- INDOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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PROBLEM TO BE SOLVED: To provide a compound having EP1 receptor antagonism, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the same and a medical use thereof. SOLUTION: There is provided a compound having EP1 receptor antagonism and represented by the general formula (I), where A is a pyridine ring or the like, Y1 is a C1-6 alkylene group or the like, Y2 is a single bond or the like, R1 is a hydrogen atom or the like, R2 is a C3-6 cycloalkylene group with a ring substituted by a C1-6 alkyl group or the like, R3 is a carboxyl group or the like, R4 is a hydrogen atom, R5 is a hydrogen atom or the like, R6 is a C1-6 alkyl group or the like and R7 represents a hydrogen atom or the like, or a pharmaceutically acceptable salt thereof. The compound (I) can further used as a therapeutic agent or prophylactic agent for various symptoms of LUTS, especially OABs. COPYRIGHT: (C)2015,JPOandINPIT
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Paragraph 0202
(2020/10/21)
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- Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
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The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
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- 4. Synthese von Plectranthonen, diterpenoiden Phenanthren-1,4-chinonen
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The following phenanthrene-1,4-diones have been synthesized by using the photocyclization of the corresponding highly substituted stilbenes as the key step: 3-hydroxy-5,7,8-trimethyl-2-(prop-2-enyl)phenanthrene-1,4-dione (1), (RS)-, (R)-, and (S)-2--1-methylethyl)acetate (2, 31, and 32, resp.), 3-hydroxy-7,8-dimethyl-2-(prop-2-enyl)phenanthrene-1,4-dione (3), 3-hydroxy-7,8,10-trimethyl-2-(prop-2-enyl)phenanthrene-1,4-dione (4), 5,7,8-trimethyl-2-(prop-2-enyl)phenanthrene-1,4-dione (17) and 3-hydroxy-2-methylphenanthrene-1,4-dione (42).The quinones 1 and 3 proved to be identical with recently isolated plectranthons A and C.Compounds 2, 31, and 32 exhibited the same UV/VIS, IR, 1H-NMR and mass spectra as natural plectranthon B, but had different melting points.This might be due either to crystal modifications or to diastereoisomerism caused by the helical structure of the phenanthrene-1,4-dione skeleton.The spectral data of synthetic 4 were not compatible with those of natural plectranthon D for which structure 4 had been proposed based mainly on 1H-NMR arguments concerning the chemical shifts of H-C(9) and H-C(10) in 1-3.Extensive 1H-NMR investigations have now revealed that the currently stated assignments of the H-C(9)/H-C(10) AB system have to be reversed for highly substituted phenanthrene-1,4-diones: in the model compounds 2-methylphenanthrene-1,4-dione (41) and 2, H-C(10) resonates at lower field as expected (peri-position), whereas in the highly substituted congeners 1, 2, 3, 31, and 32, H-C(9) is shifted paramagnetically, a fact which had lead to the erroneous assignment of structure 4 for natural plectranthon D.
- Kaliakoudas, Dimitrios,Eugster, Conrad Hans,Rueedi, Peter
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