RS52825B2 - Postupci za lečenje poremećaja ili bolesti povezanih sa hiperlipidemijom i hiperholesterolemijom uz minimizaciju sporednih efekata - Google Patents

Postupci za lečenje poremećaja ili bolesti povezanih sa hiperlipidemijom i hiperholesterolemijom uz minimizaciju sporednih efekata

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Publication number
RS52825B2
RS52825B2 RS20130054A RSP20130054A RS52825B2 RS 52825 B2 RS52825 B2 RS 52825B2 RS 20130054 A RS20130054 A RS 20130054A RS P20130054 A RSP20130054 A RS P20130054A RS 52825 B2 RS52825 B2 RS 52825B2
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Serbia
Prior art keywords
use according
day
mtp inhibitor
dose level
inhibitor
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RS20130054A
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English (en)
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Daniel J Rader
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Univ Pennsylvania
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34975320&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RS52825(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Univ Pennsylvania filed Critical Univ Pennsylvania
Publication of RS52825B publication Critical patent/RS52825B/sr
Publication of RS52825B2 publication Critical patent/RS52825B2/sr

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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)

Claims (24)

  1. 52825 B2 Patentni zahtevi 1. Upotreba inhibitora MIP u proizvodnji leka za lečenje subjekta koji pati od poremećaja povezanog sa hiperlipidemijom i/ili hiperholesterolemijom, naznačen time što navedeno lečenje sadrži primenu na man e tri oste eno rastućih doza navedeno inhibitora MIP na navedenog subjek
    ili njegove farmaceutski prihvatljive soli ili njegovog piperidin N-oksida.
  2. 2. Inhibitor MTP za upotrebu u lečenju subjekta koji pati od poremećaja povezanog sa hiperlipidemijom i/ili hiperholesterolemijom, naznačen time što navedeno lečenje sadrži primenu najmanje tri postepeno rastuće doze navedenog inhibitora MTP na navedenog subjekta, i gde navedeni inhibitor MTP ima strukturu:
    ili njegove farmaceutski prihvatljive soli ili njegovog piperidin N-oksida.
  3. 3. Upotreba prema patentnom zahtevu 1 ili inhibitor MTP za upotrebu prema patentnom zahtevu 2, naznačeni time što je poremećaj teška hiperholesterolemija.
  4. 4. Upotreba prema patentnom zahtevu 1 ili patentnom zahtevu 3 ili inhibitor MTP za upotrebu prema patentnom zahtevu 2 ili patentnom zahtevu 3, naznačeni time što se inhibitor MTP primenjuje oralno.
  5. 5. Upotreba prema bilo kom od patentnih zahteva 1, 3 i 4 ili inhibitor MTP za upotrebu prema bilo kom od patentnih zahteva 2 do 4, naznačeni time što navedene rastuće doze sadrže najmanje prvi nivo doze, drugi nivo doze i treći nivo doze.
  6. 6. Upotreba prema patentnom zahtevu 5 ili inhibitor MTP za upotrebu prema patentnom zahtevu 5, naznačeni time što navedene rastuće doze dalje sadrže četvrti nivo doze.
  7. 7. Upotreba prema patentnom zahtevu 5 ili inhibitor MTP za upotrebu prema patentnom zahtevu 5, naznačeni time što navedene rastuće doze dalje sadrže četvrti i peti nivo doze.
  8. 8. Upotreba prema patentnom zahtevu 7 ili inhibitor MTP za upotrebu prema patentnom zahtevu 7, naznačeni time što je prvi nivo doze 6.25 mg/dan, drugi nivo doze je 12.5 mg/dan, treći nivo doze je 25 mg/dan, četvrti nivo doze je 37.5 mg/dan i peti nivo doze je 50 mg/dan.
  9. 9. Upotreba prema bilo kom od patentnih zahteva 1 i 3 do 7 ili inhibitor MTP za upotrebu prema bilo kom od patentnih zahteva 2 do 7, naznačeni time što svaka od navedenih rastućih doza nije više od 50% od neposredno sledećeg nivoa doze.
  10. 10. Upotreba prema bilo kom od patentnih zahteva1i 3 do 7 ili inhibitor MTP za upotrebu prema bilo kom od patentnih zahteva 2 do 7, naznačeni time što svaki od navedenih rastućih nivoa doze nije više od 20% od neposredno sledećeg nivoa doze.
  11. 11. Upotreba prema patentnom zahtevu 7 ili inhibitor MTP za upotrebu prema patentnom zahtevu 7, naznačeni time što je navedeni prvi nivo doze od oko 2 do oko 13 mg/dan, navedeni drugi nivo doze je od oko 5 do oko 30 mg/dan, navedeni treći nivo doze je od oko 10 do oko 50 mg/dan, navedeni četvrti nivo doze je od oko 20 do oko 60 mg/dan, i navedeni peti nivo doze je od oko 30 do oko 75 mg/dan.
  12. 12. Upotreba prema patentnom zahtevu 6 ili inhibitor MTP za upotrebu prema patentnom zahtevu 6, naznačeni time što je prvi nivo doze 12.5 mg/dan, drugi nivo doze je 25 mg/dan, treći nivo doze je 37.5 mg/dan i četvrti nivo doze je 50 mg/dan.
  13. 13. Upotreba prema patentnom zahtevu 5 ili inhibitor MTP za potrebu prema patentnom zahtevu 5, naznačeni time što, prvi nivo doze je 6.25 mg/dan, drugi nivo doze je 12.5 mg/dan i treći nivo doze je 50 mg/dan.
  14. 14. Upotreba prema bilo kom od patentnih zahteva 1i 3 do 13 ili inhibitor MTP za upotrebu prema bilo kom od patentnih zahteva 2 do 13, naznačeni time što se navedeni inhibitor MTP primenjuje na navedenog subjekta u kombinaciji sa dodatnim jedinjenjem za modifikaciju lipida.
  15. 15. Upotreba prema patentnom zahtevu 14 ili inhibitor MTP za upotrebu prema patentnom zahtevu 14, naznačeni time što su jedinjenja za modifikaciju lipida izabrana iz grupe koju čine inhibitori HMG CoA reduktaze, inhibitori apsorpcije holesterola, ezetimib, inhibitori skvalen sintetaze, fibrati, sekvestranti žučne kiseline, statini, probukol i derivati, niacin, derivati niacina, agonisti PPAR alfa, fibrati, agonisti PPAR gama, tiazolidindioni i inhibitori proteina za transfer holesterol estra (CETP).
  16. 16. Upotreba prema bilo kom od patentnih zahteva 1i 3 do 13 ili inhibitor MTP za upotrebu prema bilo kom od patentnih zahteva 2 do 13, naznačeni time što se svaki nivo doze primenjuje na subjekta od oko 1 do 4 nedelje.
  17. 17. Upotreba prema patentnom zahtevu 14 ili inhibitor MTP za upotrebu prema patentnom zahtevu 14, naznačeni time što su inhibitor MTP i jedinjenja za modifikaciju lipida prisutni u istoj jedinici doze.
  18. 18. Upotreba inhibitora MTP u proizvodnji leka za lečenje subjekta koji pati od poremećaja koji je izabran iz grupe koju čine ili homozigotna/heterozigotna porodična hiperholesterolemija ili hipertrigliceridemija, gde navedeni inhibitor MTP ima strukturu:
    ili njegove farmaceutski prihvatljive soli ili njegovog piperidin N-oksida.
  19. 19. Inhibitor MTP za upotrebu u lečenju subjekta koji pati od poremećaja izabranog iz grupe koja se sastoji od homozigotne/heterozigotne porodične hiperholesterolemije ili hipertrigliceridemije, gde navedeni inhibitor MTP ima strukturu:
    ili njegove farmaceutski prihvatljive soli ili njegovog piperidin N-oksida.
  20. 20. Upotreba prema patentnom zahtevu 18 ili inhibitor MTP za upotrebu prema patentnom zahtevu 19, naznačeni time što se navedeni inhibitor MTP primenjuje na navedenog subjekta u kombinaciji sa dodatnim jedinjenjem za modifikaciju lipida.
  21. 21. Upotreba prema patentnom zahtevu 18 ili patentnom zahtevu 20 ili inhibitor MTP za upotrebu prema patentnom zahtevu 19 ili patentnom zahtevu 20, naznačeni time što su jedan ili više od ukupnog holesterola, LDL, triglicerida u stanju gladovanja (TG), VLDL, lipoproteina (a) (Lp(a)), i apolipoproteina A-I, A-II, B i E sniženi za najmanje 15%, u poređenju sa kontrolnim nivoima.
  22. 22. Upotreba prema bilo kom od patentnih zahteva 18, 20 i 21 ili inhibitor MTP prema bilo kom od patentnih zahteva 19 do 21, naznačeni time što su jedinjenja za modifikaciju lipida izabrana iz grupe koja se sastoji od inhibitora HMG CoA reduktaze, inhibitora apsorpcije holesterola, ezetimiba, inhibitora skvalen sintetaze, fibrata, sekvestranata žučne kiseline, starina, probukola i derivata, niacina, derivata niacina, agonista PPAR alfa, fibrata, agonista PPAR gama, tiazolidindiona i inhibitora proteina za transfer holesterol estra (CETP).
  23. 23. Komplet za lečenje poremećaja povezanog sa hiperlipidemijom i/ili hiperholesterolemijom kod subjekta, naznačen time što sadrži: a) najmanje četiri seta farmaceutskih jedinica doze inhibitora MTP, pri čemu prvi set jedinica doze obezbeđuje 6-25 mg/dan za prvi interval, drugi set jedinica doze obezbeđuje 12.5 mg/dan za drugi interval, treći set jedinica doze obezbeđuje 37.5 mg/dan za treći interval, četvrti set jedinica doze obezbeđuje 50 mg/dan za četvrti interval; i b) uputstva za upotrebu, gde navedeni inhibitor MTP ima strukturu:
    ili njegove farmaceutski prihvatljive soli ili njegovog piperidin N-oksida.
  24. 24. Komplet za lečenje poremećaja koji je povezan sa hiperlipidemijom i/ili hiperholesterolemijom kod subjekta, naznačen time što sadrži: a) najmanje pet setova farmaceutskih jedinica doze inhibitora MTP, pri čemu prvi set jedinica doze obezbeđuje od oko 2 do oko 13 mg/dan za prvi interval, drugi set jedinica doze obezbeđuje od oko 5 do oko 30 mg/dan za drugi interval, treći set jedinica doze obezbeđuje od oko 10 do oko 50 mg/dan za treći interval, četvrti set jedinica doze obezbeđuje od oko 20 do oko 60 mg/dan za četvrti interval i peti set jedinica doze obezbeđuje od oko 30 do oko 75 mg/dan za peti interval; i b) uputstva za upotrebu, gde navedeni inhibitor MTP ima strukturu:
    ili njegove farmaceutski prihvatljive soli ili njegovog piperidin N-oksida.
RS20130054A 2004-03-05 2005-03-07 Postupci za lečenje poremećaja ili bolesti povezanih sa hiperlipidemijom i hiperholesterolemijom uz minimizaciju sporednih efekata RS52825B2 (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55091504P 2004-03-05 2004-03-05
PCT/US2005/007435 WO2005087234A1 (en) 2004-03-05 2005-03-07 Methods for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side-effects
EP05724887.4A EP1725234B2 (en) 2004-03-05 2005-03-07 Methods for treating disorders or diseases associated with hyperlipidemia and hypercholesterolemia while minimizing side-effects

Publications (2)

Publication Number Publication Date
RS52825B RS52825B (sr) 2013-10-31
RS52825B2 true RS52825B2 (sr) 2018-03-30

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RS20130054A RS52825B2 (sr) 2004-03-05 2005-03-07 Postupci za lečenje poremećaja ili bolesti povezanih sa hiperlipidemijom i hiperholesterolemijom uz minimizaciju sporednih efekata

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US (11) US7932268B2 (sr)
EP (1) EP1725234B2 (sr)
JP (4) JP5697296B2 (sr)
KR (2) KR20060129082A (sr)
AU (1) AU2005221656B2 (sr)
BE (1) BE2014C002I2 (sr)
CA (2) CA2558766A1 (sr)
CY (2) CY1114218T1 (sr)
DK (1) DK1725234T4 (sr)
ES (1) ES2399721T5 (sr)
FR (1) FR14C0003I2 (sr)
HR (1) HRP20130115T4 (sr)
LT (1) LTC1725234I2 (sr)
ME (1) ME02070B (sr)
NL (1) NL300634I2 (sr)
NZ (1) NZ549721A (sr)
PL (1) PL1725234T5 (sr)
PT (1) PT1725234E (sr)
RS (1) RS52825B2 (sr)
SI (2) SI1725234T2 (sr)
WO (1) WO2005087234A1 (sr)

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