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

Suritozole, MDL-26479

舒立托唑Chemical Name: 5-(3-Fluorophenyl)-2,4-dimethyl-3,4-dihydro-2H-1,2,4-triazole-3-thione
CAS No. 110623-33-1
项目整合开发状态: Phase II
项目研究机构: Aventis Pharma (Originator)
合成路线:The reaction of me...
参考文献标题:MDL 26,479: A potential antidepressant whose mechanism of action involves interaction at the GABAA receptor complex
文献作者:Dudley,M.W.; Baron,B.M.; Sorensen,S.M.; Miller,F.P.
参考来源:29th Annu Meet Amer Coll Neuropsychopharmacol (Dec 10-14,San Juan) 1990,Abst

Tritiozine, Trithiozine

舒美吗啉Chemical Name: 4-(3,4,5-Trimethoxyphenylcarbonothioyl)morpholine
CAS No. 35619-65-9
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:By heating a mixture of 3,4,5-trimethoxybenzaldehyde (I),...
参考文献标题:Trithiozine
文献作者:Castar,J.; de Angelis,L.
参考来源:Drugs Fut 1976,1(8),397

Sulmepride

舒美必利Chemical Name: 5-(Aminosulfonyl)-2-methoxy-N-(1-methylpyrrolidin-2-ylmethyl)benzamide
CAS No. 57479-88-6
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The reaction of imidazole (I) with p...
参考文献标题:Sulmepride
文献作者:Blancafort,P.; Serradell,M.N.; Castar,J.; Sungurbey,J.
参考来源:Drugs Fut 1981,6(2),108

BIA-2-093

艾司利卡西平醋酸盐Chemical Name: Acetic acid 5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10(S)-yl ester
CAS No. 236395-14-5
项目整合开发状态: Phase II
项目研究机构: Bial
合成路线:Oxcarbazepine (I) was reduced wi...
参考文献标题:Substd.dihydrodibenzo[b,f]azepines,method of their preparation,their use in the treatment of some central nervous system disorders,and pharmaceutical compsns.containing them
文献作者:Benes,J.; Vieira Araujo Soares da Silva,P.M.(Portela & Ca.,SA)
参考来源:EP 0751129; US 5753646

Esmolol hydrochloride, ASL-8052, Brevibloc

艾司洛尔Chemical Name: (?-3-[4-[2-Hydroxy-3-(isopropylamino)propoxy]phenyl]propionic acid methyl ester hydrochloride; (?-Methyl p-[2-hydroxy-3-(isopropylamino)propoxy]hydrocinnamate hydrochloride
CAS N...
参考文献标题:Method for treatment or prophylaxis of cardiac disorders
文献作者:Erhardt,P.W.; Bogman,R.J.; O'Donnell,J.P.(Baxter International Inc.)
参考来源:EP 0053435; EP 0065542; US 4387103; WO 8201869

Idebenone, QSA-10, A-68500, CV-2619, Cerestabon, Mnesis, Avan

艾地苯醌Chemical Name: 2,3-Dimethoxy-5-methyl-6-(10'-hydroxydecyl)-1,4-benzoquinone
CAS No. 58186-27-9
项目整合开发状态: Launched-1986
项目研究机构: Takeda (Originator), TAP (Originator), Seber (Licensee)
合...
参考文献标题:Method of producing quinone derivatives
文献作者:Watanabe,M.; Imada,I.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0058057; JP 57131735; US 4831265

ED-71

艾地骨化醇Chemical Name: 2beta-(3-Hydroxypropoxy)-1alpha,25-dihydroxyvitamin D3; (1alpha,2beta,3beta,5Z,7E)-2-(3-Hydroxypropoxy)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
CAS No. 104121-92-8
项...
参考文献标题:Vitamin D3 derivs.having a substituent at 2-position
文献作者:Miyamoto,K.; Kubodera,N.; Ochi,K.; Matsunaga,I.; Murayama,E.(Chugai Pharmaceutical Co.Ltd.)
参考来源:EP 0184206; JP 1986267549; US 4666634

Edonentan hydrate, BMS-207940-02, BMS-207940(anhydrous)

艾多南坦单水合物艾多南坦 Chemical Name: N-[2'-(4,5-Dimethylisoxazol-3-ylsulfamoyl)-4-(2-oxazolyl)biphenyl-2-ylmethyl]-N,3,3-trimethylbutyramide hydrate
CAS No. 264609-13-4, 210891-04-6 (anhydrous), 210891-08-...
参考文献标题:Endothelin antagonists: N-[[2'-[[4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl) [1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphenyl]-2-
文献作者:Barrish,J.C.; Murugesan,N.; Gu,Z.; Morrison,R.A.(Bristol-Myers Squibb Co.)
参考来源:EP 0996618; JP 2002513397; US 6043265; WO 9833780

Elvucitabine, ACH-126443, L-D4FC, beta-L-Fd4C

艾夫他滨Chemical Name: beta-L-2',3'-Didehydro-2',3'-dideoxy-5-fluorocytidine
CAS No. 181785-84-2
项目整合开发状态: Phase II
项目研究机构: Yale University (Originator), Achillion (Licensee), Vion (Licensee)
...
参考文献标题:L-2',3'-Dideoxy nucleoside analogs as anti-hepatitis B (HBV) and anti-HIV agents
文献作者:Lin,T.-S.; Cheng,Y.-C.(Yale University)
参考来源:EP 0707481; JP 1996510747; US 5627160; WO 9427616

Izonsteride, LY-320236

艾宗特来Chemical Name: (4aR,10bR)-8-(4-Ethylbenzothiazol-2-ylsulfanyl)-4,10b-dimethyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolin-3-one
CAS No. 176975-26-1
项目整合开发状态: Phase I/II
项目研究机构: Lilly (Or...
参考文献标题:5alpha-Reductase inhibitors
文献作者:Audia,J.E.; Haehl,K.L.; Kress,T.J.; McQuaid,L.A.; Neubauer,B.L.; Rocco,V.P.; Wepsiec,J.P.(Eli Lilly and Company)
参考来源:CA 2158609; EP 0703221; JP 1996225533; WO 9609046