1204-23-5Relevant academic research and scientific papers
PHARMACEUTICALLY ACCEPTABLE SALTS OF BENZODICYCLOALKANE DERIVATIVE, POLYMORPHIC SUBSTANCE THEREOF, AND APPLICATION THEREOF
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Paragraph 0211; 0215; 0228, (2021/04/02)
The present invention provides a pharmaceutically acceptable salt of benzodicycloalkane derivative and a polymorph thereof, and an application thereof. Specifically, the present invention provides a polymorph of benzobicyclic alkane derivative or a pharma
BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
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Paragraph 0155; 0158, (2019/06/19)
It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
DEZOCINE ANALOGUE
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Paragraph 0086; 0089; 0090, (2018/11/27)
Disclosed in the present invention is a Dezocine analogue, and particularly disclosed are compounds represented by formula (I), (II) and (III), a pharmaceutically acceptable salt or tautomer thereof.
A key intermediate for the preparation method of Eptazocine
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Paragraph 0019-0020; 0022-0023, (2017/11/16)
The present invention discloses a dezocine key intermediate preparation method, 7-methoxy-2-tetralone is used as a starting material for first benzyl-site methylation and then ortho alkylation of the carbonyl group, the dezocine key intermediate can be prepared by three strategies of stepwise synthesis, two-step and one-pot methods. The dezocine key intermediate preparation method has the advantages of simple synthetic route, less steps, high yield simple operation, great reduction of the synthesis cycle, mild reaction conditions, and improvement of the safety of the technology, the low raw material cost and easy industrialization. The preparation cost is greatly reduced by the simple synthesis method, the patient dosage cost is reduced, the national social security spending can be reduced to some extent, and some of the social and economic benefits are produced.
Synthesis of 2-tetralone derivatives by Bi(OTf)3-catalyzed intramolecular hydroarylation/isomerization of propargyl alcohols
Yun, Jihee,Park, Jungmin,Kim, Jaehyun,Lee, Kooyeon
, p. 1045 - 1048 (2015/02/19)
Compared to 1-tetralones, 2-tetralones are expensive, less stable, and difficult to synthesize. A concise Bi-catalyzed method was developed for the synthesis of 2-tetralones from 5-phenylpent-1-yn-3-ol derivatives. Diverse 2-tetralones were obtained in moderate to good yields under mild conditions.
Diterpenoid compounds, compositions thereof and their use as anti-cancer or anti-fungal agents
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, (2008/06/13)
The present invention relates to Diterpenoid Compounds, compositions comprising an effective amount of a Diterpenoid Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering an effective amount of a Diterpenoid Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, or for inducing apoptosis in a cancer or neoplastic cell. The compounds, compositions, and methods of the invention are further useful for treating or preventing a fungal infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a fungus.
Heterocyclic compounds for the treatment of pain and use thereof
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, (2008/06/13)
PCT No. PCT/CA96/00467 Sec. 371 Date Mar. 25, 1998 Sec. 102(e) Date Mar. 25, 1998 PCT Filed Jul. 12, 1996 PCT Pub. No. WO97/03978 PCT Pub. Date Feb. 6, 1997Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 and R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. For the treatment of pain and pharmaceutically acceptable compositions comprising those compounds. The compounds of this invention acts as agonists at the opiate receptor.
POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS
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, (2008/06/13)
Polycyclic alkaloids of formula (I), wherein R 1 is H, C. sub.1-6 alkyl, or C 6-12 aryl optionally substituted with polar groups; R. sub.2 and R 3 are independently H, OH, C 1-6 alkyl,--C(NH)--NH. sub.2, a positively charged group, or C 7-13 aralkyl optionally substituted with NH 2, OH, C 1-6 alkyl, or halogen; or R 2 and R 3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R 4 is H, C 1-6 alkyl, OR 6, SR. sub.6, or N(R. sub.6) 2, wherein each R 6 is independently H, C. sub.1-3 alkyl; X ix O, S, SO, SO 2, or N--R 5, wherein each R 5 is independently H, C 1-6 alkyl, or C 7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor. STR1
Isosteres of the DNA polymerase inhibitor aphidicolin as potential antiviral agents against human herpes viruses
Selwood,Challand,Champness,Gillam,Hibberd,Jandu,Lowe,Pether,Selway,Trantor
, p. 3503 - 3510 (2007/10/02)
A variety of isosteres of the DNA polymerase inhibitor aphidicolin were synthesized as potential antiherpes agents. Modeling studies indicated that the bicyclooctane C, D rings of aphidicolin could be replaced by an aromatic moiety while maintaining the spatial arrangement of the hydroxyl group equivalent to the essential C18 hydroxyl group of aphidicolin. Of the racemic isosteres synthesized only 13, the compound with the greatest structural similarity to aphidicolin, showed any significant antiviral activity in primary assays. An enantioselective synthesis of the compound was carried out and the 4aS isomer 36 was shown to account for the observed antiviral activity noted against herpes simplex virus 1 and human cytomegalovirus.
