C07D207/34

HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS
20230233516 · 2023-07-27 · ·

The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

HIGH PENETRATION COMPOSITIONS AND THEIR APPLICATIONS
20230233516 · 2023-07-27 · ·

The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. For example, HPCs of NSAIA have demonstrated indications such as treating hair loss and bold. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

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.

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.

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

PROCESS FOR THE CONTINUOUS MANUFACTURE OF STATINS

The present invention relates to process for the continuous manufacture of Statins or salts thereof. The present invention relates to process for the continuous manufacture of Atorvastatin or a salt thereof. The present invention relates to a continuous manufacturing process for the crystallization of Atorvastatin calcium. The present invention also relates to a continuous manufacturing process for the crystallization of Atorvastatin calcium Form I.

PROCESS FOR THE CONTINUOUS MANUFACTURE OF STATINS

The present invention relates to process for the continuous manufacture of Statins or salts thereof. The present invention relates to process for the continuous manufacture of Atorvastatin or a salt thereof. The present invention relates to a continuous manufacturing process for the crystallization of Atorvastatin calcium. The present invention also relates to a continuous manufacturing process for the crystallization of Atorvastatin calcium Form I.

Photoresponsive low-molecular weight material, adhesive, toner, and image forming method

Disclosed is a compound containing a specific structure having an azomethine part, the compound being reversibly fluidized and non-fluidized by being irradiated with light.

Photoresponsive low-molecular weight material, adhesive, toner, and image forming method

Disclosed is a compound containing a specific structure having an azomethine part, the compound being reversibly fluidized and non-fluidized by being irradiated with light.