ECSP077836A - Compuestos mejorados farmacocinéticamente - Google Patents

Compuestos mejorados farmacocinéticamente

Info

Publication number
ECSP077836A
ECSP077836A EC2007007836A ECSP077836A ECSP077836A EC SP077836 A ECSP077836 A EC SP077836A EC 2007007836 A EC2007007836 A EC 2007007836A EC SP077836 A ECSP077836 A EC SP077836A EC SP077836 A ECSP077836 A EC SP077836A
Authority
EC
Ecuador
Prior art keywords
pharmacocinetic
improved compounds
rock2
methods
rock1
Prior art date
Application number
EC2007007836A
Other languages
English (en)
Inventor
Stewart Campbell
Paul Sweetnam
Alexandra Bartolozzi
Hope Foudoulakis
Brian Kirk
Siya Ram
Original Assignee
Surface Logix Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37054004&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP077836(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Surface Logix Inc filed Critical Surface Logix Inc
Publication of ECSP077836A publication Critical patent/ECSP077836A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00—Drugs for disorders of the urinary system
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/00—Drugs for disorders of the senses
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08—Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y30/00—Nanotechnology for materials or surface science, e.g. nanocomposites
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Nanotechnology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Physics & Mathematics (AREA)
  • Composite Materials (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Materials Engineering (AREA)
  • General Physics & Mathematics (AREA)
  • Condensed Matter Physics & Semiconductors (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)

Abstract

La presente invención se relaciona con inhibidores de ROCK1 y ROCK2 y con métodos para modular las propiedades farmacocinéticas y/o farmacodinámicas de esos compuestos. También se proporcionan métodos para inhibir ROCK1 y ROCK2 que son útiles para el tratamiento de la enfermedad.
EC2007007836A 2005-03-25 2007-10-23 Compuestos mejorados farmacocinéticamente ECSP077836A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US66516505P 2005-03-25 2005-03-25

Publications (1)

Publication Number Publication Date
ECSP077836A true ECSP077836A (es) 2008-01-23

Family

ID=37054004

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2007007836A ECSP077836A (es) 2005-03-25 2007-10-23 Compuestos mejorados farmacocinéticamente

Country Status (21)

Country Link
US (6) US8357693B2 (es)
EP (1) EP1865958B1 (es)
JP (2) JP2008534518A (es)
KR (1) KR20080081122A (es)
CN (1) CN101208094B (es)
AU (1) AU2006230159A1 (es)
BR (1) BRPI0622285A2 (es)
CA (1) CA2602254C (es)
CR (1) CR9465A (es)
EA (1) EA022875B1 (es)
EC (1) ECSP077836A (es)
ES (1) ES2549397T3 (es)
GE (1) GEP20105029B (es)
IL (1) IL186299A0 (es)
MX (1) MX2007011859A (es)
NO (1) NO20075145L (es)
NZ (1) NZ562083A (es)
SG (1) SG155163A1 (es)
UA (1) UA96126C2 (es)
WO (1) WO2006105081A2 (es)
ZA (1) ZA200708858B (es)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7846915B2 (en) 2004-10-20 2010-12-07 Resverlogix Corporation Stilbenes and chalcones for the prevention and treatment of cardiovascular diseases
CR9465A (es) * 2005-03-25 2008-06-19 Surface Logix Inc Compuestos mejorados farmacocineticamente
US8410109B2 (en) 2005-07-29 2013-04-02 Resverlogix Corp. Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
WO2007125331A2 (en) 2006-04-26 2007-11-08 Cancer Research Technology Limited Amino-ethyl-amino-aryl (aeaa) compounds and their use
CN101528042A (zh) * 2006-08-24 2009-09-09 表面线段公司 药代动力学改进的化合物
EP2099458A4 (en) * 2006-12-01 2011-05-11 Harvard College COMPOUNDS AND METHODS FOR ENZYME-MEDIATED TUMOR PRESENTATION AND THERAPY
MX2009008099A (es) 2007-02-01 2009-12-14 Resverlogix Corp Compuestos para la prevencion y tratamiento de enfermedades cardiovasculares.
ES2431163T3 (es) * 2007-03-01 2013-11-25 Novartis Ag Inhibidores de PIM quinasa y métodos para su uso
RU2010101416A (ru) * 2007-06-19 2011-07-27 Такеда Фармасьютикал Компани Лимитед (Jp) Профилактическое/лекарственное средство от рака
KR101629356B1 (ko) 2008-06-26 2016-06-13 리스버로직스 코퍼레이션 퀴나졸리논 유도체의 제조방법
CN104311480A (zh) 2008-09-02 2015-01-28 诺华股份有限公司 作为激酶抑制剂的吡啶甲酰胺衍生物
CA2747417C (en) 2009-01-08 2017-01-03 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular disease
JP2012519732A (ja) * 2009-03-09 2012-08-30 サーフェイス ロジックス，インコーポレイティド Ｒｈｏキナーゼ阻害剤
KR101913109B1 (ko) 2009-03-18 2018-10-31 리스버로직스 코퍼레이션 신규한 소염제
DK2421533T3 (en) 2009-04-22 2019-01-07 Resverlogix Corp Hitherto unknown anti-inflammatory agents
US8658676B2 (en) * 2010-10-12 2014-02-25 The Medicines Company Clevidipine emulsion formulations containing antimicrobial agents
LT2773354T (lt) 2011-11-01 2019-08-12 Resverlogix Corp. Geriamosios greitai atsipalaiduojančios pakeistų chinozolinų vaisto formos
CA2873672A1 (en) 2012-05-21 2013-11-28 Novartis Ag Novel ring-substituted n-pyridinyl amides as kinase inhibitors
WO2013191244A1 (ja) * 2012-06-21 2013-12-27 大正製薬株式会社 ピリドピリミジン－４－オン誘導体
WO2014055996A2 (en) * 2012-10-05 2014-04-10 Kadmon Corporation, Llc Rho kinase inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014096965A2 (en) 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
CN105407894A (zh) 2013-03-14 2016-03-16 康威基内有限公司 用于抑制含布罗莫结构域的蛋白质的方法和组合物
NZ718190A (en) 2013-08-23 2017-10-27 Neupharma Inc Substituted quinazolines for inhibiting kinase activity
EP3270694A4 (en) 2015-02-17 2018-09-05 Neupharma, Inc. Certain chemical entities, compositions, and methods
JP6903585B2 (ja) 2015-03-13 2021-07-14 レスバーロジックス コーポレイション 補体関連疾患の治療のための組成物および治療方法
WO2016210190A1 (en) 2015-06-24 2016-12-29 Nitto Denko Corporation Ionizable compounds and compositions and uses thereof
US10508106B2 (en) * 2015-11-25 2019-12-17 Convergene Llc Bicyclic BET bromodomain inhibitors and uses thereof
AU2017312561B2 (en) 2016-08-15 2022-06-30 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2018201006A1 (en) * 2017-04-28 2018-11-01 Kadmon Corporation, Llc Treatment of inflammatory conditions and autoimmune diseases with glucose uptake inhibitors
WO2019000683A1 (zh) 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
KR102563325B1 (ko) 2017-06-30 2023-08-03 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Ｒｈｏ-관련 단백질 키나아제 억제제, Ｒｈｏ-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도
WO2019001572A1 (zh) * 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho 相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
WO2019018562A1 (en) 2017-07-19 2019-01-24 Ideaya Biosciences, Inc. AMIDO COMPOUND AS MODULATORS OF AHR
US11542256B2 (en) 2017-09-03 2023-01-03 Angion Biomedica Corp. Vinylheterocycles as Rho-associated coiled-coil kinase (ROCK) inhibitors
FI3749669T6 (fi) 2018-02-06 2024-11-13 Ideaya Biosciences Inc AHR-modulaattoreita
JP7187575B2 (ja) 2018-04-18 2022-12-12 メッドシャイン ディスカバリー インコーポレイテッド Ｒｈｏキナーゼ阻害剤としてのベンゾピラゾール系化合物
CN112969694B (zh) * 2018-11-09 2023-06-13 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其用途
US12497395B2 (en) 2019-04-24 2025-12-16 Convergene, Llc Small molecule bromodomain inhibitors and uses therof
JP7252417B2 (ja) 2019-10-18 2023-04-04 メッドシャイン ディスカバリー インコーポレイテッド Ｒｈｏキナーゼ阻害剤としてのベンゾピラゾール化合物の塩形、結晶形及びその製造方法
CN114746412A (zh) * 2019-12-27 2022-07-12 广东东阳光药业有限公司 Kd-025的新晶型及其制备方法
CA3186800A1 (en) 2020-07-22 2022-01-27 Teva Pharmaceuticals International Gmbh Solid state forms of belumosudil and belumosudil salts
CN114105976B (zh) * 2020-08-28 2024-04-26 杭州邦顺制药有限公司 选择性rock2激酶抑制剂
WO2022170864A1 (zh) * 2021-02-09 2022-08-18 苏州科睿思制药有限公司 Belumosudil甲磺酸盐的晶型及其制备方法和用途
CN114573566B (zh) * 2021-03-04 2023-05-30 杭州邦顺制药有限公司 选择性rock2激酶抑制剂
CN115124514A (zh) * 2021-03-26 2022-09-30 广东东阳光药业有限公司 Kd-025的共晶及其制备方法
EP4370205A1 (en) 2021-07-16 2024-05-22 Sandoz Ag Solid-state forms of 2-(3-(4-(1h-indazol-5-ylamino)quinazolin-2-yl )phenoxy)-n- isopropylacetamide methane sulfonic acid salt
TW202404602A (zh) 2022-04-19 2024-02-01 美商凱德蒙有限責任公司 移植後肺部病症的治療方法
WO2024000060A1 (en) * 2022-06-30 2024-01-04 Apotex Inc Salts of belumosudil, crystalline forms and pharmaceutical compositions thereof and their use in the treatment of chronic graft-versus-host disease
AU2022469413A1 (en) 2022-07-14 2025-02-27 Kadmon Corporation, Llc Methods of administering belumosudil for treatment of chronic graft versus host disease
CA3178085A1 (en) 2022-07-14 2024-01-14 Kadmon Corporation, Llc Belumosudil metabolites and uses thereof in the treatment of chronic graft-versus-host disease
EP4554593A1 (en) 2022-07-14 2025-05-21 Kadmon Corporation, LLC Methods of administering belumosudil for treatment of chronic graft versus host disease in patient subpopulations
KR20250035000A (ko) 2022-07-14 2025-03-11 카드몬 코포레이션, 엘엘씨 Cyp3a 유도제 및/또는 양성자 펌프 저해제와 조합하여 벨루모수딜을 투여하는 방법
CN115385899B (zh) * 2022-09-08 2024-04-02 药康众拓(江苏)医药科技有限公司 ROCK2抑制剂belumosudil的氘代药物及用途
WO2024063770A1 (en) 2022-09-21 2024-03-28 Kadmon Corporation, Llc Liquid formulation of belumosudil
IL320719A (en) 2022-11-11 2025-07-01 Assia Chem Ind Ltd Solid forms of blomosodil and processes for obtaining blomosodil
EP4626434A1 (en) 2022-11-29 2025-10-08 Kadmon Corporation, LLC Solid dispersion comprising amorphous 2-[3-[4-(lh-indazol-5- ylamino)quinazolin-2-yl]phenoxy]-n-propan-2-yl-acetamide
WO2024124084A1 (en) 2022-12-09 2024-06-13 Kadmon Corporation, Llc Methods of administering belumosudil for treatment of multiple myeloma
CN116444443B (zh) * 2023-03-15 2025-09-05 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） 一种苯甲酰-喹唑啉酮衍生物及其制备方法与应用
AU2024292342A1 (en) 2023-07-17 2026-02-26 Graviton Bioscience Bv Formulations and uses of rock2 inhibitors for als
WO2025069008A1 (en) 2023-09-28 2025-04-03 Graviton Bioscience Bv Therapy for treating type 1 diabetes using rock2 and dyrk1 inhibitors
WO2025069009A1 (en) 2023-09-29 2025-04-03 Graviton Bioscience Bv Rock2 inhibitors in the treatment of obesity
WO2025076350A1 (en) 2023-10-06 2025-04-10 Kadmon Corporation, Llc Methods of administering belumosudil in combination with transport protein substrates
CN119954779A (zh) * 2023-11-07 2025-05-09 江苏东科康德药业有限公司 甲磺酸贝舒地尔杂质、制备及检测方法
WO2025110992A1 (en) 2023-11-21 2025-05-30 Kadmon Corporation, Llc Method of administering belumosudil for patient subpopulations with hepatic impairment
WO2025184133A1 (en) 2024-02-29 2025-09-04 Kadmon Corporation, Llc Methods of treating chronic graft versus host disease with belumosudil after ceasing administration of ruxolitinib
CN119751424B (zh) * 2025-01-04 2025-12-05 重庆圣华曦药业股份有限公司 一种合成甲磺酸贝舒地尔的方法

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE212993T1 (de) * 1995-07-06 2002-02-15 Novartis Erfind Verwalt Gmbh Pyrolopyrimidine und verfahren zu ihrer herstellung
ATE359822T1 (de) * 1996-08-12 2007-05-15 Mitsubishi Pharma Corp Medikamente enthaltend rho-kinase inhibitoren
TWI284642B (en) * 1999-01-18 2007-08-01 Hoffmann La Roche Novel heterocyclic sulfonamides
HK1049837B (en) * 2000-03-16 2007-01-19 Mitsubishi Pharma Corporation Amide compounds and uses
DE60125026T2 (de) * 2000-03-23 2007-06-28 Takeda Pharmaceutical Co. Ltd. Fluorisochinolinderivate, verfahren zu ihrer herstellung und ihre anwendung
US6699665B1 (en) 2000-11-08 2004-03-02 Surface Logix, Inc. Multiple array system for integrating bioarrays
TWI261055B (en) * 2001-03-23 2006-09-01 Bayer Corp Rho-Kinase Inhibitors
PE20020958A1 (es) * 2001-03-23 2002-11-14 Bayer Corp Inhibidores de la rho-quinasa
AU2002327385A1 (en) 2001-07-27 2003-02-17 Surface Logix, Inc. Resealable and sealable devices for biochemical assays
CA2458844A1 (en) 2001-08-27 2003-03-06 Surface Logix, Inc. Immobilization of biological molecules onto surfaces coated with monolayers
JP2003221386A (ja) * 2001-11-26 2003-08-05 Takeda Chem Ind Ltd 二環性誘導体、その製造法およびその用途
DE10162435A1 (de) 2001-12-19 2003-07-17 Joerg Lahann Verfahren zur Erzeugung von Oberflächenbeschichtungen, die die Adsorption von Proteinen bzw. die Adhäsion von Bakterien und/oder Zellen vermindern
GB0206860D0 (en) * 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
US7645878B2 (en) * 2002-03-22 2010-01-12 Bayer Healthcare Llc Process for preparing quinazoline Rho-kinase inhibitors and intermediates thereof
EP1567528A1 (en) * 2002-11-21 2005-08-31 Eli Lilly And Company Mixed lineage kinase modulators
GB0301016D0 (en) * 2003-01-16 2003-02-19 Univ London Treatment of benign prostatic hyperplasia
WO2004105757A2 (en) * 2003-05-29 2004-12-09 Schering Aktiengesellschaft Use of rho-kinase inhibitors in the treatment of aneurysm and cardiac hypertrophy
US20070275961A1 (en) * 2003-06-04 2007-11-29 Vernalis (Cambridge) Limited. Triazolo ' 1, 5-A ! Pyrimidines and Their Use in Medicine
CA2536954C (en) * 2003-08-29 2012-11-27 Exelixis, Inc. C-kit modulators and methods of use
UA83509C2 (en) * 2003-10-15 2008-07-25 Оси Фармасьютикалз, Инк. Imidazopyrazines as tyrosine kinase inhibitors
AU2006213985C1 (en) * 2005-02-18 2012-03-15 Surface Logix, Inc. Pharmacokinetically improved compounds
EA200701752A1 (ru) * 2005-02-18 2008-04-28 Сурфейс Логикс Инк. Способ получения усовершенствованных фармакокинетических соединений, включающих функциональные остатки или группы, и фармацевтические композиции, содержащие эти соединения
CR9465A (es) * 2005-03-25 2008-06-19 Surface Logix Inc Compuestos mejorados farmacocineticamente
CN101528042A (zh) * 2006-08-24 2009-09-09 表面线段公司 药代动力学改进的化合物

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