公开(公告)号：US20240018099A1

公开(公告)日：2024-01-18

申请号：US18253311

申请日：2021-11-19

Applicant: NOVARTIS AG

Inventor： Fritz ANDREAE

IPC: C07C273/18

CPC classification number: C07C273/1809

Abstract: The present disclosure relates to the synthesis of prostate specific membrane antigen (PSMA) ligands that are useful in the treatment of diseases like cancer. In particular, the disclosure relates to a method for synthesizing PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal.

公开(公告)号：US10059660B2

公开(公告)日：2018-08-28

申请号：US15370980

申请日：2016-12-06

Applicant: Millendo Therapeutics, Inc.

Inventor： Stephen Warren Hunt, III ,  Martin Douglas Phillips ,  Robert Matunas ,  Herman Chen ,  Aimesther Betancourt ,  Charles Uzarama ,  Roch Thibert

IPC: A61K9/50 ,  C07C275/28 ,  C07C273/18 ,  A61K9/20 ,  A61K31/17

CPC classification number: C07C275/28 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2081 ,  A61K9/5084 ,  A61K31/17 ,  C07C273/1809 ,  C07C2601/08

Abstract: A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.

公开(公告)号：US20170253557A1

公开(公告)日：2017-09-07

申请号：US15444776

申请日：2017-02-28

Applicant: NerPharMa S.r.l.

Inventor： Attilio TOMASI ,  Ilaria Candiani ,  Francesco Corcella ,  Francesco Saverio Caldarelli

IPC: C07C273/18

CPC classification number: C07C273/1854 ,  C07C273/1809 ,  C07C273/1836 ,  C07C275/08 ,  C07C275/68 ,  C07D233/60 ,  C07D233/61

Abstract: Carmustine may be safely and efficiently produced by reacting 2-chloroethylamine hydrochloride and 1,1′-carbonyldiimidazole to afford 1,3-bis(2-chloroethyl)-1-urea, followed by nitrosation to give the final product.

公开(公告)号：US20110130350A1

公开(公告)日：2011-06-02

申请号：US12961705

申请日：2010-12-07

Applicant: Jens Riedner ,  Gavin Dunne

Inventor： Jens Riedner ,  Gavin Dunne

IPC: A61K38/05 ,  C07C231/14 ,  C07C231/24 ,  C07C231/10 ,  C07C227/16

CPC classification number: C07C231/02 ,  C07C273/1809 ,  C07C273/1854 ,  C07C275/10 ,  C07C275/16 ,  Y02P20/55 ,  C07C235/06

Abstract: The present invention is concerned with an improved method of producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide) comprising the 0-methylation of a compound of formula (I) to produce a compound of formula (II) in a single step reaction.

Abstract translation: 本发明涉及一种制备（R）-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺（lacosamide）的改进方法，其包括式（I）化合物的O-甲基化以产生式（II）化合物 ）在一步反应。

公开(公告)号：US07884134B2

公开(公告)日：2011-02-08

申请号：US11664316

申请日：2005-09-30

Applicant: Jens Riedner ,  Gavin Dunne

Inventor： Jens Riedner ,  Gavin Dunne

IPC: C07C237/08 ,  A61K31/16

CPC classification number: C07C231/02 ,  C07C273/1809 ,  C07C273/1854 ,  C07C275/10 ,  C07C275/16 ,  Y02P20/55 ,  C07C235/06

Abstract: The present invention is concerned with an improved method of producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide) comprising the O-methylation of a compound of formula I to produce a compound of formula II in a single step reaction.

Abstract translation: 本发明涉及制备（R）-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺（lacosamide）的改进方法，该方法包括式I化合物的O-甲基化以在单一化合物中制备式II化合物 一步反应。

公开(公告)号：US20100217029A1

公开(公告)日：2010-08-26

申请号：US11921972

申请日：2006-06-09

Applicant: Jörg Sundermeyer ,  Fuming Mei

Inventor： Jörg Sundermeyer ,  Fuming Mei

IPC: C07C263/14 ,  C07C269/00

CPC classification number: C07C269/00 ,  C07C263/04 ,  C07C263/14 ,  C07C269/04 ,  C07C273/1809 ,  C07C265/12 ,  C07C271/28 ,  C07C275/28

Abstract: The invention relates to a method for producing N-aryl carbamates (urethanes) and N-aryl isocyanates. According to said method, aromatic nitro compounds are subjected to a reductive carbonylation in the presence of carbon dioxide and organic compounds that bear hydroxyl groups and the carbonylation is carried out in the presence of metal complexing catalysts. Anionic N,O-chelate ligands of the general formulae [M(N˜O)−2] and [M(O˜N˜N˜O)2−], containing a divalent or trivalent transition metal of groups 5-11 are used for the catalysts.

Abstract translation: 本发明涉及生产N-芳基氨基甲酸酯（氨基甲酸酯）和N-芳基异氰酸酯的方法。 根据所述方法，芳族硝基化合物在二氧化碳和具有羟基的有机化合物的存在下进行还原羰基化，羰基化在金属络合催化剂存在下进行。 含有5-11的二价或三价过渡金属的通式[M（N-O）-2]和[M（O〜N〜N-O）2-]]的阴离子N，O-螯合配体是 用于催化剂。

公开(公告)号：US20090275771A1

公开(公告)日：2009-11-05

申请号：US12321995

申请日：2009-01-28

Applicant: Andreas Jacob ,  Stefan Wershofen ,  Stephan Klein ,  Jorg Sundermeyer ,  Fuming Mei

Inventor： Andreas Jacob ,  Stefan Wershofen ,  Stephan Klein ,  Jorg Sundermeyer ,  Fuming Mei

IPC: C07C263/04 ,  C07C269/04

CPC classification number: C07C269/00 ,  B01J31/183 ,  B01J31/1835 ,  C07C263/04 ,  C07C269/04 ,  C07C273/18 ,  C07C273/1809 ,  C07C271/12 ,  C07C271/28 ,  C07C275/28

Abstract: Urethanes are prepared by oxidative carbonylation of at least one amino compound in the presence of carbon monoxide, oxygen and organic, at least one hydroxyl-group-carrying compound. The carbonylation is carried out in the absence of halogen-containing promoters. The carbonylation is also carried out in the presence of a metal complex catalyst which contains neutral bidentate N-chelate ligands of the (N˜N) type, two monoanionic N,O-chelate ligands of the general type (N˜O)− or tetradentate dianionic chelate ligands (O˜N˜N˜O)2−.

Abstract translation: 在一氧化碳，氧和有机物，至少一种含羟基化合物的存在下，通过氧化羰基化至少一种氨基化合物制备聚氨酯。 在不含卤素促进剂的情况下进行羰基化。 羰基化还可以在金属络合物催化剂的存在下进行，该催化剂含有（N〜N）型的中性二齿N-螯合配体，一般类型（N〜O）的两个单阴离子N，O-螯合配体，或 四齿二离子螯合配体（O〜N〜N〜O）2-。

公开(公告)号：US06372933B1

公开(公告)日：2002-04-16

申请号：US09763743

申请日：2001-02-27

Applicant: Neil H. Baine ,  Ann Marie Eldridge ,  Marvin Sungwhan Yu

Inventor： Neil H. Baine ,  Ann Marie Eldridge ,  Marvin Sungwhan Yu

IPC: C07C25500

CPC classification number: C07C273/1809 ,  C07C275/42

Abstract: This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.

Abstract translation: 本发明涉及一种通过使用路易斯酸来制备某些苯基脲化合物以通过胺进行苯并恶唑啉酮的开环的方法。

公开(公告)号：US5852160A

公开(公告)日：1998-12-22

申请号：US914831

申请日：1997-08-19

Applicant: Mark Andrew Scialdone

Inventor： Mark Andrew Scialdone

IPC: C07D295/20 ,  C07B43/00 ,  C07B61/00 ,  C07C273/18 ,  C07C275/24 ,  C07C275/26 ,  C07C275/28 ,  C07D213/75 ,  C07D295/215 ,  C07D307/14 ,  C07D317/58 ,  C07D405/12 ,  C08F8/00 ,  C08F8/18 ,  C08F8/30 ,  C08G2/00 ,  C07C49/00 ,  C07C281/00

CPC classification number: C07D295/215 ,  C07C273/1809 ,  C08G12/06 ,  C07C2101/14 ,  C40B40/00

Abstract: This invention relates to methods for preparing novel, solid-phase transfer reagents, specifically phosgenated oxime resins and non-symmetrical ureas, that are useful as supports in combinatorial synthesis for the creation of libraries of compounds for lead identification.

公开(公告)号：US5686645A

公开(公告)日：1997-11-11

申请号：US902615

申请日：1992-06-23

Applicant: Mahmoud K. Faraj

Inventor： Mahmoud K. Faraj

IPC: C07C269/00 ,  C07C273/18 ,  C07C275/28 ,  C07C261/00 ,  C07C271/00

CPC classification number: C07C273/1809 ,  C07C269/00

Abstract: A selective process for the production of unsymmetric carbamates and ureas is disclosed. In the process, a primary formamide is reacted with a dialkyl amine or an alcohol in the presence of a Group VIII transition metal catalyst. The unsymmetric carbamates and ureas are useful precursors to isocyanates.

Abstract translation: 公开了生产非对称氨基甲酸酯和脲的选择性方法。 在此过程中，在VIII族过渡金属催化剂的存在下，使一级甲酰胺与二烷基胺或醇反应。 不对称的氨基甲酸酯和脲是异氰酸酯的有用前体。