HRP20191725T1 - Orvepitant za liječenje kroničnog kašlja - Google Patents

Orvepitant za liječenje kroničnog kašlja Download PDF

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Publication number
HRP20191725T1
HRP20191725T1 HRP20191725TT HRP20191725T HRP20191725T1 HR P20191725 T1 HRP20191725 T1 HR P20191725T1 HR P20191725T T HRP20191725T T HR P20191725TT HR P20191725 T HRP20191725 T HR P20191725T HR P20191725 T1 HRP20191725 T1 HR P20191725T1
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Croatia
Prior art keywords
orvepitant
pharmaceutically acceptable
use according
acceptable salt
phenyl
Prior art date
Application number
HRP20191725TT
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English (en)
Inventor
Mike TROWER
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Nerre Therapeutics Limited
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Publication of HRP20191725T1 publication Critical patent/HRP20191725T1/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
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/194Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (21)

1. [1-(R)-(3,5-bis-trifluorometil-fenil)-etil]-metilamid 2-(R)-(4-Fluoro-2-metil-fenil)-4-(S)-((8aS)-6-okso-heksahidro-pirolo[1,2-a]-pirazin-2-il)-piperidin-1-karboksilne kiseline (orvepitant) ili njegova farmaceutski prihvatljiva sol, za uporabu u liječenju kroničnog kašlja.
2. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s patentnim zahtjevom 1, naznačen time što je kronični kašalj kronični refraktorni kašalj.
3. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s patentnim zahtjevom 1 ili 2, pri čemu je kronični kašalj posljedica ili je povezan sa sarkoidozom, emfizemom ili idiopatskom plućnom fibrozom (IPF).
4. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s patentnim zahtjevom 1 ili 2, pri čemu je kronični kašalj posljedica ili je povezan s astmom, kroničnim bronhitisom, kroničnim postnazalnim curenjem, eozinofilnim bronhitisom ili kroničnom opstruktivnom bolešću pluća (COPD).
5. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s patentnim zahtjevom 1 ili 2, pri čemu je kronični kašalj posljedica ili je povezan s kroničnim infekcijama kao što su bronhiektazija, tuberkuloza ili cistična fibroza.
6. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s patentnim zahtjevom 1 ili 2, pri čemu je kronični kašalj posljedica ili je povezan s tumorima pluća kao što su bronhogeni karcinom, karcinom alveolarnih stanica, benigni tumori dišnih puteva ili tumori sredoprsja.
7. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s patentnim zahtjevom 1 ili 2, pri čemu je kronični kašalj posljedica ili je povezan s kardiovaskularnom bolešću kao što su zatajenje lijeve klijetke, infarkt pluća ili aneurizma aorte.
8. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s patentnim zahtjevom 1 ili 2, pri čemu je kronični kašalj posljedica ili je povezan s refluksnim ezofagitisom, rekurentnom aspiracijom, endobronhijalnim šavovima, sindromom postnazalnog curenja ili rinosinusitisom.
9. Orvepitant ili njegova farmaceutski prihvatljiva sol, za uporabu u skladu s bilo kojim od patentnih zahtjeva 1 do 8, pri čemu je farmaceutski prihvatljiva sol orvepitanta maleat.
10. Orvepitant maleat za uporabu u skladu s patentnim zahtjevom 9, pri čemu je orvepitant maleat orvepitant maleat oblika 1.
11. [1-(R)-(3,5-bis-trifluorometil-fenil)-etil]-metilamid 2-(R)-(4-Fluoro-2-metil-fenil)-4-(S)-((8aS)-6-okso-heksahidro-pirolo[1,2-a]-pirazin-2-il)-piperidin-1-karboksilne kiseline (orvepitant) ili njegova farmaceutski prihvatljiva sol u kombinaciji s jednim ili više terapeutskih tvari, odabranih od antagonista P2X3 purinergičkog receptora, antagonista muskarinskog receptora ili agonista beta-2 adrenoceptora; za uporabu u liječenju kroničnog kašlja.
12. Kombinacija za uporabu u skladu s patentnim zahtjevom 11, pri čemu je kronični kašalj kronični refraktorni kašalj.
13. Kombinacija za uporabu u skladu sa patentnim zahtjevom 11 ili 12, pri čemu su antagonisti P2X3 purinergičkog receptora 5-(2,4-diamino-pirimidin-5-iloksi)-4-izopropil-2-metoksi-benzensulfonamid (AF-219) ili AF-130.
14. Kombinacija za uporabu u skladu s patentnim zahtjevom 11 ili 12, pri čemu je agonist beta-2 adrenoceptora salbutamol.
15. Kombinacija za uporabu u skladu s patentnim zahtjevom 11 ili 12, pri čemu je antagonist muskarinskog receptora ipratropij bromid.
16. Kombinacija za uporabu u skladu s bilo kojim od patentnih zahtjeva 11-15, pri čemu je farmaceutski prihvatljiva sol orvepitanta maleat.
17. Kombinacija za uporabu u skladu s patentnim zahtjevom 16, pri čemu je orvepitant maleat bezvodni kristalni oblik 1.
18. Farmaceutski pripravak koji sadrži [1-(R)-(3,5-bis-trifluorometil-fenil)-etil]-metilamid 2-(R)-(4-Fluoro-2-metil-fenil)-4-(S)-((8aS)-6-okso-heksahidro-pirolo[1,2-a]-pirazin-2-il)-piperidin-1-karboksilne kiseline (orvepitant) ili njegovu farmaceutski prihvatljivu sol i jedan ili više farmaceutski prihvatljivih nosača ili ekscipijenata za uporabu u liječenju kroničnog kašlja.
19. Farmaceutski pripravak koji sadrži [1-(R)-(3,5-bis-trifluorometil-fenil)-etil]-metilamid 2-(R)-(4-Fluoro-2-metil-fenil)-4-(S)-((8aS)-6-okso-heksahidro-pirolo[1,2-a]-pirazin-2-il)-piperidin-1-karboksilne kiseline (orvepitant) ili farmaceutski prihvatljivu sol i jedan ili više farmaceutski prihvatljivih nosača ili ekscipijenata za uporabu u skladu s patentnim zahtjevom 18, pri čemu je kronični kašalj kronični refraktorni kašalj.
20. Farmaceutski pripravak koji sadrži [1-(R)-(3,5-bis-trifluorometil-fenil)-etil]-metilamid 2-(R)-(4-Fluoro-2-metil-fenil)-4-(S)-((8aS)-6-okso-heksahidro-pirolo[1,2-a]-pirazin-2-il)-piperidin-1-karboksilne kiseline (orvepitant) ili farmaceutski prihvatljivu sol i jedan ili više farmaceutski prihvatljivih nosača ili ekscipijenata za uporabu u skladu s patentnim zahtjevom 18 ili 19, pri čemu je farmaceutski prihvatljiva sol orvepitanta maleat.
21. Farmaceutski pripravak koji sadrži [1-(R)-(3,5-bis-trifluorometil-fenil)-etil]-metilamid 2-(R)-(4-Fluoro-2-metil-fenil)-4-(S)-((8aS)-6-okso-heksahidro-pirolo[1,2-a]-pirazin-2-il)-piperidin-1-karboksilne kiseline (orvepitant) ili farmaceutski prihvatljivu sol i jedan ili više farmaceutski prihvatljivih nosača ili ekscipijenata za uporabu u skladu s patentnim zahtjevom 20, pri čemu je orvepitant maleat bezvodni kristalni oblik 1.
HRP20191725TT 2016-01-08 2019-09-24 Orvepitant za liječenje kroničnog kašlja HRP20191725T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662276237P 2016-01-08 2016-01-08
US201662408921P 2016-10-17 2016-10-17
PCT/EP2016/082698 WO2017118584A1 (en) 2016-01-08 2016-12-27 Orvepitant for the treatment of chronic cough
EP16819325.8A EP3377064B1 (en) 2016-01-08 2016-12-27 Orvepitant for the treatment of chronic cough

Publications (1)

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HRP20191725T1 true HRP20191725T1 (hr) 2019-12-27

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HRP20191725TT HRP20191725T1 (hr) 2016-01-08 2019-09-24 Orvepitant za liječenje kroničnog kašlja

Country Status (21)

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US (2) US9750739B2 (hr)
EP (1) EP3377064B1 (hr)
JP (1) JP6621534B2 (hr)
KR (1) KR102136017B1 (hr)
CN (2) CN108430475B (hr)
AU (1) AU2016384267B2 (hr)
BR (1) BR112018013903B1 (hr)
CA (1) CA3009283C (hr)
CY (1) CY1122170T1 (hr)
DK (1) DK3377064T3 (hr)
ES (1) ES2738678T3 (hr)
HR (1) HRP20191725T1 (hr)
HU (1) HUE045764T2 (hr)
LT (1) LT3377064T (hr)
MX (1) MX371178B (hr)
PL (1) PL3377064T3 (hr)
PT (1) PT3377064T (hr)
RS (1) RS59313B1 (hr)
RU (1) RU2746601C2 (hr)
SI (1) SI3377064T1 (hr)
WO (1) WO2017118584A1 (hr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180235931A1 (en) * 2017-01-17 2018-08-23 Menlo Therapeutics Inc. Use of neurokinin-1 antagonists as antitussives
SG11202100580UA (en) * 2018-07-23 2021-02-25 Trevi Therapeutics Inc Treatment of chronic cough, breathlessness and dyspnea
CN112823795B (zh) * 2019-11-20 2023-04-14 天津医科大学总医院 一种特发性肺纤维化药物组合及其应用
IL296635A (en) * 2020-04-03 2022-11-01 Nerre Therapeutics Ltd An nk-1 receptor antagonist for the treatment of a disease selected from sepsis, septic shock, acute respiratory distress syndrome (ARDS), or multiple organ dysfunction syndrome (MODS)
CA3177477A1 (en) 2020-06-02 2021-12-09 Nerre Therapeutics Limited Neurokinin (nk)-1 receptor antagonists for use in the treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs
CN114732818B (zh) * 2022-04-29 2023-02-10 首都医科大学附属北京胸科医院 一种抗特发性肺纤维化药物尼达尼布在结核病治疗中的应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ321575A (en) * 1995-10-30 1999-05-28 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives
GB0203020D0 (en) * 2002-02-08 2002-03-27 Glaxo Group Ltd Chemical compounds
GB0806652D0 (en) * 2008-04-11 2008-05-14 Glaxo Group Ltd Anhydrous crystal form of orvepitant maleate
US9603849B2 (en) * 2012-10-11 2017-03-28 Nerre Therapeutics Limited Uses of orvepitant

Also Published As

Publication number Publication date
JP2019501162A (ja) 2019-01-17
CN113274392A (zh) 2021-08-20
ES2738678T3 (es) 2020-01-24
KR20180100651A (ko) 2018-09-11
BR112018013903A2 (pt) 2018-12-18
CA3009283C (en) 2023-10-03
CY1122170T1 (el) 2020-11-25
US9750739B2 (en) 2017-09-05
BR112018013903B1 (pt) 2023-11-07
CN108430475B (zh) 2021-03-16
US20170196860A1 (en) 2017-07-13
RS59313B1 (sr) 2019-10-31
WO2017118584A1 (en) 2017-07-13
HUE045764T2 (hu) 2020-01-28
CA3009283A1 (en) 2017-07-13
SI3377064T1 (sl) 2019-11-29
LT3377064T (lt) 2019-09-10
RU2018122121A (ru) 2020-02-11
JP6621534B2 (ja) 2019-12-18
MX371178B (es) 2020-01-21
KR102136017B1 (ko) 2020-07-20
AU2016384267B2 (en) 2022-02-03
DK3377064T3 (da) 2019-09-23
PT3377064T (pt) 2019-07-23
EP3377064B1 (en) 2019-06-26
EP3377064A1 (en) 2018-09-26
MX2018008439A (es) 2018-08-14
PL3377064T3 (pl) 2020-02-28
US20170326140A1 (en) 2017-11-16
AU2016384267A1 (en) 2018-07-05
RU2018122121A3 (hr) 2020-06-26
RU2746601C2 (ru) 2021-04-16
CN108430475A (zh) 2018-08-21

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