公开(公告)号：US3694456A

公开(公告)日：1972-09-26

申请号：US3694456D

申请日：1970-05-08

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： NOGUCHI SHUNSAKU ,  KISHIMOTO SHOJI ,  KAWAI KIYOHISA

IPC: C07D231/12 ,  C07D49/20

CPC classification number: C07D231/12 ,  Y10S514/906 ,  Y10S514/916

Abstract: 1-(Disubstituted-amino)pyrazole compounds are provided herein of the formula: WHEREIN EACH OF R1 and R2 stands for lower alkyl or R1 and R2, taken together with the adjacent N-atom form morpholino, piperidino, pyrrolidino, N-methylpiperazino, N-benzylpiperazino and N-phenylpiperazino, R''s, which are the same or different from each other, stand for hydrogen, alkyl having one to ten carbon atoms, phenyl, naphthyl, phenyl or naphthyl substituted by halogen or lower alkyl, respectively, and R3 stands for hydrogen, lower alkyl, N,N-di-loweralkylaminoethyl, N-morpholinomethyl, Npiperidinomethyl, N-pyrrolidinomethyl, N-methylpiperazinomethyl, N-benzylpiperazinomethyl and N-phenylpiperazinomethyl. The above compounds as well as the pharmaceutically acceptable salts thereof are useful as analgesics, antipyretics and mild muscle relaxants.

Abstract translation: 本文提供下式的1-（二取代 - 氨基）吡唑化合物：

公开(公告)号：US3886207A

公开(公告)日：1975-05-27

申请号：US37152773

申请日：1973-06-19

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： KISHIMOTO SHOJI ,  AONO TETSUYA ,  NOGUCHI SHUNSAKU

IPC: C07C61/39 ,  C07C51/00 ,  C07C61/12 ,  C07C61/40 ,  C07C67/00 ,  C07C69/753 ,  C07C233/58 ,  C07C63/44

CPC classification number: C07C61/12 ,  Y10S514/916

Abstract: 5-Cycloalkyl-6-halogenoindan-1-carboxylic acid (cycloalkyl group herein is six- or five-membered one) is produced through halogenation of indan-1-carboxylic acid to introduce halogen at its 6-position selectively, and following alkylation to introduce cycloalkyl group at the 5-position. The latter reaction is effectively conducted by acting on 6-halogenoindan-1-carboxylic acid a cycloalkyhalide, a cycloalkanol, its sulfonates or a cycloalkene. The product may be converted into the form of its pharmaceutically acceptable salts. The products are useful as antipyretic, analgesic or anti-inflammatory agent for human or animal use.

Abstract translation: 5-环烷基-6-卤代茚满-1-羧酸（本文环烷基是六或五元一个）是通过茚满-1-羧酸的卤化反应制备的，以在其6-位选择性地引入卤素，并在烷基化至 在5位引入环烷基。 后一反应通过作用于6-卤代茚满-1-羧酸环烷基卤化物，环烷醇，其磺酸盐或环烯烃而有效地进行。 产物可以转化为其药学上可接受的盐的形式。 该产品可用作人或动物使用的解热止痛剂或抗炎剂。

公开(公告)号：US3704241A

公开(公告)日：1972-11-28

申请号：US3704241D

申请日：1970-11-17

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： NOGUCHI SHUNSAKU ,  KISHIMOTO SHOJI

IPC: C07D231/12 ,  C07D49/18

CPC classification number: C07D231/12 ,  Y10S514/87

Abstract: 4-PYRAZOLE ACETIC ACID OR ESTERS THEREOF OF THE FORMULA:

R1-NHNH2 (III)SP@ WHEREIN R1 HAS THE SAME MEANING AS ABOVE, AND, IF DESIRED, HYDROLYZING THE THUS OBTAINED COMPOUND. THE COMPOUNDS POSSESS ANTI-INFLAMMATORY AND ANALGESIC ACTION.

WHEREIN R3 REPRESENTS ALKYL, WITH A HYDRAZINE OF THE FORMULA:

(PHENYL-CO-CH(-CH2-COO-R3)-CO-)BENZENE

WHEREIN R1 IS HYDROGEN, LOWER ALKYL, ARYL OR ARALKYL, THE AROMATIC RING OF THE SAID ARYL OR ARALKYL BEING SUBSTITUTED OR UNSUBSTITUTED, AND R2 IS HYDROGEN OR ALKYL ARE PREPARED BY REACTING A B,B-DIBENZOYLPROPIONATE OF THE FORMULA:

1-R1,3,5-DI(PHENYL),4-(R2-OOC-CH2-)PYRAZOE