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PE20201148A1 - Compuestos biciclicos 5,6-fusionados y composiciones para el tratamiento de enfermedades parasitarias - Google Patents

Compuestos biciclicos 5,6-fusionados y composiciones para el tratamiento de enfermedades parasitarias

Info

Publication number
PE20201148A1
PE20201148A1 PE2019002477A PE2019002477A PE20201148A1 PE 20201148 A1 PE20201148 A1 PE 20201148A1 PE 2019002477 A PE2019002477 A PE 2019002477A PE 2019002477 A PE2019002477 A PE 2019002477A PE 20201148 A1 PE20201148 A1 PE 20201148A1
Authority
PE
Peru
Prior art keywords
treatment
parasitic diseases
haloalkyl
substituted
compositions
Prior art date
Application number
PE2019002477A
Other languages
English (en)
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
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 PE20201148A1 publication Critical patent/PE20201148A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/417Imidazole-alkylamines, e.g. histamine, phentolamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/555Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • 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)

Abstract

Referido a un compuesto de formula I, o una sal farmaceuticamente aceptable del mismo, o estereoisomero del mismo; en donde el anillo A es fenilo o piridinilo; R1 se selecciona entre: (a) C1-6 alquilo no sustituido o sustituido por 1 a 3 sustituyentes, entre otros; (b) C1-4 alcoxi no sustituido por C1-4 haloalquilo; (c) -NR5R5b en donde R5a y R5b son independientmente H, C1-4 alquilo, C1-4 haloalquilo, entre otros; (d) C3-6 cicloalquilo, C3-6 cicloalquenilo, o espiropentilo monociclico, entre otros; (e) fenilo o heteroarilo de 5-6 miembros que comprende 1 a 2 heteroatomos independientemente seleccionados entre N, O y S; R3 es H o halogeno; n es 0 o 1; R4 es H, halogeno, C1-6 haloalquilo o C1-6 alquilo no sustituido o sustituido por C3-6cicloalquilo, entre otros. Estos compuestos biciclicos 5,6-fusionados se usan para el tratamiento de enfermedades parasitarias, en donde se usan en combinacion con agentes farmacologicamente activos.
PE2019002477A 2017-05-31 2018-05-29 Compuestos biciclicos 5,6-fusionados y composiciones para el tratamiento de enfermedades parasitarias PE20201148A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762513211P 2017-05-31 2017-05-31
US201762581919P 2017-11-06 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
PE20201148A1 true PE20201148A1 (es) 2020-10-26

Family

ID=62749123

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2019002477A PE20201148A1 (es) 2017-05-31 2018-05-29 Compuestos biciclicos 5,6-fusionados y composiciones para el tratamiento de enfermedades parasitarias

Country Status (26)

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

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
CN115397807B (zh) * 2020-04-17 2024-08-13 帝斯曼知识产权资产管理有限公司 用于制备取代的烯胺化合物的方法
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
BRPI0407811A (pt) 2003-02-27 2006-02-14 Uriach Y Compania S A J composto derivados de pirazolopiridina, processo para a preparação dos mesmos, composição farmacêutica e respectivos uso
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
DK2925757T3 (en) 2012-11-19 2018-01-15 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
WO2014151729A1 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
UY35400A (es) 2013-03-15 2014-10-31 Novartis Ag Compuestos y composiciones para el tratamiento de enfermedades parasitarias
HRP20182021T1 (hr) * 2013-12-19 2019-01-25 Novartis Ag Derivati [1,2,4]triazolo[1,5-a]pirimidina kao inhibitori proteazoma protozoe za liječenje parazitskih bolesti poput lišmenijaze
ES2700352T3 (es) 2014-12-02 2019-02-15 Bayer Cropscience Ag Compuestos bicíclicos como pesticidas
WO2016144351A1 (en) 2015-03-11 2016-09-15 E. I. Du Pont De Nemours And Company Heterocycle-substituted bicyclic azole pesticides
CA2987329A1 (en) * 2015-05-29 2016-12-08 Glaxosmithkline Intellectual Property Development Limited Imidazo[1,2-b][1,2,4]triazine derivatives as antiparasitic agents
DK3331885T3 (da) * 2015-08-07 2021-01-18 Glaxosmithkline Ip Dev Ltd Forbindelser
EP3763704A1 (en) 2016-05-03 2021-01-13 Bayer Pharma Aktiengesellschaft Aromatic sulfonamide derivatives
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
AU2018276190B2 (en) 2020-05-14
JP2020521775A (ja) 2020-07-27
EP3630771B1 (en) 2022-06-29
DOP2019000299A (es) 2019-12-15
PH12019502652A1 (en) 2020-07-13
CO2019013254A2 (es) 2020-01-17
UY37745A (es) 2019-01-02
MX389106B (es) 2025-03-20
CL2019003467A1 (es) 2020-03-13
CN110678468B (zh) 2022-07-29
IL270927A (en) 2020-01-30
US20220324863A1 (en) 2022-10-13
RU2738647C1 (ru) 2020-12-15
WO2018220531A1 (en) 2018-12-06
AR111826A1 (es) 2019-08-21
KR20200010275A (ko) 2020-01-30
IL270927B (en) 2022-01-01
ES2927207T3 (es) 2022-11-03
ECSP19084722A (es) 2019-12-27
US20200109142A1 (en) 2020-04-09
JP7187490B2 (ja) 2022-12-12
MX2019014321A (es) 2020-02-05
MA50495A (fr) 2021-04-28
CU20190095A7 (es) 2020-10-20
EP3630771A1 (en) 2020-04-08
TW201902894A (zh) 2019-01-16
CU24543B1 (es) 2021-08-06
AU2018276190A1 (en) 2019-11-07
CA3060990A1 (en) 2018-12-06
BR112019024804A2 (pt) 2020-06-09
JOP20190278A1 (ar) 2019-11-28
CR20190545A (es) 2020-01-15
CN110678468A (zh) 2020-01-10
US11384078B2 (en) 2022-07-12

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