Abstract: 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.
Type:
Grant
Filed:
June 8, 2022
Date of Patent:
March 12, 2024
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: 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.
Type:
Application
Filed:
May 11, 2023
Publication date:
February 22, 2024
Applicant:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan WILES, Avinash S. PHADKE, Dawei CHEN, Venkat Rao GADHACHANDA, Joel Charles BARRISH, Atul AGARWAL, Kyle J. EASTMAN
Abstract: This invention provides stable, highly crystalline forms of Complement factor D inhibitors Compound 1 for advantageous therapeutic pharmaceutical efficacy and dosage form stability.
Type:
Grant
Filed:
September 6, 2019
Date of Patent:
November 14, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Avinash Phadke, Akihiro Hashimoto, Wei Ma, Lee M. Katrincic
Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce excessive activation of complement.
Type:
Grant
Filed:
September 6, 2019
Date of Patent:
November 14, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Venkat Rao Gadhachanda, Kyle J. Eastman, Godwin Pais
Abstract: 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.
Type:
Grant
Filed:
May 7, 2021
Date of Patent:
August 8, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Dawei Chen, Venkat Rao Gadhachanda, Joel Charles Barrish, Atul Agarwal, Kyle J. Eastman
Abstract: 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.
Type:
Grant
Filed:
July 2, 2021
Date of Patent:
July 25, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, Joel Charles Barrish, William Greenlee, Kyle J. Eastman
Abstract: 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.
Type:
Grant
Filed:
December 28, 2020
Date of Patent:
May 16, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: 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.
Type:
Grant
Filed:
December 28, 2020
Date of Patent:
May 16, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: This disclosure provides an ocular tissue depot of a selected complement factor D (CFD) inhibitor for the extended treatment of an ocular disorder mediated by complement factor D. In particular, the disclosure includes the creation of a drug depot within the choroid-retina pigmented epithelium (C-RPE) and/or the iris-ciliary body (I-CB) of the eye by means of the systemic (oral or parenteral) administration of the compound, where the compound accumulates in ocular tissue and is released over an extended period for the treatment of a posterior and/or anterior eye disorder.
Type:
Application
Filed:
March 9, 2021
Publication date:
April 27, 2023
Applicant:
Achillion Pharmaceuticals, Inc.
Inventors:
Mingjun Huang, Steven Zelenkofske, David Boyer, Jose Rivera, Jason Allan Wiles
Abstract: This invention provides stable, highly crystalline forms of Complement factor D inhibitors Compound 1 and Compound 2 for advantageous therapeutic pharmaceutical efficacy and dosage form stability.
Type:
Application
Filed:
September 6, 2019
Publication date:
March 30, 2023
Applicant:
Achillion Pharmaceuticals, Inc.
Inventors:
Avinash Phadke, Akihiro Hashimoto, Wei Ma, Lee M. Katrincic
Abstract: This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl-mediated disorders.
Type:
Application
Filed:
March 20, 2020
Publication date:
March 16, 2023
Applicant:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Venkat Rao Gadhachanda, Kyle J. Eastman
Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.
Type:
Application
Filed:
August 20, 2019
Publication date:
January 26, 2023
Applicant:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Venkat Rao Gadhachanda, Kyle J. Eastman, Godwin Pais
Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce excessive activation of complement.
Type:
Application
Filed:
September 6, 2019
Publication date:
December 1, 2022
Applicant:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Venkat Rao Gadhachanda, Kyle J. Eastman, Godwin Pais
Abstract: 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.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
September 20, 2022
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, Joel Charles Barrish, William Greenlee, Kyle J. Eastman
Abstract: 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.
Type:
Grant
Filed:
May 5, 2020
Date of Patent:
August 9, 2022
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: The dosages and methods described herein provide desirable pharmacokinetic (PK) and pharmacodynamics (PD) characteristics which inhibit alternative pathway complement activity, for example at least 85% or more inhibition of AP activity in vivo at dosages from about 120 mg to 200 mg BID that provides a plasma level Ctrough at least about 65 ng/ml, which provides sufficient AP inhibition to reduce the risk of complement breakthrough. In addition, the dosage form described herein provides a significantly low Cmax, providing additional safety margin and better dosing flexibility.
Abstract: 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.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
August 10, 2021
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, Joel Charles Barrish, William Greenlee, Kyle J. Eastman
Abstract: 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.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
July 6, 2021
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Dawei Chen, Venkat Rao Gadhachanda, Joel Charles Barrish, Atul Agarwal, Kyle J. Eastman