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1. 发明授权

US3864330A Benzodiazepine derivatives and production thereof 失效
标题翻译：苯并二氮杂衍生物及其制备
公开(公告)号：US3864330A
公开(公告)日：1975-02-04
申请号：US28201272
申请日：1972-08-21
申请人： SUMITOMO CHEMICAL CO
发明人： KATSUBE JUNKI , TAKASHIMA YOSHINORI , HIROHASHI TOSHIYUKI , ISHIZUMI KIKUO , AKATSU MITSUHIRO , MORI KAZUO , KATSUKI ISAO , KUME YOSHIHARU , SATO HIROMI , INABA SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D243/24 , C07D243/26 , C07D53/06
CPC分类号： C07D243/24
摘要： The present invention relates to 1,4-benzodiazepine derivatives represented by the general formula:

D R A W I N G
(WHEREIN EACH OF R6 and R7 represents hydrogen, C1 - C6 alkyl, C2 - C6 alkenyl or alkynyl, C3 - C6 cycloalkyl- C1 - C4 alkyl, substituted or unsubstituted hydroxy, substituted or unsubstituted hydroxy- C1 - C4 alkyl, or substituted or unsubstituted amino, or substituted or unsubstituted amino- C1 - C4 alkyl group), -CN, -R8 (wherein R8 represents C1 - C10 alkyl, or C1 - C4 alkoxyC1- C4 alkyl group), -OCH2-R9 (wherein R9 represents hydrogen, C1 - C6 alkyl, C2 - C6 alkenyl or alkynyl, phenyl, or phenyl- C1 - C4 alkyl group), OR -C*C-R10 (wherein R10 represents hydrogen, or C1 - C6 alkyl groups which may be substituted by a secondary amino group or by a substituted or unsubstituted hydroxy group).

WHEREIN R1 is a member selected from the group consisting of hydrogen, halogen, nitro, and trifluoromethyl group, R2 represents a member selected from the group consisting of hydrogen, C1 - C6 alkyl, C2 - C6 alkenyl or alkynyl, C3 - C6 cycloalkyl- C1 - C4 alkyl, and substituted or unsubstituted hydroxy- C1 - C4 alkyl group, R3 represents alkyl group having 1 - 4 carbon atoms, EACH OF R4 and R5 represents a member selected from the group consisting of hydrogen, halogen, C1 - C4 alkyl, and trifluoromethyl group, AND Z represents
摘要翻译：本发明涉及由以下通式表示的1,4-苯并二氮杂衍生物：其中R 1为选自氢，卤素，硝基和三氟甲基的成员，R 2表示选自氢， C 1 -C 6烷基，C 2 -C 6烯基或炔基，C 3 -C 6环烷基-C 1 -C 4烷基和取代或未取代的羟基-C 1 -C 4烷基，R 3表示具有1-4个碳原子的烷基，每个R 4和R 5 表示选自氢，卤素，C 1 -C 4烷基和三氟甲基的成员，Z表示（其中R 6和R 7各自表示氢，C 1 -C 6烷基，C 2 -C 6烯基或炔基，C 3 -C 6 环烷基-C 1 -C 4烷基，取代或未取代的羟基，取代或未取代的羟基-C 1 -C 4烷基或取代或未取代的氨基，或取代或未取代的氨基-C 1 -C 4烷基），-CN，-R 8（其中R 8表示 C1-C10烷基，或 C 1 -C 4烷氧基-C 1 -C 4烷基），-OCH 2 -R 9（其中R 9表示氢，C 1 -C 6烷基，C 2 -C 6烯基或炔基，苯基或苯基-C 1 -C 4烷基），OR -C 3 C-R 10（其中R 10表示氢，或可被仲氨基取代或被取代或未取代的羟基取代的C 1 -C 6烷基）。

2. 发明授权

US3906003A Benzodiazepine derivatives and preparation thereof 失效
标题翻译：苯并二氮杂衍生物及其制备
公开(公告)号：US3906003A
公开(公告)日：1975-09-16
申请号：US19469071
申请日：1971-11-01
申请人： SUMITOMO CHEMICAL CO
发明人： AKATSU MITSUHIRO , KUME YOSHIHARU , HIROHASHI TOSHIYUKI , INABA SHIGEHO , YAMAMOTO HISAO , SATO HIROMI
IPC分类号： C07D243/24 , C07D243/26 , C07D243/28 , C07D243/30 , C07D405/06 , C07D53/06
CPC分类号： C07D243/24 , C07D243/26 , C07D243/28 , C07D243/30 , C07D243/36 , C07D405/06
摘要： Novel benzodiazepines having valuable pharmaceutical properties, which are represented by the formula

WHEREIN R1 represents hydrogen, halogen, nitro or trifluoromethyl; R2 represents pyridyl, cyclohexenyl or a group of the formula

(IN WHICH R7 and R8 each represent hydrogen, halogen, lower alkyl or trifluoromethyl); R3 represents hydrogen, lower alkyl, aryl or aralkyl; R4 represents hydroxy, lower alkoxy or acyloxy; R5 represents hydrogen, hydroxy or acyloxy, provided that R4 and R5 are not hydroxy group simultaneously; or R4 and R5 together may be joined to form a group of the formula,

(in which R9 and R10 each represents hydrogen, lower alkyl, lower alkenyl, aryl, aralkyl, cycloalkyl or cycloalkylalkyl; R11 represents hydrogen, lower alkyl or halogen; and B represents oxygen or sulfur); R6 represents hydrogen, cyano, acyloxy, alkoxycarbonyl or a group of the formula,

(in which R12 and R13 each represent hydrogen or lower alkyl, or R12 and R13 may form an optionally substituted 5- or 6-membered heterocyclic ring together with the adjacent nitrogen atom, and said heterocyclic ring may further contain one or more hetero atom; R14 represents hydrogen, acyl, lower alkyl, lower alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, polyhaloalkyl or cyanoalkyl; A represents oxygen, sulfur, sulfinyl or sulfonyl; and p represents 0 or 1); l represents 0 or 1; m represents 0, 1, 2 or 3; and n represents 1, 2, 3 or 4.
摘要翻译：具有有价值药物性质的新型苯并二氮杂由式R4R5表示| CnH2n-CH-CH-CmH2m-R6 | O并行N-C（I）角度CH-R3 C = N |＆Darr＆R2（O）l 其中R1表示氢，卤素，硝基或三氟甲基; R 2表示吡啶基，环己烯基或式[基团，其中R 7和R 8各自表示氢，卤素，低级烷基或三氟甲基]; R3表示氢，低级烷基，芳基或芳烷基; R4表示羟基，低级烷氧基或酰氧基; R5表示氢，羟基或酰氧基，条件是R4和R5不同时为羟基; 或R 4和R 5一起可以连接形成下式基团：R9R10 R9R10 || ANGLE C ANGLE CH-CH || OO，OO || || B或PARALLEL CO角度角OO角度角O [其中R9和 R 10各自表示氢，低级烷基，低级烯基，芳基，芳烷基，环烷基或环烷基烷基; R 11表示氢，低级烷基或卤素; B代表氧或硫]; R 12表示氢，氰基，酰氧基，烷氧基羰基或下式基团：R 12 R 12 -N ANGLE，-CO-N ANGLE或 - （A）p -R 14 R 13 R 13 [其中R 12和R 13各自表示氢或低级烷基，或R 12和R 13可以与相邻的氮原子一起形成任选取代的5元或6元杂环，并且所述杂环可以进一步含有一个或多个杂原子; R14代表氢，酰基，低级烷基，低级烯基，环烷基，环烷基烷基，芳基，芳烷基，多卤代烷基或氰基烷基; A代表氧，硫，亚磺酰基或磺酰基; 和p代表0或1]; l表示0或1; m表示0,1,2或3; n表示1,2,3或4。

3. 发明专利

CH622763A5 Process for the preparation of 9-formyl-9,10-dihydro-9,10-methanoanthracene 未知
公开(公告)号：CH622763A5
公开(公告)日：1981-04-30
申请号：CH10980
申请日：1980-01-08
申请人： SUMITOMO CHEMICAL CO
发明人： SUNAGAWA MAKOTO , SATO HIROMI , KATSUBE JUNKI , YAMAMOTO HISAO
IPC分类号： C07C47/235 , C07C47/238 , C07C47/453 , C07C57/50 , C07C61/39 , C07D295/02 , C07D295/03 , C07D295/125 , C07C45/51
摘要： 9-Formyl-9,10-dihydro-9,10-methanoanthracene of the formula is prepared from 9-amino-12-hydroxy-9,10-dihydro-9,10-ethanoanthracene of the formula by treatment with nitrous acid or with a metal nitrite in an acidic medium. As an intermediate, the compound is of prime importance in the synthesis of therapeutically valuable 9-aminoalkyl derivatives of 9,10-dihydro-9,10-methanoanthracene. The starting material A is prepared from a 9-carboxy-12-(hydroxy or R'O)-9,10-dihydro-9,10-ethanoanthracene, where R' denotes a protective group, by Curtius or Hoffmann degradation and, in the case of R'O, hydrolytic elimination of the protective group.

4. 发明专利

NO143153C 未知
公开(公告)号：NO143153C
公开(公告)日：1980-12-29
申请号：NO754237
申请日：1975-12-12
申请人： SUMITOMO CHEMICAL CO
发明人： SUNAGAWA MAKOTO , SATO HIROMI , KATSUBE JUNKI , YAMAMOTO HISAO
IPC分类号： C07C20060101 , C07C87/06

5. 发明专利

CA1060015A MORPHOLINE DERIVATIVES AND PRODUCTION THEREOF 未知
公开(公告)号：CA1060015A
公开(公告)日：1979-08-07
申请号：CA256337
申请日：1976-07-06
申请人： SUMITOMO CHEMICAL CO
发明人： SUNAGAWA MAKOTO , SATO HIROMI , KATSUBE JUNKI , YAMAMOTO HISAO
IPC分类号： C07C1/22 , C07C47/453 , C07C57/50 , C07D265/30 , C07D265/32 , C07D303/04
摘要： NOVEL MORPHOLINE DERIVATIVES AND PRODUCTION THEREOF Novel morpholine compounds of the formula: wherein R1 represents hydrogen, C1-C4 alkyl, C3-C5 alkenyl, aryl(C1-C4)alkyl or (C3-C6)cycloalkyl(C1-C4)alkyl and n represents 1 or 2, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

6. 发明专利

FI54312C 未知
公开(公告)号：FI54312C
公开(公告)日：1978-11-10
申请号：FI136973
申请日：1973-04-27
申请人： SUMITOMO CHEMICAL CO
发明人： HIROHSHI TOSHIYUKI , SATO HIROMI , INABA SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D333/36 , C07D333/66 , C07D495/04
摘要： 1397501 Thienopyrimidines SUMITOMO CHEMICAL CO Ltd 7 May 1973 [9 May 1972 3 July 1972 26 July 1972 9 Dec 1972 14 Dec 1972] 21647/73 Heading C2C Novel compounds (I), (II), (III) and (IV) wherein D is a hydrogen atom, an alkyl group or a group of the formula R 1 is a hydrogen atom, an alkyl group, an alkoxy group, a nitro group, a trifluoromethyl group, an alkylthio group, an alkylsulfonyl group, a halogen atom or R 1 and R 2 may together from a trimethylene, tetramethylene or pentamethylene group; R 2 and R 3 are independently a hydrogen atom, an alkyl group, an alkoxy group, a nitro group, a trifluoromethyl group, an alkylthio group, an alkylsulfonyl group or a halogen atom; R is a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an alkoxyalkyl group, a cycloalkylalkyl group, a haloalkyl group, an alkylthioalkyl group, an alkoxycarbonylalkyl group, an alkanoyloxyalkyl group, or a group of the formula (wherein A is an alkylene group ; R 4 , R 5 , R 6 and R 7 are independently a hydrogen atom or an alkyl group, which may form together with the adjacent nitrogen atom an unsubstituted or optionally substituted 5- or 6-membered heterocyclic ring, which may further contain a hetero atom, are made by standard methods, especially by cyclizing compounds (IV) (W is oxygen or imino) or by halogenation, nitration and alkylation of appropriate thieno-pyrimidines; (IV) are themselves prepared by hydrolysing the corresponding N-methylacetamido-compounds (obtained from the corresponding acetamidocompounds). Pharmaceutical preparations having antiinflammatory, analgesic, antiviral, uricosuric, diuretic and CNS actions contain (I), (II) and/or (III) as active ingredient; administration is orally or parenterally.

7. 发明专利

NO138599B 未知
公开(公告)号：NO138599B
公开(公告)日：1978-06-26
申请号：NO190373
申请日：1973-05-08
申请人： SUMITOMO CHEMICAL CO
发明人： HIROHASHI TOSHIYUKI , SATO HIROMI , INABA SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D333/36 , C07D333/66 , C07D495/04
摘要： 1397501 Thienopyrimidines SUMITOMO CHEMICAL CO Ltd 7 May 1973 [9 May 1972 3 July 1972 26 July 1972 9 Dec 1972 14 Dec 1972] 21647/73 Heading C2C Novel compounds (I), (II), (III) and (IV) wherein D is a hydrogen atom, an alkyl group or a group of the formula R 1 is a hydrogen atom, an alkyl group, an alkoxy group, a nitro group, a trifluoromethyl group, an alkylthio group, an alkylsulfonyl group, a halogen atom or R 1 and R 2 may together from a trimethylene, tetramethylene or pentamethylene group; R 2 and R 3 are independently a hydrogen atom, an alkyl group, an alkoxy group, a nitro group, a trifluoromethyl group, an alkylthio group, an alkylsulfonyl group or a halogen atom; R is a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an alkoxyalkyl group, a cycloalkylalkyl group, a haloalkyl group, an alkylthioalkyl group, an alkoxycarbonylalkyl group, an alkanoyloxyalkyl group, or a group of the formula (wherein A is an alkylene group ; R 4 , R 5 , R 6 and R 7 are independently a hydrogen atom or an alkyl group, which may form together with the adjacent nitrogen atom an unsubstituted or optionally substituted 5- or 6-membered heterocyclic ring, which may further contain a hetero atom, are made by standard methods, especially by cyclizing compounds (IV) (W is oxygen or imino) or by halogenation, nitration and alkylation of appropriate thieno-pyrimidines; (IV) are themselves prepared by hydrolysing the corresponding N-methylacetamido-compounds (obtained from the corresponding acetamidocompounds). Pharmaceutical preparations having antiinflammatory, analgesic, antiviral, uricosuric, diuretic and CNS actions contain (I), (II) and/or (III) as active ingredient; administration is orally or parenterally.

8. 发明专利

CA1010033A BENZODIAZEPINE DERIVATIVES AND PREPARATION THEREOF 未知
公开(公告)号：CA1010033A
公开(公告)日：1977-05-10
申请号：CA125391
申请日：1971-10-18
申请人： SUMITOMO CHEMICAL CO
发明人： AKATSU MITSUHIRO , KUME YOSHIHARU , HIROHASHI TOSHIYUKI , ISHIZUMI KIKUO , YAMAMOTO MICHIHIRO , MARUYAMA ISAMU , MORI KAZUO , IZUMI TAKAHIRO , INABA SHIGEHO , YAMAMOTO HISAO , SATO HIROMI
IPC分类号： C07D243/24 , C07D243/26 , C07D243/28 , C07D243/30 , C07D405/06
摘要： Novel benzodiazepines having valuable pharmaceutical properties, which are represented by the formula R4R5 ¦¦ CnH2n-CH-CH-CmH2m-R6 ¦O PARALLEL N--C (I) ANGLE ANGLE CH-R3 C=N ¦ &darr& R2(O)l WHEREIN R1 represents hydrogen, halogen, nitro or trifluoromethyl; R2 represents pyridyl, cyclohexenyl or a group of the formula [IN WHICH R7 and R8 each represent hydrogen, halogen, lower alkyl or trifluoromethyl]; R3 represents hydrogen, lower alkyl, aryl or aralkyl; R4 represents hydroxy, lower alkoxy or acyloxy; R5 represents hydrogen, hydroxy or acyloxy, provided that R4 and R5 are not hydroxy group simultaneously; or R4 and R5 together may be joined to form a group of the formula, R9R10 R9R10 ¦¦ ANGLE C ANGLE CH-CH ¦¦ OO, OO ¦¦ ¦¦ B or PARALLEL C O ANGLE ANGLE O O ANGLE ANGLE O [in which R9 and R10 each represents hydrogen, lower alkyl, lower alkenyl, aryl, aralkyl, cycloalkyl or cycloalkylalkyl; R11 represents hydrogen, lower alkyl or halogen; and B represents oxygen or sulfur]; R6 represents hydrogen, cyano, acyloxy, alkoxycarbonyl or a group of the formula, R12 R12 -N ANGLE , -CO-N ANGLE or-(A)p-R14 R13 R13 [in which R12 and R13 each represent hydrogen or lower alkyl, or R12 and R13 may form an optionally substituted 5- or 6-membered heterocyclic ring together with the adjacent nitrogen atom, and said heterocyclic ring may further contain one or more hetero atom; R14 represents hydrogen, acyl, lower alkyl, lower alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, polyhaloalkyl or cyanoalkyl; A represents oxygen, sulfur, sulfinyl or sulfonyl; and p represents 0 or 1]; l represents 0 or 1; m represents 0, 1, 2 or 3; and n represents 1, 2, 3 or 4.

9. 发明专利

CA976158A BENZODIAZEPINE DERIVATIVES AND PRODUCTION THEREOF 未知
公开(公告)号：CA976158A
公开(公告)日：1975-10-14
申请号：CA150714
申请日：1972-08-31
申请人： SUMITOMO CHEMICAL CO
发明人： KATSUBE JUNKI , AKATSU MITSUHIRO , TAKASHIMA YOSHINORI , KATSUKI ISAO , HIROHASHI TOSHIYUKI , ISHIZUMI KIKUO , MORI KAZUO , KUME YOSHIHARU , SATO HIROMI , INABO SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D243/24 , C07D243/26

10. 发明专利

CA950904A PROCESS FOR PRODUCING BENZODIAZEPINE DERIVATIVES 未知
公开(公告)号：CA950904A
公开(公告)日：1974-07-09
申请号：CA122106
申请日：1971-09-03
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO HISAO , AKASE TAKESHI , INABA SHIGEHO , IZUMI TAKAHIRO , SATO HIROMI , KUME YOSHIHARU , OKAMOTO TADASHI , HIROHASHI TOSHIYUKI , ISHIZUMI KIKUO , AKATSU MITSUHIRO , YAMAMOTO MICHIHIRO , MARUYAMA ISAMU , KOBAYSAHI TSUYOSHI , MORI KAZUO
IPC分类号： C07D209/04 , C07D241/08 , C07D487/04 , C07D243/16

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