- Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity
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We synthesized derivatives of a natural alkaloid, conolidine, and evaluated these derivatives in the acetic acid-induced writhing test and formalin test in ddY mice after oral administration. As a result, we identified (5S)-6-methyl-1,3,4,5,6,8-hexahydro-7H-2,5-methano[1,5]diazonino[7,8-b]indol-7-one sulfate salt, 15a (DS54360155), with a unique and original bicyclic skeleton, as an analgesic more potent than conolidine. Moreover, 15a did not exhibit mu-opioid receptor agonist activity.
- Arita, Tsuyoshi,Asano, Masayoshi,Kubota, Kazufumi,Domon, Yuki,Machinaga, Nobuo,Shimada, Kousei
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- (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride and synthesis method therefor
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The invention discloses (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride and a synthesis method therefor and belongs to the technical field of organic chemical synthesis. The synthesis methodcomprises the following procedures: subjecting (R)-3-pyridonyl-1-tert-butyl carboxylate, which serves as a raw material, to reactions of four steps, i.e., methanesulfonate synthesis, methyl amination, acetyl loading and tert-butyloxycarbonyl removing salt forming, thereby obtaining the (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride. The synthesis method for the (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride, provided by the invention, is safe, convenient and economical, the obtained (S)-N-methyl-N-(pyrrolidin-3-yl)acetamide dihydrochloride is stable in performance and can be conveniently stored and transported.
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- CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY
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The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
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- Thienopyrimidinone bis-aminopyrrolidine ureas as potent melanin-concentrating hormone receptor-1 (MCH-R1) antagonists
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A series of thienopyrimidinone bis-aminopyrrolidine ureas were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor-1. These compounds exhibit potent binding affinity (Ki = 3 nM) and good in vitro metabolic stability.
- Zhang, Mingzhu,Tamiya, Junko,Nguyen, Linh,Rowbottom, Martin W.,Dyck, Brian,Vickers, Troy D.,Grey, Jonathan,Schwarz, David A.,Heise, Christopher E.,Haelewyn, Jason,Mistry, Monica S.,Goodfellow, Val S.
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p. 2535 - 2539
(2008/02/01)
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- NOVEL COMPOUNDS
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A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R1 is H, C1-6alkyl, - C(A)D, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl or het-C1-4/sub
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Page/Page column 43-44
(2008/06/13)
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