公开(公告)号：US4096265A

公开(公告)日：1978-06-20

申请号：US739546

申请日：1976-11-08

申请人： Anil Chandra Ghosh ,  Raj Kumar Razdan

发明人： Anil Chandra Ghosh ,  Raj Kumar Razdan

IPC分类号： C07D491/04 ,  C07D491/052 ,  A61K31/44

CPC分类号： C07D491/04 ,  Y10S514/929

摘要： Benzopyrano[3,4-d]pyridine-2-cyano, carboxamidoximes and carboximidates of the formula ##STR1## wherein R represents -C.ident.N, ##STR2## R.sub.1 is a lower alkyl, R.sub.2 is hydrogen or a lower alkyl and R.sub.3 is a straight or branched alkyl having 1 to 20 carbons, a cycloalkyl-lower alkyl group in which the cycloalkyl group has 3 to 8 carbons or it is an arylalkyl group, and R.sub.4 is a lower alkyl group.The compounds are useful for lowering blood pressure.

摘要翻译： 苯并吡喃并[3,4-d]吡啶-2-氰基，甲酰氨基肟和式ⅩⅧ的肟基，其中R表示-C = N，R 1是低级烷基，R 2是氢或低级烷基，R 3是 碳原子数为1〜20的直链或支链烷基，环烷基为碳原子数为3〜8的环烷基 - 低级烷基或芳基烷基，R4为低级烷基。

公开(公告)号：US4025521A

公开(公告)日：1977-05-24

申请号：US624666

申请日：1975-10-22

申请人： David Edward Portlock

发明人： David Edward Portlock

IPC分类号： A61K31/435 ,  A61P25/04 ,  C07D221/28 ,  C07D489/00

CPC分类号： C07D221/28

摘要： The reaction of thebaine or dihydrothebaine-.phi. with potassium in liquid ammonia respectively in the absence or presence of catalyst yields .beta.-dihydrothebaine.

摘要翻译： 在不存在或存在催化剂的情况下，蒂巴因或二氢本可可碱与液氨中的钾的反应分别产生β-二氢图他那。

公开(公告)号：US3946111A

公开(公告)日：1976-03-23

申请号：US524626

申请日：1974-11-18

申请人： Martin Winn ,  Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Joyce Ruth Krei

发明人： Martin Winn ,  Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Joyce Ruth Krei

IPC分类号： C07D333/38 ,  A61K31/38

CPC分类号： C07D333/38

摘要： 1,2-Dihydro-4H-thieno-[2,3-c][1]benzopyrans of the formulae ##SPC1##Wherein R is a lower alkyl group having 1 to 5 carbons, R.sub.1 is hydrogen or a lower alkyl group having 1 to 5 carbons, R.sub.2 is a lower alkyl group and R.sub.3 is an alkyl group having 1 to 20 carbon atoms, a phenyl-lower alkyl group or a cycloalkyl-lower alkyl group. The compounds have analgesic, antihypertensive, antidepressant, anticonvulsant, antianxiety, sedative-hypnotic and/or tranquilization activity.

摘要翻译： 1,2-二氢-4H-噻吩并[2,3-c] [1]苯并吡喃，式WHEREIN R是具有1至5个碳的低级烷基，R 1是氢或具有1至5个碳的低级烷基 R2为低级烷基，R3为碳原子数1〜20的烷基，苯基 - 低级烷基或环烷基 - 低级烷基。 该化合物具有镇痛，抗高血压，抗抑郁，抗惊厥，抗焦虑，镇静催眠和/或镇静作用。

公开(公告)号：US4051152A

公开(公告)日：1977-09-27

申请号：US647050

申请日：1976-01-07

申请人： Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Patricia Herlihy

发明人： Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Patricia Herlihy

IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P25/04 ,  A61P25/20 ,  C07D311/80 ,  C07D311/94 ,  C07D307/83

CPC分类号： C07D311/94 ,  C07D311/80

摘要： Benzopyrans of the formula ##STR1## wherein n represents 0 or 1, R is an alkyl group having 1 to 20 carbon atoms, an aryl-lower alkyl group or a cycloalkyl-lower alkyl group, R.sub.1 is hydrogen or ##STR2## wherein R.sub.4 is lower alkyl, phenyl, cycloalkyl-lower alkyl or aryl-lower alkyl, R.sub.2 is a lower alkyl and R.sub.3 is hydrogen or one or two lower alkyl groups, pharmaceutical compositions containing the compounds, and uses of the compounds as tranquilizers and analgesics.

摘要翻译： 其中n表示0或1，R是具有1至20个碳原子的烷基，芳基 - 低级烷基或环烷基 - 低级烷基，R 1是氢或其中R 4是 低级烷基，苯基，环烷基 - 低级烷基或芳基 - 低级烷基，R2是低级烷基，R3是氢或一个或两个低级烷基，含有该化合物的药物组合物，以及该化合物作为镇定剂和止痛剂的用途。

公开(公告)号：US4020163A

公开(公告)日：1977-04-26

申请号：US594713

申请日：1975-07-10

申请人： Louis Selig Harris ,  Harry George Pars ,  Raj Kumar Razdan ,  John Clark Sheehan ,  Barbara Zitko Terris

发明人： Louis Selig Harris ,  Harry George Pars ,  Raj Kumar Razdan ,  John Clark Sheehan ,  Barbara Zitko Terris

IPC分类号： A61K31/44 ,  A61K31/445 ,  A61K31/535 ,  A61K31/54

CPC分类号： A61K31/44

摘要： Heterocyclic esters of 1,4-ethano-1,2,3,4-tetrahydro-5H-[1]benzopyrano[3,4-b]pyridines and 1,4-ethano-1,2,3,4,13,14-hexahydro-5H-[1]benzopyrano[3,4-b]pyridines. The esters have the formulas ##STR1## wherein R.sub.2 is lower alkyl, R.sub.3 is an alkyl having one to twenty carbon atoms, a cycloalkyl-lower alkyl or a phenyl-lower alkyl, Y is a straight or branched chain alkylene having one to eight carbon atoms, and R.sub.4 is a group of the formula ##STR2## wherein a is an integer from 1 to 4, b is an integer from 1 to 4 and X is CH.sub.2, O, S or N--R.sub.5 with R.sub.5 being hydrogen or lower alkyl, and R.sub.6 is hydrogen or a lower alkyl group bonded to a carbon in the ring.The compounds have pharmacological activity, including analgesic, anti-convulsive and tranquilizing activity in animals. The compounds can be administered in pharmaceutical composition form.

摘要翻译： 1,4-亚磺酰-1,2,3,4-四氢-5H- [1]苯并吡喃并[3,4-b]吡啶和1,4-亚磺酰基-1,2,3,4,13， 14-六氢-5H- [1]苯并吡喃并[3,4-b]吡啶。 酯具有下式：其中R 2是低级烷基，R 3是具有1-20个碳原子的烷基，环烷基 - 低级烷基或苯基 - 低级烷基，Y是直链 或具有1-8个碳原子的支链亚烷基，R4是下式的基团：其中a是1至4的整数，b是1至4的整数，X是CH 2，O，S或N -R5，其中R5是氢或低级烷基，R6是氢或与环中的碳键合的低级烷基。

公开(公告)号：US3951970A

公开(公告)日：1976-04-20

申请号：US402481

申请日：1973-10-01

申请人： Raj Kumar Razdan ,  Harry George Pars

发明人： Raj Kumar Razdan ,  Harry George Pars

IPC分类号： C07D295/096 ,  C07D295/08

CPC分类号： C07D295/096

摘要： Compounds of the formula ##SPC1##And acid addition salts thereof, wherein R represents an alkyl group having 1 to 20 carbon atoms, an arylalkyl group, or a cycloalkyl-lower alkyl group, R.sub.1 and R.sub.2 represent hydrogen or the same or different lower alkyl or lower alkanoyl groups; and Z represents --NH.sub.2, --NHR.sub.3, --NR.sub.3 R.sub.4, or ##EQU1## WHERE R.sub.3 is lower alkyl, or phenyl-lower alkyl, R.sub.4 is lower alkyl or phenyl-lower alkyl, m is an integer from 0 to 6, n is an integer from 0 to 6, m + n is an integer from 3 to 6, and X is CH.sub.2, CHR.sub.3, O, S, or NR.sub.3.The compounds have pharmacological activity, including antidepressant and anti-hypertensive activity, in animals.

摘要翻译： 式的化合物及其酸加成盐，其中R表示碳原子数1〜20的烷基，芳烷基或环烷基 - 低级烷基，R 1和R 2表示氢或相同或不同的低级烷基或低级烷酰基 团体 Z表示-NH 2，-NHR 3，-NR 3 R 4或（CH 2）n -NX（CH 2）m，其中R 3为低级烷基或苯基 - 低级烷基，R 4为低级烷基或苯基 - 低级烷基，m为 0〜6，n为0〜6的整数，m + n为3〜6的整数，X为CH 2，CHR 3，O，S或NR 3。

公开(公告)号：US3941782A

公开(公告)日：1976-03-02

申请号：US361897

申请日：1973-05-21

申请人： Louis Selig Harris ,  Harry George Pars ,  Raj Kumar Razdan ,  John Clark Sheehan

发明人： Louis Selig Harris ,  Harry George Pars ,  Raj Kumar Razdan ,  John Clark Sheehan

IPC分类号： C07D295/15 ,  C07D311/80 ,  C07D311/94 ,  C07D311/78

CPC分类号： C07D295/15 ,  C07D311/80 ,  C07D311/94

摘要： This invention relates to novel esters of benzopyrans represented by the formulae ##SPC1##Wherein R and R' are hydrogen or C.sub.1 -C.sub.6 alkyl and when alkyl are on the same or different carbons; R.sub.1 is C.sub.1 -C.sub.6 alkyl; R.sub.2 is C.sub.1 -C.sub.20 alkyl, lowercycloalkyloweralkyl or lowercycloalkyl; n is an integer from 3 to 7, and particularly 3 to 5; Y is a straight or branched chain C.sub.1 -C.sub.8 alkylene; and R.sub.3 is ##EQU1## WHEREIN A IS AN INTEGER FROM 1 TO 4, B IS AN INTEGER FROM 1 TO 4, X is O,S, CH.sub.2 or NR.sub.4 and R.sub.4 is hydrogen C.sub.1 -C.sub.6 alkyl, and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and the acid addition salts thereof. The compounds exhibit analgesic and central nervous system activity.

摘要翻译： 本发明涉及由式WHEREIN R和R'表示的苯并吡喃的新型酯是氢或C 1 -C 6烷基，当烷基在相同或不同的碳上时; R1是C1-C6烷基; R2是C1-C20烷基，低级环烷基低级烷基或低级环烷基; n为3〜7的整数，特别是3〜5的整数。 Y是直链或支链C1-C8亚烷基; 并且R 3是（CH 2）a R 5 | -N角度X（CH 2）b，其中A是从1到4的整数，B是从1到4的整数，X是O，S，CH 2或NR 4，并且R 4是氢C1 -C6烷基，R5为氢或C1-C6烷基; 及其酸加成盐。 该化合物显示镇痛和中枢神经系统活性。

公开(公告)号：US4042694A

公开(公告)日：1977-08-16

申请号：US664907

申请日：1976-03-08

申请人： Louis Selig Harris ,  Harry George Pars ,  John Clark Sheehan ,  Raj Kumar Razdan

发明人： Louis Selig Harris ,  Harry George Pars ,  John Clark Sheehan ,  Raj Kumar Razdan

IPC分类号： C07D211/14 ,  C07D491/052 ,  C07D491/04

CPC分类号： C07D211/14

摘要： Novel heterocyclic esters of benzopyranopyridines represented by the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower alkanoyl, cycloalkyl-lower alkyl, cycloalkyl-lower alkanoyl, lower alkenyl, lower alkynyl, halo-loweralkenyl, phenyl-lower alkyl, phenyl-lower alkenyl or phenyl-lower alkynyl; R.sub.2 is lower alkyl; R.sub.3 is an alkyl having one to twenty carbon atoms or a cycloalkyl-lower alkyl, Y is a straight or branched chain alkylene having one to eight carbon atoms, and R.sub.4 is a group of the formula ##STR2## a is an integer from 1 to 4, b is an integer from 1 to 4 and X is CH.sub.2, O, S or N--R.sub.5 with R.sub.5 being hydrogen or lower alkyl, with the limitation that when X is O, S or N--R.sub.5, a and b each must be 2 and R.sub.6 is hydrogen or a lower alkyl group bonded to a carbon in the ring; and the acid addition salts thereof.

摘要翻译： 其中R 1为氢，低级烷基，低级烷酰基，环烷基 - 低级烷基，环烷基 - 低级烷酰基，低级烯基，低级炔基，卤代低级烯基，苯基 - 低级烷基，苯基 - 低级烷基， 低级烯基或苯基 - 低级炔基; R2是低级烷基; R3是具有1-20个碳原子的烷基或环烷基 - 低级烷基，Y是具有1-8个碳原子的直链或支链亚烷基，R4是下式的基团：a是从1到 4，b为1〜4的整数，X为CH 2，O，S或N-R 5，其中R 5为氢或低级烷基，限制在X为O，S或N-R 5时，a和b各自为 是2，R6是氢或与环中的碳键合的低级烷基; 及其酸加成盐。

公开(公告)号：US4007207A

公开(公告)日：1977-02-08

申请号：US594534

申请日：1975-07-09

申请人： Martin Winn ,  Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Joyce Ruth Krei

发明人： Martin Winn ,  Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Joyce Ruth Krei

IPC分类号： C07D311/78

CPC分类号： Y10S514/96

摘要： 1,2,3,4-Tetrahydrocyclopenta[c][1]benzopyrans of the formulae ##STR1## wherein R is a lower alkyl group having 1 to 5 carbons, R.sub.1 is hydrogen or a lower alkyl group having 1 to 5 carbons, R.sub.2 is a lower alkyl group and R.sub.3 is an alkyl group having 1 to 20 carbon atoms, a phenyl-lower alkyl group or a cycloalkyl-lower alkyl group. The compounds have anti-hypertensive, antidepressant, analgesic, anticonvulsant, anti-anxiety, sedative-hypnotic and tranquilizing activity in animals.

摘要翻译： 其中R为具有1至5个碳原子的低级烷基，R 1为氢或低级烷基，具有1至5个碳原子的低级烷基， 5个碳，R2为低级烷基，R3为碳原子数1〜20的烷基，苯基 - 低级烷基或环烷基 - 低级烷基。 该化合物在动物体内具有抗高血压，抗抑郁，镇痛，抗惊厥，抗焦虑，镇静催眠和镇静作用。

公开(公告)号：US3992550A

公开(公告)日：1976-11-16

申请号：US594533

申请日：1975-07-09

申请人： Martin Winn ,  Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Joyce Ruth Krei

发明人： Martin Winn ,  Raj Kumar Razdan ,  Haldean Cloyce Dalzell ,  Joyce Ruth Krei

IPC分类号： A61K31/335

摘要： 1,2,3,4-Tetrahydrocyclopenta[c] [1]benzopyrans of the formulae ##SPC1##Wherein R is a lower alkyl group having 1 to 5 carbons, R.sub.1 is hydrogen or a lower alkyl group having 1 to 5 carbons, R.sub.2 is a lower alkyl group and R.sub.3 is an alkyl group having 1 to 20 carbon atoms, a phenyl-lower alkyl group or a cycloalkyl-lower alkyl group. The compounds have anti-hypertensive, antidepressant, analgesic, anticonvulsant, anti-anxiety and tranquilizing activity in animals.

摘要翻译： 1,2,3,4-四氢环戊二烯并[c] [1]苯并吡喃，式为WHEREIN R为碳原子数1〜5的低级烷基，R1为氢或碳原子数为1〜5的低级烷基，R2为低级 烷基，R 3为碳原子数1〜20的烷基，苯基 - 低级烷基或环烷基 - 低级烷基。 该化合物在动物中具有抗高血压，抗抑郁，止痛，抗惊厥，抗焦虑和镇静作用。