CN111032647B - 溶血磷脂酸受体1(lpar1)抑制剂化合物 - Google Patents

溶血磷脂酸受体1(lpar1)抑制剂化合物 Download PDF

Info

Publication number
CN111032647B
CN111032647B CN201880053540.2A CN201880053540A CN111032647B CN 111032647 B CN111032647 B CN 111032647B CN 201880053540 A CN201880053540 A CN 201880053540A CN 111032647 B CN111032647 B CN 111032647B
Authority
CN
China
Prior art keywords
methyl
mmol
phenyl
pyrazol
amino
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201880053540.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN111032647A (zh
Inventor
马天伟
吴亮
张学军
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN111032647A publication Critical patent/CN111032647A/zh
Application granted granted Critical
Publication of CN111032647B publication Critical patent/CN111032647B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CN201880053540.2A 2017-09-04 2018-08-28 溶血磷脂酸受体1(lpar1)抑制剂化合物 Active CN111032647B (zh)

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)
CNPCT/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
CN111032647A CN111032647A (zh) 2020-04-17
CN111032647B true CN111032647B (zh) 2023-05-02

Family

ID=63528947

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880053540.2A Active CN111032647B (zh) 2017-09-04 2018-08-28 溶血磷脂酸受体1(lpar1)抑制剂化合物

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 (9)

* 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
TWI838626B (zh) 2020-06-03 2024-04-11 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
AU2021282986B2 (en) 2020-06-03 2024-03-07 Gilead Sciences, Inc. LPA receptor antagonists and uses thereof
KR20240005892A (ko) 2021-05-11 2024-01-12 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
AU2022405082B2 (en) 2021-12-08 2025-09-25 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
CN120322431A (zh) * 2022-11-24 2025-07-15 罗特斯生物公司 用于治疗与lpa受体活性相关的病症的化合物和组合物
WO2024249867A1 (en) * 2023-06-02 2024-12-05 Am Sciences Compounds for treating fibrotic diseases

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012138648A1 (en) * 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors
CN103347510A (zh) * 2010-12-07 2013-10-09 艾米拉医药股份有限公司 溶血磷脂酸受体拮抗剂及其在治疗纤维化中的用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2466121B (en) * 2008-12-15 2010-12-08 Amira Pharmaceuticals Inc Antagonists of lysophosphatidic acid receptors
GB2474120B (en) * 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
GB2474748B (en) * 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
EP2694496A1 (en) * 2011-04-05 2014-02-12 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
US9526091B2 (en) * 2012-03-16 2016-12-20 Intel Corporation Method and apparatus for coordination of self-optimization functions in a wireless network
CA3005811A1 (en) * 2015-11-20 2017-05-26 Ube Industries, Ltd. Pharmaceutical composition for treatment or prevention of nash

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103347510A (zh) * 2010-12-07 2013-10-09 艾米拉医药股份有限公司 溶血磷脂酸受体拮抗剂及其在治疗纤维化中的用途
WO2012138648A1 (en) * 2011-04-06 2012-10-11 Irm Llc Compositions and methods for modulating lpa receptors

Also Published As

Publication number Publication date
AU2018323969B2 (en) 2020-07-16
KR20200035440A (ko) 2020-04-03
US12145924B2 (en) 2024-11-19
AU2018323969A1 (en) 2020-02-20
CN111032647A (zh) 2020-04-17
JP2020532550A (ja) 2020-11-12
IL273000A (en) 2020-04-30
CA3073983A1 (en) 2019-03-07
US11365185B2 (en) 2022-06-21
IL273000B2 (en) 2023-08-01
SA520411406B1 (ar) 2022-08-28
EP3679032B1 (en) 2023-10-04
WO2019041340A1 (en) 2019-03-07
EA039482B1 (ru) 2022-02-01
ES2966827T3 (es) 2024-04-24
IL273000B1 (en) 2023-04-01
EP3679032A1 (en) 2020-07-15
US20220281845A1 (en) 2022-09-08
KR102341064B1 (ko) 2021-12-20
MX2020002430A (es) 2020-07-13
EA202090368A1 (ru) 2020-06-09
BR112020002217A2 (pt) 2020-07-28
US20200231568A1 (en) 2020-07-23
WO2019046239A1 (en) 2019-03-07
CA3073983C (en) 2023-10-17
JP6854386B2 (ja) 2021-04-07

Similar Documents

Publication Publication Date Title
CN111032647B (zh) 溶血磷脂酸受体1(lpar1)抑制剂化合物
CN110337294B (zh) 作为cftr增效剂的吡咯并嘧啶
TWI628176B (zh) 蛋白質激酶抑制劑
CN105120864B (zh) 表现出抗癌活性和抗增殖活性的2‑氨基嘧啶‑6‑酮及类似物
CN103118680B (zh) 杂芳基甲酰胺
CN103249720B (zh) 作为hdl-胆固醇升高剂的肟化合物
KR20220003173A (ko) 화합물 및 이의 용도
WO2014020350A1 (en) Par2 receptor antagonists
KR20090125779A (ko) 브라디키닌 ｂ2 수용체 조절제로서 8-옥시-퀴놀린 유도체
KR20210005593A (ko) 화합물 및 이의 용도
TW201623239A (zh) 新穎２－胺基－吡啶及２－胺基－嘧啶衍生物及其醫藥用途
TW202118759A (zh) 用於治療癌症之１，２，４—二唑—５—酮衍生物
JP2020531488A (ja) ピリジンアミン−ピリドンおよびピリミジンアミン−ピリドン化合物
CN104039766A (zh) 药物化合物
KR20170016988A (ko) 할로겐 치환 헤테로환 화합물의 염
CN115605467A (zh) Phd抑制剂化合物、组合物和其用途
WO2021104486A1 (zh) 一种含苯环的化合物及其应用
KR102707476B1 (ko) 피라졸-카르복스아미드 유도체 화합물 및 이의 용도
CN103153957B (zh) N-吡啶-3-基或n-吡嗪-2-基甲酰胺类
IL296632A (en) phd inhibitory compounds, compositions and use
CN103781765A (zh) 作为hdl-胆固醇升高剂的3-吡啶甲酰肼类
BR112020002217B1 (pt) Compostos inibidores do receptor de ácido lisfosfatídico 1 (lpar1)
CN115279747A (zh) 新型fyn和vegfr2激酶抑制剂
HK1138844A (en) 8-oxy-quinoline derivatives as bradykinin b2 receptor modulators
HK1209119B (en) Pyrazol-1-yl benzene sulfonamides as ccr9 antagonists

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant