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

Thaliblastine, Thalicarpine, NSC-68075

唐松草碱Chemical Name: [S-(R*,R*)]-9-[4,5-Dimethoxy-2-[(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-isoquinolinyl)methyl]phenoxy]-5,6,6a,7-tetrahydro-1,2,10-trimethoxy-6-methyl-4H-dibenzo[de,g]quinoline 参考文献标题:Thaliblastine
文献作者:Todorov,D.K.
参考来源:Drugs Fut 1988,13(3),234

Zoliprofen, 156-S, 480156-S

唑利洛芬Chemical Name: alpha-Methyl-4-(2-thiazolyloxy)benzeneacetic acid; 2-[4-(2-Thiazolyloxy)phenyl]propionic acid
CAS No. 56355-17-0
项目整合开发状态: Phase II
项目研究机构: Shionogi (Originator)
合成路线:Th...
参考文献标题:Improved process for the production of 2-(4-(2-thiazolyloxy)phenyl)propionic acid
文献作者:Hamada,Y.; Ando,S.(Shionogi & Co.Ltd.)
参考来源:CA 1188699; EP 0088008; JP 58148870

Zonampanel, YM-872

唑南帕奈Chemical Name: 2-[7-(1-Imidazolyl)-6-nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-1-yl]acetic acid
CAS No. 210245-80-0, 179010-47-0 (monoHCl)
项目整合开发状态: Phase II
项目研究机构: Yamanouchi (Origin...
参考文献标题:1,2,3,4-Tetrahydroquinoxalindione deriv.
文献作者:Shishikura,J.; Inami,H.; Sakamoto,S.; Tsukamoto,S.; Sasamata,M.; Okada,M.; Fujii,M.(Yamanouchi Pharmaceutical Co.,Ltd.)
参考来源:EP 0784054; US 6096743; WO 9610023

Zosuquidar trihydrochloride, LY-335979, RS-33295-198

唑喹达三盐酸盐 (6R,7R)-7-[[2-[2-(氨基甲基)苯基]乙酰]氨基]-3-[[1-(羧甲基)四唑-5-基]硫甲基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸 Chemical Name: (1aR,6S,10bS)-1,1-Difluoro-6-[4-[2(R)-hydroxy-3-(quinolin-5-yloxy)propyl]piperazin-1-yl...
参考文献标题:10,11-Methanodibenzosuberane derivs.used as chemosensitizing agents
文献作者:Pfister,J.R.; Slate,D.L.(Syntex (USA) LLC)
参考来源:EP 0695293; EP 0866063; JP 1996509223; WO 9424107

Zonisamide, E-2090, CI-912, AD-810, Zonegran, Excegran

唑尼沙胺唑尼沙胺钠 Chemical Name: 3-(Sulfamoylmethyl)-1,2-benzisoxazole; 1,2-Benzisoxazole-3-methanesulfonamide
CAS No. 68291-97-4, 68291-98-5 (Na salt)
项目整合开发状态: Launched-1989
项目研究机构: Elan (Supplier...
参考文献标题:Methane-sulfonamide derivatives,the preparation thereof and composition comprising the same
文献作者:Uno,H.; et al.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:US 4172896

Zaltidine, CP-57361

唑替丁Chemical Name: [4-(2-Methylmidazol-5-yl)-2-thiazolyl]guanidine
CAS No. 85604-00-8, 90274-23-0 (diHCl)
项目整合开发状态: Phase II
项目研究机构: Pfizer (Originator)
合成路线:The bromination of 4-acetyl-2-m...
参考文献标题:2-Guanidino-4-(2-methyl-4-imidazlyl)thiazoles in the treatment of rheumatoid arthritis
文献作者:Larson,D.L.(Pfizer Inc.)
参考来源:EP 0178822; JP 1986091122; US 4591595

Zoledronic acid monohydrate, CGP-42446(anhydrous), ZOL-446, CGP-42446A(disodium salt), CGP-42446B(triNa salt, hydrate), Zometa

唑来磷酸唑来膦酸唑来膦酸二钠盐四水合物Chemical Name: 1-Hydroxy-2-(1-imidazolyl)ethylene-1,1-diphosphonic acid monohydrate
CAS No. 165800-06-6, 118072-93-8 (anhydrous), 165800-07-7 (diNa salt), 157432-59-2 (Mg salt)...
参考文献标题:Substituted alkanediphosphonic acids and pharmaceutical use
文献作者:Jaeggi,K.A.; Widler,L.(Novartis AG)
参考来源:AU 8781453; EP 0275821; JP 1988150291; US 4939130

Zopolrestat, CP-73850, Alond, Xedia

唑泊司他Chemical Name: 2-[4-Oxo-3-[5-(trifluoromethyl)benzothiazol-2-ylmethyl]-3,4-dihydrophthalazin-1-yl]acetic acid
CAS No. 110703-94-1, 110765-49-6 (Na salt)
项目整合开发状态: Phase II
项目研究机构: Pfizer ...
参考文献标题:Heterocyclic oxophthalazinylacetic acids
文献作者:Mylari,B.L.; Larson,E.R.; Zembrowski,W.J.(Pfizer Inc.)
参考来源:EP 0222576; JP 1987114988; US 4939140

Supimide, CG-3033

唑砜吡酮Chemical Name: 2-(2-Oxopiperidin-3-yl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide
CAS No. 49785-74-2
项目整合开发状态: Not Determined
项目研究机构:
合成路线:This compound can be prepared in two different...
参考文献标题:
文献作者:Graudums,I.; et al.
参考来源:BE 796167; CA 982586; CH 581652; CH 583733; CH 590861; DE 2210166; FR 2174924; GB 1377896; JP 73103572; JP 76125076; JP 76125077; JP 7620510; JP 7734625; JP 7734626; NL 7301783; US 3951985; US 4067985; ZA 7300468

Covidarabine, Deoxycoformycin, Pentostatin, CL-67310465, PD-81565, YK-176, CI-825, NSC-218321, Coforin, Oncopent, Nipent

喷司他丁Chemical Name: (R)-3-(2-Deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol; 2'-Deoxycoformycin; 2'-Deoxycholmycin
CAS No. 53910-25-1, 59979-24-7 (deleted CA...
参考文献标题:2-Amino-1-(5-amino-1H-imidazol-4-yl)ethanone and method of preparation
文献作者:Baker,D.C.; Putt,S.R.(Pfizer Inc.)
参考来源:DE 2835144; ES 472478; ES 479618; GB 2005661; GB 2013680; US 4117229