JP7187490B2 - 寄生虫症の治療のための５，６－縮合二環式化合物及び組成物 - Google Patents

寄生虫症の治療のための５，６－縮合二環式化合物及び組成物 Download PDF

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JP7187490B2
JP7187490B2 JP2019565535A JP2019565535A JP7187490B2 JP 7187490 B2 JP7187490 B2 JP 7187490B2 JP 2019565535 A JP2019565535 A JP 2019565535A JP 2019565535 A JP2019565535 A JP 2019565535A JP 7187490 B2 JP7187490 B2 JP 7187490B2
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alkyl
compound
independently selected
unsubstituted
pharmaceutically acceptable
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JP2020521775A (ja
JP2020521775A5 (enExample
Inventor
ジリセック，ジャン
ケー． レラリオ，イザベル
リアン，ファン
リウ，シャオドン
モルテニ，バレンティーナ
スレッシュ ネーグル，アドベイト
パーリー ウン，シュイ
ラトニコフ，マキシム
エム． スミス，ジェフリー
シエ，ヨンピン
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ノバルティス アーゲー
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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
    • 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
    • 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
    • A61K31/185—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
    • A61K31/33—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
    • A61K31/33—Heterocyclic compounds
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • 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
    • 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
    • A61K31/13—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
    • A61K31/33—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
    • 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)
JP2019565535A 2017-05-31 2018-05-29 寄生虫症の治療のための５，６－縮合二環式化合物及び組成物 Expired - Fee Related JP7187490B2 (ja)

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 (3)

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JP2020521775A JP2020521775A (ja) 2020-07-27
JP2020521775A5 JP2020521775A5 (enExample) 2021-07-26
JP7187490B2 true JP7187490B2 (ja) 2022-12-12

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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)
UY (1) UY37745A (enExample)
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Families Citing this family (3)

* Cited by examiner, † Cited by third party
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

Citations (8)

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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
WO2014151729A1 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
WO2014151784A1 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
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
JP2017501177A (ja) 2013-12-19 2017-01-12 ノバルティス アーゲー リーシュマニア症などの寄生虫病を処置するための原生動物のプロテアソーム阻害剤としての［１，２，４］トリアゾロ［１，５−ａ］ピリミジン誘導体
WO2017025416A1 (en) 2015-08-07 2017-02-16 Glaxosmithkline Intellectual Property Development Limited Compounds
JP2019519484A (ja) 2016-05-03 2019-07-11 バイエル・ファルマ・アクティエンゲゼルシャフト 芳香族スルホンアミド誘導体

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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
LT2925757T (lt) 2012-11-19 2017-12-27 Novartis Ag Junginiai ir kompozicijos, skirti parazitinių ligų gydymui
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
JOP20190278A1 (ar) * 2017-05-31 2019-11-28 Novartis Ag مركبات 5، 6-ثنائية الحلقة مندمجة وتركيبات لعلاج الأمراض الطفيلية

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2014151729A1 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
WO2014151784A1 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
JP2017501177A (ja) 2013-12-19 2017-01-12 ノバルティス アーゲー リーシュマニア症などの寄生虫病を処置するための原生動物のプロテアソーム阻害剤としての［１，２，４］トリアゾロ［１，５−ａ］ピリミジン誘導体
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
JP2019519484A (ja) 2016-05-03 2019-07-11 バイエル・ファルマ・アクティエンゲゼルシャフト 芳香族スルホンアミド誘導体

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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
AU2018276190B2 (en) 2020-05-14
CN110678468B (zh) 2022-07-29
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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