HRP20192132T1 - Antagonist nk-1/nk-3 receptora za liječenje valunga - Google Patents

Antagonist nk-1/nk-3 receptora za liječenje valunga Download PDF

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Publication number
HRP20192132T1
HRP20192132T1 HRP20192132TT HRP20192132T HRP20192132T1 HR P20192132 T1 HRP20192132 T1 HR P20192132T1 HR P20192132T T HRP20192132T T HR P20192132TT HR P20192132 T HRP20192132 T HR P20192132T HR P20192132 T1 HRP20192132 T1 HR P20192132T1
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Croatia
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compound
formula
xrd
treatment
use according
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HRP20192132TT
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English (en)
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Mike TROWER
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Nerre Therapeutics Limited
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Publication of HRP20192132T1 publication Critical patent/HRP20192132T1/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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine 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
    • A61K31/33Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Multicomponent Fibers (AREA)
  • Food Preservation Except Freezing, Refrigeration, And Drying (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Claims (6)

1. Spoj formule (A) ili njegova farmaceutski prihvatljiva sol za uporabu u liječenju valunga.
2. Spoj formule (A) za uporabu prema patentnom zahtjevu 1, gdje je spoj (A) u kristalnom anhidriranom obliku.
3. Spoj formule (A) za uporabu prema patentnim zahtjevima 1 ili 2, pri čemu je spoj formule (A) u obliku kristalnog anhidrida 1, naznačen time što osigurava rendgenski difraktogram praha (XRD) izražen preko 2 teta kuteva i dobiven pomoću difraktometra koji koristi Kα rendgensko zračenje bakra, i gdje XRD kristalogram sadrži pikove 2 teta ugla na 4.3±0.1, 7.9±0.1, 9.8±0.1, 10.7±0.1, 10.8±0.1, 13.3±0.1, 14.0±0.1, 15.1±0.1 stupnjeva, što odgovara redom d-rastojanju od 20.4, 11.1, 9.0, 8.3, 8.2, 6.6, 6.3 i 5.9 angstrema (Å).
4. Farmaceutska kompozicija za uporabu u liječenju valunga koja sadrži spoj formule (A) ili njegovu farmaceutski prihvatljivu sol i farmaceutski prihvatljive ekscipijense.
5. Farmaceutska kompozicija za uporabu prema patentnom zahtjevu 4, gdje je spoj formule (A) u kristalnom anhidriranom obliku.
6. Farmaceutska kompozicija za uporabu prema patentnim zahtjevima 4 ili 5, gdje je spoj formule (A) u obliku kristalnog anhidrida 1, naznačena time što osigurava rendgenski difraktogram praha (XRD) izražen preko 2 teta kuteva i dobiven pomoću difraktometra koji koristi Kα rendgensko zračenje bakra, i gdje XRD kristalogram sadrži pikove 2 teta kuta na 4.3±0.1, 7.9±0.1, 9.8±0.1, 10.7±0.1, 10.8±0.1, 13.3±0.1, 14.0±0.1, 15.1±0.1 stupnjeva, što redom odgovara d-razmaku od 20.4, 11.1, 9.0, 8.3, 8.2, 6.6, 6.3 i 5.9 angstrema (Å).
HRP20192132TT 2015-05-18 2019-11-27 Antagonist nk-1/nk-3 receptora za liječenje valunga HRP20192132T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562162870P 2015-05-18 2015-05-18
EP16723107.5A EP3297631B1 (en) 2015-05-18 2016-05-16 Nk-1/nk-3 receptor antagonist for the treatment of hot flushes
PCT/EP2016/060945 WO2016184829A1 (en) 2015-05-18 2016-05-16 Dual nk-1/nk-3 receptor antagonists for the treatment of sex-hormone-dependent diseases

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HRP20192132T1 true HRP20192132T1 (hr) 2020-02-21

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US (3) US10195205B2 (hr)
EP (2) EP3574907B1 (hr)
JP (1) JP6902682B2 (hr)
KR (1) KR102704783B1 (hr)
CN (4) CN114306347A (hr)
AU (2) AU2016264034B2 (hr)
BR (1) BR112017024852B1 (hr)
CA (1) CA2984591A1 (hr)
CY (1) CY1122180T1 (hr)
DK (1) DK3297631T3 (hr)
ES (1) ES2753539T3 (hr)
HR (1) HRP20192132T1 (hr)
HU (1) HUE047732T2 (hr)
LT (1) LT3297631T (hr)
MX (2) MX2017012720A (hr)
PL (1) PL3297631T3 (hr)
PT (1) PT3297631T (hr)
RS (1) RS59608B1 (hr)
RU (1) RU2743206C2 (hr)
SI (1) SI3297631T1 (hr)
WO (1) WO2016184829A1 (hr)

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CN112261942A (zh) * 2018-04-19 2021-01-22 艾伯维公司 治疗重度月经出血的方法
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US20210128574A1 (en) 2021-05-06
EP3297631A1 (en) 2018-03-28
CN107635557A (zh) 2018-01-26
PT3297631T (pt) 2019-10-10
US20160339037A1 (en) 2016-11-24
AU2020201074A1 (en) 2020-03-05
PL3297631T3 (pl) 2020-03-31
CN114306347A (zh) 2022-04-12
AU2016264034B2 (en) 2020-03-05
EP3574907B1 (en) 2023-08-23
EP3297631B1 (en) 2019-09-04
EP3574907C0 (en) 2023-08-23
EP3574907A1 (en) 2019-12-04
ES2753539T3 (es) 2020-04-13
RU2743206C2 (ru) 2021-02-16
RU2017134908A3 (hr) 2019-10-23
HUE047732T2 (hu) 2020-05-28
RS59608B1 (sr) 2020-01-31
RU2017134908A (ru) 2019-06-18
BR112017024852A2 (pt) 2018-08-07
MX2020011668A (es) 2021-01-15
CY1122180T1 (el) 2020-11-25
CA2984591A1 (en) 2016-11-24
CN114272242A (zh) 2022-04-05
DK3297631T3 (da) 2019-11-11
KR20180004815A (ko) 2018-01-12
CN114306335A (zh) 2022-04-12
SI3297631T1 (sl) 2019-12-31
JP6902682B2 (ja) 2021-07-14
US20210236506A1 (en) 2021-08-05
US10195205B2 (en) 2019-02-05
LT3297631T (lt) 2019-10-25
AU2016264034A1 (en) 2017-10-26
MX2017012720A (es) 2018-02-09
AU2020201074B2 (en) 2021-07-29
WO2016184829A1 (en) 2016-11-24
KR102704783B1 (ko) 2024-09-10
BR112017024852B1 (pt) 2023-10-31
JP2018515445A (ja) 2018-06-14

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