CN110678468B - 用于治疗寄生虫病的5,6-稠合双环化合物及其组合物 - Google Patents

用于治疗寄生虫病的5,6-稠合双环化合物及其组合物 Download PDF

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Publication number
CN110678468B
CN110678468B CN201880034658.0A CN201880034658A CN110678468B CN 110678468 B CN110678468 B CN 110678468B CN 201880034658 A CN201880034658 A CN 201880034658A CN 110678468 B CN110678468 B CN 110678468B
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China
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pyridin
pyrazolo
fluoro
carboxamide
phenyl
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Chinese (zh)
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CN110678468A (zh
Inventor
J·基里塞克
I·K·勒拉里奥
梁芳
刘晓东
V·莫尔泰尼
A·S·内格尔
S·P·恩哥
M·拉特尼科夫
J·M·史密斯
谢永平
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Novartis AG
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed 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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/417—Imidazole-alkylamines, e.g. histamine, phentolamine
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201880034658.0A 2017-05-31 2018-05-29 用于治疗寄生虫病的5,6-稠合双环化合物及其组合物 Active CN110678468B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762513211P 2017-05-31 2017-05-31
US62/513,211 2017-05-31
US201762581919P 2017-11-06 2017-11-06
US62/581,919 2017-11-06
PCT/IB2018/053818 WO2018220531A1 (en) 2017-05-31 2018-05-29 5,6-fused-bicyclic compounds and compositions for the treatment of parasitic diseases

Publications (2)

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CN110678468A CN110678468A (zh) 2020-01-10
CN110678468B true CN110678468B (zh) 2022-07-29

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US (2) US11384078B2 (https=)
EP (1) EP3630771B1 (https=)
JP (1) JP7187490B2 (https=)
KR (1) KR20200010275A (https=)
CN (1) CN110678468B (https=)
AR (1) AR111826A1 (https=)
AU (1) AU2018276190B2 (https=)
BR (1) BR112019024804A2 (https=)
CA (1) CA3060990A1 (https=)
CL (1) CL2019003467A1 (https=)
CO (1) CO2019013254A2 (https=)
CR (1) CR20190545A (https=)
CU (1) CU24543B1 (https=)
DO (1) DOP2019000299A (https=)
EC (1) ECSP19084722A (https=)
ES (1) ES2927207T3 (https=)
IL (1) IL270927B (https=)
JO (1) JOP20190278A1 (https=)
MA (1) MA50495A (https=)
MX (1) MX389106B (https=)
PE (1) PE20201148A1 (https=)
PH (1) PH12019502652A1 (https=)
RU (1) RU2738647C1 (https=)
TW (1) TW201902894A (https=)
UY (1) UY37745A (https=)
WO (1) WO2018220531A1 (https=)

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Publication number Priority date Publication date Assignee Title
JOP20190278A1 (ar) * 2017-05-31 2019-11-28 Novartis Ag مركبات 5، 6-ثنائية الحلقة مندمجة وتركيبات لعلاج الأمراض الطفيلية
EP4136066A1 (en) * 2020-04-17 2023-02-22 DSM IP Assets B.V. A process for preparation of substituted enamine compounds
WO2021259163A1 (zh) * 2020-06-23 2021-12-30 上海美悦生物科技发展有限公司 一种稠和吡唑类化合物的制备方法

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WO2014151784A1 (en) * 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
CN106029666A (zh) * 2013-12-19 2016-10-12 诺华股份有限公司 作为原生动物蛋白酶体抑制剂用于治疗寄生虫疾病例如利什曼病的[1,2,4]三唑并[1,5-a]嘧啶衍生物
WO2016193111A1 (en) * 2015-05-29 2016-12-08 Glaxosmithkline Intellectual Property Development Limited Imidazo[1,2-b][1,2,4]triazine derivatives as antiparasitic agents
WO2017025416A1 (en) * 2015-08-07 2017-02-16 Glaxosmithkline Intellectual Property Development Limited Compounds

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DE10053275A1 (de) * 2000-10-27 2002-05-02 Dresden Arzneimittel Neue 7-Azaindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
KR101312736B1 (ko) 2003-02-27 2013-09-27 팔라우 파르마 에스에이 피라졸로피리딘 유도체
TW201238487A (en) 2011-02-25 2012-10-01 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
WO2013067302A1 (en) * 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
WO2013106254A1 (en) * 2012-01-11 2013-07-18 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
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US9186361B2 (en) * 2013-03-15 2015-11-17 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
EP3227288B1 (de) 2014-12-02 2018-08-29 Bayer CropScience AG Bicyclische verbindungen als schädlingsbekämpfungsmittel
CN112608300B (zh) 2015-03-11 2024-04-26 Fmc公司 杂环取代的二环唑杀有害生物剂
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WO2014151784A1 (en) * 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
CN106029666A (zh) * 2013-12-19 2016-10-12 诺华股份有限公司 作为原生动物蛋白酶体抑制剂用于治疗寄生虫疾病例如利什曼病的[1,2,4]三唑并[1,5-a]嘧啶衍生物
WO2016193111A1 (en) * 2015-05-29 2016-12-08 Glaxosmithkline Intellectual Property Development Limited Imidazo[1,2-b][1,2,4]triazine derivatives as antiparasitic agents
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KR20200010275A (ko) 2020-01-30
US20220324863A1 (en) 2022-10-13
IL270927B (en) 2022-01-01
CU20190095A7 (es) 2020-10-20
US11384078B2 (en) 2022-07-12
JP7187490B2 (ja) 2022-12-12
JP2020521775A (ja) 2020-07-27
ES2927207T3 (es) 2022-11-03
JOP20190278A1 (ar) 2019-11-28
BR112019024804A2 (pt) 2020-06-09
CU24543B1 (es) 2021-08-06
DOP2019000299A (es) 2019-12-15
AU2018276190B2 (en) 2020-05-14
CO2019013254A2 (es) 2020-01-17
EP3630771A1 (en) 2020-04-08
MX389106B (es) 2025-03-20
AU2018276190A1 (en) 2019-11-07
US20200109142A1 (en) 2020-04-09
ECSP19084722A (es) 2019-12-27
IL270927A (en) 2020-01-30
AR111826A1 (es) 2019-08-21
EP3630771B1 (en) 2022-06-29
CN110678468A (zh) 2020-01-10
UY37745A (es) 2019-01-02
PH12019502652A1 (en) 2020-07-13
WO2018220531A1 (en) 2018-12-06
CA3060990A1 (en) 2018-12-06
TW201902894A (zh) 2019-01-16
CR20190545A (es) 2020-01-15
CL2019003467A1 (es) 2020-03-13
MA50495A (fr) 2021-04-28
RU2738647C1 (ru) 2020-12-15
MX2019014321A (es) 2020-02-05
PE20201148A1 (es) 2020-10-26

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