AU2018323969B2 - Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds - Google Patents

Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds Download PDF

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Publication number
AU2018323969B2
AU2018323969B2 AU2018323969A AU2018323969A AU2018323969B2 AU 2018323969 B2 AU2018323969 B2 AU 2018323969B2 AU 2018323969 A AU2018323969 A AU 2018323969A AU 2018323969 A AU2018323969 A AU 2018323969A AU 2018323969 B2 AU2018323969 B2 AU 2018323969B2
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AU
Australia
Prior art keywords
methyl
phenyl
mmol
pyrazol
pyridyl
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Active
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AU2018323969A
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AU2018323969A1 (en
Inventor
Tianwei Ma
Liang Wu
Xuejun Zhang
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Eli Lilly and Co
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Eli Lilly and Co
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Publication of AU2018323969A1 publication Critical patent/AU2018323969A1/en
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Publication of AU2018323969B2 publication Critical patent/AU2018323969B2/en
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    • 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/02—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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
AU2018323969A 2017-09-04 2018-08-28 Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds Active AU2018323969B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/CN2017/100354 WO2019041340A1 (en) 2017-09-04 2017-09-04 LYSOPHOSPHATIDE ACID RECEPTOR 1 RECEPTOR INHIBITORS (LPAR1)
AUPCT/CN2017/100354 2017-09-04
PCT/US2018/048249 WO2019046239A1 (en) 2017-09-04 2018-08-28 LYSOPHOSPHATIDE ACID RECEPTOR 1 RECEPTOR INHIBITORS (LPAR1)

Publications (2)

Publication Number Publication Date
AU2018323969A1 AU2018323969A1 (en) 2020-02-20
AU2018323969B2 true AU2018323969B2 (en) 2020-07-16

Family

ID=63528947

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2018323969A Active AU2018323969B2 (en) 2017-09-04 2018-08-28 Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds

Country Status (13)

Country Link
US (2) US11365185B2 (enExample)
EP (1) EP3679032B1 (enExample)
JP (1) JP6854386B2 (enExample)
KR (1) KR102341064B1 (enExample)
CN (1) CN111032647B (enExample)
AU (1) AU2018323969B2 (enExample)
CA (1) CA3073983C (enExample)
EA (1) EA039482B1 (enExample)
ES (1) ES2966827T3 (enExample)
IL (1) IL273000B2 (enExample)
MX (1) MX2020002430A (enExample)
SA (1) SA520411406B1 (enExample)
WO (2) WO2019041340A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114728168B (zh) 2019-11-15 2024-04-09 吉利德科学公司 三唑氨基甲酸酯吡啶基磺酰胺作为lpa受体拮抗剂及其用途
TWI843503B (zh) 2020-06-03 2024-05-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
US11702407B2 (en) 2020-06-03 2023-07-18 Gilead Sciences, Inc. LPA receptor antagonists and uses thereof
AU2022273631B2 (en) 2021-05-11 2025-04-17 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
KR20240007233A (ko) 2021-05-13 2024-01-16 길리애드 사이언시즈, 인코포레이티드 Lpa 수용체 길항제 및 이의 용도
CN113461640B (zh) * 2021-06-17 2023-08-11 中央民族大学 Lpar1抑制剂、医药用途及其制备方法
US11939318B2 (en) 2021-12-08 2024-03-26 Gilead Sciences, Inc. LPA receptor antagonists and uses thereof
TW202342017A (zh) 2022-02-25 2023-11-01 美商洛子峰生物有限公司 用於治療與ｌｐａ受體活性相關的病狀的化合物及組合物
JP2025540714A (ja) * 2022-11-24 2025-12-16 ローツェ・バイオ・インコーポレイテッド Ｌｐａ受容体活性と関連する状態を処置するための化合物および組成物
CN121419961A (zh) * 2023-06-02 2026-01-27 迈塔免疫科技股份有限公司 用于治疗纤维化疾病的化合物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010077882A2 (en) * 2008-12-15 2010-07-08 Amira Pharmaceuticals, Inc. Antagonists of lysophosphatidic acid receptors
WO2012138648A1 (en) * 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors
WO2012138797A1 (en) * 2011-04-05 2012-10-11 Amira Pharmaceuticals, Inc. 3- or 5 - bi phenyl - 4 - ylisoxazole - based compounds useful for the treatment of fibrosis, pain, cancer and respiratory, allergic, nervous system or cardiovascular disorders
US20130253004A1 (en) * 2010-12-07 2013-09-26 Amira Pharmaceuticals, Inc. Lysophosphatidic acid receptor antagonists and their use in the treatment fibrosis
WO2017086430A1 (ja) * 2015-11-20 2017-05-26 宇部興産株式会社 Ｎａｓｈの治療又は予防のための医薬組成物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2474748B (en) * 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
GB2474120B (en) * 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
US9526091B2 (en) * 2012-03-16 2016-12-20 Intel Corporation Method and apparatus for coordination of self-optimization functions in a wireless network

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010077882A2 (en) * 2008-12-15 2010-07-08 Amira Pharmaceuticals, Inc. Antagonists of lysophosphatidic acid receptors
US20130253004A1 (en) * 2010-12-07 2013-09-26 Amira Pharmaceuticals, Inc. Lysophosphatidic acid receptor antagonists and their use in the treatment fibrosis
WO2012138797A1 (en) * 2011-04-05 2012-10-11 Amira Pharmaceuticals, Inc. 3- or 5 - bi phenyl - 4 - ylisoxazole - based compounds useful for the treatment of fibrosis, pain, cancer and respiratory, allergic, nervous system or cardiovascular disorders
WO2012138648A1 (en) * 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors
WO2017086430A1 (ja) * 2015-11-20 2017-05-26 宇部興産株式会社 Ｎａｓｈの治療又は予防のための医薬組成物

Also Published As

Publication number Publication date
US20220281845A1 (en) 2022-09-08
KR102341064B1 (ko) 2021-12-20
ES2966827T3 (es) 2024-04-24
EP3679032A1 (en) 2020-07-15
EA039482B1 (ru) 2022-02-01
KR20200035440A (ko) 2020-04-03
CA3073983A1 (en) 2019-03-07
WO2019046239A1 (en) 2019-03-07
WO2019041340A1 (en) 2019-03-07
EA202090368A1 (ru) 2020-06-09
CA3073983C (en) 2023-10-17
US11365185B2 (en) 2022-06-21
IL273000A (en) 2020-04-30
JP2020532550A (ja) 2020-11-12
US12145924B2 (en) 2024-11-19
AU2018323969A1 (en) 2020-02-20
CN111032647A (zh) 2020-04-17
BR112020002217A2 (pt) 2020-07-28
US20200231568A1 (en) 2020-07-23
EP3679032B1 (en) 2023-10-04
SA520411406B1 (ar) 2022-08-28
IL273000B2 (en) 2023-08-01
JP6854386B2 (ja) 2021-04-07
CN111032647B (zh) 2023-05-02
MX2020002430A (es) 2020-07-13
IL273000B1 (en) 2023-04-01

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