HRP20220377T1 - Biljni ekstrakti obogaćeni derivatima ipolamida kao imunosupresivi za liječenje imunoloških poremećaja - Google Patents

Biljni ekstrakti obogaćeni derivatima ipolamida kao imunosupresivi za liječenje imunoloških poremećaja Download PDF

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HRP20220377T1
HRP20220377T1 HRP20220377TT HRP20220377T HRP20220377T1 HR P20220377 T1 HRP20220377 T1 HR P20220377T1 HR P20220377T T HRP20220377T T HR P20220377TT HR P20220377 T HRP20220377 T HR P20220377T HR P20220377 T1 HRP20220377 T1 HR P20220377T1
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Prior art keywords
ipolamide
formula
extract
plant biomass
derivatives
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HRP20220377TT
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English (en)
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Cristiano Ruch Werneck GUIMARÃES
Carlos Eduardo VITOR
Lisandra Ravanelli PESSA
Romulo Dragani REIS
Alessandra MASCARELLO
Fernando Henrique De Souza GAMA
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Aché Laboratórios Farmaceuticos S.A.
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Publication of HRP20220377T1 publication Critical patent/HRP20220377T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/94Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42Separation; Purification; Stabilisation; Use of additives
    • C07C51/47Separation; Purification; Stabilisation; Use of additives by solid-liquid treatment; by chemisorption
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/42Unsaturated compounds containing hydroxy or O-metal groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/76Unsaturated compounds containing keto groups
    • C07C59/90Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/76Unsaturated compounds containing keto groups
    • C07C59/92Unsaturated compounds containing keto groups containing —CHO groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/73Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
    • C07C69/738Esters of keto-carboxylic acids or aldehydo-carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/74Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C69/757Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a ring other than a six-membered aromatic ring having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrane Compounds (AREA)
  • Saccharide Compounds (AREA)

Claims (18)

1. Spojevi opće formule C, koji su derivati ipolamiida [image] pri čemu R odgovara H, OH, OGlyc (glikozid); R1, R1’, R1" odgovaraju H, OH; R2 odgovara H, COOH, COOCH3, CH3, CHO; R3 odgovara H, OH, CH3; R4, R4' odgovaraju H, OH, CH2OH, CH3.
2. Spojevi formule C prema zahtjevu 1, odabrani između: [image]
3. Spojevi formule C kako su definirani u zahtjevima 1 ili 2, za uporabu kao lijek.
4. Spojevi formule C prema zahtjevima 1 ili 2, za uporabu kao imunosupresivi u liječenju imunoloških poremećaja.
5. Spojevi formule C kako su definirani u zahtjevima 1 ili 2, za uporabu u liječenju vitiliga.
6. Farmaceutski pripravak sadrži derivate ipolamiida formule C kako je definirano u zahtjevima 1 ili 2, i farmaceutski prihvatljiv vehikul, koji izborno dodatno sadrži ipolamiid.
7. Postupak za proizvodnju ekstrakta obogaćenog derivatima ipolamiida formule C kako je definirano u zahtjevima 1 ili 2, koji sadrži korake: a) odabir ulazne biljne biomase s udjelom ipolamiida između 2.5% i 3.5% dobivene iz biljaka roda Stachytarpheta; b) podnošenje odabrane biomase iz a) sušenju u pećnici na temperaturi između 40 do 80°C, do postizanja stabilizacije vlažnosti između 10 do 12%; c) mljevenje biljne biomase; d) izvođenje ekstrakcije biljne biomase kroz korake: i. zagrijavanje biljne biomase na temperaturi od 70 do 100°C, uz stalno miješanje; ii. maceracija biljne biomase na sobnoj temperaturi; iii. zagrijavanje biljne biomase s temperaturom od 70 do 100°C.
8. Postupak za proizvodnju ekstrakta prema zahtjevu 7, dalje sadrži korake: iv. filtriranje i koncentriranje ekstrakta; v. sušenje u raspršivaču, tijekom 1 do 60 sekundi, s ulaznom temperaturom između 155 i 165°C i izlaznom temperaturom između 85 do 95°C, spojeno na odvlaživač zraka.
9. Postupak za proizvodnju ekstrakta, prema zahtjevu 7, u kojem se zagrijavanje biljne biomase d) točke iii) odvija 5 do 30 minuta.
10. Postupak za proizvodnju ekstrakta, prema zahtjevu 7, u kojem se zagrijavanje biljne biomase d) točke i) odvija 5 do 15 sati.
11. Postupak za proizvodnju ekstrakta prema zahtjevu 7, u kojem ulazna biljna biomasa obuhvaća nadzemne dijelove biljaka roda Stachytarpheta.
12. Postupak za proizvodnju ekstrakta prema zahtjevu 7, u kojem je biljka Stachytarpheta cayennensis.
13. Postupak za proizvodnju ekstrakta prema zahtjevu 7, u kojem postupak uključuje vodenu ekstrakciju.
14. Postupak za proizvodnju ekstrakta, prema bilo kojem od zahtjeva 7 do 13, koji sadrži korak predviđanja teoretskog sadržaja ipolamiida i njegovih derivata formule C u ekstraktu iz stvarnog sadržaja ipolamiida u ulaznoj biljnoj biomasi pomoću jednadžbe I: [image]
15. Ekstrakti iz biljaka roda Stachytarpheta obogaćeni derivatima ipolamiida formule C kako je definirano u zahtjevima 1 ili 2.
16. Ekstrakti biljaka iz roda Stachytarpheta obogaćeni derivatima ipolamiida formule C, dobiveni postupkom kako je definirano u bilo kojem od zahtjeva 7 do 14.
17. Ekstrakti biljaka iz roda Stachytarpheta prema zahtjevu 15 ili 16, koji sadrže od 1% do 20% ipolamiida ili derivata ipolamiida formule C.
18. Ekstrakti iz biljaka roda Stachytarpheta prema bilo kojem od zahtjeva 15 do 17, za uporabu kao imunosupresivi u liječenju imunoloških poremećaja.
HRP20220377TT 2017-02-17 2018-02-19 Biljni ekstrakti obogaćeni derivatima ipolamida kao imunosupresivi za liječenje imunoloških poremećaja HRP20220377T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
BR102017003318A BR102017003318A2 (pt) 2017-02-17 2017-02-17 compostos, processo de produção de compostos, extrato enriquecido, frações ativas de extrato enriquecido, processo de produção de extrato enriquecido, método de seleção de biomassa vegetal para produção de extrato enriquecido, composição e uso para tratamento de desordens imunológicas
PCT/BR2018/050037 WO2018148816A2 (en) 2017-02-17 2018-02-19 Compounds, process of production of compounds, enriched extract, enriched extract active fractions, enriched extract process of production, method for selecting vegetal biomass for enriched extract production, composition and use for treatment of immunological disorders
EP18707229.3A EP3583103B1 (en) 2017-02-17 2018-02-19 Plant extracts enriched with ipolamiide derivatives as immunosuppressants for treating immunological disorders

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US (1) US20200231561A1 (hr)
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CN (1) CN110475768B (hr)
AU (1) AU2018221956B2 (hr)
BR (2) BR102017003318A2 (hr)
CA (1) CA3052713A1 (hr)
CL (1) CL2019002309A1 (hr)
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EC (1) ECSP19058322A (hr)
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HR (1) HRP20220377T1 (hr)
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JPH0366682A (ja) * 1989-08-04 1991-03-22 Tsumura & Co 新規イリドイド誘導体
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AU2003224361B2 (en) * 2002-05-10 2008-01-31 Council Of Scientific And Industrial Research Hepatoprotective activity of 2'-p-Hydroxybenzoylmussaenosidic acid
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JP2008024670A (ja) 2006-07-24 2008-02-07 Daiwa Kagaku Kogyo Kk 害虫駆除剤
BRPI0700767B8 (pt) * 2007-02-15 2021-05-25 Ache Laboratorios Farmaceuticos Sa composição farmacêutica, produto farmaceutico, processo para obtenção de compostos farmaceuticos e uso de tais compostos para o tratamento do vitiligo
CN103120699B (zh) * 2011-11-18 2017-04-19 天津市国际生物医药联合研究院 环烯醚萜类化合物在制备抗sars的药物中的应用
CN103690551A (zh) * 2013-07-18 2014-04-02 江苏大学 猪殃殃中环烯醚萜苷提取物及其提取方法和医药用途
DE102015102020A1 (de) * 2015-02-12 2016-08-18 Renate Wilmanowicz Immunologisch aktives Phyto-Gemisch und seine Anwendung bei der Prävention und in einem Verfahren zur Behandlung von Effloreszenzen

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CN110475768A (zh) 2019-11-19
JP2020507607A (ja) 2020-03-12
PT3583103T (pt) 2022-03-25
CA3052713A1 (en) 2018-08-23
EP3583103A2 (en) 2019-12-25
US20200231561A1 (en) 2020-07-23
ES2909387T3 (es) 2022-05-06
CY1125187T1 (el) 2023-06-09
RS63162B1 (sr) 2022-05-31
JP2023061959A (ja) 2023-05-02
AU2018221956B2 (en) 2022-03-24
EP3583103B1 (en) 2022-01-12
EP4001270A1 (en) 2022-05-25
ECSP19058322A (es) 2019-10-31
IL268732A (en) 2019-10-31
BR112019017128A2 (pt) 2020-04-14
CN110475768B (zh) 2023-12-01
LT3583103T (lt) 2022-04-25
SG11201907375VA (en) 2019-09-27
MX2019009655A (es) 2020-07-24
AU2018221956A1 (en) 2019-08-29
SA519402443B1 (ar) 2023-02-08
PE20200449A1 (es) 2020-02-28
AU2022201835A1 (en) 2022-04-07
RU2019129095A (ru) 2021-03-17
ZA201906106B (en) 2020-08-26
JP7349362B2 (ja) 2023-09-22
WO2018148816A3 (en) 2018-10-18
MX2022012282A (es) 2022-10-27
CL2019002309A1 (es) 2020-05-29
CO2019008891A2 (es) 2020-01-17
KR20190121790A (ko) 2019-10-28
WO2018148816A4 (en) 2019-01-03
SI3583103T1 (sl) 2022-07-29
RU2019129095A3 (hr) 2021-10-27
BR102017003318A2 (pt) 2018-10-30
PL3583103T3 (pl) 2022-08-01
DK3583103T3 (da) 2022-03-14
WO2018148816A2 (en) 2018-08-23

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