TW202115086A - Bckdk抑制劑 - Google Patents

Bckdk抑制劑 Download PDF

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Publication number
TW202115086A
TW202115086A TW109121446A TW109121446A TW202115086A TW 202115086 A TW202115086 A TW 202115086A TW 109121446 A TW109121446 A TW 109121446A TW 109121446 A TW109121446 A TW 109121446A TW 202115086 A TW202115086 A TW 202115086A
Authority
TW
Taiwan
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
carboxylic acid
diabetes
Prior art date
Application number
TW109121446A
Other languages
English (en)
Chinese (zh)
Inventor
賽米特 庫瑪 巴哈特查亞
林恩 馬里 布桑
凱文 詹姆士 菲里斯基
大衛 安德魯 葛里菲斯
貝瑟尼 林 柯爾摩斯
艾爾席那 路易斯 安琪 馬堤奈茲
羅素 艾倫 米勒
馬修 理查德 李斯
法雷區 瑞秋 真 羅斯
張原
Original Assignee
美商輝瑞大藥廠
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
Application filed by 美商輝瑞大藥廠 filed Critical 美商輝瑞大藥廠
Publication of TW202115086A publication Critical patent/TW202115086A/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW109121446A 2019-06-28 2020-06-24 Bckdk抑制劑 TW202115086A (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962868057P 2019-06-28 2019-06-28
US62/868,057 2019-06-28
US202062960817P 2020-01-14 2020-01-14
US62/960,817 2020-01-14
US202063031719P 2020-05-29 2020-05-29
US63/031,719 2020-05-29

Publications (1)

Publication Number Publication Date
TW202115086A true TW202115086A (zh) 2021-04-16

Family

ID=71452516

Family Applications (1)

Application Number Title Priority Date Filing Date
TW109121446A TW202115086A (zh) 2019-06-28 2020-06-24 Bckdk抑制劑

Country Status (8)

Country Link
US (2) US11542270B2 (enExample)
EP (1) EP3990461A1 (enExample)
JP (1) JP2022540000A (enExample)
CA (1) CA3144869C (enExample)
PY (1) PY2030111A (enExample)
TW (1) TW202115086A (enExample)
UY (1) UY38768A (enExample)
WO (1) WO2020261205A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202115086A (zh) * 2019-06-28 2021-04-16 美商輝瑞大藥廠 Bckdk抑制劑
TW202228762A (zh) * 2020-01-30 2022-08-01 美商美國禮來大藥廠 提派肽(tirzepatide)之治療用途
US12569186B2 (en) 2021-01-27 2026-03-10 Koninklijke Philips N.V. Apparatus and method for augmented interpretation of magnetic resonance and ultrasound shear wave elastography for monitoring liver fibrosis
WO2022175959A1 (en) * 2021-02-21 2022-08-25 Ramino-Bio Thiophene based compounds and use thereof as bckdk inhibitors
EP4330665A1 (en) 2021-04-26 2024-03-06 Reprieve Cardiovascular, Inc. Measuring and/or detecting analytes in urine, and associated systems, devices, and methods
US20230010793A1 (en) * 2021-07-12 2023-01-12 Reprieve Cardiovascular, Inc. Fluid therapy based on estimated excess fluid, and associated systems and methods
IL312296A (en) * 2021-12-01 2024-06-01 Pfizer 3-PHENYL-1-BENZOTHIOPEN-2-CARBOXYLIC ACID DERIVATIVES AS INHIBITORS OF BRANCHED ALPHA KETO ACID DEHYDROGENSIS KINASE FOR THE TREATMENT OF DIABETES, KIDNEY DISEASES, NASH AND HEART
CN114903994A (zh) * 2022-04-19 2022-08-16 上海交通大学医学院附属瑞金医院 Bckdk作为靶点在制备2型糖尿病药物中的应用
CN121311466A (zh) 2023-04-14 2026-01-09 辉瑞大药厂 葡萄糖依赖性促胰岛素多肽受体拮抗剂及其用途
US12257416B1 (en) 2023-09-12 2025-03-25 Reprieve Cardiovascular, Inc. Fluid therapy based on sodium excretion, and associated systems, devices, and methods
AU2025209211A1 (en) 2024-01-18 2026-07-30 Tuojie Biotech (Shanghai) Co., Ltd. Pyridothiophene-2-carboxylic acid derivative, preparation method therefor and use thereof
TW202539633A (zh) 2024-02-01 2025-10-16 美商輝瑞股份有限公司 葡萄糖依賴性促胰島素多肽受體拮抗劑及其用途
US12582773B2 (en) 2024-02-16 2026-03-24 Reprieve Cardiovascular, Inc. Urine output sensing without use of an indwelling catheter, and associated systems, devices, and methods
WO2025224599A1 (en) 2024-04-22 2025-10-30 Pfizer Inc. Pyrrolidine-based glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026013531A1 (en) 2024-07-10 2026-01-15 Pfizer Inc. Spiro[2.5]octane compounds
WO2026033382A1 (en) 2024-08-07 2026-02-12 Pfizer Inc. Heterocyclic glp-1r modulators
WO2026042018A1 (en) 2024-08-21 2026-02-26 Pfizer Inc. 4-{4-[(1-{[4-(propan-2-yl)phenyl]carbamoyl)-d-prolyl)amino]cyclohexyl}benzoic acid derivatives as gipr antagonists for the treatment of diabetes
WO2026078617A1 (en) 2024-10-11 2026-04-16 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078672A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078673A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078671A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic compounds as glucose-dependent insulinotropic polypeptide receptor antagonists
WO2026078674A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic derivatives as glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078670A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic derivatives as glucose-dependent insulinotropic polypeptide receptor antagonists
WO2026088071A1 (en) 2024-10-23 2026-04-30 Pfizer Inc. Substituted fused heteroaryl lactam compounds
WO2026154417A1 (en) 2025-01-17 2026-07-23 Pfizer Inc. Fused heterocyclic amide/sulfonamide compounds as agonists of the calcitonin/amylin receptors for the treatment of obesity

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
CA1146866A (en) 1979-07-05 1983-05-24 Yamanouchi Pharmaceutical Co. Ltd. Process for the production of sustained release pharmaceutical composition of solid medical material
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
DE3438830A1 (de) 1984-10-23 1986-04-30 Rentschler Arzneimittel Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
ES2111065T5 (es) 1991-04-16 2005-06-16 Nippon Shinyaku Company, Limited Procedimiento para producir una dispersion solida.
US5340591A (en) 1992-01-24 1994-08-23 Fujisawa Pharmaceutical Co., Ltd. Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine
JP3265680B2 (ja) 1992-03-12 2002-03-11 大正製薬株式会社 経口製剤用組成物
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
DE19504832A1 (de) 1995-02-14 1996-08-22 Basf Ag Feste Wirkstoff-Zubereitungen
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
PT901786E (pt) 1997-08-11 2007-08-07 Pfizer Prod Inc Disperções farmacêuticas sólidas com biodisponibilidade melhorada
ID26984A (id) 1998-07-06 2001-02-22 Bristol Myers Squibb Co Senyawa-senyawa sulfonamida sebagai antagonis reseptor angiotensin endotelin ganda
DZ3347A1 (fr) 2000-05-22 2001-11-29 Aventis Pharma Inc Dérivés d'arylméthylamine pour leur utilisation comme inhibiteurs de la tryptase
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
GB0021831D0 (en) * 2000-09-06 2000-10-18 Astrazeneca Ab Chemical compounds
EA011086B9 (ru) 2004-05-12 2012-08-30 Пфайзер Продактс Инк. Производные пролина и их применение в качестве ингибиторов дипептидилпептидазы iv
EP2010520B1 (en) 2006-04-20 2012-09-12 Pfizer Products Inc. Heterobicyclic amides for the prevention and treatment of glucokinase-mediated diseases
KR20090024823A (ko) * 2006-06-30 2009-03-09 세프라코 아이엔시. Ｄ-아미노산 옥시다제의 융합된 헤테로사이클 억제제
US20090036425A1 (en) 2007-08-02 2009-02-05 Pfizer Inc Substituted bicyclolactam compounds
CA2729581A1 (en) 2008-07-29 2010-02-04 Pfizer Inc. Fluorinated heteroaryls
ES2380408T3 (es) 2008-08-28 2012-05-11 Pfizer Inc. Derivados de dioxa-biciclo[3.2.1]octano-2,3,4-triol
TW201038580A (en) 2009-02-02 2010-11-01 Pfizer 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl derivatives
WO2010103437A1 (en) 2009-03-11 2010-09-16 Pfizer Inc. Benzofuranyl derivatives used as glucokinase inhibitors
EP2406230A1 (en) 2009-03-11 2012-01-18 Pfizer Inc. Substituted indazole amides and their use as glucokinase activators
CA2754523A1 (en) 2009-03-20 2010-09-23 Pfizer Inc. 3-oxa-7-azabicyclo[3.3.1]nonanes
CA2759843A1 (en) 2009-05-08 2010-11-10 Pfizer Inc. Gpr 119 modulators
EP2427448A1 (en) 2009-05-08 2012-03-14 Pfizer Inc. Gpr 119 modulators
GEP20135907B (en) 2009-06-05 2013-08-12 Pfizer L-(piperidin-4-yl)-pyrazole derivatives as gpr 119 modulators
WO2011005611A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Neuromedin u receptor agonists and uses thereof
EP2954780A1 (en) 2009-07-24 2015-12-16 Baylor College Of Medicine Methods of modulation of branched chain acids and uses thereof
US20120022116A1 (en) 2010-07-20 2012-01-26 Huayun Deng Compositions and methods for the treatment of pathological condition(s) related to gpr35 and/or gpr35-herg complex
WO2018109607A1 (en) 2016-12-16 2018-06-21 Pfizer Inc. Glp-1 receptor agonists and uses thereof
CA3062602A1 (en) 2017-05-11 2018-11-15 Bristol-Myers Squibb Company Thienopyridines and benzothiophenes useful as irak4 inhibitors
TW202115086A (zh) * 2019-06-28 2021-04-16 美商輝瑞大藥廠 Bckdk抑制劑

Also Published As

Publication number Publication date
US11542270B2 (en) 2023-01-03
US20210024536A1 (en) 2021-01-28
UY38768A (es) 2021-01-29
CA3144869C (en) 2023-12-05
EP3990461A1 (en) 2022-05-04
WO2020261205A1 (en) 2020-12-30
US20210087204A1 (en) 2021-03-25
US11059833B2 (en) 2021-07-13
JP2022540000A (ja) 2022-09-14
CA3144869A1 (en) 2020-12-30
PY2030111A (es) 2021-12-20

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