CN111511363A - 用于治疗化学治疗诱导的医源性疼痛的C5aR抑制剂 - Google Patents

用于治疗化学治疗诱导的医源性疼痛的C5aR抑制剂 Download PDF

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Publication number
CN111511363A
CN111511363A CN201880080117.1A CN201880080117A CN111511363A CN 111511363 A CN111511363 A CN 111511363A CN 201880080117 A CN201880080117 A CN 201880080117A CN 111511363 A CN111511363 A CN 111511363A
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phenyl
group
ethyl
branched
amino
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Chinese (zh)
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劳拉·布兰多利尼
蒂亚戈·马塔尔·库尼亚
马尔塞洛·阿莱格雷蒂
安德烈亚·阿拉米尼
詹卢卡·比安基尼
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Dompe Farmaceutici SpA
Dompe SpA
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Dompe SpA
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles 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
    • A61K31/13—Amines
    • A61K31/145—Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
    • 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
    • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies

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  • Health & Medical Sciences (AREA)
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  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201880080117.1A 2017-12-12 2018-12-11 用于治疗化学治疗诱导的医源性疼痛的C5aR抑制剂 Pending CN111511363A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17206813.2A EP3498269A1 (en) 2017-12-12 2017-12-12 C5ar inhibitors for use in the treatment of chemotherapy-induced iatrogenic pain
EP17206813.2 2017-12-12
PCT/EP2018/084277 WO2019115493A2 (en) 2017-12-12 2018-12-11 C5ar inhibitors for use in the treatment of chemotherapy-induced iatrogenic pain

Publications (1)

Publication Number Publication Date
CN111511363A true CN111511363A (zh) 2020-08-07

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CN201880080117.1A Pending CN111511363A (zh) 2017-12-12 2018-12-11 用于治疗化学治疗诱导的医源性疼痛的C5aR抑制剂

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US (2) US12102607B2 (https=)
EP (3) EP3498269A1 (https=)
JP (2) JP7430141B2 (https=)
KR (2) KR20250041193A (https=)
CN (1) CN111511363A (https=)
AU (1) AU2018385364B2 (https=)
BR (1) BR112020009972A2 (https=)
CA (1) CA3082762A1 (https=)
IL (1) IL275132A (https=)
MA (1) MA51128A (https=)
RU (1) RU2020122678A (https=)
SG (1) SG11202004322VA (https=)
WO (1) WO2019115493A2 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4059497A1 (en) * 2021-03-17 2022-09-21 Dompé farmaceutici S.p.a. C5ar1 inhibitors for treating hypersensitivity reactions to taxanes
BR112023018826A2 (pt) * 2021-03-17 2024-03-12 Dompe Farm Spa Inibidores de c5ar1 para tratamento de reações de hipersensibilidade a taxanos
EP4397306A1 (en) * 2023-01-05 2024-07-10 Dompe' Farmaceutici S.P.A. C5ar1 inhibitors for use in the treatment of ocular mucous membrane pemphigoid and/or oral mucous membrane pemphigoid

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101360706A (zh) * 2005-11-24 2009-02-04 冬姆佩制药股份公司 (r)-芳基烷基氨基衍生物及其药物组合物
CN101827841A (zh) * 2007-10-18 2010-09-08 多派股份公司 (r)-4-(杂芳基)苯乙基衍生物及其药物组合物
EP3192504A1 (en) * 2016-01-15 2017-07-19 Dompé farmaceutici S.p.A. Il-8 inhibitors for use in the treatment of chemotherapy-induced peripheral neuropathy
WO2017121838A1 (en) * 2016-01-15 2017-07-20 Dompe' Farmaceutici S.P.A. Il-8 inhibitors for use in the treatment of chemotherapy-induced peripheral neuropathy

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL1776336T3 (pl) * 2004-03-23 2010-06-30 Dompe Farm Spa Pochodne kwasu 2-fenylopropionowego i zawierające je kompozycje farmaceutyczne
HRP20151052T1 (xx) 2007-07-19 2015-11-06 H. Lundbeck A/S Peteroäślani heterocikliäśki amidi i srodne tvari

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101360706A (zh) * 2005-11-24 2009-02-04 冬姆佩制药股份公司 (r)-芳基烷基氨基衍生物及其药物组合物
CN101827841A (zh) * 2007-10-18 2010-09-08 多派股份公司 (r)-4-(杂芳基)苯乙基衍生物及其药物组合物
EP3192504A1 (en) * 2016-01-15 2017-07-19 Dompé farmaceutici S.p.A. Il-8 inhibitors for use in the treatment of chemotherapy-induced peripheral neuropathy
WO2017121838A1 (en) * 2016-01-15 2017-07-20 Dompe' Farmaceutici S.P.A. Il-8 inhibitors for use in the treatment of chemotherapy-induced peripheral neuropathy

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
ALESSIO MORICONI等: "Targeting the minor pocket of C5aR for the rational design of an oral allosteric inhibitor for inflammatory and neuropathic pain relief", 《PNAS》 *
JIJUN XU等: "Role of Complement in Paclitaxel-induced Peripheral Neuropathy", 《ASA ABSTRACT，HTTP://WWW.ASAABSTRACTS.COM/STRANDS/ASAABSTRACTS/ABSTRACT.HTM?YEAR=2017&INDEX=3&ABSNUM=3878》 *
K.R. MAYILYAN等: "The complement system and innate immunity", 《NUCLEIC ACIDS AND MOLECULAR BIOLOGY》 *
WARWICK, CHARLES A.: "The role of complement component C5a in nociceptive sensitization", 《UNIVERSITY OF IOWA》 *

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RU2020122678A3 (https=) 2022-02-15
BR112020009972A2 (pt) 2021-02-09
MA51128A (fr) 2021-03-24
KR20200108839A (ko) 2020-09-21
IL275132A (en) 2020-07-30
KR20250041193A (ko) 2025-03-25
CA3082762A1 (en) 2019-06-20
EP3498269A1 (en) 2019-06-19
EP3723744C0 (en) 2026-03-18
EP4706762A2 (en) 2026-03-11
US20240398731A1 (en) 2024-12-05
JP2024028984A (ja) 2024-03-05
RU2020122678A (ru) 2022-01-13
US12102607B2 (en) 2024-10-01
EP3723744A2 (en) 2020-10-21
AU2018385364B2 (en) 2024-04-04
JP2021505647A (ja) 2021-02-18
EP3723744B1 (en) 2026-03-18
WO2019115493A3 (en) 2019-07-25
JP7430141B2 (ja) 2024-02-09
SG11202004322VA (en) 2020-07-29
WO2019115493A2 (en) 2019-06-20
US20200397725A1 (en) 2020-12-24
AU2018385364A1 (en) 2020-07-09

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