公开(公告)号：US10179131B2

公开(公告)日：2019-01-15

申请号：US15209150

申请日：2016-07-13

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Yao-Ling Qiu ,  Hui Cao ,  Wei Li ,  Xiaowen Peng ,  Meizhong Jin ,  Jorden Kass ,  Xuri Gao ,  Yat Sun Or

IPC: A61K31/506 ,  A61K45/06 ,  C07D417/14 ,  C07D417/12 ,  C07F9/6558 ,  A61K31/683 ,  C07D403/04 ,  C07D239/20 ,  A61K31/505 ,  C07D498/08 ,  A61K31/5386 ,  A61K31/5377 ,  C07D451/06 ,  C07D487/04

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US09765087B2

公开(公告)日：2017-09-19

申请号：US14245001

申请日：2014-04-04

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Yao-Ling Qiu ,  Ce Wang ,  Xiaowen Peng ,  Hui Cao ,  Lu Ying ,  Xuri Gao ,  Bin Wang ,  Yat Sun Or

IPC: C07D498/10 ,  C07D403/14 ,  A61K31/4184 ,  C07D401/14 ,  A61K31/444 ,  C07D405/14 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/675 ,  C07D487/08 ,  A61K31/506 ,  C07D409/14 ,  C07D413/14 ,  A61K31/422 ,  C07D491/107 ,  A61K31/517 ,  C07D417/14 ,  A61K45/06 ,  A61K38/19 ,  A61K38/21 ,  A61K31/427 ,  A61K31/7056 ,  C07F9/6558 ,  A61K31/13

CPC classification number: C07D498/10 ,  A61K31/13 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/427 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/19 ,  A61K38/21 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  C07D491/107 ,  C07F9/65583 ,  A61K2300/00 ,  A61K39/12

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20170022150A1

公开(公告)日：2017-01-26

申请号：US15216124

申请日：2016-07-21

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Yao-Ling Qiu ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Jorden Kass ,  Xuri Gao ,  Xiaowen Peng ,  Yat Sun Or

IPC: C07C235/56 ,  A61K45/06 ,  A61K31/265 ,  C07C233/66 ,  A61K31/4164 ,  A61K31/277 ,  C07C271/12 ,  A61K31/27 ,  C07D233/64 ,  A61K31/167 ,  C07C255/60

CPC classification number: C07C235/56 ,  A61K45/06 ,  C07C233/66 ,  C07C235/42 ,  C07C255/58 ,  C07C255/60 ,  C07C271/12 ,  C07C271/28 ,  C07C2601/02 ,  C07D233/64 ,  C07D233/88

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A1-Y-A2-Z-L-R  (I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract translation: 其抑制由乙型肝炎病毒（HBV）编码的蛋白质或干扰乙型肝炎病毒的HBV生命周期的功能，并且也可用作抗病毒剂。 本发明还涉及包含用于给患有HBV感染的受试者的上述化合物的药物组合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HBV感染的方法。

公开(公告)号：US20160332996A1

公开(公告)日：2016-11-17

申请号：US15152647

申请日：2016-05-12

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Yao-Ling Qiu ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Xuri Gao ,  Xiaowen Peng ,  Jorden Kass ,  Yat Sun Or

IPC: C07D405/12 ,  A61K31/454 ,  A61K45/06 ,  C07D231/38 ,  C07D403/12 ,  C07D211/46 ,  A61K31/445 ,  C07D401/14 ,  C07D231/40 ,  C07D401/12 ,  A61K31/415

CPC classification number: C07D405/12 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5377 ,  A61K45/06 ,  C07D211/46 ,  C07D231/38 ,  C07D231/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y—Z-L-R1  (I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract translation: 其抑制由乙型肝炎病毒（HBV）编码的蛋白质或干扰乙型肝炎病毒的HBV生命周期的功能，并且也可用作抗病毒剂。 本发明还涉及包含用于给患有HBV感染的受试者的上述化合物的药物组合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HBV感染的方法。

公开(公告)号：US20160058783A1

公开(公告)日：2016-03-03

申请号：US14836157

申请日：2015-08-26

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Yao-Ling Qiu ,  Xiaowen Peng ,  Xuri Gao ,  Hui Cao ,  Yat Sun Or

IPC: A61K31/7072 ,  C07H19/06 ,  C07H19/10 ,  A61K45/06

CPC classification number: A61K31/7072 ,  A61K31/7052 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K45/06 ,  C07H19/06 ,  C07H19/10 ,  A61K2300/00

Abstract: The present invention discloses compounds of formula (I), or a pharmaceutically acceptable salt thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral/anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.

Abstract translation: 本发明公开了抑制，预防或治疗异常细胞增殖和/或病毒感染，特别是HIV，HCV或HBV的式（I）化合物或其药学上可接受的盐。 因此，本发明的化合物干扰病毒的复制循环，也可用作抗病毒剂，或干扰宿主细胞生物化学过程，也可用作抗增殖剂。 本发明还涉及药物组合物，其包含用于给患有病毒感染和/或细胞增殖的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的病毒感染和/或细胞增殖的方法。 本发明涉及上文所述的新的抗病毒/抗增殖化合物，包含这些化合物的药物组合物，以及用于治疗或预防需要用所述化合物治疗的受试者的病毒感染的方法。

公开(公告)号：US12011425B2

公开(公告)日：2024-06-18

申请号：US18101258

申请日：2023-01-25

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Yao-Ling Qiu ,  Xuri Gao ,  Jorden Kass ,  Hui Cao ,  Wei Li ,  Xiaowen Peng ,  Byung-Chul Suh ,  Yat Sun Or

IPC: A61K31/167 ,  A61K31/337 ,  A61K31/34 ,  A61K31/351 ,  A61K31/357 ,  A61K31/397 ,  A61K31/401 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4192 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/513 ,  A61K31/7028 ,  A61P31/20 ,  C07C303/00 ,  C07C317/44 ,  A61K45/06

CPC classification number: A61K31/167 ,  A61K31/337 ,  A61K31/34 ,  A61K31/351 ,  A61K31/357 ,  A61K31/397 ,  A61K31/401 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4192 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/513 ,  A61K31/7028 ,  A61P31/20 ,  C07C303/00 ,  C07C317/44 ,  A61K45/06 ,  C07B2200/05 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/44 ,  C07C2602/50

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

X-A-Y-L-R  (I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US12006291B2

公开(公告)日：2024-06-11

申请号：US18095155

申请日：2023-01-10

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Kaicheng Zhu ,  Tao Wang ,  Jiajun Zhang ,  Hui Cao ,  Ruichao Shen ,  Guoqiang Wang ,  George G. Wu ,  Yat Sun Or

IPC: C07D209/42

CPC classification number: C07D209/42

Abstract: The present invention relates to processes for preparing a Compound (1):




or a pharmaceutically acceptable salt or solvate thereof. Compound (1) is useful as in many pharmaceutical agents, especially is useful as key intermediate in the synthesis of certain SARS-CoV-2 3CLpro inhibitors.

公开(公告)号：US20230234922A1

公开(公告)日：2023-07-27

申请号：US18095155

申请日：2023-01-10

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Kaicheng Zhu ,  Tao Wang ,  Jiajun Zhang ,  Hui Cao ,  Ruichao Shen ,  Guoqiang Wang ,  George G. Wu ,  Yat Sun Or

IPC: C07D209/42

CPC classification number: C07D209/42

Abstract: The present invention relates to processes for preparing a Compound (1):




or a pharmaceutically acceptable salt or solvate thereof. Compound (1) is useful as in many pharmaceutical agents, especially is useful as key intermediate in the synthesis of certain SARS-CoV-2 3CLpro inhibitors.

公开(公告)号：US20230151019A1

公开(公告)日：2023-05-18

申请号：US17983501

申请日：2022-11-09

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Hui Cao ,  Wei Li ,  Xuri Gao ,  Jiajun Zhang ,  Xiaowen Peng ,  Jorden Kass ,  Ruichao Shen ,  Guoqiang Wang ,  Yat Sun Or

IPC: C07D487/10 ,  A61P31/14

CPC classification number: C07D487/10 ,  A61P31/14

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:




which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US11472808B2

公开(公告)日：2022-10-18

申请号：US16892464

申请日：2020-06-04

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Yao-Ling Qiu ,  Xiaowen Peng ,  Wei Li ,  Xuri Gao ,  Jorden Kass ,  Byung-Chul Suh ,  Hui Cao ,  Jiajun Zhang ,  Yat Sun Or

IPC: A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06

Abstract: The present invention discloses substituted pyrrolo[1,2-c]pyrimidines, such as the compound which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.