Patent classifications
C07C217/52
Compounds for modulating mitochondrial function
Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: ##STR00001##
wherein X is absent, CH.sub.2, or C(O); R.sup.1 is H, OH, CN, NO.sub.2, halo, C.sub.1-3 alkyl, C.sub.1-3 haloalkyl, C.sub.1-3 alkoxy, C.sub.1-3 haloalkoxy, C.sub.3-7 cycloalkyl, amino, C.sub.1-3 alkylamino, or di(C.sub.1-3 alkyl)amino; R.sup.2 is H or C.sub.1-6 alkyl; R.sup.3 is H, C.sub.1-6 alkyl, C(O)(C.sub.1-3 alkyl), or C(O)O(C.sub.1-3 alkyl); R.sup.4 is C.sub.3-10 cycloalkyl, C.sub.6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R.sup.5 groups; and R.sup.5 is OH, CN, NO.sub.2, halo, C.sub.1-3 alkyl, C.sub.1-3 haloalkyl, C.sub.1-3 alkoxy, C.sub.1-3 haloalkoxy, C.sub.3-7 cycloalkyl, amino, C.sub.1-3 alkylamino, or di(C.sub.1-3 alkyl)amino.
Compounds for modulating mitochondrial function
Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: ##STR00001##
wherein X is absent, CH.sub.2, or C(O); R.sup.1 is H, OH, CN, NO.sub.2, halo, C.sub.1-3 alkyl, C.sub.1-3 haloalkyl, C.sub.1-3 alkoxy, C.sub.1-3 haloalkoxy, C.sub.3-7 cycloalkyl, amino, C.sub.1-3 alkylamino, or di(C.sub.1-3 alkyl)amino; R.sup.2 is H or C.sub.1-6 alkyl; R.sup.3 is H, C.sub.1-6 alkyl, C(O)(C.sub.1-3 alkyl), or C(O)O(C.sub.1-3 alkyl); R.sup.4 is C.sub.3-10 cycloalkyl, C.sub.6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R.sup.5 groups; and R.sup.5 is OH, CN, NO.sub.2, halo, C.sub.1-3 alkyl, C.sub.1-3 haloalkyl, C.sub.1-3 alkoxy, C.sub.1-3 haloalkoxy, C.sub.3-7 cycloalkyl, amino, C.sub.1-3 alkylamino, or di(C.sub.1-3 alkyl)amino.
Compounds for modulating mitochondrial function
Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: ##STR00001##
wherein X is absent, CH.sub.2, or C(O); R.sup.1 is H, OH, CN, NO.sub.2, halo, C.sub.1-3 alkyl, C.sub.1-3 haloalkyl, C.sub.1-3 alkoxy, C.sub.1-3 haloalkoxy, C.sub.3-7 cycloalkyl, amino, C.sub.1-3 alkylamino, or di(C.sub.1-3 alkyl)amino; R.sup.2 is H or C.sub.1-6 alkyl; R.sup.3 is H, C.sub.1-6 alkyl, C(O)(C.sub.1-3 alkyl), or C(O)O(C.sub.1-3 alkyl); R.sup.4 is C.sub.3-10 cycloalkyl, C.sub.6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R.sup.5 groups; and R.sup.5 is OH, CN, NO.sub.2, halo, C.sub.1-3 alkyl, C.sub.1-3 haloalkyl, C.sub.1-3 alkoxy, C.sub.1-3 haloalkoxy, C.sub.3-7 cycloalkyl, amino, C.sub.1-3 alkylamino, or di(C.sub.1-3 alkyl)amino.
CATIONIC LIPID
The present invention provides novel cationic lipids having excellent encapsulation and delivery stability of nucleic acid medicines. Provided is a compound represented by Formula (I) or a pharmacologically acceptable salt thereof. In the Formula (I), R.sup.1 is a substituted or unsubstituted formula: (CH.sub.2).sub.aL.sub.1(CH.sub.2).sub.bCH.sub.3; R.sup.2 is a substituted or unsubstituted C5-C20 alkyl group or a substituted or unsubstituted formula: (CH.sub.2).sub.cL.sub.2(CH.sub.2).sub.aCH.sub.3; L.sup.1 and L.sup.2 are each independently C(?O)O, OC(?O), or OC(?O)O; a, b, c, and d are each independently an integer of at least 1, and the total of a and b and the total of c and d are each an integer of 5 to 25; R.sup.3 to R.sup.7 are each independently a hydrogen atom, a substituted or unsubstituted C.sup.1-C.sup.6 alkyl group, or the like; R.sup.8, R.sup.9, and R.sup.10 are each a hydrogen atom; the constituent atoms in the Formula (I) may form a ring; Z is OC(?O), C(?O)O, OC(?O)O, or the like; and X is O or S.
Bicyclic analgesic compounds
Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein.
Bicyclic analgesic compounds
Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein.
SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
PROCESS AND INTERMEDIATES FOR THE PRODUCTION OF 17(20)-ENE B-SECO STEROIDS
##STR00001##
The invention pertains to a process for producing a compound of formula (11) wherein R.sup.7 and R.sup.8 are each independently selected from H, halogen, alkyl, aryl, or alkylaryl, R.sup.42 is H or a protective group, R.sup.43 is H or R.sup.3, wherein R.sup.3 is a protective group, by contacting a compound of formula (10) with an olefmation reagent, wherein compound of formula (10) comprises a counter acid X.sup.1 when R.sup.42H and R.sup.43H.
PROCESS AND INTERMEDIATES FOR THE PRODUCTION OF 17(20)-ENE B-SECO STEROIDS
##STR00001##
The invention pertains to a process for producing a compound of formula (11) wherein R.sup.7 and R.sup.8 are each independently selected from H, halogen, alkyl, aryl, or alkylaryl, R.sup.42 is H or a protective group, R.sup.43 is H or R.sup.3, wherein R.sup.3 is a protective group, by contacting a compound of formula (10) with an olefmation reagent, wherein compound of formula (10) comprises a counter acid X.sup.1 when R.sup.42H and R.sup.43H.