Achillion Pharmaceuticals, Inc.

Avilar Therapeutics, Inc.

Jason Allan Wiles

Avinash S Phadke

Milind Deshpande

Qiuping Wang

Akihiro Hashimoto

Venkat Rao Gadhachanda

Godwin Pais

Dawei Chen

Xiangzhu Wang

Atul Agarwal

William J Greenlee

Kyle J Eastman

Joel Charles Barrish

Barton James Bradbury

Mark George Saulnier

Kevin Tyler Sprott

Srinivasa Karra

Jesse Jingyang Chen

Soumya Ray

Edlaine Lucien

Ha Young Kim

Michael Pucci

Godwin Clarence Gilroy Pais

Akhiro Hashimoto

Micheal John Pucci

Venkat Gadhachanada

Yongsheng Song

Quiping Wang

Michael John Pucci

Godwin Clarence Pais

Atul Ararwal

This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl-mediated disorders.

Pharmaceutical compounds for the treatment of complement mediated disorders

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I'″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

Aryl, heteroaryl, and heterocyclic compounds for treatment of immune and inflammatory disorders

Extracellular protein degraders and compositions are provided that have a potent asialoglycoprotein receptor (ASGPR) Binding Ligand bound to an Extracellular Protein Targeting Ligand for the selective degradation of the Target Extracellular Protein, for example immunoglobulin in vivo to treat disorders mediated by the extracellular protein.

Potent ASGPR-binding compounds for the degradation of immunoglobulins and other proteins

Macrocyclic 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, Formula V, Formula VI, Formula VII, and Formula VIII 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.

Macrocyclic compounds for treatment of medical disorders

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

ASGPR-binding compounds for the degradation of extracellular proteins

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

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.

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

Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein Ror Ron the A group is an aryl, heteroaryl or heterocycle (R) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Aryl, heteroaryl, and heterocyclic compounds for treatment of complement mediated 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, and Formula IV 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.

Pharmaceutical compounds for treatment of medical disorders

Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

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Madison, CT, United States of America

Jason Allan Wiles