A61P27/02

Piperidinyl-Indole Derivatives Complement Factor B Inhibitors and Uses Thereof

The present invention provides a compound of formula I:

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a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

PROTEIN TYROSINE KINASE MODULATORS AND METHODS OF USE

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

SUBSTITUTED BENZIMIDAZOLIUM COMPOUNDS USEFUL IN THE TREATMENT OF RESPIRATORY DISEASES
20180009789 · 2018-01-11 ·

The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).

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ANTI-C5 ANTIBODIES HAVING IMPROVED PHARMACOKINETICS

The disclosure provides antibodies that are useful for, among other things, inhibiting terminal complement (e.g., the assembly and/or activity of the C5b-9 TCC) and C5a anaphylatoxin-mediated inflammation and, thus, treating complement-associated disorders. The antibodies have a number of improved properties relative to eculizumab, including, e.g., increased serum half-life in a human.

CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
20180009824 · 2018-01-11 ·

Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.

(R)-2-Methyl-piperazine Derivatives as CXCR3 Receptor Modulators
20180009800 · 2018-01-11 ·

The invention relates to compounds of Formula (I)

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wherein R.sup.1 and R.sup.2 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.

Pyrimidone Compounds Used as Lp-PLA2 Inhibitors and Pharmaceutical Compositions Thereof
20180009766 · 2018-01-11 ·

The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R.sub.1, R.sub.2, R.sub.3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA.sub.2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA.sub.2 enzyme.

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METHODS OF TREATING RETINAL DISEASES

A method of treating a subject with dry-form age-related macular degeneration (AMD) is disclosed. The method comprises administering into the subretina of the subject a therapeutically effective amount of a pharmaceutical composition comprising human RPE cells, wherein at least 95% of the cells thereof co-express premelanosome protein (PMEL17) and cellular retinaldehyde binding protein (CRALBP), wherein the trans-epithelial electrical resistance of the cells is greater than 100 ohms to the subject, thereby treating the subject.

Peptide conjugates
11708392 · 2023-07-25 · ·

Methods and compositions related to the selective, specific disruption of multiple ligand-receptor signaling interactions, such as ligand-receptor interactions implicated in disease, are disclosed. These interactions may involve multiple cytokines in a single receptor family or multiple ligand receptor interactions from at least two distinct ligand-receptor families. The compositions may comprise polypeptides having composite sequences that comprise sequence fragments of two or more ligand binding sites. The methods and compositions may involve sequence fragments of two or more ligand binding sites that are arranged to conserve the secondary structure of each of the ligands from which the sequence fragments were taken.