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

TZA-2237

Chemical Name: 7alpha-Mercapto-17-oxa-17a-homoandrosta-1,4-diene-3,17a-dione
CAS No. 159822-03-4
项目整合开发状态: Preclinical
项目研究机构: Teikoku Hormone (Originator)
合成路线:Treatment of D-homo-17-oxaa...
参考文献标题:Novel 7-substd.oxa- or azasteroid cpd.
文献作者:Koizumi,N.; Takegawa,S.; Iwashita,S.; Kawachi,T.; Inoue,F.; Honma,S.; Takahashi,H.; Mieda,M.; Ueda,K.; Shibata,K.(Teikoku Hormone Manufacturing Co.,Ltd.)
参考来源:EP 0663402; JP 1994508897; US 5539127; WO 9407908

BMS-188494

Chemical Name: 1(S)-[Bis(pivaloyloxymethoxy)phosphoryl]-4-(3-phenoxyphenyl)butanesulfonic acid
CAS No. 191866-32-7 (undefined isomer)
项目整合开发状态: Phase II
项目研究机构: Bristol-Myers Squibb (Originat...
参考文献标题:Alpha-phosphorous substd.sulfonate derivs.as squalene synthetase inhibitors
文献作者:Magnin,D.R.; Biller,S.A.; Dickson,J.K.Jr.; Lawrence,M.R.; Sulsky,R.B.(Bristol-Myers Squibb Co.)
参考来源:EP 0595635; JP 1994199879; US 5712396

PNU-96988, U-96988

Chemical Name: 6-(1-Benzylpropyl)-4-hydroxy-3-(1-phenylpropyl)pyran-2-one
CAS No. 149394-65-0
项目整合开发状态: Phase I
项目研究机构: Pfizer (Originator)
合成路线:The condensation of 4-hydroxy-6-methyl-2H-p...
参考文献标题:Analogs of 4-hydroxypyrone: potent,non-peptidic HIV protease inhibitors
文献作者:Romines,K.R.; Thaisrivongs,S.
参考来源:Drugs Fut 1995,20(4),377

IB-643, SPA-S-753

Chemical Name: 21-[3,6-Dideoxy-3-[2-(dimethylamino)acetamido]-beta-D-mannopyranosyloxy]-N-[2-(dimethylamino)ethyl]-15,19-epoxy-3,7,9,11,13,15,17,41-octahydroxy-36,38-dimethyl-43-[4-(methylamino)phenyl...
参考文献标题:Partricin derivs
文献作者:Bruzzese,T.; Signorini,M.; Ottoni,F.(SPA (Societa Prodotti Antibiotici))
参考来源:EP 0489308; US 5298495

MEN-10979

Chemical Name: 12-Ethyl-7-methyl-7,12-dihydro-6H-pyrido[3,2-b]pyrido[2',3':4,5]thieno[3,2-e][1,4]diazepine-6-thione
CAS No. 158150-79-9
项目整合开发状态: Preclinical
项目研究机构: Menarini (Originator)
...
参考文献标题:Diazepin derivs.and antiviral compsns.
文献作者:Giannotti,D.; Pestellini,V.; Viti,G.; Bellarosa,D.; Nannicini,R.; Giachetti,A.(Menarini Industrie Farma Riunite srl)
参考来源:WO 9417075

S-21663, PMS-812

Chemical Name: 1-(2,4-Dichlorobenzyl)-2-(4,5-dihydro-1H-imidazol-2-yl)-4-methylpiperazine
CAS No. 162510-01-2
项目整合开发状态: Preclinical
项目研究机构: Servier (Originator), Univ. Pierre et Marie Curie -...
参考文献标题:Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type II diabetes.1.Synthesis and biological activities of N-benzyl-N'-(arylalkyl)-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines
文献作者:Rondu,F.; Le Bihan,G.; Wang,X.; Lamouri,A.; Touboul,E.; Dive,G.; Bellahsene,T.; Pfeiffer,B.; Renard,P.; Guardiola-Lemaitre,B.; Manechez,D.; Penicaud,L.; Ktorza,A.; Godfroid,J.J.
参考来源:J Med Chem 1997,40(23),3793

Altohyrtin A, Spongistatin 1

Chemical Name: (1S,3S,5R,9R,10R,11R,13R,14S,15R,17S,18R,19R,23Z,25R,27S,29S,31S,33S,36S,37S,38R,41S,43S,49S)-3,37-Diacetoxy-11-[7-chloro-4(S)-hydroxy-2-methylene-5(E),7-octadienyl]-10,14,15,17,27,43-h...
参考文献标题:Total synthesis of altohyrtin A (spongistatin 1): Part 1
文献作者:Guo,J.; et al.
参考来源:Angew Chem.Int Ed Engl 1998,37(1-2),187

ICI-197067

Chemical Name: (-)-2-(3,4-Dichlorophenyl)-N-methyl-N-[2-methyl-1(S)-(pyrrolidin-1-ylmethyl)propyl]acetamide hydrochloride
CAS No. 115199-69-4, 136328-64-8 (free base)
项目整合开发状态: Preclinical
项目...
参考文献标题:2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]-acetamides: The use of conformational analysis in the development of a novel series of potent opioid kappa agonists
文献作者:Costello,G.F.; et al.
参考来源:J Med Chem 1991,34(1),181-9

T-1815

Chemical Name: (?-1-(3,4-Dimethoxybenzyloxymethyl)-N,N-dimethyl-1-(2-thienyl)propylamine 2-(4-hydroxybenzoyl)benzoic acid salt
CAS No. 149998-21-0
项目整合开发状态: Preclinical
项目研究机构: Tanabe Seiyaku...
参考文献标题:T-1815
文献作者:Ozaki,Y.; Sai,H.; Yamada,K.; Onoda,Y.
参考来源:Drugs Fut 1995,20(8),788

Saussureamine A

Chemical Name: (+)-1-[(3R,3aS,6E,10E,11aS)-6,10-Dimethyl-2-oxo-2,3,3a,4,5,8,9,11a-octahydrocyclodeca[b]furan-3-ylmethyl]pyrrolidine-2(S)-carboxylic acid
CAS No. 148245-82-3
项目整合开发状态: Biological ...
参考文献标题:Absolute stereostructures and syntheses of saussureamines A,B,C,D and E,amino acid-sesquiterpene conjugates with gastroprotective effect,from the roots of Saussurea lappa
文献作者:Matsuda,H.; et al.
参考来源:Tetrahedron 2000,56(39),7763