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

Lonapalene, RS-43179

氯萘帕林Chemical Name: 1,4-Diacetoxy-6-chloro-2,3-dimethoxynaphthalene
CAS No. 91431-42-4
项目整合开发状态: Phase III
项目研究机构: Roche Bioscience (Originator), AstraZeneca (Licensee)
合成路线:The chlorinatio...
参考文献标题:1,4-Acyloxynaphthalene derivs.,topical compsns.containing them,methods for their preparation,and intermediates therefor
文献作者:Jones,G.H.; Venuti,M.C.; Young,J.M.(Syntex (USA),Inc.)
参考来源:EP 0107512; US 4466981

Losigamone, ADD-137022, AO-33

氯西加酮Chemical Name: (5R*)-5-[(alphaS*)-o-Chloro-alpha-hydroxybenzyl]-4-methoxy-2(5H)-furanone; threo-5-(2-Chloro-alpha-hydroxybenzyl)-4-methoxy-2,5-dihydrofuran-2-one; (R*,S*)-(?-5-[(2-Chlorophenyl)hyd...
参考文献标题:5-Arylalkyl-4-alkoxy-2(5H)-furanone derivs.,intermediates and process for their preparation as well as use as therapeutic agents
文献作者:Chatterjee,S.S.; Klessing,K.(Willmar Schwabe GmbH)
参考来源:DE 3615157; EP 0247320; JP 1988022087; US 4855320

Loxiglumide, CR-1505, Loxizin

氯谷胺Chemical Name: (?-4-(3,4-Dichlorobenzamido)-N-(3-methoxypropyl)-N-phenylglutaramic acid; (?-4-(3,4-Dichlorobenzamido)-5-[N-(3-methoxypropyl)pentylamino)-5-oxopentanoic acid
CAS No. 107097-80-3 参考文献标题:Pharmaceutically active derivatives of glutamic and aspartic acids
文献作者:Makovec,F.; Chist? R.; Rovati,C.L.; Rovati,A.L.(Rotta Research Laboratorium SpA)
参考来源:WO 8703869

Loratadine, Sch-29851, Civeran, Versal, Lisino, Clarityne, Clarityn, Claritin

氯雷他定Chemical Name: 8-Chloro-11-[N-(ethoxycarbonyl)piperidin-4-ylidene]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine; 4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1...
参考文献标题:Antihistaminic 11-(4-piperidylidene)-5H-benzo-[5,6
文献作者:Villani,F.J.(Schering Corp.)
参考来源:US 4282233

Romazarit sodium, Ro-31-3948/002

氯马扎利Chemical Name: 2-[[2-(4-Chlorophenyl)-4-methyl-5-oxazolyl]methoxy]-2-methylpropionic acid sodium salt
CAS No. 109543-76-2 (free acid)
项目整合开发状态: Phase II
项目研究机构: Roche (Originator)
合成路线...
参考文献标题:ROMAZARIT SODIUM < Prop INNM; BAN >
文献作者:Bradshaw,D.; Sedgwick,A.D.; Self,C.R.
参考来源:Drugs Fut 1989,14(9),867

Denotivir, Wratizolin, Vratizolin, T15, ITCL

氰基甲酸乙酯Chemical Name: 5-(Benzoylamino)-N-(4-chlorophenyl)-3-methyl-4-isothiazolecarboxamide; 5-Benzamido-4'-chloro-3-methyl-4-isothiazolecarboxanilide
CAS No. 51287-57-1
项目整合开发状态: Phase I
项目研究...
参考文献标题:Vratizolin
文献作者:Machon,Z.
参考来源:Drugs Fut 1988,13(5),426

Cianopramine, Ro-112465

氰帕明Chemical Name: 5-[3-(Dimethylamino)propyl]-10,11-dihydro-5H-dibenz[b,f]azepine-3-carbonitrile; 3-Cyano-N-[3-(dimethylamino)propyl]iminodibenzyl
CAS No. 66834-24-0, 66834-20-6 (HCl)
项目整合开发状态: ...
参考文献标题:3-Cyano-N-(N,N-dimethylaminopropyl)-iminodibenzyl and salts thereof
文献作者:Dostert,P.(Hoffmann-La Roche,Inc.)
参考来源:US 4138482

Cianergoline, 355/1057

氰麦角林Chemical Name: (alpha-RS)-alpha-Cyano-6-methylergoline-8beta-propionamide
CAS No. 74627-35-3
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:By reaction of 6-methylergoline-8beta-methanol p...
参考文献标题:Antihypertensive ergolinepropionamides
文献作者:Bernardi,L.; Bosisio,G.; Mantegani,S.; Sapini,O.; Temperelli,A.; Salvati,P.; Di Salle,E.; Arcari,G.; Bianchi,G.
参考来源:Arzneim-Forsch 1983,331094

Ortataxel, Bay-59-8862, IDN-5109, SB-T-101131

沃塔紫杉醇Chemical Name: 3(S)-(tert-Butoxycarbonylamino)-2(R)-hydroxy-5-methylhexanoic acid [2aR-[2aalpha,4beta,4abeta,6beta,9alpha,10beta,11beta,12alpha,12aalpha,12balpha]]-6,12b-diacetoxy-10,11-(carbonyl...
参考文献标题:Anti-tumor cpds.,pharmaceutical compsns.,methods for preparation thereof and for treatment
文献作者:Ojima,I.; Bombardelli,E.(Affymax Technologies,NV; State University of New York,Albany)
参考来源:US 5705508

Thalidomide, NSC-66847, K-17, Talizer, Thalomid, Synovir

沙利度胺Chemical Name: (?-2-(2,6-Dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione; (?-N-(2,6-Dioxopiperidin-3-yl)phthalimide; (?-alpha-(N-Phthalimido)glutarimide
CAS No. 50-35-1
项目整合开发状态: Lau...
参考文献标题:Novel products of the amino-piperidine-2,6-dione series
文献作者:(Gr黱enthal GmbH)
参考来源:GB 0768821