- Pyrazolo [3, 4 - c] pyridine - 7 - ketone compound and use thereof
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Belonging to the technical field of medicine, the invention relates to a 4, 5-dihydro-1H-pyrazolo[3, 4-c]pyridine-7-one containing derivative shown as general formula I, and pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein the substituents A, R1 and R2 have meanings given in the specification. The preparation also relates to a preparation method of the general formula I compound and its pharmaceutically acceptable salt or prodrug, medicinal compositions containing the compound and application of the compound as an Xa factor inhibitor, especially application in preparation of drugs for treatment and/or prevention of thromboembolic diseases. (formula I).
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Paragraph 0197; 0238; 0241; 0242
(2017/09/01)
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- A morpholine-free process amenable convergent synthesis of apixaban: a potent factor Xa inhibitor
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A convergent synthesis of the anti-coagulant drug apixaban has been efficiently demonstrated on a multi-gram scale. The synthetic route is noteworthy for its brevity and fact that it completely avoids the use of morpholine, a toxic and flammable reagent, in constructing the 5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one core present in apixaban. Graphical abstract: [Figure not available: see fulltext.].
- Nevuluri, Narasimha Rao,Rapolu, Rajesh Kumar,Iqbal, Javed,Kandagatla, Bhaskar,Sen, Saikat,Dahanukar, Vilas H.,Oruganti, Srinivas
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p. 1477 - 1482
(2017/07/18)
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- HYDRAZINE COMPOUND AS BLOOD COAGULATION FACTOR Xa INHIBITOR
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Provided is a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is selected from a 3-9 membered carbon ring or its phenyl ring, and a 4-10 membered heterocyclic ring or its benzo ring; Y and Z are independently selected from 4-9 membered saturated heterocyclic rings respectively; RI-3 are independently selected from H, F, Cl, Br, I, CN, OH, SH,NH2, CHO, COOH respectively, or selected from C1-10 alkyls or heteroalkyls optionally substituted by R01, C3-10 alkyls ring hydrocarbon groups or heterocyclic hydrocarbon groups, C1-10 alkyls or heteroalkyls substituted by C3-10 ring hydrocarbon groups or heterocyclic hydrocarbon group. The compound can be used as an anticoagulant for treating and preventing thrombotic disorders, and can meet the real needs of selectivity and a potent inhibitor for coagulation Xa.
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Paragraph 0083
(2017/04/11)
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- Containing a lactam substituent pyrazole piperidine ketone compound, and its composition and use thereof
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The present invention relates to a pyrazolo piperidone compound and a pharmaceutically acceptable composition thereof and use thereof in preparation of medicines for treating Xa-factor associated diseases, and particularly relates to a novel lactam substituent-containing pyrazolo piperidone compound and a pharmaceutical composition containing the compound and use of the compound in preparation of the medicines for the treating Xa-factor associated diseases.
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Paragraph 0151; 0152; 0153
(2016/10/08)
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- Pyrazole substituent comprising cyclonexane and piperidine ketone compound, and its composition and use thereof
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The invention relates to a pyrazolo piperidone compound and a pharmaceutically acceptable composition thereof and application thereof to preparation of medicaments for treating diseases associated with an Xa factor. In particular, the invention relates to a novel pyrazolo piperidone compound containing a cyclohexane substituent, the pharmaceutical composition containing the compound, and application of the compounds to preparation of medicaments for treating diseases associated with the Xa factor.
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Paragraph 0150; 0151; 0152
(2016/10/08)
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- Aromatic ring containing substituted methyl substituted pyrazole piperidine ketone compound, and its composition and use thereof
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The invention relates to pyrazolopiperidone compounds, pharmaceutically-acceptable salts of the compounds and use of the compounds in preparation of medicines for treating Xa factor related diseases. Particularly, the invention relates to novel methyl substituted aromatic ring substituent-containing pyrazolopiperidone compounds, pharmaceutical compositions containing the compounds and use of the compounds in the preparation of the medicines for treating the Xa factor related diseases.
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Paragraph 0155; 0156; 0157
(2016/10/09)
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- Containing thiazole pyrazole piperidine ketone compound, and its composition and use thereof
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The invention relates to a pyrazolo piperidone compound and a pharmaceutically acceptable composition thereof and application thereof to preparation of medicaments for treating diseases associated with an Xa factor. In particular, the invention relates to a novel pyrazolo piperidone compound containing thiazole, the pharmaceutical composition containing the compound, and application of the compounds to preparation of medicaments for treating diseases associated with the Xa factor.
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Paragraph 0147; 0148
(2016/10/10)
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- Containing substituted butynyl pyrazole piperidine ketone compound, and its composition and use thereof
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The invention relates to pyrazolopiperidone compounds, pharmaceutically-acceptable salts of the compounds and use of the compounds in preparation of medicines for treating Xa factor related diseases. Particularly, the invention relates to novel substitute butynyl-containing pyrazolopiperidone compounds, pharmaceutical compositions containing the compounds and use of the compounds in the preparation of the medicines for treating the Xa factor related diseases.
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Paragraph 0151; 0152; 0153
(2016/10/10)
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- Containing diketone substituent pyrazole piperidine ketone compound, and its composition and use thereof
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The invention relates to a pyrazolo piperidone compound and a pharmaceutically acceptable composition thereof and application thereof to preparation of medicaments for treating diseases associated with an Xa factor. In particular, the invention relates to a novel pyrazolo piperidone compound containing a dione substituent, the pharmaceutical composition containing the compound, and application of the compounds to preparation of medicaments for treating diseases associated with the Xa factor.
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Paragraph 0140-0141
(2017/01/17)
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- Fused-ring pyrazoles and piperidine ketone compound, and its composition and use thereof (by machine translation)
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The invention relates to a pyrazolo piperidone compound and a pharmaceutically acceptable composition thereof and application thereof to preparation of medicaments for treating diseases associated with an Xa factor. In particular, the invention relates to a novel pyrazolo piperidone compound containing condensed ring, the pharmaceutical composition containing the compound, and application of the compounds to preparation of medicaments for treating diseases associated with the Xa factor.
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Paragraph 0154; 0155
(2017/02/24)
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- Containing acyl piperazones substituent pyrazole piperidine ketone compound, and its composition and use thereof (by machine translation)
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The invention relates to pyrazolopiperidone compounds, pharmaceutically-acceptable salts of the compounds and use of the compounds in preparation of medicines for treating Xa factor related diseases. Particularly, the invention relates to novel acyl piperazinone substituent-containing pyrazolopiperidone compounds, pharmaceutical compositions containing the compounds and use of the compounds in the preparation of the medicines for treating the Xa factor related diseases.
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Paragraph 0144-0146
(2017/02/28)
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- Containing oxime substituent pyrazole piperidine ketone compound, and its composition and use thereof
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The invention relates to pyrazolopiperidone compounds, pharmaceutically-acceptable salts of the compounds and use of the compounds in preparation of medicines for treating Xa factor related diseases. Particularly, the invention relates to novel oxime substituent-containing pyrazolopiperidone compounds, pharmaceutical compositions containing the compounds and use of the compounds in the preparation of the medicines for treating the Xa factor related diseases.
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Paragraph 0153-0155
(2017/02/28)
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- CA amide analogs and its preparation method and application
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The invention relates to the technical field of medicines. Piplartine is alkaloid extracted from perennial herbaceous vine piper longum of piperaceae. The invention provides a Piplartine analogue, which comprises a cis-trans-isomer, and any arbitrary mixture in those forms or medicinal salt thereof, and the structural formula of the Piplartine analogue is shown in a general formula (I). The invention also provides a preparation method of substituted Piplartine compounds, and an application thereof in preparation of an antitumor medicament.
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- Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents
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In an effort to expand the structure-activity relationship of the natural anticancer compound piperlongumine, we have prepared sixteen novel piperlongumine derivatives with halogen or morpholine substituents at C2 and alkyl substituents at C7. Most of 2-halogenated piperlongumines showed potent in vitro activity against four cancer cells and modest selectivity for lung normal cells. The highly active anticancer compound 11h exhibited obvious ROS elevation and excellent in vivo antitumor potency with suppressed tumor growth by 48.58% at the dose of 2 mg/kg. The results indicated that halogen substituents as electrophilic group at C2 played an important role in increasing cytotoxicity.
- Wu, Yuelin,Min, Xiao,Zhuang, Chunlin,Li, Jin,Yu, Zhiliang,Dong, Guoqiang,Yao, Jiangzhong,Wang, Shengzheng,Liu, Yang,Wu, Shanchao,Zhu, Shiping,Sheng, Chunquan,Wei, Yunyang,Zhang, Huojun,Zhang, Wannian,Miao, Zhenyuan
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p. 545 - 551
(2014/07/07)
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- LINEAR CHAIN SUBSTITUTED MONOCYCLIC AND BICYCLIC DERIVATIVES AS FACTOR XA INHIBITORS
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The present application descirbes linear chain subtituted monocyclic and byciclic compounds and derivatives thereof of formula (I): P4-P-M-M4 or pharmaceutically acceptable salts from thereof, P-M are rings substituted by a linear group. Compounds of the present invention are useful as inhibitors of trypsin like serine proteases, specifically factor Xa.
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- Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones
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A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.
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