HRP20121074T1 - Derivati kinolina i njihovi farmaceutski sastavi - Google Patents

Derivati kinolina i njihovi farmaceutski sastavi Download PDF

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Publication number
HRP20121074T1
HRP20121074T1 HRP20121074TT HRP20121074T HRP20121074T1 HR P20121074 T1 HRP20121074 T1 HR P20121074T1 HR P20121074T T HRP20121074T T HR P20121074TT HR P20121074 T HRP20121074 T HR P20121074T HR P20121074 T1 HRP20121074 T1 HR P20121074T1
Authority
HR
Croatia
Prior art keywords
compound according
hydroxy
indan
ylamino
hydroxyethyl
Prior art date
Application number
HRP20121074TT
Other languages
English (en)
Inventor
Olivier Lohse
Stéphanie MONNIER
Jean-Louis Reber
Original Assignee
Novartis Ag
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
Priority claimed from GB0613160A external-priority patent/GB0613160D0/en
Priority claimed from GB0613156A external-priority patent/GB0613156D0/en
Priority claimed from GB0613158A external-priority patent/GB0613158D0/en
Priority claimed from GB0613159A external-priority patent/GB0613159D0/en
Priority claimed from EP06117129A external-priority patent/EP1878722A1/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of HRP20121074T1 publication Critical patent/HRP20121074T1/hr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/24—Oxygen atoms attached in position 8
    • C07D215/26—Alcohols; Ethers thereof
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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

Landscapes

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

Claims (16)

1. Spoj, naznačen time, da ima formulu I [image] u obliku kristalne soli ili kristalnog solvata, gdje je W skupina formule [image] i A je acetat ili ksinafoat.
2. Spoj prema zahtjevu 1, naznačen time, da je to kristal (R)-5-[2-(5,6-dietil-indan-2-ilamino)-1-hidroksietil]-8-hidroksi-1H-kinolin-2-on-acetata.
3. Spoj prema zahtjevu 2, naznačen time, da u svojem uzorku difrakcije X-zraka ima čvrstu vršnu vrijednost (2θ) do 4,3°.
4. Spoj prema zahtjevu 2, naznačen time, da u svojem uzorku difrakcije X-zraka ima sljedeće karakteristične difrakcijske linije (2θ): 4,3 °, 8,4 °, 11,4 °, 15,1 °, 17,0 °, 18,6 °, 19,1 °, 19,7 °, 20,5 °, 22,9 °, 23,3 °, 23,5 °, 24,6 °, 25,6 °, 28,9 ° i 30,5°.
5. Spoj prema zahtjevu 1, naznačen time, da je to kristal (R)-5-[2-(5,6-dietil-indan-2-ilamino)-1-hidroksietil]-8-hidroksi-1H-kinolin-2-on-ksinafoata.
6. Spoj prema zahtjevu 5, naznačen time, da u svojem uzorku difrakcije X-zraka ima čvrstu vršnu vrijednost (2θ) do 4,1°.
7. Spoj prema zahtjevu 5, naznačen time, da u svojem uzorku difrakcije X-zraka ima sljedeće karakteristične difrakcijske linije (2θ): 4,1 °, 10,0 °, 12,2 °, 12,9 °, 18,2 °, 20,9 ° i 25,9°.
8. Farmaceutski sastav, naznačen time, da kao aktivni sastojak, obuhvaća učinkovitu količinu spoja prema zahtjevu 1, opcijski zajedno s farmaceutski prihvatljivim nosačem.
9. Farmaceutski sastav prema zahtjevu 8, naznačen time, da je aktivni sastojak kristal (R)-5-[2-(5,6-dietil-indan-2-ilamino)-1-hidroksietil]-8-hidroksi-1H-kinolin-2-on-acetata ili kristal (R)-5-[2-(5,6-dietil-indan-2-ilamino)-1-hidroksietil]-8-hidroksi-1H-kinolin-2-on-ksinafoata.
10. Farmaceutski sastav prema zahtjevu 8 ili zahtjevu 9, naznačen time, da je u obliku koji se može inhalirati.
11. Farmaceutski sastav prema zahtjevu 8, naznačen time, da kao aktivni sastojak, nadalje obuhvaća jednu, dvije, tri ili više protuupalnih, bronhodilatornih, antihistaminskih/protualergijskih ili antitusivnih ljekovitih tvari.
12. Farmaceutski sastav prema zahtjevu 11, naznačen time, da kao aktivni sastojak, nadalje obuhvaća jedan od spojeva ili oba spoja mometason furoata i glikopirolata.
13. Spoj prema zahtjevu 1, naznačen time, da se upotrebljava za liječenje upalnih ili opstrukcijskih bolesti dišnih puteva.
14. Kristal (R)-5-[2-(5,6-dietil-indan-2-ilamino)-1-hidroksietil]-8-hidroksi-1H-kinolin-2-on-acetata, naznačen time, da se upotrebljava za liječenje astme ili kronične opstrukcijske plućne bolesti.
15. Kristal (R)-5-[2-(5,6-dietil-indan-2-ilamino)-1-hidroksietil]-8-hidroksi-1H-kinolin-2-on-ksinafoata, naznačen time, da se upotrebljava za liječenje astme ili kronične opstrukcijske plućne bolesti.
16. Postupak proizvodnje spoja prema zahtjevu 1, naznačen time, da obuhvaća: (i) reakciju slobodne baze s octenom kiselinom, za proizvodnju spojeva formule I, gdje A je acetat; ili (ii) reakciju slobodne baze s 1-hidroksi 2-naftolnom kiselinom, za proizvodnju spojeva formule I, gdje A je ksinafoat.
HRP20121074TT 2006-06-30 2007-07-02 Derivati kinolina i njihovi farmaceutski sastavi HRP20121074T1 (hr)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GB0613160A GB0613160D0 (en) 2006-06-30 2006-06-30 Organic Compounds
GB0613156A GB0613156D0 (en) 2006-06-30 2006-06-30 Organic Compounds
GB0613158A GB0613158D0 (en) 2006-06-30 2006-06-30 Organic compounds
GB0613159A GB0613159D0 (en) 2006-06-30 2006-06-30 Organic Compounds
EP06117129A EP1878722A1 (en) 2006-07-13 2006-07-13 Quinolinone derivatives and their pharmaceutical compositions
PCT/EP2007/056632 WO2008000839A1 (en) 2006-06-30 2007-07-02 Quinolinone derivatives and their pharmaceutical compositions

Publications (1)

Publication Number Publication Date
HRP20121074T1 true HRP20121074T1 (hr) 2013-01-31

Family

ID=38610531

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20121074TT HRP20121074T1 (hr) 2006-06-30 2007-07-02 Derivati kinolina i njihovi farmaceutski sastavi

Country Status (28)

Country Link
US (2) US8198450B2 (hr)
EP (1) EP2044025B1 (hr)
JP (1) JP5253392B2 (hr)
KR (1) KR101402398B1 (hr)
CN (1) CN101479245B (hr)
AU (1) AU2007264946B2 (hr)
BR (1) BRPI0713951B8 (hr)
CA (1) CA2654801C (hr)
CY (3) CY1113733T1 (hr)
DK (1) DK2044025T3 (hr)
ES (1) ES2396987T3 (hr)
FI (2) FIC20200047I1 (hr)
FR (2) FR20C1054I1 (hr)
HR (1) HRP20121074T1 (hr)
HU (2) HUS2000043I1 (hr)
IL (1) IL195796A (hr)
LT (2) LTC2044025I2 (hr)
LU (2) LUC00185I2 (hr)
MA (1) MA30540B1 (hr)
MX (1) MX2008016542A (hr)
MY (1) MY150468A (hr)
NO (3) NO341709B1 (hr)
NZ (1) NZ573292A (hr)
PL (1) PL2044025T3 (hr)
PT (1) PT2044025E (hr)
SI (1) SI2044025T1 (hr)
WO (1) WO2008000839A1 (hr)
ZA (1) ZA200809948B (hr)

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CN101861314B (zh) 2007-09-05 2013-07-24 里格尔制药公司 N4-[(2,2-二氟-4h-苯并[1,4]*嗪-3-酮)-6-基]-5-氟-n2-[3-(甲基氨基羰基亚甲基氧基)苯基]-2,4-嘧啶二胺的1-羟基-2-萘甲酸盐
JOP20120023B1 (ar) 2011-02-04 2022-03-14 Novartis Ag صياغات مساحيق جافة من جسيمات تحتوي على واحد أو اثنين من المواد الفعالة لعلاج امراض ممرات الهواء الانسدادية او الالتهابية
US9452139B2 (en) 2013-03-14 2016-09-27 Novartis Ag Respirable agglomerates of porous carrier particles and micronized drug
CN105209013B (zh) 2013-03-14 2019-04-26 诺华股份有限公司 喷雾干燥制剂经喷雾混合的脱非晶化
ES2747905T3 (es) 2015-09-29 2020-03-12 Inke Sa Solvato mixto de L-tartrato de (R)-5-[2-(5,6-dietilindan-2-ilamino)-1-hidroxietil]-8-hidroxi-1H-quinolin-2-ona
CN110724095B (zh) * 2019-09-12 2023-06-09 上海方予健康医药科技有限公司 一种茚达特罗乙酸盐的制备方法
WO2026027448A1 (en) 2024-07-29 2026-02-05 Inke, S.A. Micronization process of indacaterol acetate

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Also Published As

Publication number Publication date
CN101479245B (zh) 2013-05-22
NO341709B1 (no) 2018-01-02
BRPI0713951A2 (pt) 2012-12-04
NO2020041I1 (no) 2020-11-23
HUS2000043I1 (hu) 2020-12-28
HK1127597A1 (en) 2009-10-02
IL195796A0 (en) 2009-09-01
FR20C1063I1 (fr) 2021-01-22
DK2044025T3 (da) 2013-01-14
BRPI0713951B8 (pt) 2021-05-25
IL195796A (en) 2016-03-31
CY2020038I2 (el) 2021-03-12
BRPI0713951B1 (pt) 2019-08-13
JP2009541455A (ja) 2009-11-26
LUC00185I2 (hr) 2024-07-01
AU2007264946A1 (en) 2008-01-03
US20120316142A1 (en) 2012-12-13
WO2008000839A1 (en) 2008-01-03
MX2008016542A (es) 2009-01-19
MY150468A (en) 2014-01-30
NO2020044I1 (no) 2020-12-07
MA30540B1 (fr) 2009-06-01
CY2020041I2 (el) 2021-03-12
AU2007264946B2 (en) 2011-01-20
NZ573292A (en) 2011-03-31
CA2654801A1 (en) 2008-01-03
SI2044025T1 (sl) 2013-01-31
PL2044025T3 (pl) 2013-02-28
CY2020038I1 (el) 2021-03-12
KR101402398B1 (ko) 2014-06-03
ZA200809948B (en) 2009-05-25
NO20090312L (no) 2009-01-28
ES2396987T3 (es) 2013-03-01
JP5253392B2 (ja) 2013-07-31
CA2654801C (en) 2014-08-19
CN101479245A (zh) 2009-07-08
CY1113733T1 (el) 2016-06-22
LTPA2020535I1 (lt) 2020-12-28
LTPA2020538I1 (lt) 2021-01-11
LUC00188I2 (hr) 2024-07-01
PT2044025E (pt) 2012-12-17
US20090325912A1 (en) 2009-12-31
CY2020041I1 (el) 2021-03-12
EP2044025A1 (en) 2009-04-08
KR20090023651A (ko) 2009-03-05
FIC20200047I1 (fi) 2020-11-27
LTC2044025I2 (lt) 2022-10-10
FIC20200050I1 (fi) 2020-12-16
US8198450B2 (en) 2012-06-12
HUS2000053I1 (hu) 2020-12-28
EP2044025B1 (en) 2012-10-03
FR20C1054I1 (fr) 2020-12-25

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