摘要:
This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
摘要:
A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or(3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.
摘要:
A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1–C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen or (C1–C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, or (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, (C1–C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen, or (C1–C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1–C6) lower alkyl, halogen, or (C1–C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1–C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.
摘要:
This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds. ##STR1##
摘要:
This disclosure describes novel 3 or 4 substituted oxotremorine derivatives having polar substituted oxygen or sulfur groups. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and processes for the production of the compounds.
摘要:
Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed.The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity.Also disclosed are other intermediates and processes for their production.
摘要:
Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed.The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity.Also disclosed are other intermediates and processes for their production.
摘要:
This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.
摘要:
This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds. ##STR1##
摘要:
This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds. ##STR1##