C07C257/10

PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS

A process for preparing and purifying a compound of Formula I is provided:

##STR00001##

thereof, wherein the subscript m is an integer of from 0 to 3; each R.sup.a is independently selected from the group consisting of (C.sub.3-C.sub.8)cycloalkyl, (C.sub.1-C.sub.4)haloalkyl, halogen, —OH, —OR.sup.1, —SH, —SR.sup.1, —S(O)R.sup.1, —S(O).sub.2R.sup.1, —SO.sub.2NH.sub.2, —C(O)NH.sub.2, —C(O)NHR.sup.1, —C(O)N(R.sup.1).sub.2, —C(O)R.sup.1, —C(O)H, —CO.sub.2H, —CO.sub.2R.sup.1, —NO.sub.2, —NH.sub.2, —NHR.sup.1, —N(R.sup.1).sub.2, wherein each R.sup.1 is independently (C.sub.1-C.sub.8)alkyl; L is a linking group selected from the group consisting of a bond or CH.sub.2; Q.sup.a, Q.sup.b, and Q.sup.c are each members independently selected from the group consisting of N, S, O and C(R.sup.q) wherein each R.sup.q is independently selected from the group consisting of H, C.sub.1-8 alkyl, halo and phenyl, and the ring having Q.sup.a, Q.sup.b, Q.sup.c and Y as ring vertices is a five-membered ring having two double bonds; and
Y is selected from the group consisting of C and N.

BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF HYPERCHOLEMIA AND CHOLESTATIC LIVER DISEASE

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

Processes for preparing plasma kallikrein inhibitors

A process for preparing and purifying a compound of Formula I is provided: ##STR00001##
or a salt thereof, wherein the subscript m is an integer of from 0 to 3; each R.sup.a is independently selected from the group consisting of (C.sub.3-C.sub.8)cycloalkyl, (C.sub.1-C.sub.4)haloalkyl, halogen, —OH, —OR.sup.1, —SH, —SR.sup.1, —S(O)R.sup.1, —S(O).sub.2R.sup.1, —SO.sub.2NH.sub.2, —C(O)NH.sub.2, —C(O)NHR.sup.1, —C(O)N(R.sup.1).sub.2, —C(O)R.sup.1, —C(O)H, —CO.sub.2R.sup.1, —NO.sub.2, —NH.sub.2, —NHR.sup.1, —N(R.sup.1).sub.2, wherein each R.sup.1 is independently (C.sub.1-C.sub.8)alkyl; L is a linking group selected from the group consisting of a bond or CH.sub.2; Q.sup.a, Q.sup.b, and Q.sup.c are each members independently selected from the group consisting of N, S, O and C(R.sup.q) wherein each R.sup.q is independently selected from the group consisting of H, C.sub.1-8 alkyl, halo and phenyl, and the ring having Q.sup.a, Q.sup.b, Q.sup.c and Y as ring vertices is a five-membered ring having two double bonds; and
Y is selected from the group consisting of C and N.

Phenoxyhalogenphenylamidines and the use thereof as fungicides

The present invention relates phenoxyhalogenphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the phenoxyhalogenphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

Phenoxyhalogenphenylamidines and the use thereof as fungicides

The present invention relates phenoxyhalogenphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the phenoxyhalogenphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS

A process for preparing and purifying a compound of Formula I is provided:

##STR00001##

or a salt thereof, wherein the subscript m is an integer of from 0 to 3; each R.sup.a is independently selected from the group consisting of (C.sub.3-C.sub.8)cycloalkyl, (C.sub.1-C.sub.4)haloalkyl, halogen, OH, OR.sup.1, SH, SR.sup.1, S(O)R.sup.1, S(O).sub.2R.sup.1, SO.sub.2NH.sub.2, C(O)NH.sub.2, C(O)NHR.sup.1, C(O)N(R.sup.1).sub.2, C(O)R.sup.1, C(O)H, CO.sub.2R.sup.1, NO.sub.2, NH.sub.2, NHR.sup.1, N(R.sup.1).sub.2, wherein each R.sup.1 is independently (C.sub.1-C.sub.8)alkyl; L is a linking group selected from the group consisting of a bond or CH.sub.2; Q.sup.a, Q.sup.b, and Q.sup.c are each members independently selected from the group consisting of N, S, O and C(R.sup.q) wherein each R.sup.q is independently selected from the group consisting of H, C.sub.1-8 alkyl, halo and phenyl, and the ring having Q.sup.a, Q.sup.b, Q.sup.c and Y as ring vertices is a five-membered ring having two double bonds; and
Y is selected from the group consisting of C and N.

BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF HYPERCHOLEMIA AND CHOLESTATIC LIVER DISEASE

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF HYPERCHOLEMIA AND CHOLESTATIC LIVER DISEASE

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

Hair-growth promoting composition and usage thereof
11931325 · 2024-03-19 · ·

Novel compositions that promote hair growth or hair restoration, and compositions that prevent hair loss. Compositions including an iNOS inhibitor as an active ingredient are provided. Advantageous affects for hair growth or hair restoration are obtained when a composition including an iNOS inhibitor as an active ingredient is administered to a mammal. For the iNOS inhibitor, a low-molecular compound, an antibody, or a nucleic acid drug such as an antisense oligonucleotide or siRNA may be used. A method of screening for effective substances for promotion of hair growth or hair restoration or prevention of hair loss is also provided.

Hair-growth promoting composition and usage thereof
11931325 · 2024-03-19 · ·

Novel compositions that promote hair growth or hair restoration, and compositions that prevent hair loss. Compositions including an iNOS inhibitor as an active ingredient are provided. Advantageous affects for hair growth or hair restoration are obtained when a composition including an iNOS inhibitor as an active ingredient is administered to a mammal. For the iNOS inhibitor, a low-molecular compound, an antibody, or a nucleic acid drug such as an antisense oligonucleotide or siRNA may be used. A method of screening for effective substances for promotion of hair growth or hair restoration or prevention of hair loss is also provided.