HRP20171304T1 - Sol s jantarnom kiselinom 1-[2-(2-klor-4-{[(r)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilaminometil]}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline i njezina upotreba u liječenju plućnih poremećaja - Google Patents
Sol s jantarnom kiselinom 1-[2-(2-klor-4-{[(r)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilaminometil]}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline i njezina upotreba u liječenju plućnih poremećaja Download PDFInfo
- Publication number
- HRP20171304T1 HRP20171304T1 HRP20171304TT HRP20171304T HRP20171304T1 HR P20171304 T1 HRP20171304 T1 HR P20171304T1 HR P20171304T T HRP20171304T T HR P20171304TT HR P20171304 T HRP20171304 T HR P20171304T HR P20171304 T1 HRP20171304 T1 HR P20171304T1
- Authority
- HR
- Croatia
- Prior art keywords
- hydroxy
- salt
- inflammatory agent
- succinic acid
- ester
- Prior art date
Links
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical class OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 title claims 11
- -1 8-hydroxy-2-oxo-1, 2-dihydroquinolin-5-yl Chemical group 0.000 title claims 8
- QMOVGVNKXUTCQU-UHFFFAOYSA-N (2-phenylphenyl)carbamic acid Chemical compound OC(=O)NC1=CC=CC=C1C1=CC=CC=C1 QMOVGVNKXUTCQU-UHFFFAOYSA-N 0.000 title claims 5
- 208000019693 Lung disease Diseases 0.000 title claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 title 1
- 239000002294 steroidal antiinflammatory agent Substances 0.000 claims 8
- 239000000825 pharmaceutical preparation Substances 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229960000289 fluticasone propionate Drugs 0.000 claims 3
- WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical group C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 239000001384 succinic acid Substances 0.000 claims 3
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- 150000003890 succinate salts Chemical class 0.000 claims 2
- QEZGRWSAUJTDEZ-UHFFFAOYSA-N 2-[4-[2-(2,3-dihydro-1H-inden-2-ylamino)pyrimidin-5-yl]-3-(piperidine-1-carbonyl)pyrazol-1-yl]-1-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethanone Chemical compound C1C(CC2=CC=CC=C12)NC1=NC=C(C=N1)C=1C(=NN(C=1)CC(=O)N1CC2=C(CC1)NN=N2)C(=O)N1CCCCC1 QEZGRWSAUJTDEZ-UHFFFAOYSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- 238000010521 absorption reaction Methods 0.000 claims 1
- 238000000862 absorption spectrum Methods 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000008121 dextrose Substances 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 238000002844 melting Methods 0.000 claims 1
- 230000008018 melting Effects 0.000 claims 1
- 229920000747 poly(lactic acid) Polymers 0.000 claims 1
- 239000004626 polylactic acid Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 238000009331 sowing Methods 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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 two hetero rings
- C07D401/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61P11/16—Central respiratory analeptics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Pulmonology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (20)
1. Sol s jantarnom kiselinom 1-[2-(2-klor-4-{[(R)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilamino]metil}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline, koja je Oblik 1 kristalnog oblika čvrstog stanja, naznačena time što ima uzorak difrakcije rendgenskih zraka na prahu, s difrakcijskim maksimumima kod vrijednosti 2θ od 5,0, 5,7, 7,1, 10,0, 12,6, 13,8, 14,4, 15,5, 16,1, 16,4, 16,9, 17,8, 18,5, 20,2, 20,5, 21,4, 25,3, 25,8 i 26,3.
2. Kristalni Oblik 1 soli s jantarnom kiselinom u skladu s patentnim zahtjevom 1, naznačen time što sol ima:
a. otisak diferencijalne skenirajuće kalorimetrije koji pokazuje talište u rasponu od 170 °C do 180 °C; ili
b. infracrveni apsorpcijski spektar sa značajnim apsorpcijskim vrpcama na otprilike 3265, 2832, 1735, 1718, 1679, 1669, 1591, 1540, 1518, 1493, 1439, 1405, 1339, 1302, 1283, 1239, 1202, 1163, 1144, 1107, 1095, 1039, 1009, 973, 921, 885, 868, 838, 773, 751, te 707 cm–1.
3. Kristalni Oblik 1 soli s jantarnom kiselinom u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je u mikroniziranom obliku.
4. Farmaceutski pripravak, naznačen time što sadrži farmaceutski prihvatljivu podlogu uz kristalni Oblik 1 soli s jantarnom kiselinom u skladu s bilo kojim od patentnih zahtjeva 1 do 3.
5. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što pripravak dodatno sadrži steroidno protuupalno sredstvo.
6. Farmaceutski pripravak u skladu s patentnim zahtjevom 5, naznačen time što je steroidno protuupalno sredstvo S-fluormetilni ester 6α,9α-difluor-17α-[(2-furanilkarbonil)oksi]-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline, ili njegov solvat.
7. Farmaceutski pripravak u skladu s patentnim zahtjevom 5, naznačen time što je steroidno protuupalno sredstvo flutikazon-propionat.
8. Farmaceutski pripravak u skladu s bilo kojim od patentnih zahtjeva 4 do 7, naznačen time što je pripravak formuliran za primjenu inhaliranjem.
9. Farmaceutski pripravak u skladu s patentnim zahtjevom 4, naznačen time što je u mikroniziranom obliku.
10. Farmaceutski pripravak u skladu s patentnim zahtjevom 8, naznačen time što je podloga laktoza, škrob, manitol, dekstroza, polimliječna kiselina, polilaktid-ko-glikolid, ili njihova kombinacija.
11. Kombinacija, naznačena time što sadrži:
(a) kristalni Oblik 1 soli s jantarnom kiselinom u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2; i
(b) steroidno protuupalno sredstvo.
12. Kombinacija u skladu s patentnim zahtjevom 11, naznačena time što je steroidno protuupalno sredstvo S-fluormetilni ester 6α,9α-difluor-17α-[(2-furanilkarbonil)oksi]-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline, ili njegov solvat.
13. Kombinacija u skladu s patentnim zahtjevom 11, naznačena time što je steroidno protuupalno sredstvo flutikazon-propionat.
14. Kristalni Oblik 1 soli s jantarnom kiselinom 1-[2-(2-klor-4-{[(R)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilamino]metil}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time što je namijenjen upotrebi u terapiji ili kao medikament.
15. Upotreba kristalnog Oblika 1 soli s jantarnom kiselinom 1-[2-(2-klor-4-{[(R)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilamino]metil}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline, u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačena time što je kristalni Oblik 1 namijenjen proizvodnji medikamenta za liječenje plućnog poremećaja.
16. Upotreba u skladu s patentnim zahtjevom 15, naznačena time što je plućni poremećaj kronična opstruktivna plućna bolest ili astma.
17. Upotreba:
(a) kristalnog Oblika 1 soli s jantarnom kiselinom 1-[2-(2-klor-4-{[(R)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilamino]metil}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline, u skladu s bilo kojim od patentnih zahtjeva 1-3; i
(b) steroidnog protuupalnog sredstva;
naznačena time što su kristalni Oblik 1 i steroidno protuupalno sredstvo namijenjeni proizvodnji medikamenta za liječenje plućnog poremećaja.
18. Upotreba u skladu s patentnim zahtjevom 17, naznačena time što je steroidno protuupalno sredstvo S-fluormetilni ester 6α,9α-difluor-17α-[(2-furanilkarbonil)oksi]-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline, ili njegov solvat.
19. Upotreba u skladu s patentnim zahtjevom 17, naznačena time što je steroidno protuupalno sredstvo flutikazon-propionat.
20. Postupak dobivanja Oblika 1 sukcinatne soli u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što se navedeni postupak sastoji u koracima:
otapanja sukcinatne soli u vodenoj otopini THF-a (10-18%, primjerice 10-16%), na temperaturi u rasponu od 18 do 23 °C, primjerice otprilike 20 °C;
dodavanju prvog volumena nižeg alkohola, primjerice etanola ili izopropanola, osobito izopropanola, te zagrijavanju do 32-40 °C;
izbornom zasijavanju Oblikom 1;
dodavanju drugog volumena nižeg alkohola, primjerice tijekom nekoliko sati, po mogućnosti otprilike 12 sati;
hlađenju do temperature u rasponu od 18 do 23 °C, primjerice otprilike 20 °C; i
prikupljanju kristalnog produkta.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0602778.3A GB0602778D0 (en) | 2006-02-10 | 2006-02-10 | Novel compound |
| EP07704449.3A EP1981872B1 (en) | 2006-02-10 | 2007-02-08 | Succinic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[ (r)-2-hydroxy-2- (8-hydroxy-2-oxo-1, 2-dihydroquinolin-5-yl) eth ylaminoimethyl]} -5-methoxyphenylcarbamoyl) ethyl]piperidin-4-yl ester and its use for the treatment of pulmonary disorders |
| PCT/EP2007/051196 WO2007090859A1 (en) | 2006-02-10 | 2007-02-08 | Succinic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{ [ (r)-2-hydroxy-2- (8-hydroxy-2-oxo-1, 2-dihydroquinolin-5-yl) eth ylaminoimethyl] } -5-methoxyphenylcarbamoyl) ethyl] piperidin-4-yl ester and its use for the treatment of pulmonary disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20171304T1 true HRP20171304T1 (hr) | 2017-10-20 |
Family
ID=36119909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20171304TT HRP20171304T1 (hr) | 2006-02-10 | 2017-08-30 | Sol s jantarnom kiselinom 1-[2-(2-klor-4-{[(r)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilaminometil]}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline i njezina upotreba u liječenju plućnih poremećaja |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US7960551B2 (hr) |
| EP (1) | EP1981872B1 (hr) |
| JP (1) | JP5616021B2 (hr) |
| KR (1) | KR101488691B1 (hr) |
| CN (1) | CN101379057B (hr) |
| AR (2) | AR059409A1 (hr) |
| AU (1) | AU2007213767B2 (hr) |
| BR (1) | BRPI0707559B8 (hr) |
| CA (1) | CA2641769C (hr) |
| CR (1) | CR10227A (hr) |
| CY (1) | CY1119238T1 (hr) |
| DK (1) | DK1981872T3 (hr) |
| EA (1) | EA016580B1 (hr) |
| ES (1) | ES2640226T3 (hr) |
| GB (1) | GB0602778D0 (hr) |
| HR (1) | HRP20171304T1 (hr) |
| HU (1) | HUE034315T2 (hr) |
| IL (1) | IL193103A (hr) |
| JO (1) | JO3389B1 (hr) |
| LT (1) | LT1981872T (hr) |
| MA (1) | MA30273B1 (hr) |
| MY (1) | MY153656A (hr) |
| NO (1) | NO341343B1 (hr) |
| NZ (1) | NZ570242A (hr) |
| PE (2) | PE20071249A1 (hr) |
| PL (1) | PL1981872T3 (hr) |
| PT (1) | PT1981872T (hr) |
| SG (1) | SG169404A1 (hr) |
| SI (1) | SI1981872T1 (hr) |
| TW (1) | TWI401251B (hr) |
| UA (1) | UA100364C2 (hr) |
| WO (1) | WO2007090859A1 (hr) |
| ZA (1) | ZA200806782B (hr) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8519138B2 (en) | 2009-04-14 | 2013-08-27 | Glaxo Group Limited | Process for the preparation of a biphenyl-2-yl carbamic acid ester |
| AU2015234331B2 (en) * | 2009-04-23 | 2017-08-03 | Theravance Biopharma R&D Ip, Llc | Diamide compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity |
| PL3210981T3 (pl) * | 2009-04-23 | 2019-06-28 | Theravance Respiratory Company, Llc | Związki diamidowe wykazujące działanie jako antagonista receptora muskarynowego i agonista antagonista receptora beta 2 adrenergicznego |
| WO2011081937A1 (en) | 2009-12-15 | 2011-07-07 | Gilead Sciences, Inc. | Corticosteroid-beta-agonist-muscarinic antagonist compounds for use in therapy |
| EP2386555A1 (en) | 2010-05-13 | 2011-11-16 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities |
| ITRM20110083U1 (it) | 2010-05-13 | 2011-11-14 | De La Cruz Jose Antonio Freire | Piastra per la costruzione di carrelli per aeroplani |
| AR083115A1 (es) | 2010-09-30 | 2013-01-30 | Theravance Inc | Sales oxalato cristalinas de un compuesto diamida |
| EA026453B1 (ru) * | 2011-08-02 | 2017-04-28 | Сигма-Тау Индустрие Фармасьютике Риуните С.П.А. | Применение окисленного авидина для ингаляции |
| EP2592078A1 (en) | 2011-11-11 | 2013-05-15 | Almirall, S.A. | New cyclohexylamine derivatives having beta2 adrenergic agonist and M3 muscarinic antagonist activities |
| BR112015013628A2 (pt) * | 2012-12-18 | 2017-07-11 | Almirall Sa | derivados de carbamato de ciclo-hexila e quinuclidinila tendo atividades agonista adrenérgica de beta2 e antagonista muscarínica de m3 |
| TWI643853B (zh) | 2013-02-27 | 2018-12-11 | 阿爾米雷爾有限公司 | 同時具有β2腎上腺素受體促效劑和M3毒蕈鹼受體拮抗劑活性之2-氨基-1-羥乙基-8-羥基喹啉-2(1H)-酮衍生物之鹽類 |
| TWI641373B (zh) | 2013-07-25 | 2018-11-21 | 阿爾米雷爾有限公司 | 具有蕈毒鹼受體拮抗劑和β２腎上腺素受體促效劑二者之活性的２－胺基－１－羥乙基－８－羥基喹啉－２（１Ｈ）－酮衍生物之鹽 |
| TW201517906A (zh) | 2013-07-25 | 2015-05-16 | Almirall Sa | 含有ｍａｂａ化合物和皮質類固醇之組合 |
| TW201617343A (zh) | 2014-09-26 | 2016-05-16 | 阿爾米雷爾有限公司 | 具有β２腎上腺素促效劑及Ｍ３蕈毒拮抗劑活性之新穎雙環衍生物 |
| GB201500447D0 (en) * | 2015-01-12 | 2015-02-25 | Glaxosmithkline Ip Dev Ltd | Novel Combination Product |
| CN106632257B (zh) * | 2016-12-15 | 2019-02-12 | 上海市奉贤区中心医院 | Gsk961081及其中间体的合成方法 |
| US11484531B2 (en) | 2018-08-30 | 2022-11-01 | Theravance Biopharma R&D Ip, Llc | Methods for treating chronic obstructive pulmonary disease |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4022776A (en) | 1974-01-31 | 1977-05-10 | Otsuka Pharmaceutical Company Limited | 5-[1-Hydroxy-2-(substituted-amino)]ethyl-8-hydroxycarbostyril derivatives |
| DE3134590A1 (de) | 1981-09-01 | 1983-03-10 | Boehringer Ingelheim KG, 6507 Ingelheim | Neue benzo-heterocyclen |
| US4460581A (en) | 1982-10-12 | 1984-07-17 | Boehringer Ingelheim Kg | (1-Hydroxy-2-amino-alkyl)-substituted benzoxazinones and benzoxazolinones |
| ZW6584A1 (en) | 1983-04-18 | 1985-04-17 | Glaxo Group Ltd | Phenethanolamine derivatives |
| US4894219A (en) | 1988-03-29 | 1990-01-16 | University Of Florida | Beta-agonist carbostyril derivatives, assay method and pharmacological composition |
| DK443489D0 (da) | 1989-09-08 | 1989-09-08 | Ferrosan As | Substituerede urinstofforbindelser, deres fremstilling og anvendelse |
| EP0972773A1 (en) | 1992-03-31 | 2000-01-19 | Glaxo Group Limited | 2-Oxadiazolyl- or 2-thiadiazolyl-phenylcarbamate and -phenylurea derivatives, their preparation and their use as intermediates |
| CA2123728A1 (en) | 1993-05-21 | 1994-11-22 | Noriyoshi Sueda | Urea derivatives and their use as acat inhibitors |
| AU7545894A (en) | 1993-09-02 | 1995-03-22 | Yamanouchi Pharmaceutical Co., Ltd. | Carbamate derivative and medicine containing the same |
| CA2182568A1 (en) | 1994-02-10 | 1995-08-17 | Makoto Takeuchi | Novel carbamate derivative and medicinal composition containing the same |
| EP0863141B1 (en) | 1995-10-13 | 2001-09-12 | Banyu Pharmaceutical Co., Ltd. | Substituted heteroaromatic derivatives |
| PE92198A1 (es) | 1996-08-01 | 1999-01-09 | Banyu Pharma Co Ltd | Derivados de 1,4-piperidina disustituida que contienen fluor |
| US6040344A (en) | 1996-11-11 | 2000-03-21 | Sepracor Inc. | Formoterol process |
| CA2313125A1 (en) | 1997-12-12 | 1999-06-24 | Laramie Mary Gaster | Quinolinepiperazine and quinolinepiperidine derivatives, their preparation and their use as combined 5-ht1a, 5-ht1b and 5-ht1d receptor antagonists |
| US6362371B1 (en) | 1998-06-08 | 2002-03-26 | Advanced Medicine, Inc. | β2- adrenergic receptor agonists |
| EP1086066A4 (en) | 1998-06-08 | 2001-08-08 | Advanced Medicine Inc | MUSCARINIC RECEPTOR ANTAGONISTS |
| US6713651B1 (en) | 1999-06-07 | 2004-03-30 | Theravance, Inc. | β2-adrenergic receptor agonists |
| US6693202B1 (en) | 1999-02-16 | 2004-02-17 | Theravance, Inc. | Muscarinic receptor antagonists |
| GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
| US6593497B1 (en) | 1999-06-02 | 2003-07-15 | Theravance, Inc. | β2-adrenergic receptor agonists |
| UA73543C2 (uk) | 1999-12-07 | 2005-08-15 | Тераванс, Інк. | Похідні сечовини, фармацевтична композиція та застосування похідного при приготуванні лікарського засобу для лікування захворювання, яке опосередковується мускариновим рецептором |
| DE60021282T2 (de) | 1999-12-07 | 2006-05-18 | Theravance, Inc., South San Francisco | Carbamat-derivate als muscarin-rezeptor antonisten |
| UA73965C2 (en) | 1999-12-08 | 2005-10-17 | Theravance Inc | b2 ADRENERGIC RECEPTOR ANTAGONISTS |
| AU2930501A (en) * | 2000-01-07 | 2001-07-24 | Transform Pharmaceuticals, Inc. | High-throughput formation, identification, and analysis of diverse solid-forms |
| CA2411351A1 (en) | 2000-06-05 | 2001-12-13 | Altana Pharma Ag | Compounds effective as beta-2-adrenoreceptor agonists as well as pde4-inhibitors |
| EP1345937B1 (en) | 2000-12-22 | 2005-09-28 | Almirall Prodesfarma AG | Quinuclidine carbamate derivatives and their use as m3 antagonists |
| GB0103630D0 (en) | 2001-02-14 | 2001-03-28 | Glaxo Group Ltd | Chemical compounds |
| US20030018019A1 (en) | 2001-06-23 | 2003-01-23 | Boehringer Ingelheim Pharma Kg | Pharmaceutical compositions based on anticholinergics, corticosteroids and betamimetics |
| US6653323B2 (en) | 2001-11-13 | 2003-11-25 | Theravance, Inc. | Aryl aniline β2 adrenergic receptor agonists |
| TWI249515B (en) | 2001-11-13 | 2006-02-21 | Theravance Inc | Aryl aniline beta2 adrenergic receptor agonists |
| JP2005529111A (ja) | 2002-04-12 | 2005-09-29 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | β模倣薬と新規な抗コリンエステラーゼ剤を含む薬剤 |
| EP1507754A1 (en) | 2002-05-28 | 2005-02-23 | Theravance, Inc. | Alkoxy aryl beta-2 adrenergic receptor agonists |
| GB0217225D0 (en) | 2002-07-25 | 2002-09-04 | Glaxo Group Ltd | Medicinal compounds |
| UY27927A1 (es) | 2002-08-06 | 2003-12-31 | Glaxo Group Ltd | Antagonistas del receptor muscarínico m3 de acetilcolina |
| PE20040950A1 (es) * | 2003-02-14 | 2005-01-01 | Theravance Inc | DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS |
| WO2004089892A2 (en) | 2003-04-01 | 2004-10-21 | Theravance, Inc. | Diarylmethyl and related compounds having beta2 andrenergic receptor agonist and muscarinic receptor antagonist activity |
| JP4616264B2 (ja) | 2003-05-28 | 2011-01-19 | セラヴァンス， インコーポレーテッド | ムスカリン性レセプターアンタゴニストとしてのアザビシクロアルカン化合物 |
| JP4851937B2 (ja) | 2003-11-21 | 2012-01-11 | セラヴァンス， インコーポレーテッド | β２アドレナリン作動性受容体作動薬活性およびムスカリン受容体拮抗薬活性を有する化合物 |
| US7320990B2 (en) | 2004-02-13 | 2008-01-22 | Theravance, Inc. | Crystalline form of a biphenyl compound |
| US7528253B2 (en) | 2004-08-16 | 2009-05-05 | Theravance, Inc. | Compounds having β2 adrenergic receptor agonist and muscarinic receptor antagonist activity |
| WO2006023460A2 (en) | 2004-08-16 | 2006-03-02 | Theravance, Inc. | COMPOUNDS HAVING β2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY |
| TWI374883B (en) | 2004-08-16 | 2012-10-21 | Theravance Inc | Crystalline form of a biphenyl compound |
-
2006
- 2006-02-10 GB GBGB0602778.3A patent/GB0602778D0/en not_active Ceased
-
2007
- 2007-02-08 US US11/672,536 patent/US7960551B2/en active Active
- 2007-02-08 BR BRPI0707559A patent/BRPI0707559B8/pt active IP Right Grant
- 2007-02-08 AU AU2007213767A patent/AU2007213767B2/en active Active
- 2007-02-08 PE PE2007000135A patent/PE20071249A1/es not_active Application Discontinuation
- 2007-02-08 WO PCT/EP2007/051196 patent/WO2007090859A1/en active Application Filing
- 2007-02-08 JP JP2008553758A patent/JP5616021B2/ja active Active
- 2007-02-08 EA EA200801691A patent/EA016580B1/ru unknown
- 2007-02-08 CN CN2007800050282A patent/CN101379057B/zh active Active
- 2007-02-08 PE PE2010000996A patent/PE20110120A1/es active IP Right Grant
- 2007-02-08 CA CA2641769A patent/CA2641769C/en active Active
- 2007-02-08 ES ES07704449.3T patent/ES2640226T3/es active Active
- 2007-02-08 SG SG201100933-9A patent/SG169404A1/en unknown
- 2007-02-08 JO JOP/2007/0037A patent/JO3389B1/ar active
- 2007-02-08 PT PT77044493T patent/PT1981872T/pt unknown
- 2007-02-08 PL PL07704449T patent/PL1981872T3/pl unknown
- 2007-02-08 SI SI200731963T patent/SI1981872T1/sl unknown
- 2007-02-08 TW TW096104636A patent/TWI401251B/zh active
- 2007-02-08 EP EP07704449.3A patent/EP1981872B1/en active Active
- 2007-02-08 LT LTEP07704449.3T patent/LT1981872T/lt unknown
- 2007-02-08 HU HUE07704449A patent/HUE034315T2/en unknown
- 2007-02-08 NZ NZ570242A patent/NZ570242A/en not_active IP Right Cessation
- 2007-02-08 AR ARP070100537A patent/AR059409A1/es not_active Application Discontinuation
- 2007-02-08 KR KR20087022160A patent/KR101488691B1/ko active IP Right Grant
- 2007-02-08 DK DK07704449.3T patent/DK1981872T3/en active
- 2007-08-02 UA UAA200809940A patent/UA100364C2/ru unknown
-
2008
- 2008-07-29 IL IL193103A patent/IL193103A/en active IP Right Grant
- 2008-08-05 NO NO20083425A patent/NO341343B1/no unknown
- 2008-08-05 ZA ZA200806782A patent/ZA200806782B/xx unknown
- 2008-08-08 MY MYPI20083025A patent/MY153656A/en unknown
- 2008-08-20 CR CR10227A patent/CR10227A/es not_active Application Discontinuation
- 2008-09-10 MA MA31228A patent/MA30273B1/fr unknown
-
2016
- 2016-04-15 AR ARP160101036A patent/AR104288A2/es not_active Application Discontinuation
-
2017
- 2017-08-22 CY CY20171100887T patent/CY1119238T1/el unknown
- 2017-08-30 HR HRP20171304TT patent/HRP20171304T1/hr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20171304T1 (hr) | Sol s jantarnom kiselinom 1-[2-(2-klor-4-{[(r)-2-hidroksi-2-(8-hidroksi-2-okso-1,2-dihidrokinolin-5-il)etilaminometil]}-5-metoksifenilkarbamoil)etil]piperidin-4-ilnog estera bifenil-2-ilkarbaminske kiseline i njezina upotreba u liječenju plućnih poremećaja | |
| JP2009526018A5 (hr) | ||
| HRP20130192T1 (hr) | Kristalni oblik bifenilnog spoja | |
| AU2019200171B2 (en) | Thiosaccharide mucolytic agents | |
| BR112017005104B1 (pt) | Derivados de 5,6-di-hidro-4h-benzotieno-[2,3-d]azepina, seus usos, composição farmacêutica e processo para a preparação dos mesmos | |
| HRP20171511T1 (hr) | Ivabradin-hidroklorid, oblik iv | |
| JP2013538857A5 (hr) | ||
| JP2012176975A5 (hr) | ||
| PL204002B1 (pl) | Lek zawierający kortykosteroid oraz zestaw | |
| NO333467B1 (no) | Farmasoytisk preparat og dets anvendelse | |
| JP2013504613A5 (hr) | ||
| PT2506844T (pt) | Combinações de um antagonista do recetor muscarínico e um agonista do adrenorrecetor beta-2 | |
| JP2011522895A (ja) | 治療において使用するためのβ−アゴニスト化合物と連結したコルチコステロイド | |
| CN106414458B (zh) | 新型稠合咪唑并苯并噻唑化合物 | |
| TW201217338A (en) | Crystalline oxalate salts of a diamide compound | |
| JP2005537278A (ja) | 抗炎症性または抗アレルギー性アンドロスタン複合体 | |
| US20050043284A1 (en) | Crystalline complexes of fluticasone-2-furoate | |
| WO2009019598A2 (en) | Inhalation therapy for respiratory disorders | |
| CN104797580A (zh) | 阿哌沙班的晶型或无定形及其制备工艺 | |
| US20240016786A1 (en) | Glucosidase inhibitors for the treatment and prevention of pulmonary infections | |
| JP5555255B2 (ja) | 呼吸器疾患の治療のためのスルホンアミド化合物 | |
| CN103382179A (zh) | 英加韦林的多晶型物及其制备方法 | |
| JP2007533706A5 (hr) | ||
| HRP20210260T1 (hr) | Vodeni sastavi koji sadrže bilastin i mometazon | |
| WO2015000370A1 (zh) | 吡咯喹啉醌锂盐晶体及其制备方法和应用 |