- Alkylacetylene substituted Acyltryptophanols
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The present invention relates to acyltryptophanols of the general formula I, in which R1, R2, R3, Q and X have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example fo
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Page/Page column 31
(2009/02/10)
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- Arylmethylene substituted N-acyl-beta-amino alcohols
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The present invention relates to arylmethylene substituted N-Acyl-β-amino alcohols of the formula I in which Y is selected from the aryl or heteroaryl groups: and R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
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Page/Page column 33; 35
(2009/02/10)
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- Alpha-alkyl substituted N-acyltryptophanols
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The present invention relates to α-alkyl substituted N-acyltryptophanols of the formula I in which R1, R2, R3, R4, R5, R6, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
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Page/Page column 40; 41
(2009/03/07)
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- Cyanomethyl substituted N-Acyl Tryptamines
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The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula I in which R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and
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Page/Page column 34
(2009/03/07)
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- Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators
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Identification and synthesis of novel 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as glucokinase activators are described. Removal of an aniline structure of the prototype lead (2a) and incorporation of an alkoxy or phenoxy substituent led to the identifica
- Iino, Tomoharu,Tsukahara, Daisuke,Kamata, Kenji,Sasaki, Kaori,Ohyama, Sumika,Hosaka, Hideka,Hasegawa, Takuro,Chiba, Masato,Nagata, Yasufumi,Eiki, Jun-ichi,Nishimura, Teruyuki
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experimental part
p. 2733 - 2743
(2009/09/08)
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- Arymethylen substituted N-Acyl-gamma-aminoalcohols
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The present invention relates to arylmethylen substituted N-acyl-γ-aminoalcohols of the general formula I in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description.The compounds according to the invention are effective FSH modulators and can be used for example for fertility regulation in men or in women.
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Page/Page column 30
(2008/12/04)
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- 1,2-Diarylacetylene Derivatives of Acyltryptophanols
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The present invention relates to acyltryptophanols of the general formula I, in which Q, W, R1, R2, R3, R4, R5, R6, R7 and R8 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
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Page/Page column 36
(2008/12/06)
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- 2,3,4,9-Tetrahydro-1H-carbazoles
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The present invention relates to 2,3,4,9-tetrahydro-1 H-carbazoles of the general formula I, in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
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Page/Page column 33
(2008/12/07)
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- Synthesis and 5-HT-3 receptor binding activity of 5-[125I]iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl]benzamide and its 5-halogen-2-alkoxyl homologues
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(S)-5-Iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (MIZAC) was prepared from 5-iodo-2,3-dimethoxybenzoyl chloride and (S)-3-aminoquinuclidine. [125I]Iodode-stannylation of its corresponding 5-tri-n-butyltin derivative gave [125I]-MIZAC at 1800 Ci/mmol. Binding of [125I]-MIZAC in rat entorhinal cortex revealed a K(D) of 1.37 ± 0.21 nM. A series of racemic 2-O-alkyl derivatives of MIZAC were prepared and 5-HT-3 receptor affinities were determined by inhibition of [125I]-MIZAC binding. Optimal affinity for the receptor was obtained with small, electron-withdrawing substituents in the aromatic 5-position and with bulky substituents in the 3-position. [125I]-MIZAC is a selective radioligand useful for in vitro identification of the 5-HT-3 receptor.
- De Paulis,Hewlett,Schmidt,Mason,Trivedi,Ebert
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p. 385 - 396
(2007/10/03)
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