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ME02609B - TRPV1 ANTAGONISTI KOJI UKLJUČUJU DIHIDROKSI SUPSTITUENT l NJIHOVE UPOTREBE - Google Patents

TRPV1 ANTAGONISTI KOJI UKLJUČUJU DIHIDROKSI SUPSTITUENT l NJIHOVE UPOTREBE

Info

Publication number
ME02609B
ME02609B MEP-2017-44A MEP201744A ME02609B ME 02609 B ME02609 B ME 02609B ME P201744 A MEP201744 A ME P201744A ME 02609 B ME02609 B ME 02609B
Authority
ME
Montenegro
Prior art keywords
pharmaceutically acceptable
fumaric acid
compound
acceptable derivative
salt
Prior art date
Application number
MEP-2017-44A
Other languages
German (de)
English (en)
French (fr)
Inventor
Laykea Tafesse
Shigeru Ando
Noriyuki Kurose
Original Assignee
Purdue Pharma Lp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46513798&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02609(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Purdue Pharma Lp filed Critical Purdue Pharma Lp
Publication of ME02609B publication Critical patent/ME02609B/me

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • A61K31/395—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (17)

1. Jedinjenje formule (I): ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što: R1 je -halo ili; R4 je -H; svaki R8 i R9 je nezavisno -H, -halo, -CH3 ili -CF3; svaki halo je nezavisno -F, -Cl, -Br, ili -I; i m je ceo broj 1; gde je metil grupa vezana za piperazinski prsten (S)-2-metil grupa; i ugljenikov atom na a poziciji a-b veze je u (S) konfiguraciji; pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja sadrži farmaceutski prihvatljivu so, polimorf, pseudopolimorf, solvat, kokristal, radioobeleženi oblik, i/ili tautomer.
2. Jedinjenje iz zahteva 1, naznačeno time, što je farmaceutski prihvatljivi derivat farmaceutski prihvatljiva so, radioobeleženi oblik, ili kokristal hlorovodonične kiseline, tartarne kiseline, benzensulfonske kiseline, p-toluensulfonske kiseline ili fumarne kiseline.
3. Jedinjenje iz zahteva 2, naznačeno time, što je farmaceutski prihvatljivi derivat so fumarne kiseline, fumarno-kiselinski kokristal ili njihova kombinacija.
4. Jedinjenje iz zahteva 1, sa formulom (II): ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što: R4 je -H; R8 je -H, -F ili -CH3; R9 je -H, -halo, -CH3 ili -CF3; i svaki halo je nezavisno -F, -Cl, -Br, ili -I, gde je metil grupa vezana za piperazinski prsten (S)-2-metil grupa; i ugljenikov atom na a poziciji a-b veze je u (S) konfiguraciji; i pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja sadrži farmaceutski prihvatljivu so, polimorf, pseudopolimorf, solvat, kokristal, radioobeleženi oblik, i/ili tautomer.
5. Jedinjenje iz zahteva 4, naznačeno time, što je farmaceutski prihvatljivi derivat (i) farmaceutski prihvatljiva so, ili fumarno-kiselinski kokristal; ili (ii) so fumarne kiseline, fumarno-kiselinski kokristal, ili njihova kombinacija.
6. Jedinjenje iz zahteva 5, opcija (i), naznačeno time, što je farmaceutski prihvatljivi derivat so hlorovodonične kiseline, natrijumova so, kalijumova so, so p-toluensulfonske kiseline, so fumarne kiseline ili fumarno-kiselinski kokristal.
7. Jedinjenje iz zahteva 4 ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što su: pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja sadrži farmaceutski prihvatljivu so, polimorf. pseudopolimorf, solvat, kokristal, radioobeleženi oblik i/ili tautomer.
8. Jedinjenje iz bilo kojeg od zahteva 1 ili 7, naznačeno time, što je (i) so fumarne kiseline, fumarno-kiselinski kokristal, ili njihova kombinacija, ili (ii) slobodna baza.
9. Jedinjenje iz bilo kojeg od zahteva 1-8 ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što se koriste za lečenje bola, bola udruženog sa osteoartritisom, osteoartritisa, UI, ulcera, IBD ili IBS, pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja se sastoji od farmaceutski prihvatljive soli, polimorfa. pseudopolimorfa, solvata, kokristala, radioobeleženog oblika i/ili tautomera.
10. Proizvod kombinovanja jedinjenja iz bilo kojeg od zahteva 1-8 sa fumarnom kiselinom, naznačen time, što u proizvodu, molarni odnos (Jedinjenje Formule (I) ili (II)):(fumarna kiselina) iznosi oko 1.0:0.5.
11. Smeša, naznačena time, što sadrži (i) jedinjenje iz bilo kojeg od zahteva 1-8 ili njegov farmaceutski prihvatljivi derivat: ili (ii) proizvod iz zahteva 10;i farmaceutski prihvatljivi nosač ili ekscipijnt, pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja se sastoji od farmaceutski prihvatljive soli, polimorfa. pseudopolimorfa, solvata, kokristala, radioobeleženog oblika i/ili tautomera.
12. Proizvod iz zahteva 10 ili njegov farmaceutski prihvatljivi derivat, naznačeni time, što se koriste za lečenje bola, bola udruženog sa osteoartritisom, osteoartritisa, UI, ulcera, IBD ili IBS, pri čemu se farmaceutski prihvatljivi derivat bira iz grupe koja se sastoji od farmaceutski prihvatljive soli, polimorfa. pseudopolimorfa, solvata, kokristala, radioobeleženog oblika i/ili tautomera.
13. Jedinjenje iz zahteva 4, naznačeno time, što ima strukturu ili je fumarno-kiselinski kristal istog.
14. Jedinjenje iz zahteva 13, naznačeno time, što je u obliku kokristala nastalog kombinovanjem sa fumarnom kiselinom, pri čemu u kokristalu, molarni odnos (Jedinjenje):(fumarna kiselina) iznosi oko 1.0:0.5.
15. Fumarno-kiselinski kokristal iz zahteva 13 ili zahteva 14, naznačen time, što ima obrazac difrakcije x-zraka na prašku, koji sadrži pik na svakom od 6.5º ± 0.2º, 12.5º ± 0.2º, 16.8º ± 0.2º, i 25.3º ± 0.2º.
16. Fumarno-kiselinski kokristal iz zahteva 13 ili zahteva 14, naznačen time, što ima obrazac difrakcije x-zraka na prašku, koji sadrži pik na svakom od 6.5º ± 0.2º, 8.6º ± 0.2º, 12.5º ± 0.2º, 14.0º ± 0.2º, 16.8º ± 0.2º, 18.7º± 0.2º, i 25.3º ± 0.2º.
17. Fumarno-kiselinski kokristal iz zahteva 13 ili zahteva 14, naznačen time, što ima obrazac difrakcije x-zraka na prašku, koji sadrži pik na svakom od 6.5º ± 0.2º, 8.6º ± 0.2º, 12.5º ± 0.2º, 14.0º ± 0.2º, 16.8º ± 0.2º, 18.7º± 0.2º, 20.4º ± 0.2º, 21.3º ± 0.2º, 22.0º ± 0.2º, 23.2º ± 0.2º, 25.3º ± 0.2º i 38.5º ± 0.2º.
MEP-2017-44A 2011-06-22 2012-06-21 TRPV1 ANTAGONISTI KOJI UKLJUČUJU DIHIDROKSI SUPSTITUENT l NJIHOVE UPOTREBE ME02609B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161499989P 2011-06-22 2011-06-22
EP12735333.2A EP2723732B1 (en) 2011-06-22 2012-06-21 Trpv1 antagonists including dihydroxy substituent and uses thereof
PCT/IB2012/001252 WO2012176061A1 (en) 2011-06-22 2012-06-21 Trpv1 antagonists including dihydroxy substituent and uses thereof

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ME02609B true ME02609B (me) 2017-06-20

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US (4) US9273043B2 (me)
EP (2) EP3173411B1 (me)
JP (1) JP5699251B2 (me)
KR (2) KR20150055094A (me)
CN (2) CN105693712A (me)
AR (1) AR086709A1 (me)
AU (1) AU2012273652B2 (me)
BR (1) BR112013032658A2 (me)
CA (1) CA2837178C (me)
CL (1) CL2013003550A1 (me)
CO (1) CO6852081A2 (me)
CY (1) CY1119111T1 (me)
DK (1) DK2723732T3 (me)
ES (1) ES2620528T3 (me)
HR (1) HRP20170507T1 (me)
HU (1) HUE031372T2 (me)
IL (1) IL229817A (me)
LT (1) LT2723732T (me)
ME (1) ME02609B (me)
MX (1) MX354015B (me)
MY (1) MY185061A (me)
PE (1) PE20141531A1 (me)
PH (1) PH12013502412B1 (me)
PL (1) PL2723732T3 (me)
PT (1) PT2723732T (me)
RS (1) RS55701B1 (me)
RU (1) RU2621708C2 (me)
SG (2) SG10201605163PA (me)
SI (1) SI2723732T1 (me)
SM (1) SMT201700197T1 (me)
TW (1) TWI453205B (me)
UA (1) UA113288C2 (me)
WO (1) WO2012176061A1 (me)
ZA (1) ZA201400419B (me)

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ES2620528T3 (es) * 2011-06-22 2017-06-28 Purdue Pharma Lp Antagonistas de TRPV1 que incluyen un sustituyente dihidroxi y usos de los mismos
KR101933622B1 (ko) * 2012-10-09 2018-12-28 삼성전자주식회사 소포를 모니터링하기 위한 조성물, 키트 및 이를 이용하여 소포를 모니터링하는 방법
JP6528845B2 (ja) * 2015-07-31 2019-06-12 株式会社村田製作所 アンテナ整合回路、アンテナ回路、フロントエンド回路および通信装置
RU2755206C1 (ru) 2020-05-20 2021-09-14 Федеральное государственное бюджетное учреждение науки Тихоокеанский институт биоорганической химии им. Г.Б. Елякова Дальневосточного отделения Российской академии наук (ТИБОХ ДВО РАН) Средство пролонгированного анальгетического действия и лекарственный препарат на его основе
CN113077942B (zh) * 2021-04-12 2021-12-17 西北工业大学 一种基于功率超声制备智能柔性导电薄膜及其应用
CN120513091A (zh) 2022-10-31 2025-08-19 盐野义制药株式会社 作为trpv1拮抗剂的吡啶衍生物的用途

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