C07D209/02

ALIPHATIC PROLINAMIDE DERIVATIVES

This invention is directed to novel aliphatic prolinamide derivatives of Formula I, and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRA1. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRA1. The compounds of the invention are also useful for inhibiting HTRA1 protease activity in an eye or locus of an arthritis or related condition.

##STR00001##

Octahydrocyclopentapyrroles, their preparation and use

The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina.

Octahydrocyclopentapyrroles, their preparation and use

The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina.

BISAMIDE SARCOMERE ACTIVATING COMPOUNDS AND USES THEREOF

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

##STR00001##

BISAMIDE SARCOMERE ACTIVATING COMPOUNDS AND USES THEREOF

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

##STR00001##

HETEROCYCLIC P2Y14 RECEPTOR ANTAGONISTS

Disclosed are compounds for treating or preventing a disease or disorder responsive to antagonism of a P2Y.sub.14R receptor agonist in a mammal in need thereof, for example, compounds of formulas (I) and (II), wherein R.sup.1.sub.-R.sup.8, X, Y, Z, X, Y, Z, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.

##STR00001##

Crystal Forms Of A 9-Aminomethyl Substituted Tetracycline Compound And A Preparation Method Thereof
20190241515 · 2019-08-08 ·

The present invention belongs to the field of pharmaceutical technology, and crystal forms of a 9-aminomethyl substituted tetracycline compound and a process for preparing the same. More specifically, the present invention relates to crystal forms of the compound represented by formula (1), a process for preparing crystal forms of the compound represented by formula (1) and use of said crystal forms in manufacture of medicament for treating and/or preventing an infection disease caused by tetracycline-sensitive bacteria and/or tetracycline-resistant bacteria.

##STR00001##

Crystal Forms Of A 9-Aminomethyl Substituted Tetracycline Compound And A Preparation Method Thereof
20190241515 · 2019-08-08 ·

The present invention belongs to the field of pharmaceutical technology, and crystal forms of a 9-aminomethyl substituted tetracycline compound and a process for preparing the same. More specifically, the present invention relates to crystal forms of the compound represented by formula (1), a process for preparing crystal forms of the compound represented by formula (1) and use of said crystal forms in manufacture of medicament for treating and/or preventing an infection disease caused by tetracycline-sensitive bacteria and/or tetracycline-resistant bacteria.

##STR00001##

Magnetically separable iron-based heterogeneous catalysts for dehydrogenation of alcohols and amines

The present invention discloses an iron-based nitrogen doped graphene catalyst, process for preparation thereof and use of said catalyst in oxidant-free catalytic dehydrogenation of alcohols and amines to the corresponding carbonyl compounds, amines and N-heterocylic compounds with extraction of molecular hydrogen as the only by-product.

Magnetically separable iron-based heterogeneous catalysts for dehydrogenation of alcohols and amines

The present invention discloses an iron-based nitrogen doped graphene catalyst, process for preparation thereof and use of said catalyst in oxidant-free catalytic dehydrogenation of alcohols and amines to the corresponding carbonyl compounds, amines and N-heterocylic compounds with extraction of molecular hydrogen as the only by-product.