CA3060990A1 - 5,6-fused-bicyclic compounds and compositions for the treatment of parasitic diseases - Google Patents

5,6-fused-bicyclic compounds and compositions for the treatment of parasitic diseases Download PDF

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Publication number
CA3060990A1
CA3060990A1 CA3060990A CA3060990A CA3060990A1 CA 3060990 A1 CA3060990 A1 CA 3060990A1 CA 3060990 A CA3060990 A CA 3060990A CA 3060990 A CA3060990 A CA 3060990A CA 3060990 A1 CA3060990 A1 CA 3060990A1
Authority
CA
Canada
Prior art keywords
pyridin
pyrazolo
fluoro
carboxamide
independently selected
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.)
Pending
Application number
CA3060990A
Other languages
English (en)
French (fr)
Inventor
Jan Jiricek
Isabelle K. LERARIO
Fang Liang
Xiaodong Liu
Valentina Molteni
Advait Suresh NAGLE
Shuyi Pearly NG
Maxim RATNIKOV
Jeffrey M. Smith
Yongping Xie
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.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of CA3060990A1 publication Critical patent/CA3060990A1/en
Pending legal-status Critical Current

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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
    • A61K31/435—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
    • 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
    • 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
    • A61K31/13—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
    • A61K31/33—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
    • 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
    • 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

Landscapes

  • 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)
CA3060990A 2017-05-31 2018-05-29 5,6-fused-bicyclic compounds and compositions for the treatment of parasitic diseases Pending CA3060990A1 (en)

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 (1)

Publication Number Publication Date
CA3060990A1 true CA3060990A1 (en) 2018-12-06

Family

ID=62749123

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3060990A Pending CA3060990A1 (en) 2017-05-31 2018-05-29 5,6-fused-bicyclic compounds and compositions for the treatment of parasitic diseases

Country Status (26)

Country Link
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)
WO (1) WO2018220531A1 (enExample)

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

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
UY35400A (es) 2013-03-15 2014-10-31 Novartis Ag Compuestos y composiciones para el tratamiento de enfermedades parasitarias
US9186361B2 (en) 2013-03-15 2015-11-17 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
JP6392352B2 (ja) * 2013-12-19 2018-09-19 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
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
AR104749A1 (es) * 2015-05-29 2017-08-09 Glaxosmithkline Ip Dev Ltd Imidazo[1,2-b][1,2,4]triazina sustituida, composición farmacéutica y combinación que lo comprenden, y su uso para la fabricación de un medicamento
ES2856899T3 (es) * 2015-08-07 2021-09-28 Glaxosmithkline Ip Dev Ltd Compuestos
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

Also Published As

Publication number Publication date
PE20201148A1 (es) 2020-10-26
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
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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