HRP20190927T1 - Triciklični spojevi, pripravci koji ih sadrže i njihove uporabe - Google Patents

Triciklični spojevi, pripravci koji ih sadrže i njihove uporabe Download PDF

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Publication number
HRP20190927T1
HRP20190927T1 HRP20190927TT HRP20190927T HRP20190927T1 HR P20190927 T1 HRP20190927 T1 HR P20190927T1 HR P20190927T T HRP20190927T T HR P20190927TT HR P20190927 T HRP20190927 T HR P20190927T HR P20190927 T1 HRP20190927 T1 HR P20190927T1
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branched
straight
halogen
diseases
nitro
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HRP20190927TT
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Shmuel Ben-Sasson
Arie Dagan
Sharon PERLES
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Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd.
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Publication of HRP20190927T1 publication Critical patent/HRP20190927T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/14Quaternary ammonium compounds, e.g. edrophonium, choline
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/80[b, c]- or [b, d]-condensed
    • C07D209/82Carbazoles; Hydrogenated carbazoles
    • C07D209/86Carbazoles; Hydrogenated carbazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the ring system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/80[b, c]- or [b, d]-condensed
    • C07D209/82Carbazoles; Hydrogenated carbazoles
    • C07D209/88Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Claims (11)

1. Spoj opće formule (IV): pri čemu je svaki R1-R8 neovisno odabran iz skupine koja sadrži H, OH, SH, halogen, nitro, amino, nitrilo, nitrozo, acetil, acetamid, aciklamid, alkilamin, ravan ili razgranati C1- C5 alkil, ravan ili razgranati C1-C5 alkenil, ravan ili razgranati C1-C5 alkinil, amin, ravan ili razgranati C1-C5 alkoksi, ravan ili razgranati C1-C5 karboksil, ravan ili razgranati C1-C5 ester, ravan ili razgranati C1-C5 tioksi, ravan ili razgranati C1-C5 sulfinil i ravan ili razgranati C1-C5 tionil; R9 je ravan ili razgranati C1-C9 alkil, supstituiran grupom opće formule (V): pri čemu je svaki R’, R" i R"’ neovisno odabran iz skupine koja se sastoji od ravnog ili razgranatog C1-C9 alkila, ravnog ili razgranatog C1-C9 alkenila i ravnog ili razgranatog C1-C9 alkinila; te pri čemu je barem jedan od R1-R4 halogen; ili je barem jedan od R5-R8 halogen; ili je barem jedan od R1-R4 halogen i barem jedan od R5-R8 je halogen; ili barem jedan od R1-R4 je OH; ili barem jedan od R5-R8 je OH; ili barem jedan od R1-R4 je nitro; ili barem jedan od R1-R4 je nitro i barem jedan od R5-R8 je nitro.
2. Spoj sukladno zahtjevu 1, pri čemu je barem jedan od R1-R4 halogen.
3. Spoj sukladno bilo kojem od zahtjeva 1 - 2, pri čemu je barem jedan od R5-R8 halogen.
4. Spoj sukladno bilo kojem od zahtjeva 1 do 3, odabran od: ▪ 3-(3,6-dibromo-9H-karbazol-9-yl)-N,N,N-trimetilpropan-1-aminij ▪ 5-(2-hidroksi-9H-karbazol-9-yl)-N,N,N-trimetilpentan-1-aminij ▪ 5-(3,6-dibromo-9H-karbazol-9-yl)-N,N,N-trimetilpentan-1-aminij.
5. Pripravak koji sadrži spoj sukladno bilo kojem od zahtjeva 1 do 4 ili bilo koju njegovu sol i farmaceutski prihvatljiv nosač.
6. Pripravak sukladno zahtjevu 5, za primjenu u masno tkivo.
7. Spoj sukladno bilo kojem od zahtjeva 1 do 5, za uporabu kao medikament.
8. Spoj opće formule (IV), za uporabu u liječenju barem jedne bolesti, poremećaja ili stanja odabranog između pretilosti, prekomjerne tjelesne težine ili abnormalne raspodjele masnog tkiva te stanja i bolesti povezanih s tim: pri čemu je svaki od R1-R8 neovisno odabran iz skupine koja se sastoji od H, OH, SH, halogena, nitro, amino, nitrilo, nitrozo, acetil, acetamid, acilamid, alkilamin, ravnog ili razgranatog C1-C5 alkila, ravnog ili razgranatog C1-C5 alkenila, ravnog ili razgranatog C1-C5 alkinila, amina, ravnog ili razgranatog C1-C5 alkoksi, ravnog ili razgranatog C1-C5 karboksila, ravnog ili razgranatog C1-C5 estera, ravnog ili razgranatog C1-C5 tioksi, ravnog ili razgranatog C1-C5 sulfinila i ravnog ili razgranatog C1-C5 tionila; R9 je ravni ili razgranati C1-C9 alkil, supstituiran skupinom opće formule (V): pri čemu je svaki R’, R" i R"’ neovisno odabran iz skupine koja se sastoji od ravnog ili razgranatog C1-C9 alkila, ravnog ili razgranatog C1-C9 alkenila i ravnog ili razgranatog C1-C9 alkinila; i pri čemu je barem jedan od R1-R4 halogen; ili je barem jedan od R5-R8 halogen; ili je barem jedan od R1-R4 halogen i barem jedan od R5-R8 je halogen; ili barem jedan od R1-R4 je OH; ili barem jedan od R5-R8 je OH; ili barem jedan od R1-R4 je nitro; ili barem jedan od R1-R4 je nitro i barem jedan od R5-R8 je nitro.
9. Spoj za uporabu sukladno zahtjevu 8, pri čemu su navedena stanja ili bolesti povezane s pretilošću, prekomjernom tjelesnom težinom ili abnormalnom distribucijom masnog tkiva odabrana iz skupine dijabetesa, kardiovaskularnih bolesti, opstruktivne apneje sna, lipoma, karcinoma, osteoartritisa, endokrinoloških oboljenja i poremećaja, reproduktivnih bolesti i poremećaja, neuroloških bolesti i poremećaja i ortopedskih bolesti i poremećaja.
10. Spoj sukladno bilo kojem od zahtjeva 1 do 5, za uporabu u liječenju pretilosti i povezanih stanja ili bolesti.
11. Spoj sukladno bilo kojem od zahtjeva 1 do 5, za uporabu u liječenju abnormalne distribucije masnog tkiva te povezanih stanja i bolesti.
HRP20190927TT 2011-11-15 2019-05-20 Triciklični spojevi, pripravci koji ih sadrže i njihove uporabe HRP20190927T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161559964P 2011-11-15 2011-11-15
US201261603508P 2012-02-27 2012-02-27
PCT/IL2012/050461 WO2013072915A1 (en) 2011-11-15 2012-11-15 Tricyclic compounds, compositions comprising them and uses thereof
EP12850186.3A EP2802320B1 (en) 2011-11-15 2012-11-15 Tricyclic compounds, compositions comprising them and uses thereof

Publications (1)

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HRP20190927T1 true HRP20190927T1 (hr) 2019-08-23

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US (1) US9447040B2 (hr)
EP (1) EP2802320B1 (hr)
JP (1) JP6087367B2 (hr)
KR (1) KR101986272B1 (hr)
CN (1) CN104010636B (hr)
AU (1) AU2012338362B2 (hr)
BR (1) BR112014011641B1 (hr)
CA (1) CA2855759C (hr)
CL (1) CL2014001278A1 (hr)
CO (1) CO7020909A2 (hr)
DK (1) DK2802320T3 (hr)
ES (1) ES2729713T3 (hr)
HR (1) HRP20190927T1 (hr)
HU (1) HUE043827T2 (hr)
IN (1) IN2014CN03610A (hr)
MX (1) MX347570B (hr)
PE (1) PE20141940A1 (hr)
PL (1) PL2802320T3 (hr)
PT (1) PT2802320T (hr)
RU (1) RU2624446C9 (hr)
SG (1) SG11201402258UA (hr)
SI (1) SI2802320T1 (hr)
WO (1) WO2013072915A1 (hr)
ZA (1) ZA201404065B (hr)

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US10632102B2 (en) * 2015-06-15 2020-04-28 Raziel Therapeutics Ltd Carbazole derivatives for the treatment of fibrotic diseases and related symptoms, and conditions thereof
CN115066241A (zh) * 2019-09-15 2022-09-16 拉结尔治疗有限公司 用于治疗实体瘤的组合物
JP2023510865A (ja) * 2020-01-28 2023-03-15 ラジエル セラピューティクス エルティーディー. 血管脂肪腫の処置のための組成物
IL301325A (en) * 2020-09-16 2023-05-01 Raziel Therapeutics Ltd Compositions and methods for the treatment of lipid-related disorders
WO2022058792A1 (en) * 2020-09-16 2022-03-24 Raziel Therapeutics Ltd. Compositions for the treatment of fat related conditions and disorders
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WO2023007247A1 (en) * 2021-07-28 2023-02-02 Raziel Therapeutics Ltd. Compositions and methods for treating lipoma pain
CN115073374B (zh) * 2022-06-14 2023-10-27 五邑大学 一种α-葡萄糖苷酶抑制剂及其制备方法和应用

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AU2012338362B2 (en) 2017-05-18
RU2624446C9 (ru) 2018-04-04
CO7020909A2 (es) 2014-08-11
WO2013072915A1 (en) 2013-05-23
PL2802320T3 (pl) 2019-09-30
MX347570B (es) 2017-05-02
CL2014001278A1 (es) 2014-12-26
CA2855759C (en) 2020-03-10
SI2802320T1 (sl) 2019-08-30
US20140329877A1 (en) 2014-11-06
AU2012338362A1 (en) 2014-05-29
KR20140099492A (ko) 2014-08-12
EP2802320B1 (en) 2019-02-20
DK2802320T3 (da) 2019-05-27
MX2014005765A (es) 2015-09-23
BR112014011641B1 (pt) 2020-10-27
CA2855759A1 (en) 2013-05-23
JP2014533264A (ja) 2014-12-11
EP2802320A4 (en) 2015-08-12
IN2014CN03610A (hr) 2015-10-09
JP6087367B2 (ja) 2017-03-01
HUE043827T2 (hu) 2019-09-30
RU2014119711A (ru) 2015-12-27
PT2802320T (pt) 2019-06-17
PE20141940A1 (es) 2014-12-18
EP2802320A1 (en) 2014-11-19
CN104010636B (zh) 2017-04-12
ES2729713T3 (es) 2019-11-05
US9447040B2 (en) 2016-09-20
SG11201402258UA (en) 2014-06-27
RU2624446C2 (ru) 2017-07-04
ZA201404065B (en) 2015-11-25
KR101986272B1 (ko) 2019-06-05
CN104010636A (zh) 2014-08-27
BR112014011641A2 (pt) 2017-05-02

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