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

Wy-50295 tromethamine

(2S)-2-[6-(喹啉-2-基甲氧基)萘-2-基]丙酸Chemical Name: S-(+)-alpha-Methyl-6-(2-quinolinylmethoxy)-2-naphthaleneacetic acid 2-hydroxy-1,1-bis(hydroxymethyl)ethylamine salt
CAS No. 123016-21-7 (free acid)
项目...
参考文献标题:2-Aryl substituted heterocyclic compounds as antiallergic and antiinflammatory agents
文献作者:Kreft,A.F.; Musser,J.H.; Bicksler,J.J.; Giberson,J.W.; Kubrak,D.M.(American Home Products Corp.)
参考来源:AU 8819209; EP 0301813; GB 2207428; US 5208344

LY-341495

(2S)-2-氨基-2-[(1S,2S)-2-羧基环丙-1-基]-3-(吨-9-基)丙酸Chemical Name: 2(S)-Amino-2-[2(S)-carboxy-1(S)-cyclopropyl]-3-(9H-xanthen-9-yl)propionic acid
CAS No. 201943-63-7
项目整合开发状态: Preclinical
项目研究机构: Lil...
参考文献标题:2-Substituted (2SR)-2-amino-2-(1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors.2.Effects of aromatic substitution,pharmacological characterization,and bioavailability
文献作者:Ornstein,P.L.; Bleisch,T.J.; Brian Arnold,M.; Kennedy,J.H.; Wright,R.A.; Johnson,B.G.; Tizzano,J.P.; Helton,D.R.; Kallman,M.J.; Schoepp,D.D.; Herin,M.
参考来源:J Med Chem 1998,41(3),358

Rebimastat, D-2163, BMS-275291

(2S)-3,3-二甲基-2-甲基氨基-N-[(2S)-4-甲基-2-[[(2S)-2-硫基-4-(3,4,4-三甲基-2,5-二氧代-咪唑烷-1-基)丁酰基]氨基]戊酰]丁酰胺Chemical Name: N-[2(S)-Sulfanyl-4-(3,4,4-trimethyl-2,5-dioxoimidazolidin-1-yl)butyryl]-L-leucyl-L-tert-leucine ...
参考文献标题:Thio-substd.peptides as inhibitors for metalloproteinases and TNF liberation
文献作者:Baxter,A.D.; Montana,J.G.; Owen,D.A.(Celltech Chiroscience Ltd.)
参考来源:JP 1999512733; WO 9712902

ST-789, PCF-39

(2S)-5-(二氨基亚甲基氨基)-2-[5-(6-氧代-3H-嘌呤-9-基)戊氧基羰基氨基]戊酸Chemical Name: N2-[5-(Hypoxanthin-9-yl)pentyloxycarbonyl]-L-arginine; Nalpha-5-(1,6-Dihydro-6-oxo-9-purinyl)pentyloxycarbonyl-L-arginine
CAS No. 104...
参考文献标题:PCF-39
文献作者:Stradi,R.; Cornaglia-Ferraris,P.; Perezzani,L.S.; Forni,G.; Riccardi,C.
参考来源:Drugs Fut 1987,12(2),134

DMP-777, L-694458

(2S)-N-[(1R)-1-(1,3-苯并二氧戊环-5-基)丁基]-3,3-二乙基-2-[4-[(4-甲基-1-哌嗪基)羰基]苯氧基]-4-氧代-1-氮杂环丁烷甲酰胺Chemical Name: 3,3-Diethyl-N-[1(R)-(3,4-methylenedioxyphenyl)butyl]-2(S)-[4-(4-methylpiperazin-1-ylcarbonyl)phenoxy]...
参考文献标题:New substd.azetidinones as antiinflammatory and antidegenerative agents
文献作者:Doherty,J.B.; Finke,P.E.; Dorn,C.P.; Maccoss,M.; Durette,P.L.; Mills,S.G.; Shah,S.K.; Lanza,T.J.; Sahoo,S.P.; Hagmann,W.K.; Hale,J.J.(Merck & Co.,Inc.)
参考来源:EP 0595557; JP 1994263723; US 5591737; US 5747485; WO 9410142

DAPT, LY-374973, AN-37124

(2S)-N-[N-(3,5-二氟苯乙酰基)-L-丙氨酰]-2-苯基甘氨酸叔丁酯Chemical Name: N-[2-(3,5-Difluorophenyl)acetyl]-L-alanyl-L-(2-phenyl)glycine tert-butyl ester
CAS No. 208255-80-5
项目整合开发状态: Preclinical
项目研究机构: Elan (O...
参考文献标题:Methods and cpds.for inhibiting beta-amyloid peptide release and/or its synthesis
文献作者:Porter,W.J.; Eid,C.N.; Audia,J.E.; Britton,T.C.; Latimer,L.H.; Droste,J.J.; Scott,W.L.; Wu,J.; Tung,J.S.; Thorsett,E.D.; John,V.; Huffman,G.W.; (Athena Neurosciences,Inc.; Eli Lilly and Company)
参考来源:JP 2001503782; WO 9822494

Pobilukast, SK&F-104353-Q(as edamide, monohydrate), SK&F-104353-Z2(diNa salt), SK&F-104353

(2S,3R)-3-(2-羧基乙基硫基)-2-羟基-3-[2-(8-苯基辛基)苯基]丙酸Chemical Name: 2(S)-Hydroxy-3(R)-(2-carboxyethylthio)-3-[2-(8-phenyloctyl)phenyl]propanoic acid
CAS No. 107023-41-6, 137232-03-2 (ethylenediamine (1:1), ...
参考文献标题:High affinity leukotriene receptor antagonists.Synthesis and pharmacological characterization of 2-hydroxy-3-(2-carboxy-ethylthio)-3-[2-(8-phenoyloctyl)propanoic acids
文献作者:Gleason,J.G.; Hall,R.F.; Perchonock,C.D.; et al.
参考来源:J Med Chem 1987,30(6),959-61

Fedotozine tartrate, JO-1196

(2S,3S)-2,3-二羟基琥珀酸-(2R)-N,N-二甲基-2-苯基-1-[(3,4,5-三甲氧基苄基)氧基]-2-丁胺(1:1) 费朵托嗪 Chemical Name: (+)-(R)-alpha-Ethyl-N,N-dimethyl-alpha-(3,4,5-trimethoxyphenylmethoxymethyl)benzenemethanamine l-tartrate; (+)-...
参考文献标题:Fedotozine Tartrate
文献作者:Homerin,M.; Gen鑦e,J.; Karaus,M.; Kber,J.
参考来源:Drugs Fut 1992,17(2),101

CI-1012, PD-161374

(2S,3S)-3-甲基-2-(3-氧代-1,2-苯并噻唑-2(3H)-基)戊酸Chemical Name: 3(S)-Methyl-2(S)-(3-oxo-2,3-dihydro-1,2-benzisothiazol-2-yl)pentanoic acid
CAS No. 177785-47-6
项目整合开发状态: Phase II
项目研究机构: Pfizer (Origin...
参考文献标题:Development and pilot-scale demonstration of a process for inhibitors of the HIV nucleocapsid protein,NCp7
文献作者:Fiore,P.J.; et al.
参考来源:Org Process Res Dev 1998,2(3),151

TAK-726

(2S,3S)-N-[(1S)-1-甲酰基-2-(1H-吲哚-3-基)乙基]-3-甲基-2-[(1-萘基磺酰基)氨基]戊酰胺Chemical Name: 1-Naphthylsulfonyl-L-isoleucyl-L-tryptophanal
CAS No. 161709-56-4
项目整合开发状态: Preclinical
项目研究机构: Takeda (Originator...
参考文献标题:Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption
文献作者:Yasuma,T.; Oi,S.; Choh,N.; Nomura,T.; Furuyama,N.; Nishimura,A.; Fujisawa,Y.; Sohda,T.
参考来源:J Med Chem 1998,41(22),4301