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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Expired - Fee Related
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CN201880034658.0A
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English (en)
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)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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 Expired - Fee Related 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 (enExample)
EP (1) EP3630771B1 (enExample)
JP (1) JP7187490B2 (enExample)
KR (1) KR20200010275A (enExample)
CN (1) CN110678468B (enExample)
AR (1) AR111826A1 (enExample)
AU (1) AU2018276190B2 (enExample)
BR (1) BR112019024804A2 (enExample)
CA (1) CA3060990A1 (enExample)
CL (1) CL2019003467A1 (enExample)
CO (1) CO2019013254A2 (enExample)
CR (1) CR20190545A (enExample)
CU (1) CU24543B1 (enExample)
DO (1) DOP2019000299A (enExample)
EC (1) ECSP19084722A (enExample)
ES (1) ES2927207T3 (enExample)
IL (1) IL270927B (enExample)
JO (1) JOP20190278A1 (enExample)
MA (1) MA50495A (enExample)
MX (1) MX389106B (enExample)
PE (1) PE20201148A1 (enExample)
PH (1) PH12019502652A1 (enExample)
RU (1) RU2738647C1 (enExample)
TW (1) TW201902894A (enExample)
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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
CN113831320B (zh) * 2020-06-23 2024-04-05 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
UA81453C2 (en) 2003-02-27 2008-01-10 Pyrazolopyridine derivates
WO2012116246A2 (en) 2011-02-25 2012-08-30 Dow Agrosciences Llc Pesticidal compostions 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
LT2925757T (lt) 2012-11-19 2017-12-27 Novartis Ag Junginiai ir kompozicijos, skirti parazitinių ligų gydymui
US9186361B2 (en) 2013-03-15 2015-11-17 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
ES2700352T3 (es) 2014-12-02 2019-02-15 Bayer Cropscience Ag Compuestos bicíclicos como pesticidas
CN107635984B (zh) 2015-03-11 2021-04-13 Fmc公司 杂环取代的二环唑杀有害生物剂
CU24516B1 (es) 2016-05-03 2021-05-12 Bayer Pharma AG Derivados aromáticos de sulfonamida útiles como medicamentos contra enfermedades asociadas con dolor
JOP20190278A1 (ar) * 2017-05-31 2019-11-28 Novartis Ag مركبات 5، 6-ثنائية الحلقة مندمجة وتركيبات لعلاج الأمراض الطفيلية

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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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PE20201148A1 (es) 2020-10-26
CA3060990A1 (en) 2018-12-06
JP2020521775A (ja) 2020-07-27
WO2018220531A1 (en) 2018-12-06
TW201902894A (zh) 2019-01-16
JP7187490B2 (ja) 2022-12-12
AU2018276190B2 (en) 2020-05-14
MX2019014321A (es) 2020-02-05
US20200109142A1 (en) 2020-04-09
EP3630771A1 (en) 2020-04-08
RU2738647C1 (ru) 2020-12-15
MX389106B (es) 2025-03-20
AU2018276190A1 (en) 2019-11-07
DOP2019000299A (es) 2019-12-15
EP3630771B1 (en) 2022-06-29
KR20200010275A (ko) 2020-01-30
IL270927A (en) 2020-01-30
PH12019502652A1 (en) 2020-07-13
CL2019003467A1 (es) 2020-03-13
MA50495A (fr) 2021-04-28
ES2927207T3 (es) 2022-11-03
ECSP19084722A (es) 2019-12-27
CU20190095A7 (es) 2020-10-20
BR112019024804A2 (pt) 2020-06-09
CR20190545A (es) 2020-01-15
JOP20190278A1 (ar) 2019-11-28
US20220324863A1 (en) 2022-10-13
CO2019013254A2 (es) 2020-01-17
AR111826A1 (es) 2019-08-21
CN110678468A (zh) 2020-01-10
US11384078B2 (en) 2022-07-12
IL270927B (en) 2022-01-01
UY37745A (es) 2019-01-02
CU24543B1 (es) 2021-08-06

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