公开(公告)号：US3689492A

公开(公告)日：1972-09-05

申请号：US3689492D

申请日：1970-12-03

Applicant: HANS DETLEF SCHROEDER ,  HERBERT MERZ ,  ADOLF LANGBEIN ,  KURT FRETER ,  ZEILE KARL ,  PETER DANNEBERG ,  ROLF GIESEMANN ,  HELMUT WICK

Inventor： SCHROEDER HANS-DETLEF ,  MERZ HERBERT ,  LANGBEIN ADOLF ,  FRETER KURT

IPC: A61K31/00 ,  C07D211/32 ,  C07D29/20

CPC classification number: A61K31/00 ,  C07D211/32 ,  Y10S514/96

Abstract: Compound of the formula

AND NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, USEFUL AS ANALGESICS IN WARM-BLOODED ANIMALS.

Abstract translation: 化学式和非毒性，药理学上可接受的酸添加量，作为温血动物中的有用的有用的。

公开(公告)号：US4180573A

公开(公告)日：1979-12-25

申请号：US924149

申请日：1978-07-13

Applicant: Karl-Heinz Weber ,  Adolf Langbein ,  Claus Schneider ,  Erich Lehr ,  Karin Boke ,  Franz J. Kuhn

Inventor： Karl-Heinz Weber ,  Adolf Langbein ,  Claus Schneider ,  Erich Lehr ,  Karin Boke ,  Franz J. Kuhn

IPC: A61K31/55 ,  A61K31/5517 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D495/14 ,  A61K31/495 ,  C07D295/08 ,  C07D295/16

CPC classification number: C07D495/14

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, di(lower alkyl)amino-lower alkyl, phenyl, tolyl, methoxy-phenyl, nitro-phenyl, halo-phenyl, pyridyl, pyrimidinyl or --CO--R.sub.4, where R.sub.4 is hydrogen, alkyl or 1 to 17 carbon atoms, alkoxy of 1 to 2 carbon atoms, phenyl, tolyl, methoxy-phenyl, halo-phenyl, nitro-phenyl or pyridyl;R.sub.2 is hydrogen, fluorine, chlorine, or bromine; andR.sub.3 is chlorine, bromine or lower alkyl,and non-toxic, pharmacologically acceptable acid addition salts of certain of these compounds. The compounds as well as the salts are useful as anxiolytics, tranquilizers, sedatives or neuroleptics.

Abstract translation: 其中R 1为氢，低级烷基，卤代低级烷基，羟基 - 低级烷基，二（低级烷基）氨基 - 低级烷基，苯基，甲苯基，甲氧基 - 苯基，硝基 - 苯基，卤代苯基 ，吡啶基，嘧啶基或-CO-R 4，其中R 4是氢，烷基或1至17个碳原子，1至2个碳原子的烷氧基，苯基，甲苯基，甲氧基 - 苯基，卤代 - 苯基，硝基 - 苯基或吡啶基; R2是氢，氟，氯或溴; 并且R 3是氯，溴或低级烷基，以及这些化合物中某些化合物的无毒的，药学上可接受的酸加成盐。 化合物以及盐类可用作抗焦虑剂，止痛剂，镇静剂或精神安定药。

公开(公告)号：US4145427A

公开(公告)日：1979-03-20

申请号：US896575

申请日：1978-04-14

Applicant: Adolf Langbein ,  Karl-Heinz Weber ,  Karin Boke

Inventor： Adolf Langbein ,  Karl-Heinz Weber ,  Karin Boke

IPC: C07D211/58 ,  A61K31/18 ,  A61K31/44 ,  C07D211/96

CPC classification number: C07D211/58

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 6 carbon atoms, phenyl, substituted phenyl or heteroaryl; R.sub.2 is hydrogen or alkyl; and R.sub.3 is hydrogen, methyl, methoxy or halogen; And non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as neuroleptics.

公开(公告)号：US4010164A

公开(公告)日：1977-03-01

申请号：US599427

申请日：1975-07-28

Applicant: Adolf Langbein ,  Herbert Merz ,  Gerhard Walther ,  Klaus Stockhaus

Inventor： Adolf Langbein ,  Herbert Merz ,  Gerhard Walther ,  Klaus Stockhaus

IPC: A61K31/33 ,  C07D405/06

CPC classification number: C07D405/06 ,  A61K31/33 ,  Y10S514/823

Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or methyl, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as morphine-antagonists and analgesics.

Abstract translation: 其中R为氢或甲基的式“IMAGE”化合物及其无毒的药学上可接受的酸加成盐; 化合物及其盐可用作吗啡拮抗剂和镇痛药。

公开(公告)号：US3982005A

公开(公告)日：1976-09-21

申请号：US600374

申请日：1975-07-30

Applicant: Herbert Merz ,  Adolf Langbein ,  Gerhard Walther ,  Klaus Stockhaus

Inventor： Herbert Merz ,  Adolf Langbein ,  Gerhard Walther ,  Klaus Stockhaus

IPC: C07D221/26 ,  A61K31/435 ,  A61K31/445 ,  A61K31/485 ,  A61P25/04 ,  C07D307/14 ,  C07D405/06

CPC classification number: C07D405/06 ,  A61K31/445

Abstract: Compounds of the formula ##SPC1##Wherein R.sub.1 is methyl or phenyl, andR.sub.2 is hydrogen, methyl or acetyl, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as analgesics.

Abstract translation: 式WHEREIN R1的化合物是甲基或苯基，R 2是氢，甲基或乙酰基，以及无毒的，药学上可接受的酸加成盐; 化合物以及盐可用作止痛剂。

公开(公告)号：US3981874A

公开(公告)日：1976-09-21

申请号：US514474

申请日：1974-10-15

Applicant: Herbert Merz ,  Adolf Langbein ,  Gerhard Walther ,  Klaus Stockhaus

Inventor： Herbert Merz ,  Adolf Langbein ,  Gerhard Walther ,  Klaus Stockhaus

IPC: C07D221/26 ,  A61K31/395 ,  A61K31/435 ,  A61K31/485 ,  A61P25/04 ,  C07D221/28 ,  C07D295/00 ,  C07D405/06

CPC classification number: A61K31/395

Abstract: Compound of the formula ##SPC1##WhereinR.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 3 carbon atoms,R.sub.3 is hydrogen or methyl,R.sub.4 is ##SPC2##R.sub.5 is hydrogen, methyl or acetyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics.

Abstract translation: 可以相同或不同的式WHEREIN R 1和R 2的化合物各自为氢或1至3个碳原子的烷基，R 3为氢或甲基，R 4为R 5为氢，甲基或乙酰基，且NON - 药物，药理学上可接受的酸加药盐; 该化合物作为其有效的有效的化学物质。

公开(公告)号：US3975368A

公开(公告)日：1976-08-17

申请号：US620847

申请日：1975-10-08

Applicant: Gerhard Walther ,  Herbert Merz ,  Adolf Langbein ,  Klaus Stockhaus

Inventor： Gerhard Walther ,  Herbert Merz ,  Adolf Langbein ,  Klaus Stockhaus

IPC: A61K31/485

CPC classification number: A61K31/485

Abstract: Pharmaceutical compositions containing as an active ingredient a compound of the formula ##SPC1##WhereinR is hydrogen, methyl or acetyl,R' is hydrogen or methyl, andX is oxygen or sulfur,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as opiate antagonists, analgesics and antitussives.

Abstract translation: 含有式WHEREIN R为氢，甲基或乙酰基的化合物作为活性成分的药物组合物，R'为氢或甲基，X为氧或硫，或非毒性，药理学上可接受的酸添加盐; 以及将其用作临近拮抗剂，方法和抗菌药物的方法。

公开(公告)号：US3933832A

公开(公告)日：1976-01-20

申请号：US497455

申请日：1974-08-14

Applicant: Adolf Langbein ,  Herbert Merz ,  Gerhard Walther ,  Klaus Stockhaus

Inventor： Adolf Langbein ,  Herbert Merz ,  Gerhard Walther ,  Klaus Stockhaus

IPC: C07D401/12 ,  C07D211/58 ,  C07D213/02 ,  C07D213/40

CPC classification number: C07D211/58

Abstract: Compounds of the formula ##SPC1##WhereinR is straight or branched alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 2 carbon atoms or phenyl, andn is an integer from 2 to 4, inclusive,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as non-narcotic analgesics.

Abstract translation: 式WHEREIN R的化合物是1至3个碳原子的直链或支链烷基，1至2个碳原子的烷氧基或苯基，N是2至4的整数，包含和非毒性，药理学上可接受的酸添加物 其中 化合物作为非常有用的非甾体化学物质是有效的。

公开(公告)号：US3931194A

公开(公告)日：1976-01-06

申请号：US367114

申请日：1973-06-05

Applicant: Herbert Merz ,  Adolf Langbein ,  Klaus Stockhaus ,  Helmut Wick

Inventor： Herbert Merz ,  Adolf Langbein ,  Klaus Stockhaus ,  Helmut Wick

IPC: C07D221/26 ,  A61K31/395 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61P11/14 ,  A61P25/04 ,  A61P25/30 ,  C07D405/06 ,  C07D409/06

CPC classification number: A61K31/395 ,  Y10S514/823 ,  Y10S514/849

Abstract: Compounds of the formula ##SPC1##Wherein R is hydrogen, methyl or acetyl,R.sub.1 and R.sub.2, which may be identical to or different from each other, are each alkyl of 1 to 3 carbon atoms,R.sub.3 is hydrogen or methyl, andY is oxygen or sulfur,And non-toxic, pharmacologically acceptable acid addition salts thereof; these compounds as well as the salts are useful as analgesics and antitussives, and opiate antagonists.

Abstract translation: 式WHEREIN R是氢，甲基或乙酰基的化合物，R 1和R 2可以彼此相同或不同，分别为1-3个碳原子的烷基，R3为氢或甲基，Y为氧或硫 ，和非毒性药用植物酸补充品; 这些化合物作为盐作为有用的方法是有用的，并且是有用的，并且是有利的。