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

Nitrendipine, Bay-e-5009, Baylotensin, Baypress, Bayotensin

尼群地平Chemical Name: (?-2,6-Dimethyl-4-(4-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid ethyl methyl diester
CAS No. 39562-70-4
项目整合开发状态: Launched-1985
项目研究机构: Bayer (Originator), Almi...
参考文献标题:Verfahren zur Herstellung con neuen unsymmetrischen 1,4-Dihydropyridindicarbos鋟reestern
文献作者:Meyer,H.; Bossert,F.(Bayer AG)
参考来源:CA 934758; CH 571492; DD 104520; DE 2117573; NL 7204695

Nimodipine, Bay-e-9736, Periplum, Admon, Nimotop

尼莫地平Chemical Name: 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 3-isopropyl 5-(2-methoxyethyl) diester
CAS No. 66085-59-4
项目整合开发状态: Launched-1985
项目研究机构: Bayer (Or...
参考文献标题:Nimodipine
文献作者:Castar,J.; Serradell,M.N.; Mealy,N.E.; Blancafort,P.; Leeson,P.A.
参考来源:Drugs Fut 1981,6(2),98

Niludipine, Bay a-7168

尼鲁地平Chemical Name: 2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid bis(2-propoxyethyl) diester
CAS No. 22609-73-0
项目整合开发状态: Not Determined
项目研究机构:
合成路线:By cycliza...
参考文献标题:
文献作者:Bossert,F.; Vater,W.
参考来源:BE 712482; CA 867388; CH 515236; DE 1670824; FR 1579533; FR M 7896; GB 1173104; JP 7137349; NL 6803817; US 3488359; US 3574843

Nilutamide, RU-23908, Nilandron, Anandron

尼鲁米特Chemical Name: 5,5-Dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]-2,4-imidazolidinedione; 5,5-Dimethyl-3-(alpha,alpha,alpha-trifluoro-4-nitro-m-tolyl)hydantoin
CAS No. 63612-50-0
项目整合开发状态: L...
参考文献标题:1-(3-(4-O-Trifluoromethyl-4-(4-O-nitrophenyl)-4,4-dimethyl)imidazolidines
文献作者:Perronet,J.; Girault,P.; Bonne,C.(Aventis Pharma SA)
参考来源:DE 2649925; ES 452746; FR 2329276; FR 7533084; GB 1518444; JP 52057176; US 4097578

FR-190809

尿素,N-环庚基-N-((4-(4-氟苯氧基)苯基)甲基)-N'-(6-甲基-2,4-双(甲基磺酰)-3-吡啶基)-Chemical Name: N-Cycloheptyl-N-[4-(4-fluorophenoxy)benzyl]-N'-[6-methyl-2,4-bis(methylsulfonyl)pyridin-3-yl]urea
CAS No. 215589-63-2
项目整...
参考文献标题:Inhibitors of acyl-CoA:cholesterol O-acyltransferase.3.Discovery of a novel series of N-alkyl-N-[(fluorophenoxy)benzyl]-N'-arylureas with weak toxicological effects on adrenal glands
文献作者:Tanaka,A.; Terasawa,T.; Hagihara,H.; Ishibe,N.; Sawada,M.; Sakuma,Y.; Hashimoto,M.; Takasugi,H.; Tanaka,H.
参考来源:J Med Chem 1998,41(22),4408

Droxicam, E-3128, Drogelon, Ferpan, Ombolan

屈昔康Chemical Name: 5-Methyl-3-(2-pyridinyl)-2H,5H-1,3-oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide
CAS No. 90101-16-9
项目整合开发状态: Withdrawn
项目研究机构: Esteve (Originator), Provesan (O...
参考文献标题:A chlorobenzhydryl piperazine derivative
文献作者:Milani,C.; Carminati,G.M.; Sovera,A.(3M Pharmaceuticals)
参考来源:DE 2950378

Droloxifene, FK-435, K-060, K-21060E

屈洛昔芬枸橼酸屈洛昔芬 Chemical Name: (E)-3-[1-[4-[2-(Dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]phenol; (E)-1-[4'-(2-Dimethylaminoethoxy)phenyl]-1-(3'-hydroxyphenyl)-2-phenylbut-1-ene; (E)-alpha-[p-[2-(Di...
参考文献标题:1,1,2-triphenylbut-1-ene derivatives
文献作者:Schickaneder,H.; Ler,R.; Grill,H.(Klinge Pharma GmbH)
参考来源:DE 3046719; EP 0054168; US 5047431

Dihydrospirorenone, 1, 2-Dihydrospirorenone, Drospirenone, DRSP, SH-470, ZK-30595

屈螺酮Chemical Name: 6beta,7beta:15beta,16beta-Dimethylene-3-oxo-17alpha-preg-4-ene-21,17-carbolactone; (6R,7R,8R,9S,10R,13S,14S,15S,16S,17S)-1,2,3,6,7,8,9,10,11,12,13,14,15,16,20,21-Hexadecahydro-10,13-...
参考文献标题:Process for the preparation of 17alpha-pregnane-21,17-carbolactones
文献作者:Nickisch,K.(Schering AG)
参考来源:DE 3626838

Droxidopa, DOPS(L-threo), Dops

屈西多巴Chemical Name: (-)-threo-beta,3-Dihydroxy-L-tyrosine; (-)-threo-3-(3,4-Dihydroxyphenyl)-L-serine; (-)-(2S,3R)-2-Amino-3-hydroxy-3-(3,4-dihydroxyphenyl)propionic acid
CAS No. 23651-95-8
项目整合开...
参考文献标题:Process for the production of optically active thr
文献作者:Ohashi,N.; Nagata,S.; Ishimuzi,K.; Katsube,J.(Sumitomo Pharmaceuticals Co.,Ltd.)
参考来源:EP 0024210; US 4319040

Mycalamide A

山海绵酰胺AChemical Name: [2R-[2alpha,2[S*(S*)],5beta,6beta]]-4,8-Anhydro-3,5-dideoxy-9-C-[[hydroxy(tetrahydro-2-methoxy-5,6-dimethyl-4-methylene-2H-pyran-2-yl)acetyl]amino]-5,5-dimethyl-6-O-methyl-7,9,O-m...
参考文献标题:Total synthesis of mycalamide A and 7-epi-mycalamide A
文献作者:Roush,W.R.; Pfeifer,L.A.
参考来源:Org Lett 2000,2(6),859