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HRP20140589T1 - Derivati pirazinooksazepina - Google Patents

Derivati pirazinooksazepina Download PDF

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Publication number
HRP20140589T1
HRP20140589T1 HRP20140589AT HRP20140589T HRP20140589T1 HR P20140589 T1 HRP20140589 T1 HR P20140589T1 HR P20140589A T HRP20140589A T HR P20140589AT HR P20140589 T HRP20140589 T HR P20140589T HR P20140589 T1 HRP20140589 T1 HR P20140589T1
Authority
HR
Croatia
Prior art keywords
group
optionally substituted
compound
salt
salt according
Prior art date
Application number
HRP20140589AT
Other languages
English (en)
Inventor
Shigekazu Sasaki
Tomokazu Kusumoto
Izumi Nomura
Hironobu Maezaki
Original Assignee
Takeda Pharmaceutical Company Limited
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
Application filed by Takeda Pharmaceutical Company Limited filed Critical Takeda Pharmaceutical Company Limited
Publication of HRP20140589T1 publication Critical patent/HRP20140589T1/hr

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Classifications

    • 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Surgery (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (18)

1. Spoj, naznačen time, da je predstavljen formulom (I0): [image] gdje R1 je sljedeće: (1) morfolinil-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina, (2) piperidil-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina, (3) pirolidinil-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina koje su opcijski supstituirane s jednom ili više C1-6 alkoksi-skupina, (4) pirolil-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina, (5) imidazolil-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina, (6) amino-skupina opcijski supstituirana s 1 ili 2 supstituenta odabrana od sljedećih: (a) C1-6 alkil-skupina opcijski supstituirana s jednim ili više supstituenata odabranima od C3-6 cikloalkil-skupine i fenilne skupine, i (b) C3-6 cikloalkil-skupina, (7) C1-6 alkilsulfanil-skupina, (8) C1-6 alkoksi-skupina opcijski supstituirana s jednom ili više C3-6 cikloalkil-skupina, (9) C3-6 cikloalkil-skupina, ili (10) C3-6 cikloalkenil-skupina; R2' je atom vodika ili C1-6 alkil-skupina opcijski supstituirana s jednom ili više C1-6 alkoksi-skupina, i R3' je atom vodika, atom halogena ili C1-6 alkil-skupina, ili njegova sol.
2. Spoj ili sol prema zahtjevu 1, naznačen time, da R1 je sljedeće: (1) morfolinil-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina, (2) piperidil-skupina supstituirana s jednom ili više C1-6 alkil-skupina, (3) pirolidinil-skupina supstituirana s jednom ili više C1-6 alkil-skupina koje su opcijski supstituirane s jednom ili više C1-6 alkoksi-skupina, (4) pirolil-skupina supstituirana s jednom ili više C1-6 alkil-skupina, (5) imidazolil-skupina supstituirana s jednom ili više C1-6 alkil-skupina, (6) amino-skupina opcijski supstituirana s 1 ili 2 supstituenta odabrana od sljedećih: (a) C1-6 alkil-skupina opcijski supstituirana s jednim ili više supstituenata odabranima od C3-6 cikloalkil-skupine i fenilne skupine, i (b) C3-6 cikloalkil-skupina, (7) C1-6 alkilsulfanil-skupina, (8) C1-6 alkoksi-skupina opcijski supstituirana s jednom ili više C3-6 cikloalkil-skupina, (9) C3-6 cikloalkil-skupina, ili (10) C3-6 cikloalkenil-skupina.
3. Spoj ili sol prema zahtjevu 1, naznačen time, da je spoj predstavljen formulom (I) [image] gdje R1 je morfolino-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina, di(C1-6 alkil)amino-skupina, C1-6 alkoksi-skupina opcijski supstituirana s jednom ili više C3-6 cikloalkil-skupina, C3-6 cikloalkil-skupina ili C3-6 cikloalkenil-skupina; i R2 je atom vodika ili C1-6 alkil-skupina.
4. Spoj ili sol prema zahtjevu 3, naznačen time, da R1 je morfolino-skupina opcijski supstituirana s jednom ili više C1-6 alkil-skupina, di(C1-6 alkil)amino-skupina, C1-6 alkoksi-skupina ili C3-6 cikloalkil-skupina.
5. Spoj ili sol prema zahtjevu 3, naznačen time, da R1 je morfolino-skupina opcijski supstituirana s jednim ili više supstituenata odabranima između metilne skupine i etilne skupine, N-metil-N-(1-metiletil)amino-skupina, izopropoksi- skupina ili ciklopropil-skupina; i R2 je atom vodika ili metilna skupina.
6. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 3-(1-metiletoksi)-6,7,8,9-tetrahidropirazino[2,3-f][1,4]oksazepin ili njegova sol.
7. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 3-(3-metilmorfolin-4-il)-6,7,8,9-tetrahidropirazino[2,3-f][1,4]oksazepin ili njegova sol.
8. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 6-metil-3-(morfolin-4-il)-6,7,8,9-tetrahidropirazino[2,3-f][1,4] oksazepin ili njegova sol.
9. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 6-metil-3-(3-metilmorfolin-4-il)-6,7,8,9-tetrahidropirazino[2,3-f][1,4]oksazepin ili njegova sol.
10. Spoj ili sol prema zahtjevu 1, naznačen time, da je to N-metil-N-(1-metiletil)-6,7,8,9-tetrahidropirazino[2,3-f][1,4]oksazepin-3-amin ili njegova sol.
11. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 3-(3-etilmorfolin-4-il)-6,7,8,9-tetrahidropirazino[2,3-f][1,4]oksazepin ili njegova sol.
12. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 3-ciklopropil-6,7,8,9- tetrahidropirazino[2,3-f][1,4]oksazepin ili njegova sol.
13. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 3-(2-metilpiperidin-1-il)-6,7,8,9-tetrahidropirazino[2,3-f][1,4]oksazepin ili njegova sol.
14. Spoj ili sol prema zahtjevu 1, naznačen time, da je to 3-(2-metilpirolidin-1-il)-6,7,8,9-tetrahidropirazino[2,3-f][1,4]oksazepin ili njegova sol.
15. Lijek, naznačen time, da obuhvaća spoj ili sol prema jednom od zahtjeva 1 do 14.
16. Lijek prema zahtjevu 15, naznačen time, da je to aktivator receptora serotonina 5-HT2C.
17. Lijek prema zahtjevu 15, naznačen time, da se upotrebljava za profilaksu ili liječenje simptoma spuštenog urinarnog trakta, pretilosti i/ili propadanja organa.
18. Spoj ili sol prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava za profilaksu ili liječenje simptoma spuštenog urinarnog trakta, pretilosti i/ili propadanja organa.
HRP20140589AT 2009-06-15 2014-06-23 Derivati pirazinooksazepina HRP20140589T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2009142673 2009-06-15
PCT/JP2010/060408 WO2010147226A1 (en) 2009-06-15 2010-06-14 Pyrazinooxazepine derivatives

Publications (1)

Publication Number Publication Date
HRP20140589T1 true HRP20140589T1 (hr) 2014-08-01

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Application Number Title Priority Date Filing Date
HRP20140589AT HRP20140589T1 (hr) 2009-06-15 2014-06-23 Derivati pirazinooksazepina

Country Status (41)

Country Link
US (4) US9115139B2 (hr)
EP (1) EP2442870B1 (hr)
JP (2) JP5579262B2 (hr)
KR (1) KR101768234B1 (hr)
CN (1) CN102458579B (hr)
AR (1) AR077094A1 (hr)
AU (1) AU2010260847B2 (hr)
BR (1) BRPI1011502A2 (hr)
CA (1) CA2765239C (hr)
CL (1) CL2011003154A1 (hr)
CO (1) CO6491037A2 (hr)
CR (1) CR20120021A (hr)
CY (1) CY1115483T1 (hr)
DK (1) DK2442870T3 (hr)
DO (1) DOP2011000393A (hr)
EA (1) EA021079B1 (hr)
EC (1) ECSP12011603A (hr)
ES (1) ES2480275T3 (hr)
GE (1) GEP20146168B (hr)
HK (1) HK1169623A1 (hr)
HR (1) HRP20140589T1 (hr)
IL (1) IL216761A (hr)
JO (1) JO3087B1 (hr)
MA (1) MA33430B1 (hr)
ME (1) ME01835B (hr)
MX (1) MX2011013081A (hr)
MY (1) MY157497A (hr)
NZ (1) NZ597507A (hr)
PE (1) PE20121049A1 (hr)
PL (1) PL2442870T3 (hr)
PT (1) PT2442870E (hr)
RS (1) RS53414B (hr)
SG (1) SG176696A1 (hr)
SI (1) SI2442870T1 (hr)
SM (1) SMT201400080B (hr)
TN (1) TN2011000630A1 (hr)
TW (2) TWI542592B (hr)
UA (1) UA108357C2 (hr)
UY (1) UY32707A (hr)
WO (1) WO2010147226A1 (hr)
ZA (1) ZA201109370B (hr)

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EP2018863B9 (en) * 2006-05-16 2015-02-18 Takeda Pharmaceutical Company Limited Fused heterocyclic compound and use thereof
NZ597507A (en) * 2009-06-15 2013-09-27 Takeda Pharmaceutical Pyrazinooxazepine derivatives
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JP2014201578A (ja) * 2013-04-09 2014-10-27 武田薬品工業株式会社 線維筋痛症治療剤
JP2014214132A (ja) * 2013-04-26 2014-11-17 武田薬品工業株式会社 ニコチン依存症の予防・治療剤
WO2015066344A1 (en) 2013-11-01 2015-05-07 Arena Pharmaceuticals, Inc. 5-ht2c receptor agonists and compositions and methods of use
WO2017026538A1 (en) 2015-08-07 2017-02-16 Takeda Pharmaceutical Company Limited Production method of pyrazine
WO2017111178A1 (en) 2015-12-24 2017-06-29 Takeda Pharmaceutical Company Limited Solid preparation
US9985579B2 (en) 2016-04-12 2018-05-29 Preformed Line Products Co. Mounting assembly for mounting a solar panel
EP3733204A4 (en) * 2017-12-27 2021-09-15 Takeda Pharmaceutical Company Limited THERAPEUTIC AGENT FOR URINARY INCONTINENCE OF STRESS AND FECAL INCONTINENCE

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Publication number Publication date
AU2010260847B2 (en) 2016-11-24
JO3087B1 (ar) 2017-03-15
EA201270017A1 (ru) 2012-07-30
US8318722B2 (en) 2012-11-27
TW201529584A (zh) 2015-08-01
MY157497A (en) 2016-06-15
US9115139B2 (en) 2015-08-25
JP2012107032A (ja) 2012-06-07
IL216761A (en) 2016-03-31
CY1115483T1 (el) 2017-01-04
DOP2011000393A (es) 2012-02-15
IL216761A0 (en) 2012-02-29
JP5579262B2 (ja) 2014-08-27
CL2011003154A1 (es) 2012-06-15
US20100317651A1 (en) 2010-12-16
JP2012530051A (ja) 2012-11-29
EA021079B1 (ru) 2015-03-31
NZ597507A (en) 2013-09-27
HK1169623A1 (en) 2013-02-01
ES2480275T3 (es) 2014-07-25
US20110282054A1 (en) 2011-11-17
TN2011000630A1 (en) 2013-05-24
EP2442870B1 (en) 2014-04-16
JP5579203B2 (ja) 2014-08-27
SI2442870T1 (sl) 2014-07-31
UY32707A (es) 2011-01-31
TW201109338A (en) 2011-03-16
MX2011013081A (es) 2012-01-20
PT2442870E (pt) 2014-07-16
SG176696A1 (en) 2012-01-30
KR20120034734A (ko) 2012-04-12
CO6491037A2 (es) 2012-07-31
MA33430B1 (fr) 2012-07-03
DK2442870T3 (da) 2014-06-30
WO2010147226A1 (en) 2010-12-23
AR077094A1 (es) 2011-08-03
US20120135979A1 (en) 2012-05-31
RS53414B (en) 2014-12-31
EP2442870A1 (en) 2012-04-25
ZA201109370B (en) 2012-10-31
CN102458579A (zh) 2012-05-16
PE20121049A1 (es) 2012-08-22
CR20120021A (es) 2012-03-06
ECSP12011603A (es) 2012-03-30
GEP20146168B (en) 2014-09-25
US8314088B2 (en) 2012-11-20
CA2765239A1 (en) 2010-12-23
CN102458579B (zh) 2014-11-05
BRPI1011502A2 (pt) 2016-03-22
KR101768234B1 (ko) 2017-08-14
CA2765239C (en) 2018-08-07
TWI542592B (zh) 2016-07-21
SMT201400080B (it) 2014-09-08
PL2442870T3 (pl) 2014-12-31
US8324201B2 (en) 2012-12-04
UA108357C2 (xx) 2015-04-27
ME01835B (me) 2014-12-20
AU2010260847A1 (en) 2012-01-19
US20110288291A1 (en) 2011-11-24

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