present invention discloses a compound represented by the following formula I or a salt thereof, and an antifungal agent comprising the compound or the salt: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6-alkoxy-C1-6-alkyl group; R2 represents a hydrogen atom or an amino group; X, Y, Z, and W independently represent a nitrogen atom, an oxygen atom, a sulfur atom, or —CH—, provided that at least two among X, Y, and W are nitrogen atoms; the ring A represents a 5- or 6-membered heteroaryl ring or a benzene ring; Q represents a methylene group, an oxygen atom, —CH2O—, —OCH2—, —NH—, —NHCH2—, or —CH2NH—; and R3 represents a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, or a 5- or 6-membered heteroaryl group, each of which may have one or two substituents.
摘要翻译：本发明提供具有优异抗真菌作用的抗真菌剂，并且在其性质，安全性和代谢稳定性方面也是优异的。本发明公开了由下式I表示的化合物或其盐，以及包含该化合物或其盐的抗真菌剂：其中R1表示氢原子，卤素原子，氨基，C1-6烷基， C 1-6烷氧基或C 1-6 - 烷氧基-C 1-6 - 烷基; R2表示氢原子或氨基; X，Y，Z和W独立地表示氮原子，氧原子，硫原子或-CH-，条件是X，Y和W中的至少两个是氮原子; 环A表示5-或6-元杂芳基环或苯环; Q表示亚甲基，氧原子，-CH 2 O - ， - OCH 2 - ， - NH - ， - NHCH 2 - 或-CH 2 NH-; 并且R 3表示可以具有一个或两个取代基的C 1-6烷基，C 3-8环烷基，C 6-10芳基或5或6元杂芳基。

3. 发明申请

US20100168173A1 HETEROCYCLES SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING THEREOF 有权
公开(公告)号：US20100168173A1
公开(公告)日：2010-07-01
申请号：US12704637
申请日：2010-02-12
申请人： Keigo Tanaka , Satoshi Inoue , Norio Murai , Masayuki Matsukura , Kazutaka Nakamoto , Shuji Shirotori , Shinya Abe
发明人： Keigo Tanaka , Satoshi Inoue , Norio Murai , Masayuki Matsukura , Kazutaka Nakamoto , Shuji Shirotori , Shinya Abe
IPC分类号： A61K31/444 , C07D413/04 , A61K31/4439 , C07D401/14 , A61P31/10
CPC分类号： A01N43/56 , A01N43/80 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/14
摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.

4. 发明申请

US20090233883A1 HETEROCYCLIC RING AND PHOSPHONOXYMETHYL GROUP SUBSTITUTED PYRIDINE DERIVATIVES AND ANTIFUNGAL AGENT CONTAINING SAME 有权
标题翻译：杂环化合物和磷酰基甲基取代的吡啶衍生物和含有它的抗真菌剂
公开(公告)号：US20090233883A1
公开(公告)日：2009-09-17
申请号：US12343889
申请日：2008-12-24
申请人： Masayuki MATSUKURA
发明人： Masayuki MATSUKURA
IPC分类号： A61K31/675 , C07F9/06
CPC分类号： C07F9/65583
摘要： The present invention provides compounds that have excellent antifungal action, and are also excellent in terms of properties, such as solubility in water and safety. The compounds are represented by formula (I): The present invention is also directed to a pharmaceutical composition comprising the compound, an antifungal agent comprising the compound as an active ingredient, and a method for preventing or treating a fungal disease by administering the compound.
摘要翻译：本发明提供具有优异的抗真菌作用的化合物，并且在诸如在水中的溶解性和安全性等性质方面也是优异的。化合物由式（I）表示：本发明还涉及包含该化合物，包含该化合物作为活性成分的抗真菌剂的药物组合物，以及通过施用化合物预防或治疗真菌病的方法。

5. 发明申请

US20080275244A1 HETEROCYCLE-SUBSTITUTED PYRIDINE DERIVATIVE'S SALT OR CRYSTAL THEREOF 有权
标题翻译：杂交取代的吡啶衍生物的盐或其结晶
公开(公告)号：US20080275244A1
公开(公告)日：2008-11-06
申请号：US12109959
申请日：2008-04-25
申请人： Jun Niijima , Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Eiichi Yamamoto , Takuma Minamisono
发明人： Jun Niijima , Kazutaka Nakamoto , Masayuki Matsukura , Keigo Tanaka , Eiichi Yamamoto , Takuma Minamisono
IPC分类号： C07D213/02
CPC分类号： C07D413/14
摘要： There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.
摘要翻译：提供了杂环取代的吡啶衍生物的盐或其结晶。本发明提供3-（3-（4-（吡啶-2-基氧基甲基） - 苄基） - 异恶唑-5-基） - 吡啶-2-基胺或其结晶的酸加成盐以及生产相同。

6. 发明授权

US07253286B2 Nitrogen-containing aromatic derivatives 有权
标题翻译：含氮芳香族衍生物
公开(公告)号：US07253286B2
公开(公告)日：2007-08-07
申请号：US10420466
申请日：2003-04-18
申请人： Yasuhiro Funahashi , Akihiko Tsuruoka , Masayuki Matsukura , Toru Haneda , Yoshio Fukuda , Junichi Kamata , Keiko Takahashi , Tomohiro Matsushima , Kazuki Miyazaki , Ken-ichi Nomoto , Tatsuo Watanabe , Hiroshi Obaishi , Atsumi Yamaguchi , Sachi Suzuki , Katsuji Nakamura , Fusayo Mimura , Yuji Yamamoto , Junji Matsui , Kenji Matsui , Takako Yoshiba , Yasuyuki Suzuki , Itaru Arimoto
发明人： Yasuhiro Funahashi , Akihiko Tsuruoka , Masayuki Matsukura , Toru Haneda , Yoshio Fukuda , Junichi Kamata , Keiko Takahashi , Tomohiro Matsushima , Kazuki Miyazaki , Ken-ichi Nomoto , Tatsuo Watanabe , Hiroshi Obaishi , Atsumi Yamaguchi , Sachi Suzuki , Katsuji Nakamura , Fusayo Mimura , Yuji Yamamoto , Junji Matsui , Kenji Matsui , Takako Yoshiba , Yasuyuki Suzuki , Itaru Arimoto
IPC分类号： A61K31/47 , C07D215/16
CPC分类号： C07D213/73 , A61K31/4706 , A61K31/4745 , A61K31/517 , A61K31/519 , C07D207/34 , C07D213/26 , C07D213/68 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/18 , C07D215/233 , C07D215/36 , C07D215/38 , C07D215/48 , C07D239/34 , C07D239/42 , C07D239/47 , C07D239/88 , C07D249/04 , C07D261/14 , C07D277/48 , C07D307/68 , C07D319/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Compounds represented by the following general formula: [wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—, Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.
摘要翻译：由以下通式表示的化合物：其中A为任选取代的5至14元杂环基等; X-O是-O - ， - S-等; Y是任选取代的C 6-14芳基，任选取代的5至14元杂环基等; 并且T 1是由以下通式表示的基团：其中E是单键或-N（R 2）2 - R 1，G 1和R 2各自独立地表示氢原子，任选取代的C 1-6烷基等，Z

7. 发明授权

US07109219B2 Nitrogen-containing aromatic derivatives 有权
标题翻译：含氮芳香族衍生物
公开(公告)号：US07109219B2
公开(公告)日：2006-09-19
申请号：US10651496
申请日：2003-08-29
申请人： Akihiko Tsuruoka , Tomohiro Matsushima , Masayuki Matsukura , Kazuki Miyazaki , Keiko Takahashi , Junichi Kamata , Yoshio Fukuda
发明人： Akihiko Tsuruoka , Tomohiro Matsushima , Masayuki Matsukura , Kazuki Miyazaki , Keiko Takahashi , Junichi Kamata , Yoshio Fukuda
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： C07D401/12 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A compound represented by the general formula: wherein X1 represents a nitrogen atom or a group represented by the formula —CR10═; X2 represents a nitrogen atom or a group represented by the formula —CR11═; Y represents an oxygen atom or the like; R1 represents a C1-6 alkoxy group, an optionally substituted C6-10 aryloxy group, a group represented by the formula —NR12aR12b or the like; R2 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like; R3, R4, R5, R6, R7, R8, R10 and R11 each independently represent a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, or the like; R9 represents a group represented by the formula —NR12aR12b or the like; and R12a and R12b each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, a salt thereof, or a hydrate of the foregoing.
摘要翻译：由以下通式表示的化合物：其中X 1表示氮原子或由式-CR 10 - 表示的基团。 X 2表示氮原子或由式-CR 11-11表示的基团。 Y表示氧原子等; R 1表示C 1-6烷氧基，任选取代的C 6-10芳氧基，由-NR表示的基团 12b等等;或者， R 2表示氢原子，任选取代的C 1-6烷基等; R 3，R 4，R 5，R 6，R 7， R 8，R 10和R 11各自独立地表示氢原子，卤素原子，任选取代的C 1-6 烷基等; R 9表示由式-NR 12 R 12 R 12等表示的基团; 和R 12a和R 12b各自独立地表示氢原子，任选取代的C 1-6烷基等，盐或上述的水合物。

8. 发明授权

US5606073A Diazole-propenoic acid compounds 失效
标题翻译：二唑 - 丙烯酸化合物
公开(公告)号：US5606073A
公开(公告)日：1997-02-25
申请号：US419941
申请日：1995-04-11
申请人： Masayuki Matsukura , Keizoh Satoh , Naoki Yoneda , Makoto Kaino , Kazutoshi Miyake , Yoshiharu Daiku , Naoya Kishi , Fusayo Yoshida , Kenichi Nomoto , Toshiaki Ogawa , Tadanobu Takamura , Koichi Nose , Mikio Tomimatsu , Masanori Mizuno , Shigeto Negi , Shigeru Souda
发明人： Masayuki Matsukura , Keizoh Satoh , Naoki Yoneda , Makoto Kaino , Kazutoshi Miyake , Yoshiharu Daiku , Naoya Kishi , Fusayo Yoshida , Kenichi Nomoto , Toshiaki Ogawa , Tadanobu Takamura , Koichi Nose , Mikio Tomimatsu , Masanori Mizuno , Shigeto Negi , Shigeru Souda
IPC分类号： C07D213/38 , C07D213/61 , C07D231/12 , C07D233/54 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14
CPC分类号： C07D231/12 , C07D213/38 , C07D213/61 , C07D233/64 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14
摘要： Propenoic acid derivatives of the formula: ##STR1## where R.sup.15 and R.sup.17 are aryl or heteroalkyl groups and R.sup.16 and R.sup.18 are hydrogen, a lower alkyl or the like are intermediates used to prepare pharmaceutically active diazole propenoic acid compounds.
摘要翻译：下式的丙烯酸衍生物：其中R 15和R 17是芳基或杂烷基，R 16和R 18是氢，低级烷基等是用于制备药物活性二唑丙烯酸的中间体酸化合物。

9. 发明授权

US5506238A Biphenylmethane derivative and pharmacological use 失效
标题翻译：联苯甲烷衍生物和药理用途
公开(公告)号：US5506238A
公开(公告)日：1996-04-09
申请号：US877113
申请日：1992-05-01
申请人： Kazutoshi Miyake , Masayuki Matsukura , Naoki Yoneda , Osamu Hiroshima , Nobuyuki Mori , Hiroki Ishihara , Takashi Musha , Toshiyuki Matsuoka , Sachiyuki Hamano , Norio Minami
发明人： Kazutoshi Miyake , Masayuki Matsukura , Naoki Yoneda , Osamu Hiroshima , Nobuyuki Mori , Hiroki Ishihara , Takashi Musha , Toshiyuki Matsuoka , Sachiyuki Hamano , Norio Minami
IPC分类号： C07D235/08 , C07D235/26 , C07D235/28 , C07D403/10 , C07D471/04 , C07D487/04 , A61K31/435
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04
摘要： The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)p--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1=A2--A3=A4-- is --CH=CH--CH=CH--, --N=CH--CH=CH--, --CH=N--CH=CH--, --CH=CH--N=CH--, --CH=CH--CH=N-- or --CH=N--CH=N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.
摘要翻译：具有式（I）的联苯甲烷衍生物可用于预防和治疗高血压和心脏衰竭。其中R 1是氢，烷基，环烷基，卤代烷基，-S-R 7，-SO 2 -R 7，-C 3位C-R 7或 - （CH 2）p-OR 7，R 7是氢，烷基，环烷基或卤代烷基，p为0或1，-A1 = A2-A3 = A4-为-CH = CH-CH = CH-，-N = CH-CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-，-CH = CH-CH = N-或-CH = N-CH = N-，R2和R3各自为氢，卤素，低级烷基，烷氧基，氨基甲酰基或氰基，R4是氢或低级烷基，R5是1H-四唑-5-基，羧基（-COOH）或羧酸酯，R6是氢，卤素，羟基或低级烷氧基，或其药理学上可接受的盐。

10. 发明授权

US5328911A Biphenylmethane derivative and pharmacological use 失效
标题翻译：联苯甲烷衍生物和药理用途
公开(公告)号：US5328911A
公开(公告)日：1994-07-12
申请号：US583025
申请日：1990-09-13
申请人： Kazutoshi Miyake , Masayuki Matsukura , Naoki Yoneda , Osamu Hiroshima , Nobuyuki Mori , Hiroki Ishihara , Takashi Musha , Toshiyuki Matsuoka , Sachiyuki Hamano , Norio Minami
发明人： Kazutoshi Miyake , Masayuki Matsukura , Naoki Yoneda , Osamu Hiroshima , Nobuyuki Mori , Hiroki Ishihara , Takashi Musha , Toshiyuki Matsuoka , Sachiyuki Hamano , Norio Minami
IPC分类号： C07D235/08 , A61K31/00 , A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/44 , A61K31/496 , A61K31/505 , A61P9/00 , A61P9/12 , A61P43/00 , C07D221/02 , C07D235/02 , C07D235/06 , C07D235/10 , C07D235/12 , C07D235/26 , C07D235/28 , C07D403/10 , C07D471/04 , C07D487/04
CPC分类号： C07D403/10 , C07D235/08 , C07D235/26 , C07D235/28 , C07D471/04 , C07D487/04
摘要： The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)p--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1.dbd.A2--A3.dbd.A4-- is --CH.dbd.CH--CH.dbd.CH--, --N.dbd.CH--CH.dbd.CH--, --CH.dbd.N--CH.dbd.CH--, --CH.dbd.CH--N.dbd.CH--, --CH.dbd.CH--CH.dbd.N-- or --CH.dbd.N--CH.dbd.N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.
摘要翻译：具有式（I）的联苯甲烷衍生物可用于预防和治疗高血压和心脏衰竭。其中R 1是氢，烷基，环烷基，卤代烷基，-S-R 7，-SO 2 -R 7，-C 3位C-R 7或 - （CH 2）p-OR 7，R 7是氢，烷基，环烷基或卤代烷基，p为0或1，-A1 = A2-A3 = A4-为-CH = CH-CH = CH-，-N = CH-CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-，-CH = CH-CH = N-或-CH = N-CH = N-，R2和R3各自为氢，卤素，低级烷基，烷氧基，氨基甲酰基或氰基，R4是氢或低级烷基，R5是1H-四唑-5-基，羧基（-COOH）或羧酸酯，R6是氢，卤素，羟基或低级烷氧基，或其药理学上可接受的盐。

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