HRP20200276T1 - Stimulatori sgc - Google Patents

Stimulatori sgc Download PDF

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HRP20200276T1
HRP20200276T1 HRP20200276TT HRP20200276T HRP20200276T1 HR P20200276 T1 HRP20200276 T1 HR P20200276T1 HR P20200276T T HRP20200276T T HR P20200276TT HR P20200276 T HRP20200276 T HR P20200276T HR P20200276 T1 HRP20200276 T1 HR P20200276T1
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Croatia
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disease
pulmonary
hypertension
pharmaceutically acceptable
acceptable salt
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HRP20200276TT
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Takashi Nakai
Joel Moore
Nicholas Robert Perl
Rajesh R. Iyengar
Ara Mermerian
G-Yoon Jamie Im
Thomas Wai-Ho Lee
Colleen Hudson
Glen Robert RENNIE
James Jia
Paul Allen RENHOWE
Timothy Claude Barden
Xiang Y Yu
James Edward SHEPPECK
Karthik Iyer
Joon Jung
George Todd MILNE
Kimberly Kafadar LONG
Mark G. Currie
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Cyclerion Therapeutics, Inc.
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Publication of HRP20200276T1 publication Critical patent/HRP20200276T1/hr

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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • 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
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Claims (21)

1. Spoj predstavljen sljedećom formulom ili njegova farmaceutski prihvatljiva sol: [image]
2. Farmaceutski sastav koji sadrži spoj iz zahtjeva 1 ili njegovu farmaceutski prihvatljivu sol te jednu pomoćnu tvari ili više njih.
3. Spoj iz zahtjeva 1 ili njegova farmaceutski prihvatljiva sol, za upotrebu u liječenju bolesti, zdravstvenog stanja ili poremećaja odabranog među: (1) perifernim, plućnim, jetrenim, bubrežnim, srčanim ili cerebralnim vaskularnim / endotelnim poremećajima/stanjima ili bolestima na drugi način povezanima s cirkulacijom i odabranima među: • poremećajima povezanima s visokim krvnim tlakom i smanjenim protokom koronarne krvi; povišenim akutnim i kroničnim koronarnim krvnim tlakom; arterijskom hipertenzijom; vaskularnim poremećajem koji je posljedica srčanih i bubrežnih komplikacija, srčanih bolesti, moždanog udara, cerebralne ishemije ili zatajenja bubrega; rezistentnom hipertenzijom; dijabetičkom hipertenzijom; zatajenjem srca; kongestivnim zatajenjem srca; dijastoličkom ili sistoličkom disfunkcijom; koronarnom insuficijencijom; aritmijama; smanjenjem ventrikularnog predopterećenja; srčanom hipertrofijom; zatajenjem srca / kardiorenalnim sindromom; portalnom hipertenzijom; endotelnom disfunkcijom ili ozljedom; • tromboemboličkim poremećajima i ishemijama; infarktom miokarda; moždanim udarom; prolaznim ishemijskim napadima (TIA); opstruktivnim tromboanginitisom; stabilnom ili nestabilnom anginom pektoris; koronarnim grčevima; varijantnom anginom; Prinzmetalovom anginom; restenozom koja je posljedica terapija trombolizom; trombogenim poremećajima; • Alzheimerovom bolesti; Parkinsonovom bolesti; demencijom; vaskularnim kognitivnim oštećenjem; cerebralnim vazospazmom; traumatičnom ozljedom mozga; • perifernom arterijskom bolesti; perifernom okluzivnom arterijskom bolesti; perifernom vaskularnom bolesti; hipertonijama; Raynaudovim sindromom ili fenomenom; kritičnom ishemijom ekstremiteta; vaskulitisom; perifernom embolijom; povremenim klaudiranjem; vazookluzivnom krizom; Ducheneovom mišićnom distrofijom; Beckerovom mišićnom distrofijom; abnormalnostima mikrocirkulacije; vaskularnim curenjem ili problemima s propusnosti; • šokom; sepsom; kardiogenim šokom; kontrolom aktivacije leukocita; inhibicijom ili modulacijom agregacije trombocita; • plućnim/respiratornom stanjima; plućnom hipertenzijom; plućnom arterijskom hipertenzijom i povezanom plućnom vaskularnom pregradnjom; lokaliziranom trombozom i hipertrofijom desnog dijela srca; plućnom hipertonijom; primarnom plućnom hipertenzijom; sekundarnom plućnom hipertenzijom; obiteljskom plućnom hipertenzijom; sporadičnom plućnom hipertenzijom, prekapilarnom plućnom hipertenzijom; idiopatskom plućnom hipertenzijom; trombotskom plućnom arteriopatijom; pleksogenom plućnom arteriopatijom; cističnom fibrozom; bronhokonstrikcijom ili plućnom bronhokonstrikcijom; akutnim respiratornim distres sindromom; plućnom fibrozom; transplantacijom pluća; • plućnom hipertenzijom povezanom s disfunkcijom lijeve klijetke, hipoksemijom, hipertenzijama skupine I, II, III, IV i V SZO-a, bolestima mitralnog zaliska, konstriktivnim perikarditisom, aortnom stenozom, kardiomiopatijom, medijastinalnom fibrozom, plućnom fibrozom, anomalnom plućnom venskom drenažom, plućnom venookluzivnom bolesti, plućnim vaskulitisom, vaskularnom bolesti kolagena, kongenitalnom bolesti srca, plućnom venskom hipertenzijom, intersticijskom bolesti pluća, poremećajem disanja tijekom spavanja, apnejom za vrijeme spavanja, poremećajima alveolarne hipoventilacije, kroničnom izloženosti velikoj nadmorskoj visini, neonatalnom bolesti pluća, alveolarno-kapilarnom displazijom, bolesti srpastih stanica; poremećajima koagulacije; kroničnom tromboembolijom, plućnom embolijom zbog tumora, parazita ili stranog materijala, bolesti vezivnog tkiva, lupusom, šistosomijazom, sarkoidozom, kroničnom opstruktivnom bolesti pluća, astmom, emfizemom, kroničnim bronhitisom, hemangiomatozom plućne kapilare; histiocitozom X, limfangiomatozom i komprimiranim plućnim žilama zbog adenopatije, tumorom ili fibrozirajućim medijastinitisom; • aterosklerotskim bolestima ili stanjima; aterosklerozom; aterosklerozom povezanom s endotelnom ozljedom, adhezijom i agregacijom trombocita i monocita, proliferacijom i migracijom glatkih mišića; restenozom; restenozom razvijenom nakon terapije trombolizom, perkutanih transluminalnih angioplastika (PTA), perkutanih transluminalnih koronarnih angioplastika (PTCA) i premosnice; upalom; • kardiovaskularnom bolesti povezanom s metaboličkim sindromom, pretilošću, dislipidemijom, dijabetesom, visokim krvnim tlakom; poremećajima povezanima s lipidima kao što su dislipidemija, hiperkolesterolemija, hipertrigliceridemija, sitosterolemija, masna bolest jetre i hepatitis; preeklampsijom; napredovanjem policistične bolesti bubrega; nakupljanjem potkožnog masnog tkiva; • cirozom jetre; cirozom jetre povezanom s kroničnom bolesti jetre; hepatičnom fibrozom, aktivacijom jetrenih zvjezdanih stanica, fibroznim kolagenom jetre; ukupnom akumulacijom kolagena; bolesti jetro nekro-upalnog i/ili imunološkog porijekla; • poremećajima urogenitalnog sustava; bubrežnom fibrozom; kroničnom bolesti bubrega; zatajenjem bubrega koje je posljedica kroničnih bubrežnih bolesti ili insuficijencije; zatajenjem bubrega zbog akumulacije/taloženja i ozljede tkiva, progresivnom sklerozom i glomerulonefritisom; hipertrofijom prostate; • sistemskom sklerozom; • srčanom intersticijskom fibrozom; srčanom pregradnjom i fibrozom; srčanom hipertrofijom; (2) ishemijom, reperfuzijskim oštećenjem; ishemijom/reperfuzijom povezanom s transplantacijom organa, transplantacijom pluća, plućnom transplantacijom ili srčanom transplantacijom; očuvanjem nadomjestaka krvi u bolesnika s traumom; (3) seksualnim, ginekološkim i urološkim poremećajima odabranim među erektilnom disfunkcijom; impotencijom; preuranjenom ejakulacijom; ženskom seksualnom disfunkcijom; disfunkcijom ženskog seksualnog uzbuđenja; hipoaktivnim poremećajem seksualnog uzbuđenja; vaginalnom atrofijom; dispareunijom; atrofičnim vaginitisom; benignom hiperplazijom prostate (BPP) ili hipertrofijom ili povećanjem; opstrukcijom izlaza mjehura; sindromom bolnog mjehura (BPS); intersticijskim cistitisom (IC); preaktivnim mjehurom, neurogenim mjehurom i inkontinencijom; dijabetičkom nefropatijom; (4) očnim bolestima ili poremećajima odabrani među glaukomom, retinopatijom, dijabetičkom retinopatijom, blefaritisom, sindromom suhog oka, Sjögrenovim sindromom; (5) bolestima ili poremećajima sluha odabrani među oštećenjima sluha; djelomičnim ili potpunim gubitkom sluha; djelomičnom ili potpunom gluhoćom; zujanjem u ušima; gubitkom sluha uzrokovano bukom; (6) topičkim ili kožnim poremećajima ili stanjima odabranim među dermalnom fibrozom, sklerodermijom, fibrozom kože; (7) zacjeljivanjem rana; zacjeljivanjem rana u dijabetičara; poboljšanjem mikrovaskularne perfuzije; poboljšanjem mikrovaskularne perfuzije nakon ozljede kako bi se suzbio upalni odgovor u perioperativnoj njezi; analnim fisurama; dijabetičkim ulkusima; i (8) drugim bolestima ili stanjima odabranim među metastazom raka; osteoporozom, gastroparezom; funkcionalnom dispepsijom; dijabetičkim komplikacijama; bolestima povezanima s endotelnom disfunkcijom; i neurološkim poremećajima povezanima sa smanjenom proizvodnjom dušičnog oksida.
4. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj infarkt miokarda, stabilna ili nestabilna angina pektoris; koronarni grčevi; varijantna angina ili Prinzmetalova angina.
5. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj odabran među arterijskom hipertenzijom, plućnom hipertenzijom, plućnom arterijskom hipertenzijom, rezistentnom hipertenzijom, dijabetičkom hipertenzijom i portalnom hipertenzijom.
6. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj odabran među bubrežnom fibrozom, zatajenjem bubrega koje je posljedica kroničnih bubrežnih bolesti ili insuficijencije, kroničnom bolesti bubrega, zatajenjem bubrega zbog akumulacije/taloženja i ozljede tkiva, progresivnom sklerozom i glomerulonefritisom i napredovanjem policistične bolesti bubrega.
7. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj dijabetička nefropatija.
8. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj retinopatija ili dijabetička retinopatija.
9. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj odabran među zatajenjem srca, kongestivnim zatajenjem srca, hipertrofijom desnog dijela srca, dijastoličkom disfunkcijom, sistoličkom disfunkcijom, zatajenjem srca / kardiorenalnim sindromom, koronarnom insuficijencijom, aritmijama, smanjenjem ventrikularnog predopterećenja i srčanom hipertrofijom.
10. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 9, pri čemu je bolest zatajenje srca.
11. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 9, pri čemu je bolest dijastolička disfunkcija.
12. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 9, pri čemu je bolest zatajenje srca / kardiorenalni sindrom.
13. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 9, pri čemu je bolest srčana hipertrofija.
14. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 6, pri čemu je bolest bubrežna fibroza.
15. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 4, pri čemu je bolest zatajenje bubrega zbog akumulacije/taloženja i ozljede tkiva, progresivna skleroza, glomerulonefritis i napredovanje policistične bolesti bubrega.
16. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj vazookluzivna kriza.
17. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu se bolest, zdravstveno stanje ili poremećaj odabire među plućnim/respiratornom stanjima; plućnom hipertenzijom; plućnom arterijskom hipertenzijom i povezanom plućnom vaskularnom pregradnjom; lokaliziranom trombozom i hipertrofijom desnog dijela srca; plućnom hipertonijom; primarnom plućnom hipertenzijom; sekundarnom plućnom hipertenzijom; obiteljskom plućnom hipertenzijom; sporadičnom plućnom hipertenzijom, prekapilarnom plućnom hipertenzijom; idiopatskom plućnom hipertenzijom; trombotskom plućnom arteriopatijom; pleksogenom plućnom arteriopatijom; cističnom fibrozom; bronhokonstrikcijom ili plućnom bronhokonstrikcijom; akutnim respiratornim distres sindromom; plućnom fibrozom; i transplantacijom pluća.
18. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu se bolest, zdravstveno stanje ili poremećaj odabire među plućnom hipertenzijom povezanom s disfunkcijom lijeve klijetke, hipoksemijom, hipertenzijama skupine I, II, III, IV i V SZO-a, bolestima mitralnog zaliska, konstriktivnim perikarditisom, aortnom stenozom, kardiomiopatijom, medijastinalnom fibrozom, plućnom fibrozom, anomalnom plućnom venskom drenažom, plućnom venookluzivnom bolesti, plućnim vaskulitisom, vaskularnom bolesti kolagena, kongenitalnom bolesti srca, plućnom venskom hipertenzijom, intersticijskom bolesti pluća, poremećajem disanja tijekom spavanja, apnejom za vrijeme spavanja, poremećajima alveolarne hipoventilacije, kroničnom izloženosti velikoj nadmorskoj visini, neonatalnom bolesti pluća, alveolarno-kapilarnom displazijom, bolesti srpastih stanica; poremećajima koagulacije; kroničnom tromboembolijom, plućnom embolijom zbog tumora, parazita ili stranog materijala, bolesti vezivnog tkiva, lupusom, šistosomijazom, sarkoidozom, kroničnom opstruktivnom bolesti pluća, astmom, emfizemom, kroničnim bronhitisom, hemangiomatozom plućne kapilare; histiocitozom X, limfangiomatozom i komprimiranim plućnim žilama zbog adenopatije, tumorom ili fibrozirajućim medijastinitisom.
19. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu je bolest, zdravstveno stanje ili poremećaj kardiovaskularna bolest povezana s metaboličkim sindromom, pretilost, dislipidemija, dijabetes, visoki krvni tlak; poremećaji povezani s lipidima, dislipidemija, hiperkolesterolemija, hipertrigliceridemija, sitosterolemija, masna bolest jetre i hepatitis; preeklampsija; ili nakupljanje potkožnog masnog tkiva.
20. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu se bolest, zdravstveno stanje ili poremećaj odabire među cirozom jetre; cirozom jetre povezanom s kroničnom bolesti jetre; hepatičnom fibrozom, aktivacijom jetrenih zvjezdanih stanica i fibroznim kolagenom jetre.
21. Spoj ili farmaceutski prihvatljiva sol za uporabu u skladu sa zahtjevom 3, pri čemu se bolest, zdravstveno stanje ili poremećaj odabire među srčanom intersticijskom fibrozom, srčanom pregradnjom i fibrozom.
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