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1. 发明申请

WO1998014431A1 NITROGENOUS HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：硝基杂环化合物
公开(公告)号：WO1998014431A1
公开(公告)日：1998-04-09
申请号：PCT/JP1997003510
申请日：1997-10-01
申请人： KYOWA HAKKO KOGYO CO., LTD. , MATSUNO, Kenji , ICHIMURA, Michio , NOMOTO, Yuji , FUJIWARA, Shigeki , IDE, Shinichi , TSUKUDA, Eiji , IRIE, Junko , ODA, Shoji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D215/46
CPC分类号： C07D401/12 , A61K31/496 , A61K31/502 , A61K31/517 , C07D215/46 , C07D217/22 , C07D237/34 , C07D239/94 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/04
摘要： Nitrogenous heterocyclic compounds of general formula (I) and pharmacologically acceptable salts thereof, which hinder the phosphorylation of PDGF acceptors and the abnormal proliferation or migration of cells and so are effective in preventing or treating cell proliferative diseases such as arterial sclerosis, vascular reocclusion diseases, cancer and glomerulosclerosis, wherein V is oxygen or sulfur; W is 1,4-piperazinediyl or 1,4-homopiperazinediyl which may be substituted with unsubstituted alkyl on the ring; X is nitrogen or C-R , Y is nitrogen or C-R and Z is nitrogen or C-R , with at least one of X, Y and Z being nitrogen; R is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like; R is substituted alkyl, substituted or unsubstituted cycloalkyl or the like; R , R , R and R are each independently hydrogen, halogeno, substituted or unsubstituted alkyl, nitro, cyano, -OR , -NR R or the like; R is halogeno or the like; R is the same as defined above for R ; and R is hydrogen or -COR .
摘要翻译：通式（I）的氮杂环化合物及其药理学上可接受的盐阻碍PDGF受体的磷酸化和细胞的异常增殖或迁移等，有效预防或治疗细胞增殖性疾病如动脉硬化，血管再闭塞疾病，癌症和肾小球硬化，其中V是氧或硫; W是可以在环上被未取代的烷基取代的1,4-哌嗪二基或1,4-高哌嗪二基; X是氮或C-R 9，Y是氮或C-R 8，Z是氮或C-R 7，X，Y和Z中的至少一个是氮; R 1是氢，取代或未取代的烷基，取代或未取代的环烷基等; R 2是取代的烷基，取代或未取代的环烷基等; R 3，R 4，R 5和R 6各自独立地为氢，卤素，取代或未取代的烷基，硝基，氰基，-OR 12，-NR 15 R 16，或类似物; R 7是卤代等; R 8与上述R 7相同; R 9为氢或-COR 41。

2. 发明申请

WO1995006648A1 IMIDAZOQUINAZOLINE DERIVATIVE 审中-公开
标题翻译：咪唑啉酮衍生物
公开(公告)号：WO1995006648A1
公开(公告)日：1995-03-09
申请号：PCT/JP1994001456
申请日：1994-09-02
申请人： KYOWA HAKKO KOGYO CO., LTD. , MACHII, Daisuke , MATSUNO, Kenji , KINOSHITA, Iwao , NOMOTO, Yuji , TAKAI, Haruki , OHNO, Tetuji , NAGASHIMA, Ken , ISHIKAWA, Tomoko , YAMADA, Koji , ICHIMURA, Michio , KASE, Kiroshi
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： An imidazoquinazoline derivative represented by formula (I) or a pharmacologically acceptable salt thereof, wherein R andR may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkenyl, aryl, etc.; R represents hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aryl, etc.; and X represents O or S. This compound has a potent and selective cCMP-specific PDE inhibitor activity and is useful for treating or mitigating cardiovascular diseases such as thrombosis, angina pectoris, hypertension and arteriosclerosis, asthma, and so forth.
摘要翻译：由式（I）表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐，其中R 1和R 2可以相同或不同，各自代表氢，低级烷基，低级烯基，芳基等; R 3表示氢，低级烷基，环烷基，低级烯基，芳基等; X表示O或S.该化合物具有有效和选择性的cCMP特异性PDE抑制剂活性，可用于治疗或缓解心血管疾病如血栓形成，心绞痛，高血压和动脉硬化，哮喘等。

3. 发明申请

WO1998008848A1 IMIDAZOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译：咪唑啉酮衍生物
公开(公告)号：WO1998008848A1
公开(公告)日：1998-03-05
申请号：PCT/JP1997003023
申请日：1997-08-29
申请人： KYOWA HAKKO KOGYO CO., LTD. , ONODA, Yasuo , NOMOTO, Yuji , OHNO, Tetsuji , YAMADA, Koji , ICHIMURA, Michio
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, which have potent and selective inhibitory effects on cyclic guanosine-3',5'-monophosphate (cGMP)-specific phosphodiesterase and are useful in, for example, treating or relieving cardiovascular diseases such as thrombosis, angina pectoris, hypertension, cardiac insufficiency and arteriosclerosis, asthma, etc. and treating sexual impotence. In said formula, R represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicycloalkyl, optionally substituted tricycloalkyl, etc.; R represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicyclaolkyl, optionally substituted tricycloalkyl, optionally substituted lower alkenyl, optionally substituted aralkyl, etc.; R represents hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted bicycloalkyl, optionally substituted tricycloalkyl, optionally substituted lower alkenyl, optionally substituted aralkyl, etc., or R and R may form together with N an optionally substituted heterocyclic group; and X represents O or S.
摘要翻译：对通式（I）表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐，对环鸟嘌呤-3'，5'-单磷酸（cGMP）特异性磷酸二酯酶具有有效和选择性的抑制作用，可用于例如治疗或缓解心血管疾病如血栓形成，心绞痛，高血压，心功能不全和动脉硬化，哮喘等，并治疗性阳。。在所述式中，R 1表示氢，任选取代的低级烷基，任选取代的环烷基，任选取代的双环烷基，任选取代的三环烷基等; R 2表示氢，任选取代的低级烷基，任选取代的环烷基，任选取代的双环烷基，任选取代的三环烷基，任选取代的低级烯基，任选取代的芳烷基等; R 3表示氢，任选取代的低级烷基，任选取代的环烷基，任选取代的双环烷基，任选取代的三环烷基，任选取代的低级链烯基，任选取代的芳烷基等，或R 2和R 3可与 N为任选取代的杂环基; X表示O或S.

4. 发明申请

WO1998015555A1 FUSED PURINE DERIVATIVES 审中-公开
标题翻译：熔化的嘌呤衍生物
公开(公告)号：WO1998015555A1
公开(公告)日：1998-04-16
申请号：PCT/JP1997003586
申请日：1997-10-07
申请人： KYOWA HAKKO KOGYO CO., LTD. , TSUMUKI, Hiroshi , SAKI, Mayumi , NONAKA, Hiromi , ICHIMURA, Michio , SHIMADA, Junichi , SUZUKI, Fumio , ICHIKAWA, Shunji , KOSAKA, Nobuo
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： Fused purine derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, which show an adenosine A3 receptor antagonism and have, for example, antiasthmatic, bronchodilating and itch-relieving effects. In said formula, R represents optionally substituted aryl or an optionally substituted aromatic heterocyclic group; R represents hydrogen, lower alkyl, alicyclic alkyl, optionally substituted aralkyl, optionally substituted aryl, or an optionally substituted aromatic heterocyclic group; R represents hydrogen, lower alkyl or optionally substituted aralkyl; X and X are the same or different and each represents hydrogen, lower alkyl, optionally substituted aralkyl, or optionally substituted aryl; and n is an integer of 0 to 3.
摘要翻译：由通式（I）表示的稠合嘌呤衍生物或其药理学上可接受的盐，其表现出腺苷A3受体拮抗作用，并且具有例如止喘，支气管扩张和瘙痒缓解作用。在所述式中，R 1表示任选取代的芳基或任选取代的芳族杂环基; R 2表示氢，低级烷基，脂环族烷基，任选取代的芳烷基，任选取代的芳基或任选取代的芳族杂环基; R 3表示氢，低级烷基或任选取代的芳烷基; X 1和X 2相同或不同，各自表示氢，低级烷基，任选取代的芳烷基或任选取代的芳基; n为0〜3的整数。

5. 发明申请

WO1996036624A1 OXYGEN-CONTAINING HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：含氧杂环化合物
公开(公告)号：WO1996036624A1
公开(公告)日：1996-11-21
申请号：PCT/JP1996001327
申请日：1996-05-20
申请人： KYOWA HAKKO KOGYO CO., LTD. , KAWAKITA, Takashi , OHSHIMA, Etsuo , YANAGAWA, Koji , IIDA, Kyoichiro , KOIKE, Rie , ICHIMURA, Michio , MANABE, Haruhiko , OHMORI, Kenji , SUZUKI, Fumio , NAKASATO, Yoshisuke
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D307/80
CPC分类号： C07D307/79 , C07D307/94 , C07D405/06 , C07D405/12 , C07D405/14
摘要： Oxygen-containing heterocyclic compounds represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R and R are the same or different and each represents hydrogen, lower alkyl, cyano or -(CH2)n-E-CO-F (wherein E represents a bond, O or NH; F represents OR or NR R ; and n is an integer of from 0 to 4), or R and R together with the adjacent carbon atom may form a saturated carbocyclic ring, or R together with R or R , as will be described hereinbelow, may form a single bond; R represents hydrogen, phenyl or halogeno; R represents hydroxy, lower alkoxy, etc.; A represents -C(R )(R )- or O; B represents O, NR , -C(R )(R )- or -C(R )(R )-C(R )(R )-; D represents (1) -C(R )(R )-X- [where X represents -C(R )(R )-, S or NR ], (2) -C(R )=Y- [wherein Y represents -C(R )-Z-, {wherein Z represents CONH, CONHCH2 or a bond}, or N] or (3) a bond; and R represents aryl, heteroaryl, cycloalkyl, pyridine-N-oxide, cyano or lower alkoxycarbonyl.
摘要翻译：由通式（I）表示的含氧杂环化合物或其药理学上可接受的盐，其中R 1和R 2相同或不同，各自表示氢，低级烷基，氰基或 - （CH 2）nE-CO -F（其中E表示键，O或NH; F表示OR 6或NR 7 R 8; n为0至4的整数）或R 1和R 2 与相邻的碳原子一起可以形成饱和的碳环，或者R 2与R 11或R 13一起，如下所述，可以形成单键; R 3表示氢，苯基或卤代; R 4表示羟基，低级烷氧基等; A表示-C（R 9）（R 10） - 或O; B表示O，NR 11，-C（R 12）（R 13） - 或-C（R 14）（R 15）-C（R 16）（R 16） 17>） - ; D表示（1）-C（R 18）（R 19）-X- [其中X表示-C（R 21）（R 22） - ，S或NR 23] （2）-C（R 19）= Y- [其中Y表示-C（R 24） - Z - ，其中Z表示CONH，CONHCH2或键}或N]或（3）a 键; R 5表示芳基，杂芳基，环烷基，吡啶-N-氧化物，氰基或低级烷氧基羰基。

6. 发明申请

WO1987006265A1 NOVEL COMPOUNDS DC-88A AND DC-89A1 AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：新型化合物DC-88A和DC-89A1及其制备方法
公开(公告)号：WO1987006265A1
公开(公告)日：1987-10-22
申请号：PCT/JP1987000247
申请日：1987-04-17
申请人： KYOWA HAKKO KOGYO CO., LTD. , NAKANO, Hirofumi , TAKAHASHI, Isami , ICHIMURA, Michio , KAWAMOTO, Isao , ASANO, Kozo , TOMITA, Fusao , SANO, Hiroshi , YASUZAWA, Toru , MORIMOTO, Makoto , FUJIMOTO, Kazuhisa
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C12P01/06
CPC分类号： C12P1/06 , C12R1/465
摘要： New cpds. designated DC-88A and DC-89Al are obtd. by culture of Streptomyces species, specifically S. lydicus FERM-BP 988 or S. parvullus FERM-BP 1002. DC-88A has the molecular formula C26H25N3O8, mol. wt. (by EI-MS) 507.1624, and is sol. in methanol, ethanol, acetone, chloroform, ethyl acetate, DMSO; insol. in water, hexane. The Rf on silica gel using toluene/acetone (7:3 v/v) is 0.46. DC-89Al has the molecular formula C26H26N3O8Cl, mol. wt. 543, m.pt. 157.5-58.5 deg.C; sol. in methanol, ethanol, acetone, ethyl acetate, chloroform, DMSO; insol. in water, hexane, IR, UV, 1H NMR, 13C NMR spectral data are given for both cpds.

7. 发明申请

WO1998022455A1 OXYGENIC HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：含氧杂环化合物
公开(公告)号：WO1998022455A1
公开(公告)日：1998-05-28
申请号：PCT/JP1997004211
申请日：1997-11-19
申请人： KYOWA HAKKO KOGYO CO., LTD. , NAKASATO, Yoshisuke , OHSHIMA, Etsuo , KOIKE, Rie , ICHIMURA, Michio , MANABE, Haruhiko , SATO, Soichiro , ISHII, Hidee , YANAGAWA, Koji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D319/18
CPC分类号： C07D405/06 , C07D319/18 , C07D405/12
摘要： Oxygenic heterocyclic compounds represented by general formula (I) or pharmacologically acceptable salts thereof, wherein n is an integer of 1 to 4; R , R , R and R are the same or diffrent and each represents hydrogen, optionally substituted lower alkyl, etc.; R represents hydrogen or halogeno; R represents hydroxy or optionally substituted lower alkoxy; D represents (1): -C(R )(R )-X- or bond (2): -Y-ZR ; and R represents (1), optionally substituted lower alkyl, optionally substituted cycloalkyl, polycycloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted aromatic heterocycle, optionally substituted heterocycle, or pyridine N-oxide, (2), (3): -Y-Z-(CH2)m-N(R )R , or (4): -Y-CON(R )R .
摘要翻译：由通式（I）表示的氧杂环化合物或其药理学上可接受的盐，其中n为1至4的整数; R 1，R 2，R 3和R 4相同或不同，各自代表氢，任选取代的低级烷基等; R 5表示氢或卤素; R 6表示羟基或任选取代的低级烷氧基; D表示（1）：-C（R 8）（R 9）-X-或键（2）：-Y-ZR 14; 任选取代的芳烷基，任选取代的芳族杂环，任选取代的杂环或吡啶N-氧化物，（2），（3））：-YZ-（CH2）mN（R 16a）R 16b或（4）：-Y-CON（R 17a）R 17b。

8. 发明申请

WO1996026940A1 IMIDAZOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译：咪唑啉酮衍生物
公开(公告)号：WO1996026940A1
公开(公告)日：1996-09-06
申请号：PCT/JP1996000497
申请日：1996-03-01
申请人： KYOWA HAKKO KOGYO CO., LTD. , ONODA, Yasuo , SASAKI, Shin-ichi , MACHII, Daisuke , TAKAI, Haruki , OHNO, Tetsuji , YAMADA, Koji , ICHIMURA, Michio , KASE, Hiroshi
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R represents hydrogen, optionally substituted lower alkyl, etc.; R and R are the same or different and each represents hydrogen, optionally substituted lower alkyl, optionally substituted aralkyl, optionally substituted aryl, etc., or R and R together form an optionally substituted nitrogenous heterocycle; R represents hydrogen or optionally substituted lower alkyl; X represents O or S; Y represents a single bond or O; and n is 0, 1, 2 or 3.
摘要翻译：由通式（I）表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐，其中R 1表示氢，任选取代的低级烷基等; R 2和R 3相同或不同，各自表示氢，任选取代的低级烷基，任选取代的芳烷基，任选取代的芳基等，或R 2和R 3一起形成任选取代的含氮杂环 R 4表示氢或任选取代的低级烷基; X表示O或S; Y表示单键或O; n为0,1,2或3。

9. 发明申请

WO1998022452A1 BENZOFURAN DERIVATIVES 审中-公开
标题翻译： BENZOFURAN衍生物
公开(公告)号：WO1998022452A1
公开(公告)日：1998-05-28
申请号：PCT/JP1997004212
申请日：1997-11-19
申请人： KYOWA HAKKO KOGYO CO., LTD. , OHSHIMA, Etsuo , MATSUZAKI, Tohru , IIDA, Kyoichiro , ICHIMURA, Michio
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D307/84
CPC分类号： C07D307/86
摘要： Benzofuran derivatives represented by general formula (I) and pharmacologically acceptable salts thereof wherein R is hydrogen or substituted or unsubstituted lower alkyl; R , R and R are each independently hydrogen or the like; R is hydrogen, substituted or unsubstituted lower alkyl, cycloalkyl, polycycloalkyl, substituted or unsubstituted aryl or the like, and R is substituted or unsubstituted lower alkyl, cycloalkyl, polycycloalkyl or the like, or alternatively R and R may be united to form a substituted or unsubstituted nitrogenous heterocyclic group; and R and R are each independently hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted heteroarylalkyl or substituted or unsubstituted aralkyl, or alternatively R and R may be united to form a substituted or unsubstituted nitrogenous heterocyclic group.
摘要翻译：由通式（I）表示的苯并呋喃衍生物及其药理学上可接受的盐，其中R 1是氢或取代或未取代的低级烷基; R 2，R 3和R 4各自独立地为氢等; R 5a是氢，取代或未取代的低级烷基，环烷基，多环烷基，取代或未取代的芳基等，R 5b是取代或未取代的低级烷基，环烷基，多环烷基等，或者R 5a， R 5b可以结合形成取代或未取代的含氮杂环基; R 6a和R 6b各自独立地为氢，取代或未取代的低级烷基，取代或未取代的杂芳基烷基或取代或未取代的芳烷基，或者R 6a和R 6b可以一起形成取代或未取代的芳烷基，未取代的含氮杂环基。

10. 发明申请

WO1995000546A1 ENDOTHELIN-ANTAGONIZING PEPTIDE 审中-公开
标题翻译：内皮素 - 拮抗肽
公开(公告)号：WO1995000546A1
公开(公告)日：1995-01-05
申请号：PCT/JP1994001011
申请日：1994-06-23
申请人： KYOWA HAKKO KOGYO CO., LTD. , SHIBATA, Kenji , SUZAWA, Toshiyuki , YAMASAKI, Motoo , TANAKA, Takeo , TSUKUDA, Eiji , YAMADA, Koji , OHNO, Tetsuji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07K07/08
CPC分类号： C07K7/06 , A61K38/00 , C07K14/57536
摘要： An endothelin-antagonizing peptide compound represented by general formula (I) and a pharmacologically acceptable salt thereof: R -R -R -R -R -R -R -R -R -R -R -R -Phe-R -R -R -R -R -Ile-R -Z wherein R is X -Gly, X (a), X -SCH2CO or hydrogen; R is Asn, Asp, Phe, Tyr, Ser or a single bond; R is Trp, Ile, Pro, Ala or a single bond; R is His, Lys, Gly, Trp, Ala or a single bond; R is Gly, Thr, Trp, Val or a single bond; R is Gly, Thr, Asn, Tyr, Asp or a single bond; R is Ala, Ser, Asn, Asp, Tyr, Phe or a single bond; R is Pro, Ala, Arg or a single bond; R is (b), (c) or a single bond; R is Trp or Ala; R is Val, Pro or a single bond; R is Tyr or a single bond; R is Ala, MeAla, Ser or Cys; R is His or Trp; R is Leu or Nva; R is Asp, Thr, Asn, Ser, Gly or Glu; R is Ile, Leu, Cha, Abu, Thi, Met, Tyr, MeLeu, MeIle, Phg or Nle; R is Trp, Phe or Tyr; and Z is hydroxy, lower alkoxy or amino.
摘要翻译：由通式（I）表示的内皮素拮抗肽化合物及其药理学上可接受的盐：R 1 -R 2 -R 3 -R 4 -R 5 -R 6 - [R <7> -R <8> -R <9> -R <10> -R <11> -R <12> -Phe-R <14> -R <15> -R <16> -R <17 其中R 1为X 1 -Gly，X 3（a），X 2 -SCH 2 CO或氢; R 2是Asn，Asp，Phe，Tyr，Ser或单键; R 3是Trp，Ile，Pro，Ala或单键; R 4是His，Lys，Gly，Trp，Ala或单键; R 5是Gly，Thr，Trp，Val或单键; R 6是Gly，Thr，Asn，Tyr，Asp或单键; R 7是Ala，Ser，Asn，Asp，Tyr，Phe或单键; Pro，Ala，Arg或单键; R 9为（b），（c）或单键; R 10是Trp或Ala; R 11是Val，Pro或单键; R 12是Tyr或单键; R 14是Ala，MeAla，Ser或Cys; R 15是His或Trp; R 16是Leu或Nva; R 17是Asp，Thr，Asn，Ser，Gly或Glu; R 18是Ile，Leu，Cha，Abu，Thi，Met，Tyr，MeLeu，MeIle，Phg或Nle; R 20是Trp，Phe或Tyr; Z为羟基，低级烷氧基或氨基。

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