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

Amylin CAS Registry Number: 106602-62-4

Additional Names: Diabetes-associated peptide; insulinoma amyloid peptide; islet amyloid polypeptide; IAPP
Literature References: Peptide hormone co-secreted with insulin by pancreatic beta cells in response to a meal or other nutrient stimuli. Affects carbohydrate absorption and disposition; modulates the effects of insulin. Major component of pancreatic amyloid deposits characteristic of noninsulin-dependent diabetes and thought to be involved in insulin resistance. Amylin deficiency occurs in insulin-dependent diabetes and may contribute to excessive insulin sensitivity and a heightened tendency to hypoglycemia. Structurally homologous with calcitonin gene related peptide, sharing certain bioactivities such as vasodilation, osteoclast inhibition, and appetite suppression. Isoln from human insulinoma amyloid: P. Westermark et al., Biochem. Biophys. Res. Commun. 140, 827 (1986); from diabetic islet amyloid: idem et al., Am. J. Pathol. 127, 414 (1987); G. J. S. Cooper et al., Proc. Natl. Acad. Sci. USA 84, 8628 (1987). Review of bioactivities: B. J. Edwards, J. E. Morley, Life Sci. 51, 1899-1912 (1992); T. J. Rink et al., Trends Pharmacol. Sci. 14, 113-118 (1993). Review of role in insulin resistance: B. Leighton, G. J. S. Cooper, Trends Biochem. Sci. 15, 295-299 (1990); in carbohydrate metabolism: A. Young et al., Biochem. Soc. Trans. 23, 325 (1995). Effects on appetite regulation and memory: J. E. Morley et al., Can. J. Physiol. Pharmacol. 73, 1042-1046 (1995). Review of role in age-related disease and therapeutic potential: G. J. S. Cooper, C. A. Tse, Drugs Aging 9, 202-212 (1996).

Charybdotoxin CAS Registry Number: 95751-30-7 卡律(布德)蝎毒素

Additional Names: ChTX; CTX
Percent Composition: C 49.21%, H 6.50%, N 18.58%, O 20.48%, S 5.22%
Literature References: Peptide inhibitor of K+ channels isolated from the venom of the scorpion Leiurus quinquestriatus var. hebraeus. Single chain of 4.3 kDa comprised of 37 amino acids with 3 disulfide linkages. Identification: C. Miller et al., Nature 313, 316 (1985). Purification and amino acid sequence: G. Gimenez-Gallego et al., Proc. Natl. Acad. Sci. USA 85, 3329 (1988). Synthesis: E. E. Sugg et al., J. Biol. Chem. 265, 18745 (1990); P. Lambert et al., Biochem. Biophys. Res. Commun. 170, 684 (1990). NMR structural study: F. Bontems et al., Eur. J. Biochem. 196, 19 (1991). Mechanism of channel block: R. MacKinnon, C. Miller, J. Gen. Physiol. 91, 335 (1988). Characterization of binding sites: J. Vázquez et al., J. Biol. Chem. 264, 20902 (1989); J. Vázquez et al., ibid. 265, 15564 (1990). Use as probe for K+ channels: M. Garcia, G. Gimenez-Gallego, US 4960867 (1990 to Merck Co.).

Pidotimod CAS Registry Number: 121808-62-6 匹多莫德

CAS Name: (4R)-3-[[(2S)-5-Oxo-2-pyrrolidinyl]carbonyl]-4-thiazolidinecarboxylic acid
Additional Names: 3-L-pyroglutamyl-L-thiazolidine-4-carboxylic acid; (R)-3-[(S)-5-oxoprolyl]-4-thiazolidinec...
Literature References: Peptide-like biological response modifier. Prepn: S. Poli, EP 276752; idem, US 4839387 (1988, 1989 both to Poli). Immunostimulant effect in nude mice: A. Vacca et al., Int. J. Immunother. 9, 85 (1993); on human peripheral blood monocytes: M. O. Borghi et al., ibid. 10, 35 (1994). HPLC determn in plasma and urine: G. Coppi, M. Barchielli, J. Chromatogr. 563, 385 (1991). Clinical trial in recurrent acute tonsillitis: P. Careddu et al., Adv. Otorhinolaryngol. 47, 328 (1992). Toxicity study: G. Coppi et al., Arzneim.-Forsch. 44, 1448 (1994). Series of articles on chemistry, pharmacology, toxicology and clinical experience: ibid., 1399-1530.

Carbidopa CAS Registry Number: 28860-95-9 卡别多巴

CAS Name: (aS)-a-Hydrazino-3,4-dihydroxy-a-methylbenzenepropanoic acid monohydrate
Additional Names: (-)-L-a-hydrazino-3,4-dihydroxy-a-methylhydrocinnamic acid monohydrate; a-hydrazino-a-methyl...
Literature References: Peripheral decarboxylase inhibitor. Prepn of DL-form: Pfister, FR M1553 (1962 to Merck Co.), C.A. 59, 12921e (1963); Sletzinger et al., J. Med. Chem. 6, 101 (1963); GB 940596; Chemerda et al., US 3462536 (1963, 1969 both to Merck Co.). Synthesis of the L-form: Karady et al., DE 2062285; DE 2062332 (both 1971 to Merck Co.), C.A. 75, 118122t, 118120r (1971); eidem, J. Org. Chem. 36, 1946, 1949 (1971). Inhibition of dopa decarboxylase: Porter et al., Biochem. Pharmacol. 11, 1067 (1962); Moran, Sourkes, J. Pharmacol. Exp. Ther. 148, 252 (1962); Watanabe et al., Clin. Pharmacol. Ther. 11, 740 (1970). Only the L-form is pharmacologically active: Lotti, Porter, J. Pharmacol. Exp. Ther. 172, 406 (1970).

Fedotozine CAS Registry Number: 123618-00-8 费朵托嗪

CAS Name: (aR)-a-Ethyl-N,N-dimethyl-a-[[(3,4,5-trimethoxyphenyl)methoxy]methyl]benzenemethanamine
Additional Names: (+)-(R)-a-ethyl-N,N-dimethyl-a-[[(3,4,5-trimethoxybenzyl)oxy]methyl]benzylami...
Literature References: Peripheral kappa opioid receptor agonist. Prepn of racemate: NL 80 03601; D. R. Torossian et al., US 4301163 (both 1981 to Soc. Ind. Prod. Synth.); of isomers: G. G. Aubard et al., EP 384088; eidem, US 5245080 (1990, 1993 both to Jouveinal). Mechanism of action and pharmacokinetics in dogs: N. Pascaud et al., J. Pharm. Pharmacol. 42, 546 (1990). Clinical trial in nonulcer dyspepsia: B. Fraitag et al., Dig. Dis. Sci. 39, 1072 (1994).

Alvimopan CAS Registry Number: 156053-89-3 爱维莫潘

CAS Name: N-[(2S)-2-[[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]glycine
Additional Names: [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl...
Literature References: Peripheral mu-opioid receptor antagonist. Prepn: B. E. Cantrell et al., EP 506478; eidem, US 5250542 (1992, 1993 both to Lilly); D. M. Zimmerman et al., J. Med. Chem. 37, 2262 (1994). Improved synthesis: J. A. Werner et al., J. Org. Chem. 61, 587 (1996). Clinical pharmacology: S. S. Liu et al., Clin. Pharmacol. Ther. 68, 66 (2000). Clinical trial in postoperative ileus: A. Taguchi et al., N. Engl. J. Med. 345, 935 (2001); E. R. Viscusi et al., Surg. Endosc. 20, 64 (2006). Review of clinical experience: W. K. Schmidt, Am. J. Surg. 182, Suppl., 27S-38S (2001); and pharmacology: P. Neary, C. P. Delaney, Expert Opin. Invest. Drugs 14, 479-488 (2005).

Methylnaltrexone Bromide CAS Registry Number: 73232-52-7; 83387-25-1 (methylnaltrexonium) 溴甲纳曲酮

CAS Name: 17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-17-methyl-6-oxo-morphinanium bromide
Additional Names: N-cyclopropylmethyl-noroxymorphone methobromide; naltrexone methobromide
Perc...
Literature References: Peripheral opioid receptor antagonist; quaternary derivative of naltrexone, q.v., that does not readily cross the blood brain barrier. Prepn: L. I. Goldberg et al., US 4176186 (1979 to Boehringer Ing.). Determn by HPLC and solid phase extraction in plasma and urine: J. Osinski et al., J. Chromatogr. B 780, 251 (2002). Clinical evaluation in methadone-induced constipation: C.-S. Yuan et al., J. Am. Med. Assoc. 283, 367 (2000). Clinical pharmacokinetics: idem et al., J. Clin. Pharmacol. 45, 538 (2005). Review of therapeutic potential in opioid-induced bowel dysfunction: J. F. Foss, Am. J. Surg. 182, 19S-26S (2001); of preclinical and clinical experience: C.-S. Yuan, J. Support Oncol. 2, 111-117 (2004).

Cadralazine CAS Registry Number: 64241-34-5 2-(6-(乙基(2-羟丙基)氨基)哒嗪-3-基)肼甲酸乙酯

CAS Name: 2-[6-[Ethyl(2-hydroxypropyl)amino]-3-pyridazinyl]hydrazinecarboxylic acid ethyl ester
Additional Names: ethyl 6-[ethyl(2-hydroxypropyl)amino]-3-pyridazinecarbazate; 3-(2-carbethoxyhyd...
Literature References: Peripheral vasodilator similar to hydralazine, q.v. Prepn: C. Carpi et al., BE 811847; eidem, US 3925381; US 4002753 (1974, 1975, 1977 all to ISF); F. Parravicini et al., Farmaco Ed. Sci. 34, 299 (1979). Analytical profile: L. Citerio et al., Boll. Chim. Farm. 120, 222 (1981). Pharmacology: C. Semeraro et al., J. Cardiovasc. Pharmacol. 3, 455 (1981). HPLC determn in plasma and urine: T. Crolla et al., J. Chromatogr. 310, 139 (1984). Hemodynamic effects in dogs: L. Dorigotti et al., Arzneim.-Forsch. 34, 984 (1984); in humans: B. Persson et al., Eur. J. Clin. Pharmacol. 31, 513 (1987). Pharmacokinetics and metabolism in humans: H. Schütz et al., Eur. J. Drug Metab. Pharmacokinet. 10, 147 (1985); S. A. Hauffe et al., ibid. 217. Preliminary clinical evaluations: R. Buoninconti, M. Motolese, Int. J. Clin. Pharmacol. Ther. Toxicol. 23, 613 (1985); A. Salvadeo et al., Arzneim.-Forsch. 35, 623 (1985).

Ciclosidomine CAS Registry Number: 66564-16-7 环西多明

CAS Name: N-(Cyclohexylcarbonyl)-3-(4-morpholinyl)sydnone imine
Percent Composition: C 55.70%, H 7.19%, N 19.99%, O 17.12%
Literature References: Peripheral vasodilator similar to molsidomine. Prepn: FR 1551013; GB 1198283 (1968, 1970 both to Boehringer, Ing.). Clinical evaluation: J. Vos, E. J. D. Mees, Br. J. Clin. Pharmacol. 8, 155 (1979). Effect on blood pressure and heart rate: R. G. Shanks et al., ibid. 18, 232 (1984). Tissue distribution and excretion: M. R. Matteo et al., Arzneim.-Forsch. 35, 329 (1985).

Propentofylline CAS Registry Number: 55242-55-2 普罗潘非林

CAS Name: 3,7-Dihydro-3-methyl-1-(5-oxohexyl)-7-propyl-1H-purine-2,6-dione
Additional Names: 3-methyl-1-(5-oxohexyl)-7-propylxanthine; 1-(5'-oxohexyl)-3-methyl-7-propylxanthineTrademarks: Hexto...
Literature References: Peripheral vasodilator which inhibits cyclic AMP phosphodiesterase. Prepn: W. Mohler et al., DE 2330742; eidem, US 4289776 (1975, 1981 both to Hoechst). Cardiovascular effects in animals: O. Hudlicka et al., Br. J. Pharmacol. 72, 723 (1981). Effect on cAMP phosphodiesterase: K. Nagata et al., Arzneim.-Forsch. 35, 1034 (1985). Inhibition of adenosine uptake: B. B. Fredholm, K. Lindström, Acta Pharmacol. Toxicol. 58, 187 (1986). Cerebrovascular effects in animals: J. J. Grome et al., Drug Dev. Res. 5, 111 (1985). Effect on postischemic brain edema: B. B. Mrsulja et al., ibid. 6, 339 (1985). Effect on cognitive function in humans: I. Hindmarch, Z. Subhan, ibid. 5, 379 (1985). Acute toxicity: M. Inazu et al., Oyo Yakuri 31, 357 (1986), C.A. 104, 218960a (1986).