公开(公告)号：US3488354A

公开(公告)日：1970-01-06

申请号：US3488354D

申请日：1967-09-27

Applicant: AMERICAN CYANAMID CO

Inventor： BROWN JOHN JOHNSTON ,  HARDY ROBERT ALLIS JR ,  NORA CAROL THERESE

IPC: C07D489/12 ,  C07D43/28 ,  A61K27/00

CPC classification number: C07D489/12

公开(公告)号：US3464992A

公开(公告)日：1969-09-02

申请号：US3464992D

申请日：1968-03-25

Applicant: RECKITT & SONS LTD

Inventor： MAYOR PHILIP ARTHUR ,  HADDLESEY DAVID IAN ,  LEWIS JOHN WILLIAM ,  BENTLEY KENNETH WALTER

IPC: C07D489/12 ,  C07D43/28 ,  A61K27/00

CPC classification number: C07D489/12 ,  Y10S514/849

公开(公告)号：US3433791A

公开(公告)日：1969-03-18

申请号：US3433791D

申请日：1968-05-03

Applicant: RECKITT & SONS LTD

Inventor： BENTLEY KENNETH WALTER

IPC: C07D489/12 ,  C07D43/28 ,  A61K25/00

CPC classification number: C07D489/12 ,  Y10S514/823

公开(公告)号：US3318884A

公开(公告)日：1967-05-09

申请号：US51134565

申请日：1965-12-03

Applicant: AMERICAN CYANAMID CO

Inventor： BROWN JOHN J ,  HARDY JR ROBERT ALLIS ,  THERESE NORA CAROL

IPC: C07D489/12

CPC classification number: C07D489/12

公开(公告)号：US11905296B2

公开(公告)日：2024-02-20

申请号：US17790042

申请日：2021-01-27

Applicant: AZAD PHARMA AG

Inventor： Hartmut Zinser ,  Tamar Danielyan ,  Meri Grigoryan ,  Mariam Gharibyan ,  Mikayel Movsisyan ,  Kristine Nerkararyan

IPC: C07D489/12 ,  C07B49/00 ,  C07B43/08 ,  C07B43/04 ,  C07B31/00 ,  C07B37/12 ,  C07D498/12 ,  A61P25/36 ,  A61P25/04

CPC classification number: C07D489/12 ,  A61P25/04 ,  A61P25/36 ,  C07B31/00 ,  C07B37/12 ,  C07B43/04 ,  C07B43/08 ,  C07B49/00 ,  C07D498/12 ,  C07D489/12 ,  C07B49/00 ,  C07D489/12 ,  C07B43/08 ,  C07D489/12 ,  C07B43/04 ,  C07D489/12 ,  C07B31/00 ,  C07D489/12 ,  C07B37/12

Abstract: The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.

公开(公告)号：US20240050573A1

公开(公告)日：2024-02-15

申请号：US18343554

申请日：2023-06-28

Applicant: Monash University

Inventor： Christopher John Porter ,  Jamie Simpson ,  Natalie Trevaskis ,  Tim Quach ,  Sifei Han ,  Luojuan Hu

IPC: A61K47/54 ,  A61K31/568 ,  A61K31/27 ,  A61K31/365 ,  A61K31/485 ,  C07C219/06 ,  C07C235/36 ,  C07D307/88 ,  A61K31/222 ,  C07C271/24 ,  C07D489/12 ,  C07J1/00 ,  A61K31/165 ,  A61K9/00 ,  A61K31/138 ,  A61K31/167 ,  A61K45/06

CPC classification number: A61K47/542 ,  A61K31/568 ,  A61K31/27 ,  A61K31/365 ,  A61K31/485 ,  C07C219/06 ,  C07C235/36 ,  C07D307/88 ,  A61K31/222 ,  C07C271/24 ,  C07D489/12 ,  C07J1/0029 ,  A61K31/165 ,  C07J1/0025 ,  A61K9/0053 ,  A61K31/138 ,  A61K31/167 ,  A61K45/06 ,  C07C2602/26

Abstract: The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that promote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.

公开(公告)号：US11136331B2

公开(公告)日：2021-10-05

申请号：US16755719

申请日：2018-10-12

Applicant: Cambrex Charles City, Inc.

Inventor： Par Holmberg ,  Lars Eklund ,  David Adams ,  Michael Letourneau ,  Margus Eek ,  Alo Soone

IPC: C07D489/12 ,  A61K31/485

Abstract: There is provided a novel process for the preparation of a compound of formula I, wherein R1, R2, W, Z and are as described in the description, by demethylation of a corresponding O-methyl derivative with a borohydride-based reagent. This process may be used in the preparation of buprenorphine.

公开(公告)号：US20210188862A1

公开(公告)日：2021-06-24

申请号：US16755719

申请日：2018-10-12

Applicant: Cambrex Charles City, Inc.

Inventor： Par HOLMBERG ,  Lars EKLUND ,  David ADAMS ,  Michael LETOURNEAU ,  Margus EEK ,  Alo SOONE

IPC: C07D489/12

Abstract: There is provided a novel process for the preparation of a compound of formula I, wherein R1, R2, W, Z and are as described in the description, by demethylation of a corresponding O-methyl derivative with a borohydride-based reagent. This process may be used in the preparation of buprenorphine.

公开(公告)号：US10745406B2

公开(公告)日：2020-08-18

申请号：US15336970

申请日：2016-10-28

Applicant: EURO-CELTIQUE S.A.

Inventor： Steve Whitelock ,  Deborah Phyllis Harding ,  Carl David Turner

IPC: A61K31/485 ,  C07D489/12 ,  C07D489/02 ,  A61K9/70

Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.

公开(公告)号：US20190314364A1

公开(公告)日：2019-10-17

申请号：US16446397

申请日：2019-06-19

Applicant: Rhodes Technologies

Inventor： C. Frederick M. HUNTLEY ,  Erik Wayne KATAISTO ,  Helge Alfred REISCH ,  Archana SHARMA

IPC: A61K31/485 ,  A61P25/04 ,  C07D489/12

Abstract: The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.