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

Tigemonam, SQ-30213

替吉莫南双(2-羟基-N,N,N-三甲基乙胺)({[(1Z)-1-(2-氨基-1,3-噻唑-4-基)-2-{[(3S)-2,2-二甲基-4-氧代-1-(磺纳托氧)阿捷丁-3-酰基]氨基}-2-氧基乙基苯丙胺]氧)乙酸盐 Chemical Name: 3beta(S)-[2-(2-Aminothiazol-4-yl)-2(Z)-(carboxymethoxyimino)acetamido]-1-h...
参考文献标题:Preparation of 4,4-dialkyl-2-azetidinones
文献作者:Slusarchyk,W.A.; Dejneka,T.; Kostes,W.H.(Bristol-Myers Squibb Co.)
参考来源:AU 8652460; BE 090411; DE 3602347; ES 8706112; ES 8800897; FR 2576596; GB 2170201; US 4638061

Tipifarnib, NSC-702818, R-115777, Zarnestra

替吡法尼 6-[氨基-(4-氯苯基)-(3-甲基咪唑-4-基)甲基]-4-(3-氯苯基)-1-甲基喹啉-2-酮 Chemical Name: (+)-(R)-6-[1-Amino-1-(4-chlorophenyl)-1-(1-methylimidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one
CAS No. 1...
参考文献标题:Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivs.
文献作者:Venet,M.G.; Angibaud,P.R.; Muller,P.; Sanz,G.C.(Janssen Pharmaceutica NV)
参考来源:EP 0865440; JP 1998511405; US 6037350; WO 9721701

Tiquizium bromide, HSR-902, Thiaton

替喹溴铵Chemical Name: 3-(Di-2-thienylmethylene)-5-methyl-trans-quinolizidinium bromide
CAS No. 71731-58-3
项目整合开发状态: Launched-1984
项目研究机构: Abbott (Originator)
合成路线:The reaction of 2-piperidine...
参考文献标题:Substituted quinolizidine and indolizidine derivatives and the preparation thereof
文献作者:Kato,H.; Koshinaka,E.; Ogawa,N.; Kurata,S.; Yamagishi,K.; Ishikuza,M.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:BE 0866988; DE 2820687; FR 2390956; GB 1602927; JP 8034148

Tedisamil hydrochloride, KC-8857, Tedangin

替地沙米Chemical Name: 3,7-Di(cyclopropylmethyl)-9,9-tetramethylene-3,7-diazabicyclo[3.3.1]nonane dihydrochloride; 3',7'-Bis(cyclopropylmethyl)spiro[cyclopentane-1,9'-[3,7]diazabicylo[3.3.1]nonane dihydro...
参考文献标题:New 3,7-diazabicylo[3.3.1]nonanes
文献作者:Sh鰊,U.; Hachmeister,B.; Kehrbach,W.; K黨l,U.; Buschmann,G.(Kali-Chemie AG)
参考来源:DE 3234697; EP 0103833; JP 1993247039

Teniloxazine maleate, Sulfoxazine maleate, Y-8894, Luceran, Metatone

替尼沙秦马来酸盐替尼沙秦Chemical Name: 2-[2-(2-Thenyl)phenoxymethyl]morpholine maleate
CAS No. 62473-80-7, 63342-78-9 (1:1), 62473-79-4 (free base)
项目整合开发状态: Phase III
项目研究机构: Mitsubishi Pharma (Originat...
参考文献标题:Y-8894
文献作者:Serradell,M.N.; Blancafort,P.; Castar,J.
参考来源:Drugs Fut 1981,6(7),423

Tenilsetam, CAS-997

替尼西坦Chemical Name: (?-3-(2-Thienyl)-2-piperazinone
CAS No. 86696-86-8
项目整合开发状态: Discontinued
项目研究机构: Aventis Pharma (Originator)
合成路线:The cyclization of ethyl 2-(2-thienyl)glyoxylate (I) w...
参考文献标题:Novel piperazinones,their preparation and use
文献作者:Beyerle,R.; Bender,H.; Schindler,U.; Nitz,R.-E.; Martorana,P.A.(Cassella AG)
参考来源:DE 3132882; US 4598079

Ebanicline, Tebanicline, A-98593(S-isomer), ABT-594

替巴克兰Chemical Name: (R)-2-Chloro-5-(2-azetidinylmethoxy)pyridine
CAS No. 198283-73-7, 209326-19-2 (diHCl), 209326-18-1 (monobenzoate salt), 203564-54-9 (monoHCl), 198283-74-8 (monotosylate salt)
...
参考文献标题:3-Pyridyl enantiomers and their use as analgesics
文献作者:Wasicak,J.T.; Ehrlich,P.P.; Sullivan,J.P.; Ryther,K.B.; Or,Y.S.; Lin,N.-H.; Dart,M.J.; Bai,H.; Arneric,S.P.; Holladay,M.W.; Lynch,J.K.(Abbott Laboratories Inc.)
参考来源:EP 0950057; JP 2001504857; WO 9825920

Tirapazamine, SR-259075, NSC-130181, Win-59075, SR-4233, Tirazone

替拉扎明Chemical Name: 3-Amino-1,2,4-benzotriazine 1,4-dioxide
CAS No. 27314-97-2
项目整合开发状态: Phase III
项目研究机构: Sanofi-Aventis (Originator), SRI (Originator), National Cancer Institute (Not Determi...
参考文献标题:3-Amino-1,2,4-benzotriazine-1,4-di-N-oxides and processes for their preparation
文献作者:Ley,K.; Seng,F.; Metzer,K.G.(Bayer AG)
参考来源:US 3868371; US 3980779; US 4001410

Tirilazad mesylate, ISV-600, U-74006F, Tridax, Freedox

替拉扎特Chemical Name: 16alpha-Methyl-21-[4-[2,6-bis(pyrrolidino)-4-pyrimidinyl]-1-piperazinyl]pregna-1,4,9(11)triene-3,20-dione monomethanesulfonate hydrate; 21-[4-[2,6-Bis(pyrrolidino)pyrimidin-4-yl]pip...
参考文献标题:THE 21-AMINOSTEROIDS: POTENT INHIBITORS OF LIPID PEROXIDATION FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM TRAUMA AND ISCHEMIA
文献作者:Braughler,J.M.; Hall,E.D.; Jacobsen,E.J.; McCall,J.M.; Means,E.D.
参考来源:Drugs Fut 1989,14(2),143

CMDA

替拉那韦Chemical Name: 4-[N-(2-Chloroethyl)-N-[2-(mesyloxy)ethyl]amino]benzoyl-L-glutamic acid
CAS No. 122665-73-0
项目整合开发状态: Phase I
项目研究机构: Institute of Cancer Research (Originator)
合成路线:The ...
参考文献标题:CMDA
文献作者:Springer,C.J.
参考来源:Drugs Fut 1993,18(3),212