公开(公告)号：US10259821B2

公开(公告)日：2019-04-16

申请号：US15873571

申请日：2018-01-17

Applicant: Astellas Pharma Inc. ,  Cytokinetics, Incorporated

Inventor： Ippei Sato ,  Takashi Kamikubo ,  Masanori Miura ,  Yuji Matsushima ,  Hiroaki Tanaka ,  Yasuhiro Shiina ,  Susumu Yamaki ,  Tomoyuki Saito ,  Hiroshi Kiyohara ,  Munemichi Ohe ,  Kayoko Mihara ,  Bradley Paul Morgan ,  Fady Malik ,  Scott Emile Collibee ,  Luke Ashcraft ,  Pu-Ping Lu ,  Jeffrey Michael Warrington ,  Marc Garard

IPC: C07D491/20 ,  C07D491/107 ,  C07D471/04 ,  C07D471/10 ,  C07D217/24 ,  C07D217/26

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

公开(公告)号：US20180148458A1

公开(公告)日：2018-05-31

申请号：US15873571

申请日：2018-01-17

Applicant: Astellas Pharma Inc. ,  Cytokinetics, Incorporated

Inventor： Ippei Sato ,  Takashi Kamikubo ,  Masanori Miura ,  Yuji Matsushima ,  Hiroaki Tanaka ,  Yasuhiro Shiina ,  Susumu Yamaki ,  Tomoyuki Saito ,  Hiroshi Kiyohara ,  Munemichi Ohe ,  Kayoko Mihara ,  Bradley Paul Morgan ,  Fady Malik ,  Scott Emile Collibee ,  Luke Ashcraft ,  Pu-Ping Lu ,  Jeffrey Michael Warrington ,  Marc Garard

IPC: C07D491/20 ,  C07D491/107 ,  C07D471/04 ,  C07D471/10 ,  C07D217/24 ,  C07D217/26

CPC classification number: C07D491/20 ,  C07D217/24 ,  C07D217/26 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

公开(公告)号：US09914741B2

公开(公告)日：2018-03-13

申请号：US15429738

申请日：2017-02-10

Applicant: Astellas Pharma Inc. ,  Cytokinetics, Incorporated

Inventor： Ippei Sato ,  Takashi Kamikubo ,  Masanori Miura ,  Yuji Matsushima ,  Hiroaki Tanaka ,  Yasuhiro Shiina ,  Susumu Yamaki ,  Tomoyuki Saito ,  Hiroshi Kiyohara ,  Munemichi Ohe ,  Kayoko Mihara ,  Bradley Paul Morgan ,  Fady Malik ,  Scott Emile Collibee ,  Luke Ashcraft ,  Pu-Ping Lu ,  Jeffrey Michael Warrington ,  Marc Garard

IPC: C07D491/20 ,  C07D471/10 ,  C07D471/04 ,  C07D217/26 ,  C07D491/107 ,  C07D217/24

CPC classification number: C07D491/20 ,  C07D217/24 ,  C07D217/26 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

公开(公告)号：US11479561B2

公开(公告)日：2022-10-25

申请号：US16871532

申请日：2020-05-11

Applicant: Cytokinetics, Incorporated

Inventor： Ippei Sato ,  Takashi Kamikubo ,  Masanori Miura ,  Yuji Matsushima ,  Hiroaki Tanaka ,  Yasuhiro Shiina ,  Susumu Yamaki ,  Tomoyuki Saito ,  Hiroshi Kiyohara ,  Munemichi Ohe ,  Kayoko Mihara ,  Bradley Paul Morgan ,  Fady Malik ,  Scott Emile Collibee ,  Luke Ashcraft ,  Pu-Ping Lu ,  Jeffrey Michael Warrington ,  Marc Garard

IPC: A61K31/4747 ,  A61K31/472 ,  C07D491/20 ,  C07D491/107 ,  C07D217/24 ,  C07D471/04 ,  C07D217/26 ,  C07D471/10 ,  A61P21/00

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

公开(公告)号：US10689393B2

公开(公告)日：2020-06-23

申请号：US16291481

申请日：2019-03-04

Applicant: Astellas Pharma Inc. ,  Cytokinetics, Incorporated

Inventor： Ippei Sato ,  Takashi Kamikubo ,  Masanori Miura ,  Yuji Matsushima ,  Hiroaki Tanaka ,  Yasuhiro Shiina ,  Susumu Yamaki ,  Tomoyuki Saito ,  Hiroshi Kiyohara ,  Munemichi Ohe ,  Kayoko Mihara ,  Bradley Paul Morgan ,  Fady Malik ,  Scott Emile Collibee ,  Luke Ashcraft ,  Pu-Ping Lu ,  Jeffrey Michael Warrington ,  Marc Garard

IPC: C07D491/20 ,  C07D471/10 ,  C07D217/26 ,  C07D491/107 ,  C07D471/04 ,  C07D217/24 ,  A61P21/00

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

公开(公告)号：US11986474B1

公开(公告)日：2024-05-21

申请号：US18342387

申请日：2023-06-27

Applicant: Cytokinetics, Incorporated

Inventor： Fady Malik

IPC: A61K31/496 ,  A61P9/04

CPC classification number: A61K31/496 ,  A61P9/04

Abstract: Methods for treating heart failure are described herein. Treatment methods include administering a cardiac sarcomere activator (e.g., omecamtiv mecarbil, or a pharmaceutically acceptable salt and/or hydrate thereof) to a subject in need thereof. Treatment methods also include adjusting a dose level of the CSA, for example, to increase, decrease, or maintain a dose level, based on the subject's plasma concentration of the CSA determined after administration of the first dose level of the CSA has started. Provided herein are also treatment methods effective to achieve a target concentration range of the CSA and dose in a single step following a single plasma concentration determination.

公开(公告)号：US20190194220A1

公开(公告)日：2019-06-27

申请号：US16291481

申请日：2019-03-04

Applicant: Astellas Pharma Inc. ,  Cytokinetics, Incorporated

Inventor： Ippei Sato ,  Takashi Kamikubo ,  Masanori Miura ,  Yuji Matsushima ,  Hiroaki Tanaka ,  Yasuhiro Shiina ,  Susumu Yamaki ,  Tomoyuki Saito ,  Hiroshi Kiyohara ,  Munemichi Ohe ,  Kayoko Mihara ,  Bradley Paul Morgan ,  Fady Malik ,  Scott Emile Collibee ,  Luke Ashcraft ,  Pu-Ping Lu ,  Jeffrey Michael Warrington ,  Marc Garard

IPC: C07D491/20 ,  C07D471/10 ,  C07D217/26 ,  C07D491/107 ,  C07D217/24 ,  C07D471/04

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.