项目整合精选

聚焦新型临床类新产品的整合与转化. 在创新药研发领域，传统的“单一产品、单打独斗”模式正在被一种更系统化的“项目整合”思维所取代。项目整合的核心，在于将散落在研发早期、中期的创新资产，通过资金、临床资源、产业生态等多维度要素的有机组合，实现从“科学发现”到“临床价值”，再到“商业成功”的跨越。研发与商业的战略整合：从“资产思维”到“组合思维”它要求我们超越单个分子的视野，拥抱一个由技术创新、临床需求、资本支持和商业洞察共同构成的复杂网络。在这个网络中，成功的标准不再是单一的“获批上市”，而是能否通过高效的整合，将科学上的突破，转化为临床上真正可及、商业上可持续、能够惠及患者的解决方案。近年来，药物发现已从传统的小分子化药拓展至更多元的分子类型，这些新型API在项目整合中呈现出独特的开发范式，项目整合的核心挑战在于递送系统的设计与肝外靶向能力的突破。
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项目整合精选

AH-9700

Chemical Name: 1-[2-(6,7-Dimethyl-3,4-dihydro-2-naphthalenyl)ethyl]pyrrolidine fumarate
CAS No. 184638-09-3 (free base), 184639-27-8 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: Dainippon Ph...
参考文献标题:1-[omega-(3,4-Dihydro-2-naphthalenyl)alkyl]cyclic amine derivs.,process for producing the same,and medicinal compsn.containing the same
文献作者:Kai,N.; Kanehira,A.; Morie,T.; Hino,K.; Kawashima,K.; Shimizu,I.; Akiyama,K.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:EP 0825180; US 5847159; WO 9633169

L-753037, J-104132

Chemical Name: (5S,6R,7R)-2-Butyl-7-[2-[2(S)-carboxypropyl]-4-methoxyphenyl]-5-(3,4-methylenedioxyphenyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-6-carboxylic acid
CAS No. 198279-45-7, 169745-53-3 (un...
参考文献标题:Stereoselective deoxygenation reaction
文献作者:Frey,L.F.; Devine,P.N.; Tschaen,D.M.; Dolling,U.H.; Tillyer,R.D.; Kato,Y.(Banyu Pharmaceutical Co.,Ltd.; Merck & Co.,Inc.)
参考来源:EP 0923557; JP 1999514676; WO 9806700

Elarofiban, RWJ-53308

Chemical Name: 3(S)-[1-[3-(4-Piperidinyl)propionyl]piperidin-3(R)-ylcarboxamido]-3-(3-pyridyl)propionic acid
CAS No. 198958-88-2
项目整合开发状态: Phase II
项目研究机构: R.W. Johnson (Originator)
合成路线:K...
参考文献标题:Carboxamide derivs.of pyrrolidine,piperidine and hexahydroazepine for the treatment of thrombosis disorders
文献作者:Costanzo,M.J.; Hoekstra,W.J.; Maryanoff,B.E.(Ortho-McNeil Pharmaceutical,Inc.)
参考来源:EP 0923555; JP 2000510111; US 6069254; WO 9741102

CCT-62

Chemical Name: 6-(4-Methylene-5-oxo-2-phenyltetrahydrofuran-2-ylmethoxy)quinolin-2(1H)-one
CAS No. 210245-19-5
项目整合开发状态: Biological Testing
项目研究机构: Kaohsiung Medical University (Originator), ...
参考文献标题:alpha-Methylidene-gamma-butyrolactones: Synthesis and evaluation of quinolin-2(1H)-one derivatives
文献作者:Wang,T.-C.; et al.
参考来源:Helv Chim Acta 1998,81(6),1038

L-375052

Chemical Name: N-(6-Amino-2-methylpyridin-3-ylmethyl)-2-[3-(benzylsulfonamido)-2-oxo-6-propyl-1,2-dihydropyridin-1-yl]acetamide
CAS No. 187162-97-6
项目整合开发状态: Preclinical
项目研究机构: Merck & Co. (...
参考文献标题:Pyridinone-thrombin inhibitors
文献作者:Sanderson,P.E.; Naylor-Olsen,A.M.; Dyer,D.L.; Vacca,J.P.; Isaacs,R.C.A.; Dorsey,B.D.; Fraley,M.E.(Merck & Co.,Inc.)
参考来源:EP 0835109; JP 1999508558; WO 9701338

GYKI-39521, RGH-1875

Chemical Name: 4-(5-Thio-beta-D-xylopyranosylsulfanyl)benzothioimidic acid S-methyl ester hydroiodide
CAS No. 214272-33-0, 201546-86-3 (free base)
项目整合开发状态: Preclinical
项目研究机构: Gedeon Richter...
参考文献标题:An economic synthesis of 1,2,3,4-tetra-O-acetyl-5-thio-D-xylopyranose and its transformation into 4-substituted-phenyl 1,5-dithio-D-xylopyranosides possessing antithrombotic activity
文献作者:Bozo,E.; Boros,S.; Kuszmann,J.; Gacs-Baitz,E.; Parkanyi,L.
参考来源:Carbohydr Res 1998,308(3-4),297

GYKI-39541, RGH-1962

Chemical Name: 1-(4-Nitrophenylsulfanyl)-1,5-dithio-beta-D-arabinopyranoside
CAS No. 218907-16-5
项目整合开发状态: Preclinical
项目研究机构: Gedeon Richter (Originator)
合成路线:The thiobenzoylation of the ...
参考文献标题:Novel anticoagulant glycosides and pharmaceutical compsns.thereof
文献作者:Szeker,G.; Boros,S.; Szab? G.; Turuczn?Ferwagner,M.; Orb醤,O.; Feher,B.; Soukupn?Kedves,R.; Kenyeres,L.; Kov醕sn?Boz? E.; Barab醩,?; Moravcsik,I.; Kasz醩,E.; Kuszmann,J.(Gedeon Richter Ltd.)
参考来源:WO 9928312

Ro-09-2474

Chemical Name: (1R,2R,3S,6R)-1-[2-Methoxy-3-methyl-3-[2-(1-methylimidazol-2-ylsulfanyl)ethyl]-6-[4-(trifluoromethoxy)phenoxymethyl]cyclohexylmethyl]-1H-1,2,4-triazole
CAS No. 212890-41-0
项目整合开发状...
参考文献标题:Synthesis of novel antifungal agents (2)
文献作者:Tsukuda,T.; Watanabe,M.; Ontsuka,H.; Hattori,K.; Shirai,M.; Shimma,N.
参考来源:Bioorg Med Chem Lett 1998,8(14),1825

Ro-09-2550

Chemical Name: (1S,2R,3R,6R)-4-[2-[2-Methoxy-1-methyl-3-(1H-1,2,4-triazol-1-ylmethyl)-4-[4-(trifluoromethoxy)phenoxymethyl]cyclohexyl]ethyl]morpholine
CAS No. 212890-42-1
项目整合开发状态: Preclinical 参考文献标题:Synthesis of novel antifungal agents (2)
文献作者:Tsukuda,T.; Watanabe,M.; Ontsuka,H.; Hattori,K.; Shirai,M.; Shimma,N.
参考来源:Bioorg Med Chem Lett 1998,8(14),1825

新产品编号:413411

Chemical Name: 2-[2-(4-Methoxy-3,5-dimethylpyridin-2-yl)ethyl-2-methyl-5-(trifluoromethyl)-2,3-dihydrobenzothiazole
CAS No. 212779-16-3
项目整合开发状态: Preclinical
项目研究机构: Il-Yang (Originator)
合...
参考文献标题:Syntheses of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]benzothiazolidine derivatives as a potential gstric H+/K+-ATPase inhibitor
文献作者:Yoon,S.-H.; Seo,S.; Lee,Y.; Hwang,S.; Kim,D.Y.
参考来源:Bioorg Med Chem Lett 1998,8(14),1909