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

Lupitidine hydrochloride, SK&F-93479

鲁匹替丁 Chemical Name: 2-[2-[(5-Dimethylaminomethylfuran-2-yl)methylthio]ethylamino]-5-(6-methylpyridyl-3-ylmethyl)pyrimid-4-one trihydrochloride
CAS No. 72716-75-7, 83903-06-4 (free base)
项目整合开发状...
参考文献标题:Pyrimidine compounds
文献作者:Brown,T.H.; Ife,R.J.(SmithKline Beecham plc)
参考来源:DD 140252; EP 0003677; ES 477667; US 4234588; US 4649141

Lubiprostone, SPI-0211, RU-0211

鲁比前列酮鲁比前列素 Chemical Name: 7-[(2R,4aR,5R,7aR)-2-(1,1-Difluoropentyl)-2-hydroxy-6-oxooctahydrocyclopenta[b]pyran-5-yl]heptanoic acid
CAS No. 333963-40-9, 136790-76-6 (tautomer)
项目整合开发状态: Phase I...
参考文献标题:Prostaglandins E and anti-ulcers containing same
文献作者:Ueno,R.; Kato,I.; Oda,T.(Ueno Fine Chemicals Industry,Ltd.)
参考来源:EP 0284180; JP 1989052753; US 5166174; US 5225439; US 5284858; US 5380709; US 5428062; US 5886034; US 6265440

Oleanolic acid

齐墩果酸Chemical Name: 3beta-Hydroxyolean-12-en-28-oic acid
CAS No. 508-02-1
项目整合开发状态: Preclinical
项目研究机构: Regional Research Laboratory, Jammu-Tawi (Originator)
合成路线:The dihydroxylation of th...
参考文献标题:An exceptionally short and simple enantioselective total synthesis of pentacyclic triterpenes of the beta-amyrin family
文献作者:Huang,A.X.; Corey,E.J.; Xiong,Z.
参考来源:J Am Chem Soc 1999,121(43),9999

TA-993

(-)-(2R,3R)-3-乙氧基-5-[2-(二甲氨基)乙基]-8-甲基-2-(4-甲基苯基)-2,3,4,5-四氢-1,5-苯并噻西平-4-一马来酸盐Chemical Name: (-)-(2R,3R)-3-Acetoxy-5-[2-(dimethylamino)ethyl]-8-methyl-2-(4-methylphenyl)-2,3,4,5-tetrahydro-1,5-benzothi...
参考文献标题:Synthesis and biological evaluation of alkyl,alkoxy,alkylthio,or amino-substituted 2,3-dihydro-1,5-benzothiazepin-4(5H)-ones
文献作者:Inoue,H.; Konda,M.; Hashiyama,T.; Otsuka,H.; Watanabe,A.; Gaino,M.; Takahashi,K.; Date,T.; Okamura,K.; Takeda,M.; Narita,H.; Murata,S.; Odawara,A.; Sasaki,H.; Nagao,T.
参考来源:Chem Pharm Bull 1997,45(6),1008

CY-208-243

(-)-(6aR,12bR)-4,6,6a,7,8,12β-六氢-7-甲基吲哚[4,3-a]菲啶Chemical Name: (-)-trans-4,6,6a,7,8,12b-Hexahydro-7-methylindolo[4,3-ab]phenanthridine; (-)-(6aR,12bR)-7-Methyl-4,6,6a,7,8,12b-hexahydroindolo[4,3-ab]ph...
参考文献标题:Indolophenanthidines,their preparation and use
文献作者:Hagenbach,A.; Seiler,M.P.; Whrich,H.J.(Novartis AG; Novartis Deutschland GmbH)
参考来源:DE 3402392; EP 0155903; ES 8606339; JP 1985197687; US 4634708

Sarizotan, EMR-62225, EMD-128130

(-)-(R)-N-(3,4-二氢-2H-1-苯并呋喃-2-基甲基)-N-[5-(4-氟苯基)-3-吡啶甲基]胺Chemical Name: (-)-(R)-N-(3,4-Dihydro-2H-1-benzofuran-2-ylmethyl)-N-[5-(4-fluorophenyl)-3-pyridylmethyl]amine
CAS No. 177975-08-5
项目整合开发状态...
参考文献标题:Amino(thio)ether derivs.as CNS active agents
文献作者:B鰐tcher,H.; Devant,R.; Greiner,H.; Bartoszyk,G.; Berthelon,J.-J.; Noblet,M.; Zeiller,J.-J.; Brunet,M.(Merck Patent GmbH)
参考来源:CA 2160447; EP 0707007; EP 1123933; JP 1996225501; US 5767132

Mivobulin isethionate, NSC-635370 [(1:1) salt], NSC-370147(racemic hydrate), NSC-350386(racemic HCl hydrate), NSC-613863 [(+)-(R)-isomer], CI-980, NSC-613862(free base)

(-)-(S)-N-(5-氨基-2-甲基-3-苯基-l,2-二氢吡啶并[3,4-b]吡嗪-7-基)氨基甲酸乙酯 2-羟基乙基磺酸盐 (-)-(S)-N-(5-氨基-2-甲基-3-苯基-l,2-二氢吡啶并[3,4-b]吡嗪-7-基)氨基甲酸乙酯 Chemical Name: (-)-(S)-N-(5-Amino-2-methyl-3-phenyl-1,2-dihydropyrido[3,4-b]py...
参考文献标题:(2S)-(5-Amino-1,2-dihydro-2-methyl-3-phenyl-pyrido[3,4-b]pyrazin-7-yl)-carbamic acid,ethyl ester
文献作者:Carroll,T.G.Jr.(Southern Research Institute)
参考来源:EP 0336345; JP 1989305087; US 4866059

KUL-7211

(-)-2-[4-[2-[2(R)-羟基-2-(4-羟基苯基)-1(S)-甲基氨基]乙基苯氧基]醋酸Chemical Name: (-)-2-[4-[2-[2(R)-Hydroxy-2-(4-hydroxyphenyl)-1(S)-methylethylamino]ethyl]phenoxy]acetic acid
CAS No. 220129-58-8
项目整合开发状态: Phase...
参考文献标题:Aminoethylphenoxyacetic acid derivs.and drugs for pain remission and calculi removal promotion in urinary lithiasis
文献作者:Tamai,T.; Akahane,M.; Mukaiyama,H.; Muranaka,H.; Tanaka,N.; Sato,M.; Hirabayashi,A.(Kissei Pharmaceutical Co.,Ltd.)
参考来源:EP 1002791; WO 9905090

MN-221, KUR-1246

(-)-2-[7(S)-[2(R)-羟基-2-[4-羟基-3-(2-羟基)苯基]乙基胺]-5,6,7,8-四氢萘-2-亚氧]-N,N-二甲基乙酰胺硫酸盐(2:1) 贝多拉君 Chemical Name: (-)-2-[7(S)-[2(R)-Hydroxy-2-[4-hydroxy-3-(2-hydroxyethyl)phenyl]ethylamino]-5,6,7,8-tetrahydronap...
参考文献标题:3,4-Disubstd.phenylethanolaminotetralincarboxamide derivs.
文献作者:Kitazawa,M.; Okazaki,K.; Tamai,T.; Saito,M.; Muranaka,H.; Tanaka,N.; Kobayahi,H.; Kikuchi,K.(Kissei Pharmaceutical Co.,Ltd.)
参考来源:EP 0882704; US 6133266; WO 9730023

Hydroxymethylacylfulvene, Irofulven, NSC-683863, 6-HMAF, HMAF, MGI-114

(-)-伊洛福芬Chemical Name: 6'(R)-Hydroxy-3'-(hydroxymethyl)-2',4',6'-trimethyl-6',7'-dihydrospiro[cyclopropane-1,5'-[5H]inden]-7'-one
CAS No. 158440-71-2
项目整合开发状态: Phase II
项目研究机构: MGI (Orphan Dr...
参考文献标题:A short synthesis of the potent antitumor agent (?-hydroxymethylacylfulvene using allenic pauson-khand type cycloaddition
文献作者:Brummond,K.M.; Lu,J.
参考来源:J Am Chem Soc 1999,121(21),5087