其它产品项目整合

项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点：源头优选：利用如N-硝胺化学等底层方法学突破，从分子层面颠覆传统高成本、高污染路线。过程强化：依托连续流技术，攻克有机金属试剂应用、光化学反应放大等“不可能”任务，实现高危工艺的本质安全。系统集成：整合“反应-淬灭-分离”全流程，利用微流控与在线分析技术，消除批次间的差异，实现药品制造的连续化与智能化。当前，中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合，将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势，将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
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其它产品项目整合

Troglitazone CAS Registry Number: 97322-87-7 曲格列酮

CAS Name: 5-[[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]phenyl]methyl]-2,4-thiazolidinedione
Additional Names: (±)-5-[4-[(6-hydroxy-2,5,7,8-tetramethylchro...
Literature References: Oral hypoglycemic agent which improves insulin sensitivity and decreases hepatic glucose production. Prepn: JP Kokai 85 51189; T. Yoshioka et al., US 4572912 (1985, 1986 both to Sankyo); T. Yoshioka et al., J. Med. Chem. 32, 421 (1989). Mechanism of action studies: T. P. Ciaraldi et al., Metabolism 39, 1056 (1990); M. Kellerer et al., Diabetes 43, 447 (1994). Clinical evaluation: T. Kuzuya et al., Diabetes Res. Clin. Pract. 11, 147 (1991). Clinical metabolic effects: S. L. Suter et al., Diabetes Care 15, 193 (1992).

Metformin CAS Registry Number: 657-24-9 二甲双胍

CAS Name: N,N-Dimethylimidodicarbonimidic diamide
Additional Names: 1,1-dimethylbiguanide; N,N-dimethyldiguanide; N'-dimethylguanylguanidine; DMGGPercent Composition: C 37.20%, H 8.58%, N 54.22...
Literature References: Oral hypoglycemic agent. Prepn: Werner, Bell, J. Chem. Soc. 121, 1790 (1922); Shapiro et al., J. Am. Chem. Soc. 81, 3728 (1959). Use as antidiabetic: J. J. Sterne, US 3174901 (1965 to Jan Marcel Didier Aron-Samuel). Toxicity: Rx Bulletin 3, 25 (1972). Determn in plasma: S. AbuRuz et al., J. Chromatogr. B 798, 203 (2003). Clinical pharmacokinetics: G. T. Tucker et al., Br. J. Clin. Pharmacol. 12, 235 (1981). Review of pharmacology: L. S. Hermann, Diabete Metab. 5, 233-245 (1979). Metabolic effects and mechanism of action study: M. Stumvoll et al., N. Engl. J. Med. 333, 550 (1995). Review of efficacy in polycystic ovary syndrome: J. M. Lord et al., Br. Med. J. 327, 951-955 (2003); in type 2 diabetes mellitus: S. M. Setter et al., Clin. Ther. 25, 2991-3026 (2003).

Sultamicillin CAS Registry Number: 76497-13-7 舒他西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Aminophenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid [[[(2S,5R)-3,3-dimethyl-4,4-dioxido-7-oxo-4-thia-1-azabicyclo[3.2.0]he...
Literature References: Orally absorbed double ester of sulbactam and ampicillin, q.q.v. Prepn: E. C. Bigham, DE 3018590; eidem, US 4244951 (1980, 1981 both to Pfizer); and pharmacology: B. Baltzer et al., J. Antibiot. 33, 1183 (1980). HPLC determn and pharmacokinetics: H. J. Rogers et al., J. Antimicrob. Chemother. 11, 435 (1983). Clinical trial in pediatric otitis media: K. H. Chan et al., Pediatr. Infect. Dis. J. 12, 24 (1993). Review of antibacterial activity, pharmacokinetics and therapeutic efficacy: H. A. Friedel et al., Drugs 37, 491-522 (1989).

Acyclovir CAS Registry Number: 59277-89-3 阿昔洛韦

CAS Name: 2-Amino-1,9-dihydro-9-[(2-hydroxyethoxy)methyl]-6H-purin-6-one
Additional Names: acycloguanosine; 9-[(2-hydroxyethoxy)methyl]guanineTrademarks: Acicloftal (Bruschettini); Avirase (Lam...
Literature References: Orally active acyclic nucleoside with inhibitory activity towards several herpes viruses. Prepn: H. J. Schaeffer, DE 2539963; idem, US 4199574 (1976, 1980 to Wellcome). Convenient synthesis from guanine: H. Matsumoto et al., Chem. Pharm. Bull. 36, 1153 (1988). Selectivity of action: G. B. Elion et al., Proc. Natl. Acad. Sci. USA 74, 5716 (1977). Chemistry, antiviral activity, metabolism: H. J. Schaeffer et al., Nature 272, 583 (1978). In vitro activity: P. Collins, D. J. Bauer, J. Antimicrob. Chemother. 5, 431 (1979). Effect on herpes simplex infections in mice: H. J. Field et al., Antimicrob. Agents Chemother. 15, 554 (1979); on herpes zoster in immunocompromised patients: H. H. Balfour et al., N. Engl. J. Med. 308, 1448 (1983). Treatment of primary episodes of genital herpes simplex infection: Y. J. Bryson et al., ibid. 916; of recurrent genital herpes: S. E. Straus et al., ibid. 310, 1545 (1984); J. M. Douglas et al., ibid. 1551. HPLC determn in serum and clinical pharmacokinetics: G. Bahrami et al., J. Chromatogr. B 816, 327 (2005). Symposia on pharmacology and clinical studies: Am. J. Med. 73, Suppl. 1A, 1-392 (1982); J. Antimicrob. Chemother. 12, Suppl. B, 1-202 (1983); Scand. J. Infect. Dis. Suppl. 47, 1-176 (1985). Review: R. J. Whitley, J. W. Gnann, Jr., N. Engl. J. Med. 327, 782-789 (1992).

Tolrestat CAS Registry Number: 82964-04-3 托雷斯萘

CAS Name: N-[[6-Methoxy-5-(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
Additional Names: tolrestatinTrademarks: Alredase (Am. Home); Lorestat (Recordati)
Percent Compositio...
Literature References: Orally active aldose reductase inhibitor. Prepn and pharmacology: K. Sestanj et al., EP 59596 (1982 to Ayerst); eidem, J. Med. Chem. 27, 255 (1984). Prevention of cataracts in galactosemic rats: N. Simard-Duquesne et al., Proc. Soc. Exp. Biol. Med. 178, 599 (1985). Kinetics and metabolism in man: D. R. Hicks et al., Clin. Pharmacol. Ther. 36, 493 (1984). Ultraviolet and HPLC determn in serum: D. R. Hicks, M. Kraml, Ther. Drug Monit. 6, 328 (1984). Effect on erythrocyte sorbitol levels in diabetic patients: P. Raskin et al., Clin. Pharmacol. Ther. 38, 625 (1985).

Lenampicillin CAS Registry Number: 86273-18-9 仑氨西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Aminophenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester
Additional Names: ampi...
Literature References: Orally active ampicillin prodrug. Prepn: F. Sakamoto et al., EP 39086; eidem, US 4342693 (1981, 1982 both to Kanebo); F. Sakamoto et al., Chem. Pharm. Bull. 32, 2241 (1984); S. Ikeda et al., ibid. 4316. Metabolism in man, dogs, rats: N. Awata et al., Jpn. J. Antibiot. 38, 1776, 1785, C.A. 104, 161479u, 122550r (1985). Human pharmacokinetics: A. Saito, M. Nakashima, Antimicrob. Agents Chemother. 29, 948 (1986). Series of articles on antibacterial activity, mutagenicity, pharmacology, clinical trials: Chemotherapy (Tokyo) 32, Suppl. 8, pp 1-772 (1984). Acute toxicity data: F. Ogino et al., ibid. 31.

Lisinopril CAS Registry Number: 83915-83-7 赖诺普利二水合物

CAS Name: (S)-1-[N2-(1-Carboxy-3-phenylpropyl)-L-lysyl]-L-proline dihydrateTrademarks: Acerbon (AstraZeneca); Alapril (Mediolanum); Carace (BMS); Coric (BMS); Novatec (Merck Co.); Prinil (Merck ...
Literature References: Orally active angiotensin-converting enzyme (ACE) inhibitor. Prepn: A. A. Patchett et al., EP 12401; E. E. Harris et al., US 4374829 (1980, 1983 both to Merck Co.); M. T. Wu et al., J. Pharm. Sci. 74, 352 (1985). Comprehensive description: D. P. Ip et al., Anal. Profiles Drug Subs. Excip. 21, 233-276 (1992). HPLC determn in urine: Y. C. Wong, B. G. Charles, J. Chromatogr. B 673, 306 (1995). Series of articles in hypertension and congestive heart failure: Am. J. Med. 85, Suppl. 3B, 1-59 (1988). Review of clinical efficacy in myocardial infarction: K. L. Goa et al., Drugs 52, 564-588 (1996). Clinical trial in diabetic retinopathy: N. Chaturvedi et al., Lancet 351, 28 (1998).

Idarubicin CAS Registry Number: 58957-92-9 依达比星

CAS Name: (7S,9S)-9-Acetyl-7-[(3-amino-2,3,6-trideoxy-a-L-lyxo-hexopyranosyl)oxy]-7,8,9,10-tetrahydro-6,9,11-trihydroxy-5,12-naphthacenedione
Additional Names: (1S,3S)-3-acetyl-1,2,3,4,6,11-hex...
Literature References: Orally active anthracycline; analog of daunorubicin, q.v. Prepn: B. Patelli et al. DE 2525633; eidem, US 4046878 (1976, 1977 both to Soc. Farmac. Ital.); and antitumor activity: F. Arcamone et al., Cancer Treat. Rep. 60, 829 (1976). Total synthesis for larger scale preparation: M. J. Broadhurst et al., Chem. Commun. 1982, 158. Synthesis of optically pure isomers: Y. Kimura et al., Bull. Chem. Soc. Jpn. 59, 423 (1986). Metabolism and biodistribution in rats: G. Zini et al., Cancer Chemother. Pharmacol. 16, 107 (1986). HPLC determn in plasma: S. S. N. De Graaf et al., J. Chromatogr. 491, 501 (1989). Clinical pharmacokinetics: H. C. Gillies et al., Br. J. Clin. Pharmacol. 23, 303 (1987). Clinical evaluation of cardiac toxicity: F. Villani et al., Eur. J. Cancer Clin. Oncol. 25, 13 (1989). Reviews of pharmacology and antitumor efficacy: A. M. Casazza, Cancer Treat. Rep. 63, 835-844 (1979); F. Ganzina et al., Invest. New Drugs 4, 85-105 (1986). Symposium on clinical experience in acute leukemias: Semin. Oncol. 17, Suppl. 2, 1-36 (1989).

Oxatomide CAS Registry Number: 60607-34-3 奥沙米特

CAS Name: 1-[3-[4-(Diphenylmethyl)-1-piperazinyl]propyl]-1,3-dihydro-2H-benzimidazol-2-one
Additional Names: 1-[3-[4-(diphenylmethyl)-1-piperazinyl]propyl]-2-benzimidazolinoneTrademarks: Celtec...
Literature References: Orally active anti-allergic agent, related structurally to cinnarizine, q.v., and having a novel biphasic mode of action. Prepn: J. Vandenberk et al., DE 2714437; eidem, US 4250176 (1977, 1981 both to Janssen). Inhibition of release and effects of allergic mediators: F. Awouters et al., Experientia 33, 1657 (1977). In vitro study of inhibition and stimulation of histamine release: M. K. Church et al., Agents Actions 10, 4 (1980). In vivo study: S. Gatti et al., Br. J. Dermatol. 103, 671 (1980). Clinical studies: S. W. Barham, F. Moran, Br. J. Clin. Pract. 34, 323 (1980); E. F. Juniper et al., Clin. Allergy 11, 61 (1981); W. Peremans et al., Dermatologia 162, 42 (1981). Review of pharmacological and clinical studies: D. M. Richards et al., Drugs 27, 210 (1984).

Tranilast CAS Registry Number: 53902-12-8 曲尼司特

CAS Name: 2-[[3-(3,4-Dimethoxyphenyl)-1-oxo-2-propenyl]amino]benzoic acid
Additional Names: N-(3',4'-dimethoxycinnamoyl)anthranilic acidTrademarks: Rizaben (Kissei)
Percent Composition: C 66...
Literature References: Orally active anti-allergic agent. Prepn: K. Harita et al., DE 2402398; idem, US 3940422 (1974, 1976 both to Kissei). Pharmacological properties: H. Azuma et al., Br. J. Pharmacol. 58, 483 (1976). Mechanism of action study: Y. Iijima et al., Biochem. Biophys. Res. Commun. 93, 912 (1980). Clinical study in pediatric bronchial asthma: H. Shioda, Allergy 34, 213 (1979). Toxicity studies: M. Nakazawa et al., Oyo Yakuri 12, 385, 407 (1976), C.A. 88, 115327-8 (1978). Series of articles on teratogenicity tests: Iyakuhin Kenkyu 9, 148-193 (1978), C.A. 88, 130930f, 146300m-303q (1978).