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

Ipexidine mesylate, CK-0569(free base)

伊培西定 Chemical Name: 1,1'-[Piperazin-1,4-diylbis(propane-3,1-diyliminocarbonimidoyl)]bis(3-hexylurea) bis(methanesulfonate)
CAS No. 69017-90-9, 69017-89-6 (free base)
项目整合开发状态: Biological Testi...
参考文献标题:
文献作者:Wohl,R.A.
参考来源:ZA 706373

Ganirelix acetate, Org-37462, RS-26306, Antagon, Orgalutran

加尼瑞克 Chemical Name: N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N6-[(ethylamino)(ethylimino)methyl]-D-lysyl-L-leucyl-N6-[(ethylamino)(ethylimi...
参考文献标题:Nonapeptide and decapeptide analogs of LHRH as LHRH antagonists
文献作者:Nestor,J.J.Jr.; Vickery,B.H.(Syntex (USA),Inc.)
参考来源:EP 0277829; JP 1988201199; US 4801577

Pivampicillin brobactam, Pivampicillin 6beta-bromopenicillanate, 2085-P, VD-2085

匹凡西林 Chemical Name: [2S-[2alpha,5alpha,6beta(S*)[[-6-[(Aminophenylacetyl)amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid (2,2-dimethy-1-oxopropoxy)methyl ester,mono[[2S...
参考文献标题:VD-2085
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1984,9(7),539

Pipecuronium bromide, RGH-1106, Arduan

哌库溴铵 Chemical Name: 2beta,16beta-Bis(4',4'-dimethylpiperazino)-3alpha,17beta-diacetoxy-5alpha-androstane dibromide dihydrate; 4,4'-(3,17-Diacetoxyandrostane-2,16-diyl)-bis(1,1-dimethylpiperazinium)d...
参考文献标题:
文献作者:Tuba,Z.; et al.
参考来源:GB 1398050

Pimonidazole hydrochloride, Ro-038799

哌莫硝唑 Chemical Name: 1-(2-Nitroimidazol-1-yl)-3-(1-piperidinyl)-2-propanol
CAS No. 70132-51-3, 70132-50-2 (free base)
项目整合开发状态: Phase III
项目研究机构: Roche (Originator)
合成路线:1) By condensatio...
参考文献标题:Preparation of polyacetylalkylenediamines
文献作者:Grimmelikhuysen,J.; Schroeder,A.(Unilever NV)
参考来源:BE 769655; DE 2133458; FR 2100320; GB 1335204

Indium In 111 pentetreotide, 111In-Pentetreotide, 111In-DTPA-octreotide, MP-1727, DTPA-SMS(noncomplexed)

喷曲肽 Chemical Name: Hydrogen [N-[2-[[2-[bis(carboxymethyl)amino]ethyl](carboxymethyl)amino]ethyl]-N-(carboxymethyl)glycyl-D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N1-...
参考文献标题:[111In-DTPA-D-Phe1]-octreotide,a potential radiopharmaceutical for imaging of somatostatin receptor-positive tumors: Synthesis,radiolabeling and in vitro validation
文献作者:Bakker,W.H.; Albert,R.; Bruns,C.; Breeman,W.A.; Hofland,L.J.; Marbach,P.; Pless,J.; Pralet,D.; Stolz,B.; Koper,J.W.; et al.
参考来源:Life Sci 1991,49(22),1583

Semapimod hydrochloride, AXD-455, CNI-1493

塞马莫德 Chemical Name: N,N'-Bis[3,5-bis[1-(2-amidinohydrazono)ethyl]phenyl]decanediamide tetrahydrochloride
CAS No. 164301-51-3, 352513-83-8 (free base)
项目整合开发状态: Phase II
项目研究机构: Picower Inst...
参考文献标题:Guanylhydrazones for treating inflammatory conditions
文献作者:Cerami,A.; Ulrich,P.; Tracey,K.J.; Bianchi,M.(Picower Institute for Medical Research)
参考来源:EP 0746312; EP 1160240; US 5599984; WO 9519767

Amacetam hydrochloride(former USAN), Pramiracetam hydrochloride, CNS-1879, CI-879, Pramistar(sulfate), Neupramir(sulfate), Remen(sulfate)

普拉西坦硫酸普拉西坦Chemical Name: N-[2-(Diisopropylamino)ethyl]-2-oxo-1-pyrrolidineacetamide hydrochloride; N-[2-[Bis(1-methylethyl)amino]ethyl-2-oxo-1-pyrrolidineacetamide hydrochloride
CAS No. 75733-50...
参考文献标题:N-(Substituted-aminoalkyl)-2-oxo-1-pyrrolidineacetamides
文献作者:L'Italien,Y.J.; Nordin,I.C.(Pfizer Inc.)
参考来源:BE 0864269; CA 1073457; DE 2808067; ES 467288; FR 2382441; GB 1588082; JP 53108966; US 4145347

Traboxopine hydrochloride, EGYT-2509

曲波索平 Chemical Name: (R,S)-2-Chloro-12H-dibenzo[d,g][1,3,6]dioxazocine 12-(N,N,beta-trimethylpropanamine) monohydrochloride
CAS No. 70133-85-6, 103624-59-5 (free base)
项目整合开发状态: Phase II
项目研...
参考文献标题:Dibenzo[d,g][1,3,6]dioxazocine derivs.
文献作者:Grasser,K.; Kiszelly,E.; Kos骳zky,I.; Pet骳z,L.; R髗sa,L.(Egis Pharmaceuticals Ltd.)
参考来源:DE 2833892; GB 2001980; US 4208410

Flutropium bromide, Ba 598 Br, Flubron

氟托溴铵 Chemical Name: endo-8-(2-Fluoroethyl)-3-(2-hydroxy-2,2-diphenylacetoxy)-8-methyl-8-azoniabicyclo[3.2.1]octane bromide
CAS No. 63516-10-9 (anti-isomer), 63516-07-4 (syn-isomer)
项目整合开发状态: L...
参考文献标题:Quaternary N-beta-substd.benzylic acid N-alkyltropinic esters
文献作者:Banholzer,R.; Bauer,R.; Heusner,A.; Schulz,W.(Boehringer Ingelheim GmbH)
参考来源:DE 2540633