C07D498/10

INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
20180009807 · 2018-01-11 ·

The present invention provides compounds of Formula I (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

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INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
20180009807 · 2018-01-11 ·

The present invention provides compounds of Formula I (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

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Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Heteroaryl substituted spiropiperidinyl derivatives and pharmaceutical uses thereof

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; ##STR00001##
wherein R.sup.1 R.sup.2, R.sup.4 and X.sup.1 are defined herein, 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.

BIFUNCTIONAL COMPOUNDS

The invention provides a bifunctional compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein said Targeting Ligand, Linker and Degron are as described herein.

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BIFUNCTIONAL COMPOUNDS

The invention provides a bifunctional compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein said Targeting Ligand, Linker and Degron are as described herein.

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PYRIDINE DERIVATIVES WITH N-LINKED CYCLIC SUBSTITUENTS AS cGAS INHIBITORS

The invention relates to new proline derivatives of formula (I) as cGAS inhibitors,

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wherein

wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and G are defined as in claim 1,

and prodrugs or pharmaceutically acceptable salts of these compounds

for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), non-alcoholic steatotic hepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).

QUINOLIN-2-ONE DERIVATIVES

Compounds of the formula I

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in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, Q and Y have the meanings indicated in claim 1,
are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.

QUINOLIN-2-ONE DERIVATIVES

Compounds of the formula I

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in which X.sup.1, X.sup.2, X.sup.3, X.sup.4, R.sup.1, R.sup.2, R.sup.3, Q and Y have the meanings indicated in claim 1,
are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.