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1. 发明授权

US5478835A Tricyclic compounds and intermediates thereof 失效
标题翻译：三环化合物及其中间体
公开(公告)号：US5478835A
公开(公告)日：1995-12-26
申请号：US236097
申请日：1994-05-02
申请人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
发明人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
IPC分类号： A61K31/335 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/55 , A61P3/06 , A61P9/10 , A61P43/00 , C07C233/65 , C07C235/46 , C07C235/48 , C07C237/40 , C07C323/40 , C07C323/62 , C07C327/26 , C07C331/08 , C07D221/16 , C07D223/20 , C07D233/58 , C07D313/12 , C07D337/12 , C07D471/04 , C07D491/04 , C07D491/044 , C07D495/04 , C07C207/00 , C07C237/00
CPC分类号： C07D491/04 , C07C233/65 , C07D223/20 , C07D313/12 , C07D337/12 , C07C2103/32 , Y10S514/824
摘要： Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
摘要翻译：公开了由式（I）表示的三环化合物：其中R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基）或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6 - 烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-S（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基） Z表示氧或硫，或其药学上可接受的盐。该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。

2. 发明授权

US5340807A Tricyclic compounds and intermediates thereof 失效
标题翻译：三环化合物及其中间体
公开(公告)号：US5340807A
公开(公告)日：1994-08-23
申请号：US989906
申请日：1992-12-11
申请人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
发明人： Toshiaki Kumazawa , Masashi Yanase , Hiroyuki Harakawa , Hiroyuki Obase , Shoji Oda , Shiro Shirakura , Koji Yamada , Kazuhiro Kubo
IPC分类号： A61K31/335 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/235 , A61K31/275 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/55 , A61P3/06 , A61P9/10 , A61P43/00 , C07C233/65 , C07C235/46 , C07C235/48 , C07C237/40 , C07C323/40 , C07C323/62 , C07C327/26 , C07C331/08 , C07D221/16 , C07D223/20 , C07D233/58 , C07D313/12 , C07D337/12 , C07D471/04 , C07D491/04 , C07D491/044 , C07D495/04 , A01N43/46 , C07D273/02 , C07D313/06
CPC分类号： C07D491/04 , C07C233/65 , C07D223/20 , C07D313/12 , C07D337/12 , C07C2103/32 , Y10S514/824
摘要： Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.14 represents hydrogen or C1-6 alkyl) and Z represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof. The compound possesses an acyl coenzyme A: cholesterol acyltransferase-inhibiting activity, and thus are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
摘要翻译：公开了由式（I）表示的三环化合物：其中R 1，R 2，R 3和R 4各自独立地表示氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基， C 1-6烷基氨基，卤代C 1-6烷基，卤代C 1-6烷氧基，卤素，硝基，氰基，羧基，C 1-6烷氧基羰基，羟甲基，CR 9 R 10 CO 2 R 11（其中R 9，R 10和R 11各自独立地表示氢或C 1-6烷基）或CONR 12 R 13（其中R 12和R 13各自独立地表示氢或C 1-6烷基）; R5表示氢或C1-6烷基; R 6，R 7和R 8各自独立地表示氢，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷酰氧基，C 1-6烷硫基，氰硫基或卤素; X表示CH或N; Y1-Y2表示CH2-O，CH2-（O）n，（其中n表示0,1或2），CH2CH2，CH = CH或CON（R14）（其中R14表示氢或C1-6烷基）和Z 表示氧或硫，或其药学上可接受的盐。该化合物具有酰基辅酶A：胆固醇酰基转移酶抑制活性，因此预期对高脂血症和动脉硬化具有预防和治疗作用。

3. 发明授权

US5679703A Tricyclic compounds having ACAT inhibiting activity 失效
标题翻译：具有ACAT抑制活性的三环化合物
公开(公告)号：US5679703A
公开(公告)日：1997-10-21
申请号：US523843
申请日：1995-09-07
申请人： Masashi Yanase , Toshiaki Kumazawa , Shiro Shirakura , Eiko Oishi , Koji Yamada
发明人： Masashi Yanase , Toshiaki Kumazawa , Shiro Shirakura , Eiko Oishi , Koji Yamada
IPC分类号： C07C275/28 , C07D313/12 , A61K31/335 , A61K31/38 , C07D337/12
CPC分类号： C07C275/28 , C07D313/12 , C07C2103/32
摘要： Disclosed is a tricyclic compound represented by formula (I): ##STR1## where X.sup.1 -X.sup.2 represents CH.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.N or S--CH.dbd.CH; Y--Z represents CH.sub.2 --O or CH.sub.2 --S; then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 represents hydrogen or lower alkyl) or CH--CR.sup.10 R.sup.11 (in which each of R.sup.10 and R.sup.11 independently represents hydrogen or lower alkyl); W represents NR.sup.4 (in which R.sup.4 represents hydrogen or lower alkyl) or O; each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen, lower alkyl, lower alkoxy, halogen, nitro, amino or mono or di-lower alkyl-substituted amino; R.sup.5 represents hydrogen or lower alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, halogen, lower alkyl or lower alkoxy; provided that when Y--Z represents CH.dbd.CH or CH.sub.2 CH.sub.2, then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 has the same meaning as defined above),or CH--CR.sup.10a R.sup.11a (in which each of R.sup.10a and R.sup.11a represents lower alkyl of R.sup.10 and R.sup.11); and a pharmaceutically acceptable salt thereto. The compound and its salt have an ACAT inhibiting activity and are expected to have preventive and therapeutic effects on hyperlipemia and arteriosclerosis.
摘要翻译：公开了由式（I）表示的三环化合物：其中X 1 -X 2表示CH = CH-CH = CH，CH = CH-CH = N或S-CH = CH; Y-Z表示CH 2 -O或CH 2 -S; 那么L-M表示C = CR9（其中R9表示氢或低级烷基）或CH-CR10R11（其中R10和R11各自独立地表示氢或低级烷基）; W表示NR4（其中R4表示氢或低级烷基）或O; R 1，R 2和R 3各自独立地表示氢，低级烷基，低级烷氧基，卤素，硝基，氨基或单或二低级烷基取代的氨基; R5代表氢或低级烷基; R 6，R 7和R 8各自独立地表示氢，卤素，低级烷基或低级烷氧基; 条件是当YZ表示CH = CH或CH 2 CH 2时，LM表示C = CR 9（其中R9具有与上述相同的含义）或CH-CR10aR11a（其中R10a和R11a各自表示R10和R11的低级烷基） ; 和其药学上可接受的盐。该化合物及其盐具有ACAT抑制活性，预期对高脂血症和动脉硬化具有预防和治疗作用。

4. 发明授权

US5378701A Tricyclic compounds 失效
标题翻译：三环化合物
公开(公告)号：US5378701A
公开(公告)日：1995-01-03
申请号：US65916
申请日：1993-05-25
申请人： Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
发明人： Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
IPC分类号： C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04 , C07D521/00 , A61K31/55 , C07D223/16 , C07D223/22
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04
摘要： A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m -- wherein m is an integer of 0 to 2; W represents ##STR2## and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.CH or CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2, ##STR3## and Q represents N or CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents CH.sub.2 CH.sub.2 ; and Z.sup.1 --Z.sup.2 represents N--(CH.sub.2).sub.n -- wherein n is an integer of 1 to 3 or a pharmaceutically acceptable salt thereof.
摘要翻译：由下式（I）表示的三环化合物：其中R 1表示氢，卤素或低级烷基; A代表氰基，羧基，四唑基，氰基取代的苯基，羧基取代的苯基或四唑基取代的苯基; V表示 - （CH 2）m - ，其中m是0至2的整数; W表示，Q1-Q2-Q3-Q4表示N = CH-CH = CH，CH = CH-CH = CH或CH2-CH2-CH2-CH2， N或CH; X1-X2-X3表示CH = CH-CH = CH，S-CH = CH或CH = CH-S; Y表示CH 2 CH 2; Z1-Z2表示N-（CH2）n-，其中n为1〜3的整数或其药学上可接受的盐。

5. 发明授权

US5478840A Tricyclic compounds 失效
标题翻译：三环化合物
公开(公告)号：US5478840A
公开(公告)日：1995-12-26
申请号：US294978
申请日：1994-08-24
申请人： Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
发明人： Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
IPC分类号： C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04 , C07D521/00 , A61K31/44
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04
摘要： A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m --(wherein m is an integer of 0 to 2); W represents ##STR2## (wherein R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, halogen, lower alkyl, cycloalkyl, halogenated lower alkyl, hydroxy, lower alkoxy, amino, lower alkylamino, carboxyl or lower alkoxycarbonyl; and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents a single bond, CH.sub.2, O, S, CH.sub.2 O, OCH.sub.2, CH.sub.2 S, SCH.sub.2, CH.sub.2 CH.sub.2 or CH.dbd.CH; and Z.sup.1 --Z.sup.2 represents C.dbd.CH, CH--CH.sub.2 or CH--CH(COOH)-- or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits antagonism to angiotensin II receptors.
摘要翻译：由下式（I）表示的三环化合物：其中R 1表示氢，卤素或低级烷基; A代表氰基，羧基，四唑基，氰基取代的苯基，羧基取代的苯基或四唑基取代的苯基; V表示 - （CH 2）m - （其中m为0〜2的整数）; W表示（其中R2，R3和R4独立地表示氢，卤素，低级烷基，环烷基，卤代低级烷基，羟基，低级烷氧基，氨基，低级烷基氨基，羧基或低级烷氧基羰基;以及Q1-Q2-Q3-Q4 表示N = CH-CH = CH; X 1 -X 2 -X 3表示CH = CH-CH = CH，S-CH = CH或CH = CH-S; Y表示单键，CH 2，O，S，CH 2 O，OCH 2 ，CH2S，SCH2，CH2CH2或CH = CH; Z1-Z2表示C = CH，CH-CH2或CH-CH（COOH） - 或其药学上可接受的盐。本发明化合物显示对血管紧张素II受体的拮抗作用。

6. 发明授权

US5607955A Tricyclic compounds on angiotensin II receptor antagonists 失效
标题翻译：三环化合物作为血管紧张素II受体拮抗剂
公开(公告)号：US5607955A
公开(公告)日：1997-03-04
申请号：US431425
申请日：1995-05-01
申请人： Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
发明人： Etsuo Ohshima , Fumihiko Kanai , Hideyuki Sato , Hiroyuki Obase , Toshiaki Kumazawa , Shiho Takahara , Tetsuji Ohno , Tomoko Ishikawa , Koji Yamada
IPC分类号： C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04 , C07D521/00 , A61K31/41 , A61K31/415 , C07D233/54 , C07D235/04 , C07D257/04
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D471/04
摘要： A tricyclic compound represented by the following formula (I): ##STR1## exhibits antagonism to angiotensin II receptors.
摘要翻译：由下式（I）表示的三环化合物：显示对血管紧张素II受体的拮抗作用。

7. 发明授权

US5116863A Dibenz[b,e]oxepin derivative and pharmaceutical compositions thereof 失效
标题翻译： DIBENZ（B，E）OXEPIN衍生物和药物组合物
公开(公告)号：US5116863A
公开(公告)日：1992-05-26
申请号：US20900
申请日：1987-03-02
申请人： Etsuo Oshima , Toshiaki Kumazawa , Shizuo Otaki , Hiroyuki Obase , Kenji Ohmori , Hidee Ishii , Haruhiko Manabe , Tadafumi Tamura , Katsuichi Shuto
发明人： Etsuo Oshima , Toshiaki Kumazawa , Shizuo Otaki , Hiroyuki Obase , Kenji Ohmori , Hidee Ishii , Haruhiko Manabe , Tadafumi Tamura , Katsuichi Shuto
IPC分类号： A61K31/40 , A61K31/00 , A61K31/335 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P29/00 , A61P37/08 , C07D313/12 , C07D405/06 , C07D405/12 , C07D413/04
CPC分类号： C07D405/06 , C07D313/12 , C07D405/12
摘要： Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.
摘要翻译：新的二苯并[b，e]氧杂七环素衍生物用于治疗和控制变应性疾病如过敏性哮喘，也用于治疗炎症。

8. 发明授权

US5239083A Indole derivatives which inhibit steroid 5.alpha. reductase 失效
标题翻译：抑制甾体5（ALPHA）还原的吲哚衍生物
公开(公告)号：US5239083A
公开(公告)日：1993-08-24
申请号：US850334
申请日：1992-03-10
申请人： Toshiaki Kumazawa , Hitoshi Takami , Hiroyuki Obase , Nobuyuki Kishibayashi , Akio Ishii
发明人： Toshiaki Kumazawa , Hitoshi Takami , Hiroyuki Obase , Nobuyuki Kishibayashi , Akio Ishii
IPC分类号： C07D209/08 , C07D401/06
CPC分类号： C07D401/06 , C07D209/08
摘要： The present invention provides Indole derivatives represented by the formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 independently represent hydrogen or lower alkyl;R.sup.4 represents hydrogen, lower alkyl or cycloalkyl;R.sup.5 represents hydrogen, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl,--CHR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 independently represent hydrogen, alkyl, alkenyl, alkynyl, substituted or unsubstituted cycloalkyl, --(CH.sub.2).sub.m OR.sup.9 (wherein m is an integer of 1-3 and R.sup.9 is lower alkyl), substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, or substituted or unsubstituted thienyl], ##STR2## (wherein Y is CH.sub.2, O, S, CH.sub.2 --CH.sub.2, CH.dbd.CH, CH.sub.2 --O or CH.sub.2 --S); R.sup.6 represents hydrogen, lower alkyl or lower alkoxy or halogen;X represents O or S(O)q (wherein q is an integer of 0-2); and n represents an integer of 1-6) or pharmaceutically acceptable salt thereof.The compound shows prominent inhibition effects on steroid 5.alpha.-reductase activity, and are useful in treating benign prostatic hypertrophy, prostate cancer, baldness and acne.

9. 发明授权

US06211227B1 Tricyclic compounds 失效
标题翻译：三环化合物
公开(公告)号：US06211227B1
公开(公告)日：2001-04-03
申请号：US09417626
申请日：1999-10-14
申请人： Makoto Yoshida , Takashi Seishi , Shigeru Aono , Tsuyoshi Yamagata , Kaoru Atsuki , Toshiaki Kumazawa , Haruki Takai , Koji Suzuki , Akira Karasawa
发明人： Makoto Yoshida , Takashi Seishi , Shigeru Aono , Tsuyoshi Yamagata , Kaoru Atsuki , Toshiaki Kumazawa , Haruki Takai , Koji Suzuki , Akira Karasawa
IPC分类号： A61K3138
CPC分类号： C07D495/04 , C07D313/12 , C07D337/12
摘要： The present invention provides tricyclic compounds which are useful for the treatment of pollakiuria and urinary incontinence and which are represented by general formula (I): (wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, etc.; X1—X2—X3 represents CR5═CR6—CR7═CR8 (wherein R5, R6, R7 and R8, which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, hydroxy, substituted or unsubstituted lower alkoxy, etc.), N(O)m═CR5—CR6═CR7 (wherein R5, R6 and R7 have the same significances as defined above, and m represents 0 or 1), S—CR7═CR8 (wherein R7 and R8 have the same significances as defined above), etc.; and when R2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, a substituted or unsubstituted N-substituted heterocyclic group, (wherein n is 0 or 1; R3 and R4, which may be the same or different, each represents hydrogen, substituted or unsubstituted lower alkyl, trifluoromethyl, etc., or R3 and R4 may be combined together to form cyclic alkyl; and Q represents hydroxy, halogen, etc.), etc., Y represents —CH2SO2—, —SCH2—, —SOCH2—, —SO2CH2—, etc.) and pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供可用于治疗尿频和尿失禁的三环化合物，其由通式（I）表示：其中R 1表示氢，取代或未取代的低级烷基等; X 1 -X 2 -X 3表示CR 5 = CR6-CR7 = CR8（其中R5，R6，R7和R8可以相同或不同，各自表示氢，取代或未取代的低级烷基，羟基，取代或未取代的低级烷氧基等），N（O）m = CR5-CR6 = CR7（其中R5，R6和R7具有与上述相同的含义，m表示0或1），S-CR 7 = CR 8（其中R 7和R 8具有与上述相同的含义）等 ;当R 2表示氢时，取代或未取代的低级烷基，取代或未取代的低级烷氧基，取代或未取代的N-取代的杂环基，（其中n为0或1; R 3和R 4各自可相同或不同）代表氢，取代或未取代的低级烷基，三氟甲基脲基甲基等，或者R 3和R 4可以组合在一起形成环烷基; 和Q表示羟基，卤素等）等，Y表示-CH 2 SO 2 - ， - CH 2 - ， - SOCH 2 - ， - SO 2 CH 2 - 等）及其药学上可接受的盐。

10. 发明授权

US06150355A Phenylpiperidine derivative 失效
标题翻译：苯基哌啶衍生物
公开(公告)号：US06150355A
公开(公告)日：2000-11-21
申请号：US43154
申请日：1998-03-13
申请人： Toshiaki Kumazawa , Hirokazu Koshimura , Shigeru Aono , Shunji Ichikawa , Shigeto Kitamura
发明人： Toshiaki Kumazawa , Hirokazu Koshimura , Shigeru Aono , Shunji Ichikawa , Shigeto Kitamura
IPC分类号： C07D211/52 , C07D401/04 , C07D405/04 , C07D491/04 , C07D491/044 , C07D211/06 , A01N43/42 , A01N43/46 , C07D221/06 , C07D498/00
CPC分类号： C07D401/04 , C07D211/52 , C07D405/04 , C07D491/04
摘要： A phenylpiperidine derivative or pharmaceutical acceptable salt thereof represented by formula (I): ##STR1## wherein X represents CH or N; Y--Z represents CH.sub.2 --O, CH.sub.2 --S, CH.sub.2 --CH.sub.2, CH.dbd.CH or CONR.sup.5 (wherein R.sup.5 represents hydrogen or lower alkyl); R.sup.1 represents hydrogen, lower alkyl, halogen, lower alkoxy or trifluoromethyl; and R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen, lower alkyl or QR.sup.6 (wherein Q represents a single bond or lower alkylene, and R.sup.6 represents hydroxy, lower alkoxyalkoxy, lower alkoxy, lower alkylthio, nitro, halogen, lower alkanoyloxy, lower alkoxycarbonyl, lower alkanoyl or carboxyl).The present invention provides novel phenylpiperidine derivatives useful as analgesics.
摘要翻译： PCT No.PCT / JP96 / 02589 Sec。 371日期1998年3月13日 102（e）1998年3月13日PCT PCT 1996年9月11日PCT公布。公开号WO97 / 10213 日期：1997年3月20日由式（I）表示的苯基哌啶衍生物或其药学上可接受的盐：其中X表示CH或N; Y-Z表示CH 2 -O，CH 2 -S，CH 2 -CH 2，CH = CH或CONR 5（其中R 5表示氢或低级烷基）。 R 1表示氢，低级烷基，卤素，低级烷氧基或三氟甲基; 并且R 2，R 3和R 4相同或不同，各自表示氢，低级烷基或QR6（其中Q表示单键或低级亚烷基，R6表示羟基，低级烷氧基烷氧基，低级烷氧基，低级烷硫基，硝基，卤素，低级烷酰氧基，低级烷氧基羰基，低级烷酰基或羧基）。本发明提供了用作止痛剂的新型苯基哌啶衍生物。

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