JP2022540000A - Ｂｃｋｄｋ阻害活性を有するチエノ［３，２－ｂ］チオフェン－２－カルボン酸化合物 - Google Patents

Ｂｃｋｄｋ阻害活性を有するチエノ［３，２－ｂ］チオフェン－２－カルボン酸化合物 Download PDF

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JP2022540000A
JP2022540000A JP2021576778A JP2021576778A JP2022540000A JP 2022540000 A JP2022540000 A JP 2022540000A JP 2021576778 A JP2021576778 A JP 2021576778A JP 2021576778 A JP2021576778 A JP 2021576778A JP 2022540000 A JP2022540000 A JP 2022540000A
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compound
pharmaceutically acceptable
carboxylic acid
acceptable salt
diabetes
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JP2022540000A5 (https=
JPWO2020261205A5 (https=
Inventor
クマール バタチャリア サミット
マリー ブゾン リアン
ジェイムズ フィリプスキ ケヴィン
アンドリュー グリフィス デヴィッド
リン カーモス べサニー
エンジェル マルティネス―アルシナ ルイ
アラン ミラー ラッセル
リチャード リース マシュー
ジェーン ロス フラック レイチェル
ザング ユアン
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ファイザー・インク
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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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (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)
JP2021576778A 2019-06-28 2020-06-26 Ｂｃｋｄｋ阻害活性を有するチエノ［３，２－ｂ］チオフェン－２－カルボン酸化合物 Pending JP2022540000A (ja)

Applications Claiming Priority (7)

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
PCT/IB2020/056066 WO2020261205A1 (en) 2019-06-28 2020-06-26 Thieno[3,2-b]thiophene-2-carboxylic acid compounds having bckdk inhibiting activity

Publications (3)

Publication Number Publication Date
JP2022540000A true JP2022540000A (ja) 2022-09-14
JP2022540000A5 JP2022540000A5 (https=) 2023-06-02
JPWO2020261205A5 JPWO2020261205A5 (https=) 2023-06-02

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

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TW202115086A (zh) * 2019-06-28 2021-04-16 美商輝瑞大藥廠 Bckdk抑制劑
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WO2022161915A1 (en) * 2021-01-27 2022-08-04 Koninklijke Philips N.V. Apparatus and method for augmented interpretation of magnetic resonance and ultrasound shear wave elastography for monitoring liver fibrosis
EP4294812A4 (en) * 2021-02-21 2025-03-26 Ramino-Bio Ltd. Thiophene based compounds and use thereof as bckdk inhibitors
US12605702B2 (en) 2021-04-26 2026-04-21 Reprieve Cardiovascular, Inc. Measuring and/or detecting analytes in urine, and associated systems, devices, and methods
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CR20240183A (es) * 2021-12-01 2024-06-07 Pfizer Inhibidores y/o degradadores de bckdk
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
EP4695226A1 (en) 2023-04-14 2026-02-18 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
US12471842B2 (en) 2023-09-12 2025-11-18 Reprieve Cardiovascular, Inc. Fluid therapy based on adjusted urine output rate, and associated systems, devices, and methods
WO2025153045A1 (zh) * 2024-01-18 2025-07-24 上海拓界生物医药科技有限公司 一种吡啶并噻吩-2-羧酸衍生物及其制备方法和用途
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
WO2025175244A1 (en) 2024-02-16 2025-08-21 Reprieve Cardiovascular, Inc. Urine output sensing without use of an indwelling catheter, and associated systems, devices, and methods
US20250326741A1 (en) 2024-04-22 2025-10-23 Pfizer Inc. 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
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WO2026078617A1 (en) 2024-10-11 2026-04-16 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2026078674A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic derivatives as 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
WO2026078671A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic compounds as glucose-dependent insulinotropic polypeptide receptor antagonists
WO2026078670A1 (en) 2024-10-13 2026-04-16 Pfizer Inc. Heterocyclic derivatives as glucose-dependent insulinotropic polypeptide receptor antagonists
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Also Published As

Publication number Publication date
US11059833B2 (en) 2021-07-13
UY38768A (es) 2021-01-29
CA3144869C (en) 2023-12-05
US20210087204A1 (en) 2021-03-25
PY2030111A (es) 2021-12-20
US11542270B2 (en) 2023-01-03
EP3990461A1 (en) 2022-05-04
WO2020261205A1 (en) 2020-12-30
TW202115086A (zh) 2021-04-16
CA3144869A1 (en) 2020-12-30
US20210024536A1 (en) 2021-01-28

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