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

MEB

Chemical Name: Butyric acid 2-(4-morpholinyl)ethyl ester hydrochloride
CAS No. 23866-07-1, 300555-03-7 (free base)
项目整合开发状态: Preclinical
项目研究机构: University of Arkansas (Originator)
合成路线:Th...
参考文献标题:Derivs.of butyric acid and uses thereof
文献作者:Gilbert,K.; Fifer,E.K.(University of Arkansas)
参考来源:US 6407107; WO 0073257

Y-931

Chemical Name: 8-Fluoro-12-(4-methylpiperazin-1-yl)-6H-[1]benzothieno[2,3-b][1,5]benzodiazepine maleate
CAS No. 221058-55-5, 221058-53-3 (free base), 221058-56-6 (fumarate salt (2:1)), 221059-36-5 ...
参考文献标题:Fused thiophene cpds.and medicinal use thereof
文献作者:Fujimura,M.; Horiuchi,H.; Tanaka,H.; Kohara,T.; Hashimoto,K.; Kimura,K.; Seio,K.; Yasumatsu,H.(Welfide Corporation)
参考来源:EP 1016664; JP 2001072684; WO 9911647

WQ-2944(free acid), WQ-3402

Chemical Name: 1-(5-Amino-2,4-difluorophenyl)-6-fluoro-8-methyl-7-(methylamino)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethanolamine salt
CAS No. 208164-93-6 (free acid)
项目整合开发状态: Preclinic...
参考文献标题:Novel pyridonecarboxylic acid derivs.or salts thereof and drugs containing the same as the active ingredient
文献作者:Sakae,N.; Yazaki,A.; Kuramoto,Y.; Yoshida,J.; Niino,Y.; Oshita,Y.; Hirao,Y.; Hayashi,N.; Amano,H.(Wakunaga Pharmaceutical Co.,Ltd.)
参考来源:EP 0945435; WO 9823592

新产品编号:595341

Chemical Name: 11-Deoxy-13-des(ethyl)-3-des(hexopyranosyloxy)-13-methyl-6-O-methyl-3-oxo-11-[4-(4-quinolinyl)butylamino]erythromycin A 11-N,12-O-cyclic carbamate
CAS No. 229319-05-5
项目整合开发状态: Pr...
参考文献标题:Ketolide antibacterials
文献作者:Chu,D.; Grant,E.; Hlasta,D.; Henninger,T.; Khosla,C.(Kosan Biosciences,Inc.; Ortho-McNeil Pharmaceutical,Inc.)
参考来源:WO 0062783

LFA-703

Chemical Name: 2(S)-Methylbutyric acid (1S,3R,7S,8S,8aR)-8-[2-[4(R)-hydroxy-1-[5-(hydroxymethyl)-6-methoxynaphthalen-2(S)-ylmethyl]-6-oxopiperidin-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphth...
参考文献标题:Mevinolin derivs.
文献作者:Hommel,U.; Bauer,W.; Meingassner,J.G.; Weitz-Schmidt,G.; Ehrhardt,C.; Kallen,J.; Banteli,R.; Cottens,S.; Nuninger,F.(Novartis AG; Novartis-Erfindungen VmbH)
参考来源:EP 1154988; WO 0048989

ST-1420

Chemical Name: 3(R)-(Dodecylsulfonamido)-4-(trimethylammonium)butyrate
CAS No. 250694-19-0, 250694-18-9 (enantiomer)
项目整合开发状态: Preclinical
项目研究机构: Sigma-Tau (Originator)
合成路线:Pentadecanoyl...
参考文献标题:Cpds.having reversible inhibiting activity of carnitine palmitoyl-transferase
文献作者:Marzi,M.; Tinti,M.O.; Giannessi,F.; Minetti,P.; De Angelis,F.; Chiodi,P.; Arduini,A.(Sigma-Tau Industrie Farmaceutiche Riunite SpA)
参考来源:EP 1077925; US 6369073; WO 9959957

CRL-8256

Chemical Name: 5,7-Dimethoxy-3-(4-methoxyphenyl)-1-[2-(1H-tetrazol-5-yl)ethyl]quinolin-2(1H)-one
CAS No. 256424-07-4
项目整合开发状态: Preclinical
项目研究机构: Lafon (Originator)
合成路线:Acylation of 3,5-...
参考文献标题:Pharmaceutical compsns.comprising 2-quinolones
文献作者:Guillaumet,G.; Darro,F.; Frydman,A.; Joseph,B.; Kiss,R.(Laboratoires L.Lafon)
参考来源:EP 1097138; FR 2781218; WO 0003990

3beta,7beta,17beta-Androstenetriol, HE-2200, Reversionex

Chemical Name: 5-Androstene-3beta,7beta,17beta-triol
CAS No. 62357-04-4 (undefined stereochem.)
项目整合开发状态: Phase II
项目研究机构: Virginia Commonwealth University (Originator), Hollis-Eden (Licensee...
参考文献标题:Enhancement of immune response
文献作者:Loria,R.(Virginia Commonwealth University)
参考来源:JP 1995508264; US 5206008

OC-229-648

Chemical Name: 3-[4-[4-[4-[(E)-2-Carboxyvinyl]phenyl]-5-[4-[(E)-3-(hexadecylamino)-3-oxo-1-propenyl]phenyl]-1H-imidazol-2-yl]phenyl]-4,5-dihydroisoxazole-5-carboxylic acid
CAS No. 274903-84-3
项目...
参考文献标题:Substd.thiazoles for treatment of human diseases involving modulators of P-,L- and E-selectin
文献作者:Kondo,H.; Inoue,Y.; Jones,T.K.; Ripka,W.C.; Yu,J.; Raheja,R.K.; Nguyen,T.N.; Slee,D.H.(NV Organon; Ontogen Corp.)
参考来源:WO 0033836; WO 0034255

新产品编号:962365

Chemical Name: 6-(N-Ethyl-N-propylamino)-1,2,3,4,5,6,7,8-octahydronaphthalen-1-one
CAS No. 500548-85-6
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:Condensation of 1,2,3,4,5,6,7,...
参考文献标题:Orally active analogues of the dopaminergic prodrug 6-(N,N-di-n-propylamino)-3,4,5,6,7,8-hexahydro- 2H-naphthalen-1-one: Synthesis and pharmacological activity
文献作者:Venhuis,B.J.; Dijkstra,D.; Wustrow,D.J.; Meltzer,L.T.; Wise,L.D.; Johnson,S.J.; Heffner,T.G.; Wikstr鰉,H.V.
参考来源:J Med Chem 2003,46(4),584