A series of ferrocene-based chiral multidentate P,P,N,N-ligands were successfully designed and synthesized. They can be directly prepared via a one-step nucleophilic substitution reaction from (S)-1-[(R)-2-(diphenylphosphino)ferrocenyl] ethyl acetate [(S_C,R_FC)-BPPFOAc]. Their ruthenium complexes were used in the asymmetric hydrogenation of 2-pyridyl ketones under mild conditions, the target chiral 1-aryl- or 1-alkyl-(pyridine-2-yl)methanols were obtained with high yields and excellent enantioselectivities. The synthetic utility of this reaction was demonstrated through its utilization in the preparation of key intermediates for a RAS inhibitor and the antihistamine drug Carbinoxamine.

2025-03-24·ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Functionalization of Pyridines at the C4 Position via Metalation and Capture

Article

作者: Hsu, Han‐Hsiang ; Sk, Md Raja ; Thomas, Andy A. ; Chen, Cheng‐Chun ; Kang, Seokmin

Abstract:

The functionalization of pyridines at positions remote to the N‐atom remains an outstanding problem in organic synthesis. The inherent challenges associated with overriding the influence of the embedded N‐atom within pyridines was overcome using n‐ butylsodium, which provided an avenue to deprotonate and functionalize the C4‐position over traditionally observed addition products that are formed with organolithium bases. In this work, we show that freshly generated 4‐sodiopyrdines could undergo transition metal free alkylation reactions directly with a variety of primary alkyl halides bearing diverse functional groups. In addition, after transmetalation to zinc chloride a simple and efficient Negishi cross‐coupling protocol was formulated for a variety of aromatic and heteroaromatic halides. The robustness of this protocol was demonstrated through the late‐stage installation of 4‐pyridyl fragments into a variety of complex active pharmaceutical ingredients including loratadine and prochlorperazine. Furthermore, through rapid injection NMR investigations, we are able to directly observe the evolution of anionic intermediates and determined that two distinct mechanistic pathways lead to the observed site selectivity: (1) the C4‐H within 2,6‐disubstituted pyridines could be removed directly and (2) the C4 selectivity of unsubstituted pyridine originates from the intermolecular exchange of metalation sites via a thermodynamic pathway.

2024-12-01·Advanced Science

Photoinduced Copper‐Catalyzed Cross‐Coupling of Acylsilanes with Heteroarenes via Bimetallic Relay

Article

作者: Peng Wang ; Ying-Chao Li ; Long Zheng ; Yichen Wu

Abstract:

The transition metal‐catalyzed direct coupling reactions involving electron‐rich Fischer carbene species are largely underdeveloped and remain a big challenge. Here, a direct coupling reaction of azoles and azine N ‐oxides is reported with Fischer copper carbene species bearing an α ‐siloxy group i, which can be in situ generated from acylsilanes catalytically under photoirradiation and redox‐neutral conditions. This coupling reaction between electron‐rich α ‐siloxy Fischer Cu‐carbene species with hard carbanion nucleophiles may undergo a bimetallic relay process, which is confirmed by the kinetic analysis and in situ NMR analysis. This reaction features mild conditions and remarkable heterocycle compatibility. Notably, this protocol tolerates a series of azole or azine N ‐oxide derivatives, including benzoxazole, benzothiazole, benzoimidazole, benzoisoxazole, oxazole, oxadiazole, triazolo[4,3 ‐a ]pyridine, purine, caffeine, pyridine N ‐oxide, quinoline N ‐oxide, pyrazine N ‐oxide, pyridazine N ‐oxide, etc. The synthetic value of this approach is demonstrated by the efficient synthesis of a histamine h4 receptor ligand and a marketed drug carbinoxamine.

项与马来酸卡比沙明相关的新闻（医药）

2025-12-16

·药品圈

FDA发布81份BE指南，包含多个国内有参比无指南复杂品种

*识林“BE指南数据库”截图，仅作示意用。 12月4日，FDA共发布了81份产品特定指南（PSG）草案，包括44份新指南和37份修订指南。54份PSG针对尚无获批ANDA的产品，其中包含19种复杂产品；28份PSG针对复杂产品，其中7份为新指南，21份为修订指南； Lachman的仿制药专家Pollock指出值得关注的PSG涵盖银屑病首创外用疗法、脂溢性皮炎治疗、营养不良性和交界性大疱性表皮松解症相关创面治疗及其他适应症，具体包括： 1.新PSG：治疗脂溢性皮炎：罗氟司特外用泡沫剂（RLD：ZORYVE，NDA 217242）；治疗罕见皮肤病（营养不良性和交界性大疱性表皮松解症）：Birch Triterpenes外用凝胶（RLD：FILSUVEZ，NDA 215064）。 2.修订PSG：银屑病非甾体辅助治疗：Tapinarof外用乳膏（RLD：VTAMA，NDA 217806），新增基于表征的BE方法；多种缓释（modified-release）药物：GDUFA新资助研究表明体外乙醇诱导的剂量倾泻研究（alcohol dose dumping studies）不再必需，故在PSG中移除此类研究，包括：Carbinoxamine Maleate口服缓释混悬液（RLD：KARBINAL ER，NDA 022556），磷酸卡维地洛口服缓释胶囊（RLD：COREG CR，NDA 022012），盐酸地尔硫卓口服缓释胶囊（RLD：CARDIZEM CD，NDA 020062），泊沙康唑口服迟释混悬剂（RLD：NOXAFIL POWDERMIX KIT，NDA 214770），曲司氯铵口服缓释胶囊（RLD：SANCTURA XR，NDA 022103）；复杂肽类药物：明确体外先天免疫反应试验建议，并规定仿制重组肽类药物的简化申报路径，包括：鲑降钙素（RLD：CALCIMAR，NDA 017769），胰高血糖素（RLD：BAQSIMI，GVOKE，NDA 210134，212097），Dasiglucagon Hydrochloride（RLD：ZEGALOGUE，NDA 214231），Pegcetacoplan（RLD：EMPAVELI，SYFOVRE，NDA 215014，217171），替尔泊肽（RLD：MOUNJARO，NDA 215866），特立帕肽（RLD：FORTEO，NDA 021318），利拉鲁肽（RLD：VICTOZA，SAXENDA，NDA 022341，206321），司美格鲁肽（RLD：WEGOVY，NDA 215256），伏索利肽（RLD：VOXZOGO，NDA 214938）。基于识林知识平台的“BE指南数据库”和“国内参比制剂数据库”进行简要调研后，编者将中美欧WHO的指南发布和国内参比发布情况列表如下，供仿制药企业立项调研时参考。如有差错，请读者指正（会员可至识林资讯页面下载excel版本）。 ● 表示查到对应指南或品规。 ✱ 表示查到对应分子，但品规不同。 N/A表示未查到对应指南或品规，或未查到官方中文通用名。

申请上市

2024-09-19

·BioSpace

Aytu BioPharma to Report Fiscal 2024 Full Year and Fourth Quarter Operational and Financial Results on September 26, 2024

DENVER, CO / ACCESSWIRE / September 19, 2024 / Aytu BioPharma, Inc. (the “Company” or “Aytu”) (NASDAQ:AYTU), a pharmaceutical company focused on commercializing novel therapeutics, will report its operational and financial results for its fiscal 2024 full year and fourth quarter, after the market close on Thursday, September 26, 2024. The Company has scheduled a conference call and webcast that same day, Thursday, September 26, 2024, at 4:30 p.m. Eastern time, to review the results followed by a question and answer session. Conference Call Details Date and Time: Thursday, September 26, 2024, at 4:30 p.m. Eastern time. Call-in Information: Interested parties can access the conference call by dialing (888) 506-0062 for United States callers or +1 (973) 528-0011 for international callers and using the participant access code 216512. Webcast Information: The webcast will be accessible live and archived at , and accessible on the Investors section of the Company’s website at under Events & Presentations. Replay: A teleconference replay of the call will be available until October 10, 2024, at (877) 481-4010 for United States callers or +1 (919) 882-2331 for international callers and using replay access code 51231. About Aytu BioPharma, Inc. Aytu is a pharmaceutical company focused on commercializing novel therapeutics. The Company’s prescription products include Adzenys XR-ODT® (amphetamine) extended-release orally disintegrating tablets (see Full Prescribing Information, including Boxed WARNING) and Cotempla XR-ODT® (methylphenidate) extended-release orally disintegrating tablets (see Full Prescribing Information, including Boxed WARNING) for the treatment of attention deficit hyperactivity disorder (ADHD), Karbinal® ER (carbinoxamine maleate), an extended-release antihistamine suspension indicated to treat numerous allergic conditions, and Poly-Vi-Flor® and Tri-Vi-Flor®, two complementary fluoride-based prescription vitamin product lines available in various formulations for infants and children with fluoride deficiency. To learn more, please visit aytubio.com. Contacts for Investors Mark Oki, Chief Financial Officer Aytu BioPharma, Inc. moki@aytubio.com Robert Blum or Roger Weiss Lytham Partners aytu@lythampartners.com SOURCE: Aytu BioPharma, Inc. View the original press release on accesswire.com

财报

2024-05-23

·BioSpace

Aytu BioPharma to Participate in the Lytham Partners Spring 2024 Investor Conference on May 30, 2024

DENVER, CO / ACCESSWIRE / May 23, 2024 / Aytu BioPharma, Inc. (the Company or "Aytu") (NASDAQ:AYTU), a pharmaceutical company focused on commercializing novel therapeutics, today announced that Josh Disbrow, CEO, will participate in a webcasted fireside chat and host one-on-one meetings with investors at the Lytham Partners Spring 2024 Investor Conference, taking place virtually on Thursday, May 30, 2024. Webcast The webcasted fireside chat will take place at 1:15pm ET on Thursday, May 30, 2024. The webcast can be accessed by visiting the conference home page at or directly at . The webcast will also be available for replay following the event. 1x1 Meetings Management will be participating in virtual one-on-one meetings throughout the event. To arrange a meeting with management, please contact Lytham Partners at 1×1@lythampartners.com or register for the event at . About Aytu BioPharma, Inc. Aytu is a pharmaceutical company focused on commercializing novel therapeutics. The Company's prescription products include Adzenys XR-ODT® (amphetamine) extended-release orally disintegrating tablets (see Full Prescribing Information, including Boxed WARNING) and Cotempla XR-ODT® (methylphenidate) extended-release orally disintegrating tablets (see Full Prescribing Information, including Boxed WARNING) for the treatment of attention deficit hyperactivity disorder (ADHD), Karbinal® ER (carbinoxamine maleate), an extended-release antihistamine suspension indicated to treat numerous allergic conditions, and Poly-Vi-Flor® and Tri-Vi-Flor®, two complementary fluoride-based prescription vitamin product lines available in various formulations for infants and children with fluoride deficiency. To learn more, please visit aytubio.com. Contacts for Investors: Mark Oki, Chief Financial Officer Aytu BioPharma, Inc. moki@aytubio.com Robert Blum or Roger Weiss Lytham Partners AYTU@lythampartners.com SOURCE: Aytu BioPharma, Inc. View the original press release on accesswire.com

100 项与马来酸卡比沙明相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01336	马来酸卡比沙明	R06AA08	DB00748

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
皮肤划痕症	美国	Aytu BioPharma, Inc.	2026-03-10
季节性常年性变应性鼻炎	美国	Aytu BioPharma, Inc.	2026-03-10
过敏反应	美国	Aytu BioPharma, Inc.	2013-03-28
血管性水肿	美国	Aytu BioPharma, Inc.	2013-03-28
变应性结膜炎	美国	Aytu BioPharma, Inc.	2013-03-28
嗜皮菌病	美国	Aytu BioPharma, Inc.	2013-03-28
超敏反应	美国	Aytu BioPharma, Inc.	2013-03-28
常年性变应性鼻炎	美国	Aytu BioPharma, Inc.	2013-03-28
季节性过敏性鼻炎	美国	Aytu BioPharma, Inc.	2013-03-28
血管舒缩性鼻炎	美国	Aytu BioPharma, Inc.	2013-03-28
荨麻疹	美国	Aytu BioPharma, Inc.	2013-03-28