CN114173803A - 氨基酸化合物的剂型和方案 - Google Patents

氨基酸化合物的剂型和方案 Download PDF

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Publication number
CN114173803A
CN114173803A CN202080041929.2A CN202080041929A CN114173803A CN 114173803 A CN114173803 A CN 114173803A CN 202080041929 A CN202080041929 A CN 202080041929A CN 114173803 A CN114173803 A CN 114173803A
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China
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dosage form
optionally substituted
salt
substituted
deuterium
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Pending
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CN202080041929.2A
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English (en)
Chinese (zh)
Inventor
J·查
董成国
T·霍姆
姜岚
K·莱夫特里斯
李慧
D·J·小摩根斯
M·穆诺茨
M·莱利
郑亚军
M·德卡里斯
S·特纳
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Pliant Therapeutics Inc
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Pliant Therapeutics Inc
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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202080041929.2A 2019-04-08 2020-04-08 氨基酸化合物的剂型和方案 Pending CN114173803A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201962831060P 2019-04-08 2019-04-08
US62/831,060 2019-04-08
US201962850530P 2019-05-20 2019-05-20
US62/850,530 2019-05-20
US201962899071P 2019-09-11 2019-09-11
US62/899,071 2019-09-11
PCT/US2020/027335 WO2020210404A1 (en) 2019-04-08 2020-04-08 Dosage forms and regimens for amino acid compounds

Publications (1)

Publication Number Publication Date
CN114173803A true CN114173803A (zh) 2022-03-11

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CN202080041929.2A Pending CN114173803A (zh) 2019-04-08 2020-04-08 氨基酸化合物的剂型和方案

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US (2) US11419869B2 (https=)
EP (1) EP3952902A4 (https=)
JP (2) JP7579805B2 (https=)
CN (1) CN114173803A (https=)
AU (1) AU2020273158A1 (https=)
IL (1) IL287004B2 (https=)
SG (1) SG11202110889WA (https=)
WO (1) WO2020210404A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024125634A1 (zh) * 2022-12-16 2024-06-20 西藏海思科制药有限公司 一种四氢萘啶类化合物及其在医药上的应用
WO2025067384A1 (zh) * 2023-09-28 2025-04-03 成都微芯药业有限公司 一类氨基酸整联蛋白抑制剂、其制备方法及其应用

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3509590A4 (en) 2016-09-07 2020-12-02 Pliant Therapeutics, Inc. N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE
US10696672B2 (en) 2016-12-23 2020-06-30 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
MX394210B (es) 2017-02-28 2025-03-04 Morphic Therapeutic Inc INHIBIDORES DE INTEGRINA AVß6.
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
FI3761980T3 (fi) 2018-03-07 2024-02-21 Pliant Therapeutics Inc Aminohappoyhdisteitä ja käyttömenetelmiä
TWI841573B (zh) 2018-06-27 2024-05-11 美商普萊恩醫療公司 具有未分支連接子之胺基酸化合物及使用方法
SI3844162T1 (sl) 2018-08-29 2025-06-30 Morphic Therapeutic, Inc. Zaviralci integrina alfa v beta6
WO2020047239A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. INHIBITING αV β6 INTEGRIN
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
TW202028179A (zh) 2018-10-08 2020-08-01 美商普萊恩醫療公司 胺基酸化合物及使用方法
CN114173803A (zh) 2019-04-08 2022-03-11 普利安特治疗公司 氨基酸化合物的剂型和方案
EP4247472A4 (en) 2020-11-19 2024-10-09 Pliant Therapeutics, Inc. INTEGRIN INHIBITORS AND USES THEREOF
WO2022165000A1 (en) * 2021-01-27 2022-08-04 Shy Therapeutics, Llc Methods for the treatment of fibrotic disease
US20240124483A1 (en) * 2021-01-27 2024-04-18 Shy Therapeutics, Llc Methods for the Treatment of Fibrotic Disease
MX2023012794A (es) * 2021-04-30 2023-12-15 Pliant Therapeutics Inc Regímenes de dosificación expandidos para inhibidores de integrina.
TW202329973A (zh) * 2021-10-14 2023-08-01 美商普萊恩醫療公司 整合素抑制劑及其與其他藥劑併用之用途
JP2025518533A (ja) * 2022-05-18 2025-06-17 プライアント・セラピューティクス・インコーポレイテッド インテグリン阻害剤の安定化
CN120091811A (zh) * 2022-07-09 2025-06-03 普利安特治疗公司 整合素抑制剂及其与其它药剂组合的用途
EP4626878A1 (en) 2022-12-02 2025-10-08 Neumora Therapeutics, Inc. Methods of treating neurological disorders
US20250197393A1 (en) 2023-12-14 2025-06-19 Pliant Therapeutics, Inc. Integrin inhibitor and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020010176A1 (en) * 1997-12-17 2002-01-24 Askew Ben C. Integrin receptor antagonists
CN104640857A (zh) * 2012-07-18 2015-05-20 圣路易斯大学 作为整合素拮抗剂的β氨基酸衍生物
US20190276449A1 (en) * 2018-03-07 2019-09-12 Pliant Therapeutics, Inc. Amino acid compounds and methods of use

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20010033248A (ko) 1997-12-17 2001-04-25 폴락 돈나 엘. 인테그린 수용체 길항제
MXPA03011046A (es) 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.
EP1537072A1 (en) 2002-09-10 2005-06-08 Pharmacia & Upjohn Company LLC Substituted aminoethers for the treatment of alzheimer s disease
ES2416354T3 (es) 2005-06-21 2013-07-31 Ajinomoto Co., Inc. Cristal de derivado de fenilalanina, método de producción del mismo y uso del mismo
WO2015048819A1 (en) 2013-09-30 2015-04-02 The Regents Of The University Of California Anti-alphavbeta1 integrin compounds and methods
WO2016145258A1 (en) 2015-03-10 2016-09-15 The Regents Of The University Of California Anti-alphavbeta1 integrin inhibitors and methods of use
EP3442352A4 (en) 2016-04-14 2020-03-11 Mars, Incorporated COMPOUNDS FOR MODULATING THE ACTIVITY OF CALCIUM-SENSITIVE RECEPTORS FOR MODULATING THE TASTE OF KOKUMI AND ANIMAL FEED PRODUCTS THEREFORE
US11192889B2 (en) 2016-07-05 2021-12-07 The Rockefeller University Tetrahydronaphthyridinepentanamide integrin antagonists
EP3509590A4 (en) 2016-09-07 2020-12-02 Pliant Therapeutics, Inc. N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE
US10696672B2 (en) 2016-12-23 2020-06-30 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
MX394210B (es) 2017-02-28 2025-03-04 Morphic Therapeutic Inc INHIBIDORES DE INTEGRINA AVß6.
MA52117A (fr) 2017-02-28 2022-04-06 Morphic Therapeutic Inc Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
WO2019118938A1 (en) 2017-12-15 2019-06-20 Apellis Pharmaceuticals, Inc. Dosing regimens and related compositions and methods
TWI841573B (zh) 2018-06-27 2024-05-11 美商普萊恩醫療公司 具有未分支連接子之胺基酸化合物及使用方法
WO2020047239A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. INHIBITING αV β6 INTEGRIN
WO2020047208A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
WO2020047207A1 (en) 2018-08-29 2020-03-05 Morphic Therapeutics, Inc. Inhibitors of (alpha-v)(beta-6) integrin
TW202028179A (zh) 2018-10-08 2020-08-01 美商普萊恩醫療公司 胺基酸化合物及使用方法
CN114173803A (zh) 2019-04-08 2022-03-11 普利安特治疗公司 氨基酸化合物的剂型和方案
WO2021097338A1 (en) 2019-11-15 2021-05-20 Pliant Therapeutics, Inc. Compositions and methods for activation of integrins
CN115989235A (zh) 2020-05-07 2023-04-18 普利安特治疗公司 使用氨基酸化合物治疗呼吸系统疾病的方法
EP4247472A4 (en) 2020-11-19 2024-10-09 Pliant Therapeutics, Inc. INTEGRIN INHIBITORS AND USES THEREOF
MX2023012794A (es) 2021-04-30 2023-12-15 Pliant Therapeutics Inc Regímenes de dosificación expandidos para inhibidores de integrina.
US20240350494A1 (en) 2021-09-03 2024-10-24 Pliant Therapeutics, Inc. Therapeutic modulation of integrins
TW202329973A (zh) 2021-10-14 2023-08-01 美商普萊恩醫療公司 整合素抑制劑及其與其他藥劑併用之用途
JP2025518533A (ja) 2022-05-18 2025-06-17 プライアント・セラピューティクス・インコーポレイテッド インテグリン阻害剤の安定化
CN120091811A (zh) 2022-07-09 2025-06-03 普利安特治疗公司 整合素抑制剂及其与其它药剂组合的用途
IL321740A (en) 2022-12-27 2025-08-01 Pliant Therapeutics Inc Alpha-V-beta-8 integrin inhibitors and their uses
WO2024155965A2 (en) 2023-01-21 2024-07-25 Pliant Therapeutics, Inc. Biomarkers for use in integrin inhibitor therapy

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020010176A1 (en) * 1997-12-17 2002-01-24 Askew Ben C. Integrin receptor antagonists
CN104640857A (zh) * 2012-07-18 2015-05-20 圣路易斯大学 作为整合素拮抗剂的β氨基酸衍生物
US20190276449A1 (en) * 2018-03-07 2019-09-12 Pliant Therapeutics, Inc. Amino acid compounds and methods of use
CN112135612A (zh) * 2018-03-07 2020-12-25 普利安特治疗公司 氨基酸化合物和使用方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PUBCHEM: "Bexotegrast, CID 135390719", pages 1 - 24, Retrieved from the Internet <URL:https://pubchem.ncbi.nlm.nih.gov/compound/135390719> *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024125634A1 (zh) * 2022-12-16 2024-06-20 西藏海思科制药有限公司 一种四氢萘啶类化合物及其在医药上的应用
WO2025067384A1 (zh) * 2023-09-28 2025-04-03 成都微芯药业有限公司 一类氨基酸整联蛋白抑制剂、其制备方法及其应用

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IL287004B1 (en) 2025-11-01
US20200352942A1 (en) 2020-11-12
IL287004B2 (en) 2026-03-01
JP7579805B2 (ja) 2024-11-08
AU2020273158A1 (en) 2021-11-11
WO2020210404A1 (en) 2020-10-15
JP2025028835A (ja) 2025-03-05
CA3136745A1 (en) 2020-10-15
SG11202110889WA (en) 2021-10-28
JP2022526818A (ja) 2022-05-26
US12390463B2 (en) 2025-08-19
EP3952902A4 (en) 2022-12-21
IL287004A (en) 2021-12-01
US11419869B2 (en) 2022-08-23
US20230117605A1 (en) 2023-04-20
EP3952902A1 (en) 2022-02-16

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