公开(公告)号：US20240122910A1

公开(公告)日：2024-04-18

申请号：US18319287

申请日：2023-05-17

Applicant: Akebia Therapeutics, Inc.

Inventor： James Densmore Copp ,  Ann W. Newman ,  Anne Luong

IPC: A61K31/444 ,  A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K31/4418 ,  C07D213/803 ,  C07D213/81

CPC classification number: A61K31/444 ,  A61K9/14 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4866 ,  A61K31/4418 ,  C07D213/803 ,  C07D213/81 ,  C07B2200/13 ,  C07D221/00

Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.

公开(公告)号：US20230227426A1

公开(公告)日：2023-07-20

申请号：US17906650

申请日：2021-03-19

Applicant: Akebia Therapeutics, Inc.

Inventor： Paul E. FLEMING ,  Thomas P. BLAISDELL ,  Senkara Rao ALLU

IPC: C07D401/04 ,  C07D401/14

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: The present invention provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (A), and sub-formulas thereof, or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatment of diseases including heart (e.g. ischemic heart disease, congestive heart failure, and valvular heart disease), lung (e.g., acute lung injury, pulmonary hypertension, pulmonary fibrosis, and chronic obstructive pulmonary disease), liver (e.g. acute liver failure and liver fibrosis and cirrhosis), and kidney (e.g. acute kidney injury and chronic kidney disease) disease.

公开(公告)号：US20230071553A1

公开(公告)日：2023-03-09

申请号：US17712709

申请日：2022-04-04

Applicant: Akebia Therapeutics, Inc.

Inventor： Alexander Smith ,  Gurudatt Ajay Chandorkar ,  Ene Ikpong Ette ,  Bradley John Maroni ,  Charlotte Suzanne Hartman ,  Ramin Farzaneh-Far ,  Jula Kern Inrig

IPC: A61K31/4418 ,  A61K9/20 ,  A61K9/28 ,  A61K31/16 ,  C07D213/81

Abstract: Provided herein are specific doses of, and dosing regimens for, using a HIF prolyl hydroxylase inhibitor in treating or preventing anemia, such as anemia secondary to or associated with chronic kidney disease, anemia secondary to or associated with non-dialysis dependent chronic kidney disease anemia associated with or resulting from chemotherapy, or anemia associated with AIDS.

公开(公告)号：US09701636B2

公开(公告)日：2017-07-11

申请号：US14541284

申请日：2014-11-14

Applicant: Akebia Therapeutics, Inc.

Inventor： James Densmore Copp ,  Ann W. Newman ,  Anne Luong

IPC: A61K31/44 ,  C07D211/72 ,  C07D211/84 ,  C07D213/62 ,  C07D213/78 ,  C07D213/81

CPC classification number: A61K31/444 ,  A61K9/14 ,  A61K9/48 ,  C07D213/803 ,  C07D213/81 ,  C07D221/00

Abstract: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.

公开(公告)号：US20170189387A1

公开(公告)日：2017-07-06

申请号：US15420617

申请日：2017-01-31

Applicant: Akebia Therapeutics, Inc.

Inventor： Richard Masaru Kawamoto ,  Shengde Wu ,  Artem G. Evdokimov ,  Kenneth D. Greis ,  Angelique Sun Boyer ,  Namal C. Warshakoon

IPC: A61K31/4418 ,  A61K31/4433

CPC classification number: A61K31/4418 ,  A61K31/4433 ,  C07C235/60 ,  C07C237/42 ,  C07C255/57 ,  C07D213/65 ,  C07D213/81 ,  C07D295/192 ,  C07D401/04 ,  C07D401/10 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04 ,  Y02A50/401

Abstract: The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

公开(公告)号：US20160339005A1

公开(公告)日：2016-11-24

申请号：US15112954

申请日：2015-01-23

Applicant: AKEBIA THERAPEUTICS, INC.

Inventor： Robert Shalwitz ,  William Daly

IPC: A61K31/4418 ,  A61K31/44 ,  A61K31/7088 ,  A61K9/00 ,  A61K45/06

CPC classification number: A61K31/4418 ,  A61K9/0048 ,  A61K9/08 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/44 ,  A61K31/7088 ,  A61K45/06 ,  A61K31/4412 ,  A61K2300/00

Abstract: Disclosed are methods for treating diseases or conditions of the eye, especially retinopathies, ocular edema and ocular neovascularization. Non-limiting examples of these diseases or conditions include diabetic macular edema, age-related macular degeneration (wet or dry form), choroidal neovascularization, diabetic retinopathy, retinal vein occlusion (central or branch), ocular trauma, surgery induced edema, surgery induced neovascularization, cystoid macular edema, ocular ischemia, uveitis, and the like. These diseases or conditions are characterized by changes in the ocular vasculature whether progressive or non-progressive, whether a result of an acute disease or condition, or a chronic disease or condition.

Abstract translation: 公开了治疗眼睛疾病或病症的方法，特别是视网膜病变，眼水肿和眼新生血管形成。 这些疾病或病症的非限制性实例包括糖尿病性黄斑水肿，年龄相关性黄斑变性（湿性或干性形式），脉络膜新生血管形成，糖尿病性视网膜病变，视网膜静脉阻塞（中枢或分支），眼部创伤，手术诱发的水肿，手术诱导 新生血管形成，囊状黄斑水肿，眼部缺血，葡萄膜炎等。 这些疾病或病症的特征在于无论是进行性还是非进行性的眼脉管系统的变化，无论是急性疾病或病症的结果，还是慢性疾病或病症。

公开(公告)号：US20160214939A1

公开(公告)日：2016-07-28

申请号：US15004034

申请日：2016-01-22

Applicant: AKEBIA THERAPEUTICS, INC.

Inventor： ROGER HANSELMANN ,  ANNE LUONG

IPC: C07D213/81

CPC classification number: C07D213/81

Abstract: Provided herein are solid forms comprising 2-(5-(3-fluorophenyl)-3-hydroxypicolinamido)acetic acid, methods of making the solid forms, methods of their use for the treatment of various diseases and/or disorders and pharmaceutical compositions comprising the solid forms.

Abstract translation: 本文提供的是包含2-（5-（3-氟苯基）-3-羟基喹啉酰氨基）乙酸的固体形式，制备固体形式的方法，其用于治疗各种疾病和/或病症的方法以及包含 固体形式。

公开(公告)号：US20150361043A1

公开(公告)日：2015-12-17

申请号：US14833222

申请日：2015-08-24

Applicant: Akebia Therapeutics, Inc.

Inventor： Christopher M. Lanthier ,  Boris Gorin ,  Jan Oudenes ,  Craig Edward Dixon ,  Alan Quigbo Lu ,  James Densmore Copp ,  John Michael Janusz

IPC: C07D213/81 ,  C07D213/79

CPC classification number: C07D213/81 ,  C07D213/79 ,  C07D213/803

Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

Abstract translation: 公开了制备[（3-羟基吡啶-2-羰基）氨基] - 链烷酸，衍生物，特别是5-芳基取代和5-杂芳基取代的[（3-羟基吡啶-2-羰基）氨基}乙酸的方法。 还公开了制备[（3-羟基吡啶-2-羰基） - 氨基]乙酸的前药的方法，例如[（3-羟基吡啶-2-羰基）氨基}乙酸酯和{[3-羟基吡啶-2 - 羰基]氨基}乙酸酰胺。所公开的化合物可用作脯氨酰羟化酶抑制剂或用于治疗需要脯氨酰羟化酶抑制的条件。

公开(公告)号：US20150119425A1

公开(公告)日：2015-04-30

申请号：US14568200

申请日：2014-12-12

Applicant: Akebia Therapeutics, Inc.

Inventor： Richard Masaru Kawamoto ,  Shengde Wu ,  Artem G. Evdokimov ,  Kenneth D. Greis ,  Angelique Sun Boyer ,  Namal C. Warshakoon

IPC: C07D213/81 ,  C07D405/04

CPC classification number: A61K31/4418 ,  A61K31/4433 ,  C07C235/60 ,  C07C237/42 ,  C07C255/57 ,  C07D213/65 ,  C07D213/81 ,  C07D295/192 ,  C07D401/04 ,  C07D401/10 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04 ,  Y02A50/401

Abstract: The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

Abstract translation: 本公开内容涉及HIF-1α脯氨酰羟化酶抑制剂，其包含本文所述的HIF-1α脯氨酰羟化酶抑制剂的组合物以及用于控制外周血管疾病（PVD），冠状动脉疾病（CAD），心力衰竭， 缺血和贫血。

公开(公告)号：US20240327376A1

公开(公告)日：2024-10-03

申请号：US18742035

申请日：2024-06-13

Applicant: Akebia Therapeutics, Inc.

Inventor： Thomas P. BLAISDELL ,  Paul E. FLEMING

IPC: C07D401/04 ,  A61K31/4439 ,  C07D213/81 ,  C07D405/14

CPC classification number: C07D401/04 ,  A61K31/4439 ,  C07D213/81 ,  C07D405/14

Abstract: The present invention provides, in part, novel small molecule inhibitors of PHD1 that are selective over PHD2 having a structure according to Formula (I), and sub-formulas thereof:




or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatment of diseases including ischemia reperfusion injury (including but not limited to stroke, myocardial infarction, and acute kidney injury) inflammatory bowel disease, cancer (including colorectal cancer), and liver disease.