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

Lodaxaprine, CM-40907

洛达普令Chemical Name: 3-(4-Hydroxypiperidino)-6-(2-chlorophenyl)pyridazine
CAS No. 93181-81-8
项目整合开发状态: Phase II
项目研究机构: Sanofi-Aventis (Originator)
合成路线:3-(4-Hydroxypiperidino)-6-(2-chlorop...
参考文献标题:CM-40907
文献作者:Lcher,W.
参考来源:Drugs Fut 1985,10(11),903

Leurubicin, E-88/032(hydrochloride), CT-012002, RP-39937, L-ADR, LEU-DOX, Doxogenix L

流柔比星Chemical Name: (8S,10S)-10-[[3-[(S)-2-Amino-4-methylvaleramido]-2,3,6-trideoxy-alphal-L-lyxo-hexopyranosyl]oxy]-8-glycoloyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-5,12-naphthacenedione; ...
参考文献标题:Novel doxorubicin derivs.,process for their preparation and pharmaceutical compsns
文献作者:Baurain,R.; Trouet,A.(Medgenix Group)
参考来源:BE 0869485; DE 2930637

BAY-41-4109

海湾41-4109外消旋 Chemical Name: (-)-4(R)-(2-Chloro-4-fluorophenyl)-2-(3,5-difluoropyridin-2-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxylic acid methyl ester
CAS No. 298708-81-3, 298708-79-9 (undefine...
参考文献标题:Dihydropyrimidines and their use in the treatment of hepatitis B
文献作者:Paessens,A.; Stoltefuss,J.; Goldmann,S.; Niew鰄ner,U.; Kr鋗er,T.; Schlemmer,K.-H.; Weber,O.; Graef,E.; Lottmann,S.; St鰈ting,J.; Deres,K.(Bayer AG)
参考来源:WO 0058302

Methylnaltrexone bromide, MRZ-2663BR

溴甲纳曲酮甲基纳曲酮 Chemical Name: 17-(Cyclopropylmethyl)-4,5alpha-epoxy-3,14-dihydroxy-17-methyl-6-oxomorphinanium bromide; N-Methylnaltrexone bromide
CAS No. 73232-52-7, 83387-25-1 (cation), 73232-53-8 ...
参考文献标题:Quaternary derivs.of noroxymorphone which relieve intestinal immobility
文献作者:Goldberg,L.I.; Stockhaus,K.; Merz,H.(Boehringer Ingelheim GmbH)
参考来源:US 4176186

Brovincamine fumarate, Sabromin

溴长春胺Chemical Name: (3alpha,14beta,16alpha)-11-Bromo-14,15-dihydro-14-hydroxyeburnamenine-14-carboxylic acid methyl ester fumarate; (12S,13aS,13bS)-9-Bromo-13a-ethyl-12-hydroxy-2,3,5,6,12,13,13a,13b-o...
参考文献标题:Substituted 5-(2-imidazolin-2-yl)aminopyrimidines
文献作者:Fleck,W.; Stenzel,W.; Armah,B.; Cohnen,E.(Beiersdorf-Lilly GmbH)
参考来源:DE 2849537; JP 1980092383

Terbufibrol, K-11267

特丁贝罗Chemical Name: 4-[3-(4-tert-Butylphenoxy)-2-hydroxypropoxy]benzoic acid
CAS No. 56488-59-6
项目整合开发状态: Not Determined
项目研究机构:
合成路线:Terbufibrol can be obtained in two different ways:1) ...
参考文献标题:
文献作者:Grill,H.; et al.
参考来源:DE 24460689

Terflavoxate hydrochloride, ND-907, REC-15/2053

特拉伏沙 Chemical Name: 3-Methyl-4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylic acid 1,1-dimethyl-2-(1-piperidinyl)ethyl ester hydrochloride; 3-Methylflavone-8-carboxylic acid 1,1-dimethyl-2-(1-piperidinyl)...
参考文献标题: 3-Methylflavone-8-carboxylic acid esters
文献作者:Nardi,D.; Tajana,A.; Cazzulati,P.; Graziani,G.; Pennini,R.; Casadio,S.(Recordati Industria Chimica e Farmaceutica SpA)
参考来源:EP 0072620; GB 2104507

Terbogrel, BIBV-308-SE, BIBV-308

特波格雷Chemical Name: 6-[3-(3-tert-Butyl-2-cyanoguanidino)phenyl]-6-(3-pyridyl)-5(E)-hexenoic acid
CAS No. 149979-74-8
项目整合开发状态: Phase II
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:The r...
参考文献标题:Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors
文献作者:Soyka,R.; Guth,B.D.; Weisenberger,H.M.; Luger,P.; Muller,T.H.
参考来源:J Med Chem 1999,42(7),1235

Terikalant fumarate, RP-62719

特立卡兰 Chemical Name: (-)-(S)-1-[2-(3,4-Dihydro-2H-1-benzopyran-4-yl)ethyl]-4-(3,4-dimethoxyphenyl)piperidine fumarate(1:1); (-)-(S)-1-[2-(4-Chromanyl)ethyl]-4-(3,4-dimethoxyphenyl)piperidine fumarate(...
参考文献标题:Novel benzopyran derivs.,their preparation and medicines containing them.(Rh鬾e-Poulenc Sant?
文献作者:Hardy,J.-C.; Renault,C.(Aventis SA)
参考来源:AU 8819713; EP 0300908; FR 2618437; JP 1989040476; US 4977166

Teriflunomide, HMR-1726, 1726, A-771726, RS-61980, SU-0020

特立氟胺Chemical Name: (Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
CAS No. 108605-62-5, 282716-73-8 (monosodium salt)
项目整合开发状态: Phase III
项目研究机构: Aventis Pharma (Originator)...
参考文献标题:Isoxazole-4-carboxamides and hydroxyalkylidene-cyanoacetamides,drugs containing these cpds.and use of such drugs
文献作者:Bartlett,R.R.; K鋗merer,F.-J.(Aventis SA)
参考来源:EP 0527736; JP 1993506425; JP 1999322700; JP 1999343285; US 5494911; US 5532259; WO 9117748