545445-40-7Relevant academic research and scientific papers
Pyrazolo [3, 4 - c] pyridine - 7 - ketone compound and use thereof
-
Paragraph 0197; 0238; 0241; 0242, (2017/09/01)
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).
A morpholine-free process amenable convergent synthesis of apixaban: a potent factor Xa inhibitor
Nevuluri, Narasimha Rao,Rapolu, Rajesh Kumar,Iqbal, Javed,Kandagatla, Bhaskar,Sen, Saikat,Dahanukar, Vilas H.,Oruganti, Srinivas
, p. 1477 - 1482 (2017/07/18)
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.].
HYDRAZINE COMPOUND AS BLOOD COAGULATION FACTOR Xa INHIBITOR
-
Paragraph 0083, (2017/04/11)
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.
Containing a lactam substituent pyrazole piperidine ketone compound, and its composition and use thereof
-
Paragraph 0151; 0152; 0153, (2016/10/08)
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.
Pyrazole substituent comprising cyclonexane and piperidine ketone compound, and its composition and use thereof
-
Paragraph 0150; 0151; 0152, (2016/10/08)
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.
Aromatic ring containing substituted methyl substituted pyrazole piperidine ketone compound, and its composition and use thereof
-
Paragraph 0155; 0156; 0157, (2016/10/09)
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.
Containing thiazole pyrazole piperidine ketone compound, and its composition and use thereof
-
Paragraph 0147; 0148, (2016/10/10)
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.
Containing substituted butynyl pyrazole piperidine ketone compound, and its composition and use thereof
-
Paragraph 0151; 0152; 0153, (2016/10/10)
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.
Containing diketone substituent pyrazole piperidine ketone compound, and its composition and use thereof
-
Paragraph 0140-0141, (2017/01/17)
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.
Fused-ring pyrazoles and piperidine ketone compound, and its composition and use thereof (by machine translation)
-
Paragraph 0154; 0155, (2017/02/24)
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.
