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HRP20171620T1 - N- (5s, 6s, 9r) - 5 amino- 6 - (2, 3 - difluorofenil) -6, 7, 8, 9 - tetrahidro - 5h - ciklohepta [b]piridin-9 -il- 4 - (2 - okso-2, 3 - dihidro - 1h - imidazo [4, 5 -b]piridin - 1 - il) piperidin - 1 - karboksilat, hemisulfatna sol - Google Patents

N- (5s, 6s, 9r) - 5 amino- 6 - (2, 3 - difluorofenil) -6, 7, 8, 9 - tetrahidro - 5h - ciklohepta [b]piridin-9 -il- 4 - (2 - okso-2, 3 - dihidro - 1h - imidazo [4, 5 -b]piridin - 1 - il) piperidin - 1 - karboksilat, hemisulfatna sol Download PDF

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Publication number
HRP20171620T1
HRP20171620T1 HRP20171620TT HRP20171620T HRP20171620T1 HR P20171620 T1 HRP20171620 T1 HR P20171620T1 HR P20171620T T HRP20171620T T HR P20171620TT HR P20171620 T HRP20171620 T HR P20171620T HR P20171620 T1 HRP20171620 T1 HR P20171620T1
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Croatia
Prior art keywords
compound
salt
hemisulfate salt
degrees
specified
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HRP20171620TT
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English (en)
Inventor
Daniel Richard Roberts
Richard Raymond Schartman
Chenkou Wei
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Bristol-Myers Squibb Company
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47844498&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20171620(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol-Myers Squibb Company filed Critical Bristol-Myers Squibb Company
Publication of HRP20171620T1 publication Critical patent/HRP20171620T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed 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
    • A61K31/435Heterocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/437Heterocyclic 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (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)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (10)

1. Hemisulfatna sol spoja (I): [image]
2. Hemisulfatna sol spoja (I) prema patentnom zahtjevu 1, gdje je navedena sol spoja (I) kristalna.
3. Hemisulfatna sol spoja (I) prema patentnom zahtjevu 1, gdje navedena sol spoja (I) je seskvihidrat.
4. Hemisulfatna sol spoja (I) prema patentnom zahtjevu 3, gdje je navedena sol kristalni oblik H1.5-1 karakteriziran sljedećim: Parametri jedinice stanice su jednaki sljedećem: Dimenzije stanice: a = 0.92 Å b = 33.04 Å c = 7.90 Å α = 90 stupnjeva β = 90 stupnjeva γ = 90 stupnjeva Prostorna grupa: P21212 Molekula spoja (I)/asimetrična jedinica: 1 Zapremina = 2851 Å3 Gustoća (izračunato) = 1.423 g/cm3, gdje je mjerenje navedenog kristalnog oblika na temperaturi od oko 25°C.
5. Hemisulfatna sol spoja (I) prema patentnom zahtjevu 4, gdje navedeni oblik H1.5-1 je karakteriziran jednim ili više od sljedećeg: a) uzorak difrakcije x-zraka praškaste supstance (CuKα λ=1.5418Å) koji sadrži 2θ vrijednosti: 5.4±0.1, 8.6±0.1, 9.7±0.1, 12.4±0.1, 14.9±0.1,17.6±0.1, 18.1±0.1, 20.5±0.1, 21.4±0.1, i 22.0±0.1, gdje je mjerenje kristalnog oblika na temperaturi od oko 25°C; i/ili b) spektri nuklearne rezonance u čvrstom stanju koji sadrže šest ili više vrhova(δ (ppm) u odnosu na TMS) koji su odabrani od: 26.6±0.1, 27.1±0.1, 28.3±0.1, 30.7±0.1, 43,1±0.1, 45.9±0.1, 47.1±0.1, 52.0±0.1, 54.2±0.1, 72.5±0.1, 117.0±0.1, 117.7±0.1, 124.2±0.1, 125.2±0.1, 128.3±0.1, 130.3±0.1, 131.4±0.1, 134.1±0.1, 140.8±0.1, 144.7±0.1, 148.7±0.1, 149.8±0.1, 151.2±0.1, 153.4±0.1, 155,1±0.1, 155.6±0.1 i 156.7±0.1.
6. Farmaceutska kompozicija koja sadrži navedenu hemisulfatnu sol spoja (I) prema patentnom zahtjevu 1; i farmaceutski prihvatljiv nosač ili razblaživač.
7. Farmaceutska kompozicija prema patentnom zahtjevu 6, gdje je navedena hemisulfatna sol spoja (I) seskvihidrat.
8. Farmaceutska kompozicija prema patentnom zahtjevu 7, gdje je navedena hemisulfatna sol spoja (I) kristalni oblik H1.5-1 karakteriziran sljedećim: Parametri jedinice stanice su jednaki sljedećem: Dimenzije stanice: a = 10.92 Å b = 33.04 Å c = 7.90 Å α = 90 stupnjeva β = 90 stupnjeva γ = 90 stupnjeva Prostorna grupa: P21212 Molekule spoja (I)/asimetrična jedinica: 1 Zapremina = 2851 Å3 Gustoća (računato) = 1.423 g/cm3, gdje je mjerenje navedenog kristalnog oblika na temperaturi od oko 25 °C.
9. Hemisulfatna sol spoja (I) prema bilo kojem patentnom zahtjevu 1 do 5 se koristi kao lijek.
10. Hemisulfatna sol spoja (I) prema bilo kojem patentnom zahtjevu 1 do 5 se koristi u liječenju poremećaja koji je povezan sa CGRP, gdje je navedeni poremećaj migrenozna glavobolja, neurogena vazodilatacija, neurogena inflamacija, termalna povreda, cirkulacijski šok, crvenilo vezano za menopauzu, inflamatorne respiratorne bolesti ili kronična opstruktivna bolest pluća (HBOP).
HRP20171620TT 2012-02-27 2013-02-25 N- (5s, 6s, 9r) - 5 amino- 6 - (2, 3 - difluorofenil) -6, 7, 8, 9 - tetrahidro - 5h - ciklohepta [b]piridin-9 -il- 4 - (2 - okso-2, 3 - dihidro - 1h - imidazo [4, 5 -b]piridin - 1 - il) piperidin - 1 - karboksilat, hemisulfatna sol HRP20171620T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261603598P 2012-02-27 2012-02-27
EP13708603.9A EP2820016B1 (en) 2012-02-27 2013-02-25 N- (5s, 6s, 9r) - 5 -amino- 6 - (2, 3 - difluorophenyl) -6, 7, 8, 9 - tetrahydro - 5h - cyclohepta [b]pyridin-9 -yl- 4 - (2 - oxo-2, 3 - dihydro - 1h- imidazo [4, 5 -b]pyridin - 1 - yl) piperidine - 1 - carboxylate, hemisulfate salt
PCT/US2013/027648 WO2013130402A1 (en) 2012-02-27 2013-02-25 N- (5s, 6s, 9r) - 5 -amino- 6 - (2, 3 - difluorophenyl) -6, 7, 8, 9 - tetrahydro - 5h - cyclohepta [b] pyridin-9 -yl- 4 - (2 - oxo-2, 3 - dihydro - 1h- imidazo [4, 5 -b] pyridin - 1 - yl) piperidine - 1 - carboxylate, hemisulfate salt

Publications (1)

Publication Number Publication Date
HRP20171620T1 true HRP20171620T1 (hr) 2017-12-01

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ID=47844498

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20171620TT HRP20171620T1 (hr) 2012-02-27 2013-02-25 N- (5s, 6s, 9r) - 5 amino- 6 - (2, 3 - difluorofenil) -6, 7, 8, 9 - tetrahidro - 5h - ciklohepta [b]piridin-9 -il- 4 - (2 - okso-2, 3 - dihidro - 1h - imidazo [4, 5 -b]piridin - 1 - il) piperidin - 1 - karboksilat, hemisulfatna sol
HRP20191655 HRP20191655T1 (hr) 2012-02-27 2019-09-16 N-(5s,6s,9r)-5-amino-6-(2,3-difluorofenil)-6,7,8,9-tetrahidro-5h-ciklohepta[b]piridin-9-il-4-(2-okso-2,3-dihidro-1h-imidazo[4,5-b]piridin-1-il)piperidin-1-karboksilat sol

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HRP20191655 HRP20191655T1 (hr) 2012-02-27 2019-09-16 N-(5s,6s,9r)-5-amino-6-(2,3-difluorofenil)-6,7,8,9-tetrahidro-5h-ciklohepta[b]piridin-9-il-4-(2-okso-2,3-dihidro-1h-imidazo[4,5-b]piridin-1-il)piperidin-1-karboksilat sol

Country Status (26)

Country Link
US (1) US8759372B2 (hr)
EP (2) EP2820016B1 (hr)
JP (2) JP6208154B2 (hr)
KR (2) KR102220969B1 (hr)
CN (1) CN104136437B (hr)
AU (1) AU2013226361B2 (hr)
BR (1) BR112014021032B1 (hr)
CA (1) CA2865585C (hr)
CY (2) CY1119448T1 (hr)
DK (2) DK3254681T3 (hr)
EA (1) EA025358B1 (hr)
ES (2) ES2642737T3 (hr)
HK (1) HK1248111B (hr)
HR (2) HRP20171620T1 (hr)
HU (2) HUE034936T2 (hr)
IL (1) IL234272B (hr)
LT (2) LT3254681T (hr)
MX (1) MX352171B (hr)
NO (1) NO2935439T3 (hr)
PL (2) PL3254681T3 (hr)
PT (2) PT3254681T (hr)
RS (2) RS56556B1 (hr)
SG (1) SG11201404834XA (hr)
SI (2) SI3254681T1 (hr)
SM (1) SMT201700489T1 (hr)
WO (1) WO2013130402A1 (hr)

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IL234272B (en) 2018-10-31
JP2017226693A (ja) 2017-12-28
LT2820016T (lt) 2017-10-25
KR102220969B1 (ko) 2021-02-25
RS56556B1 (sr) 2018-02-28
SMT201700489T1 (it) 2017-11-15
DK3254681T3 (da) 2019-09-30
ES2642737T3 (es) 2017-11-17
US20130225636A1 (en) 2013-08-29
JP6476253B2 (ja) 2019-02-27
CY1122121T1 (el) 2020-11-25
DK2820016T3 (da) 2017-11-13
RS59295B1 (sr) 2019-10-31
AU2013226361A1 (en) 2014-10-16
PT2820016T (pt) 2017-10-18
CA2865585A1 (en) 2013-09-06
HRP20191655T1 (hr) 2019-12-13
JP2015511581A (ja) 2015-04-20
AU2013226361B2 (en) 2017-09-21
CY1119448T1 (el) 2018-03-07
SI2820016T1 (sl) 2017-11-30
BR112014021032A2 (hr) 2017-06-20
HUE047050T2 (hu) 2020-04-28
EP3254681B1 (en) 2019-06-19
KR20200016993A (ko) 2020-02-17
JP6208154B2 (ja) 2017-10-04
MX352171B (es) 2017-11-13
US8759372B2 (en) 2014-06-24
MX2014009544A (es) 2014-11-10
PL2820016T3 (pl) 2018-01-31
EP2820016A1 (en) 2015-01-07
EP2820016B1 (en) 2017-08-02
CA2865585C (en) 2019-12-10
HK1248111B (en) 2020-04-17
HUE034936T2 (hu) 2018-03-28
EA025358B1 (ru) 2016-12-30
SI3254681T1 (sl) 2019-10-30
SG11201404834XA (en) 2014-09-26
NO2935439T3 (hr) 2018-03-31
BR112014021032B1 (pt) 2022-09-27
CN104136437B (zh) 2016-05-11
PL3254681T3 (pl) 2019-12-31
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EP3254681A1 (en) 2017-12-13
WO2013130402A1 (en) 2013-09-06
KR102076118B1 (ko) 2020-02-11
KR20140130140A (ko) 2014-11-07
CN104136437A (zh) 2014-11-05
ES2746031T3 (es) 2020-03-04
LT3254681T (lt) 2019-09-25
PT3254681T (pt) 2019-10-01

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