HRP20200429T1 - 3,5-diamino-6-kloro-n-(n-(4-(4-(2-(heksil(2,3,4,5,6-penta-hidroksiheksil)amino)etoksi)fenil)butil)karbamimidoil)pirazin-2-karboksamid - Google Patents
3,5-diamino-6-kloro-n-(n-(4-(4-(2-(heksil(2,3,4,5,6-penta-hidroksiheksil)amino)etoksi)fenil)butil)karbamimidoil)pirazin-2-karboksamid Download PDFInfo
- Publication number
- HRP20200429T1 HRP20200429T1 HRP20200429TT HRP20200429T HRP20200429T1 HR P20200429 T1 HRP20200429 T1 HR P20200429T1 HR P20200429T T HRP20200429T T HR P20200429TT HR P20200429 T HRP20200429 T HR P20200429T HR P20200429 T1 HRP20200429 T1 HR P20200429T1
- Authority
- HR
- Croatia
- Prior art keywords
- pharmaceutical composition
- composition according
- cftr modulator
- carboxamide
- treatment
- Prior art date
Links
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 title 1
- IPEHBUMCGVEMRF-UHFFFAOYSA-N pyrazinecarboxamide Chemical compound NC(=O)C1=CN=CC=N1 IPEHBUMCGVEMRF-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 5
- 239000000819 hypertonic solution Substances 0.000 claims 5
- 229940021223 hypertonic solution Drugs 0.000 claims 5
- PURKAOJPTOLRMP-UHFFFAOYSA-N ivacaftor Chemical group C1=C(O)C(C(C)(C)C)=CC(C(C)(C)C)=C1NC(=O)C1=CNC2=CC=CC=C2C1=O PURKAOJPTOLRMP-UHFFFAOYSA-N 0.000 claims 5
- UFSKUSARDNFIRC-UHFFFAOYSA-N lumacaftor Chemical compound N1=C(C=2C=C(C=CC=2)C(O)=O)C(C)=CC=C1NC(=O)C1(C=2C=C3OC(F)(F)OC3=CC=2)CC1 UFSKUSARDNFIRC-UHFFFAOYSA-N 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 238000012387 aerosolization Methods 0.000 claims 3
- 230000036571 hydration Effects 0.000 claims 3
- 238000006703 hydration reaction Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 208000025678 Ciliary Motility disease Diseases 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 201000009267 bronchiectasis Diseases 0.000 claims 2
- 206010006451 bronchitis Diseases 0.000 claims 2
- 206010013781 dry mouth Diseases 0.000 claims 2
- 229940112141 dry powder inhaler Drugs 0.000 claims 2
- 229940071648 metered dose inhaler Drugs 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000000065 osmolyte Effects 0.000 claims 2
- 201000009266 primary ciliary dyskinesia Diseases 0.000 claims 2
- 201000009890 sinusitis Diseases 0.000 claims 2
- 239000000243 solution Substances 0.000 claims 2
- 208000000884 Airway Obstruction Diseases 0.000 claims 1
- 239000005711 Benzoic acid Substances 0.000 claims 1
- 206010006448 Bronchiolitis Diseases 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 206010011224 Cough Diseases 0.000 claims 1
- 208000005156 Dehydration Diseases 0.000 claims 1
- 206010056361 Distal intestinal obstruction syndrome Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013786 Dry skin Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010030216 Oesophagitis Diseases 0.000 claims 1
- 206010033078 Otitis media Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010044314 Tracheobronchitis Diseases 0.000 claims 1
- 208000009470 Ventilator-Associated Pneumonia Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 208000005946 Xerostomia Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 235000010233 benzoic acid Nutrition 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 230000018044 dehydration Effects 0.000 claims 1
- 238000006297 dehydration reaction Methods 0.000 claims 1
- 208000007784 diverticulitis Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000037336 dry skin Effects 0.000 claims 1
- 210000000959 ear middle Anatomy 0.000 claims 1
- 208000006881 esophagitis Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002427 irreversible effect Effects 0.000 claims 1
- 230000000420 mucociliary effect Effects 0.000 claims 1
- 239000006199 nebulizer Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000001737 promoting effect Effects 0.000 claims 1
- 230000002441 reversible effect Effects 0.000 claims 1
- 239000012266 salt solution Substances 0.000 claims 1
- 210000001215 vagina Anatomy 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- A61K31/495—Heterocyclic 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
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- 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
-
- 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
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
- C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
- C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
- C07D241/34—(Amino-pyrazine carbonamido) guanidines
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Toxicology (AREA)
- Ophthalmology & Optometry (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
Claims (32)
1. Farmaceutski sastav koji sadrži spoj formule (I):
[image]
ili njegovu farmaceutski prihvatljivu sol i osmolit.
2. Farmaceutski sastav prema patentnom zahtjevu 1, gdje je spoj formule (I) spoj formule (Ia) :
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Farmaceutski sastav prema patentnom zahtjevu 1 ili 2, gdje je osmolit hipertonična otopina.
4. Farmaceutski sastav prema zahtjevu 3, koji sadrži spoj formule (Ia)
[image]
ili njegovu farmaceutski prihvatljivu sol i hipertoničnu otopinu.
5. Farmaceutski sastav prema zahtjevu 4, koji sadrži spoj formule (Ia)
[image]
i hipertoničnu otopinu.
6. Farmaceutski sastav prema zahtjevu 3, 4 ili 5, gdje hipertonična otopina ima koncentraciju 4%-5% mas/v.
7. Farmaceutski sastav prema zahtjevu 3, 4 ili 5, gdje hipertonična otopina ima koncentraciju oko 4%.
8. Farmaceutski sastav prema bilo kojem od zahtjeva 1-7, dalje sadrži CFTR modulator.
9. Farmaceutski sastav prema zahtjevu 8, gdje je CFTR modulator N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksokinolin-3-karboksamid.
10. Farmaceutski sastav prema zahtjevu 8, gdje je CFTR modulator (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina.
11. Farmaceutski sastav prema zahtjevu 8, gdje je CFTR modulator N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksokinolin-3-karboksamid i (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina.
12. Farmaceutski sastav prema bilo kojem od zahtjeva 1-11, gdje je sastav pogodan za inhalaciju.
13. Farmaceutski sastav prema bilo kojem od zahtjeva 1-11, gdje je sastav otopina za aerosolizaciju i davanje pomoću inhalatora.
14. Farmaceutski sastav prema bilo kojem od zahtjeva 1-11, gdje je sastav otopina za primjenu putem inhalatora s odmjeravanjem doze.
15. Farmaceutski sastav prema zahtjevu 1 ili zahtjevu 2, gdje je sastav suhi prah pogodan za primjenu putem inhalatora sa suhim prahom.
16. Farmaceutski sastav prema bilo kojem od zahtjeva 1-15, za upotrebu u postupku poboljšavanja hidratacije površina sluznica i/ili poboljšavanja mukocilijarnog klirensa kod ljudi.
17. Farmaceutski sastav prema bilo kojem od zahtjeva 1-15 za upotrebu kao lijek.
18. Farmaceutski sastav prema bilo kojem od zahtjeva 1-15 za upotrebu u postupku liječenja reverzibilne ili ireverzibilne opstrukcije dišnih puteva, kronične opstruktivne bolesti pluća (COPD), astme, bronhiektazije, akutnog bronhitisa, kroničnog bronhitisa, kašlja nakon virusne infekcije, cistične fibroze, emfizema, upale pluća, panbronhiolitisa, bronhiolitisa koji se dovodi u vezu s transplantacijom i traheobronhitisa koji se dovodi u vezu s upotrebom respiratora, ili u prevenciji upale pluća koja se dovodi u vezu s upotrebom respiratora kod čovjeka kojem je to potrebno.
19. Farmaceutski sastav prema bilo kojem od zahtjeva 1-15 za upotrebu u postupku liječenja suhoće usne šupljine (kserostomije), suhoće kože, suhoće vagine, sinusitisa, rinosinusitisa, nazalne dehidratacije, suhoće oka ili Sjogrenove bolesti, promoviranja očne hidratacije ili hidratacije rožnice, tretmana sindroma distalne crijevne opstrukcije, otitis media (upale srednjeg uha), primarne cilijarne diskinezije, ezofagitisa, zatvora ili kroničnog divertikulitisa kod čovjeka kojem je to potrebno.
20. Farmaceutski sastav za upotrebu prema zahtjevu 18, gdje je upotreba u liječenju cistične fibroze.
21. Farmaceutski sastav za upotrebu prema zahtjevu 18, gdje je upotreba u liječenju kronične opstruktivne bolesti pluća (COPD).
22. Farmaceutski sastav za upotrebu prema zahtjevu 19, gdje je upotreba u liječenju primarne cilijarne diskinezije.
23. Farmaceutski sastav za upotrebu prema zahtjevu 19, gdje je upotreba u liječenju bronhiektazije.
24. Farmaceutski sastav za upotrebu prema bilo kojem od zahtjeva 16, ili 18-23, gdje postupak obuhvaća davanje efikasne količine farmaceutskog sastava prema bilo kojem od zahtjeva 1-15 i CFTR modulatora.
25. Farmaceutski sastav za upotrebu prema zahtjevu 24, gdje je CFTR modulator N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksokinolin-3-karboksamid.
26. Farmaceutski sastav za upotrebu prema zahtjevu 24, gdje je CFTR modulator (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina.
27. Farmaceutski sastav za upotrebu prema zahtjevu 24, gdje je CFTR modulator N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksokinolin-3-karboksamid i (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeva kiselina.
28. Farmaceutski sastav za upotrebu prema bilo kojem od zahtjeva 24-27, gdje farmaceutski sastav prema bilo kojem od zahtjeva 1-15 i CFTR modulator su davani zajedno ili uzastopno u bilo kojoj terapeutski prikladnoj kombinaciji.
29. Pribor koji sadrži farmaceutski sastav prema bilo kojem od zahtjeva 1-15; uređaj za aerosolizaciju izabran između raspršivača, inhalatora suhog praha i inhalatora za odmjeravanje doze; upute za davanje farmaceutskog sastava; i spremnik.
30. Pribor prema zahtjevu 29, dalje sadrži farmaceutski sastav koji sadrži N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksokinolin-3-karboksamid, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il)benzojeve kiseline ili kombinaciju oba.
31. Pribor prema zahtjevu 30, gdje su farmaceutski sastavi u odvojenim spremnicima.
32. Pribor prema zahtjevu 31, gdje je spremnik boca, bočica, blister pakiranja ili njihova kombinacija, s bar jednim spremnikom pogodnim za upotrebu u uređaju za aerosolizaciju.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161501687P | 2011-06-27 | 2011-06-27 | |
US201261635745P | 2012-04-19 | 2012-04-19 | |
EP15184092.3A EP3034497B1 (en) | 2011-06-27 | 2012-06-26 | 3,5-diamino-6-chloro-n-(n-(4-(4-(2-(hexyl(2,3,4,5,6-penta-hydroxyhexyl)amino)ethoxy)phenyl)butyl) carbamimidoyl)pyrazine-2-carboxamide |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20200429T1 true HRP20200429T1 (hr) | 2020-06-12 |
Family
ID=46466941
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20151346TT HRP20151346T1 (hr) | 2011-06-27 | 2015-12-08 | 3,5-diamino-6-klor-n-(n-(4-(4-(2-(heksil(2,3,4,5,6-pentahidroksiheksil)amino)etoksi)fenil)butil)karbamimidoil)pirazin-2-karboksamid |
HRP20200429TT HRP20200429T1 (hr) | 2011-06-27 | 2020-03-16 | 3,5-diamino-6-kloro-n-(n-(4-(4-(2-(heksil(2,3,4,5,6-penta-hidroksiheksil)amino)etoksi)fenil)butil)karbamimidoil)pirazin-2-karboksamid |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20151346TT HRP20151346T1 (hr) | 2011-06-27 | 2015-12-08 | 3,5-diamino-6-klor-n-(n-(4-(4-(2-(heksil(2,3,4,5,6-pentahidroksiheksil)amino)etoksi)fenil)butil)karbamimidoil)pirazin-2-karboksamid |
Country Status (37)
Country | Link |
---|---|
US (4) | US8669262B2 (hr) |
EP (3) | EP3693361A1 (hr) |
JP (6) | JP6010617B2 (hr) |
KR (1) | KR102120252B1 (hr) |
CN (2) | CN103764633B (hr) |
AP (1) | AP2014007464A0 (hr) |
AR (1) | AR086745A1 (hr) |
AU (4) | AU2012275502B2 (hr) |
BR (1) | BR112013033511B1 (hr) |
CA (1) | CA2838251C (hr) |
CL (1) | CL2013003759A1 (hr) |
CO (1) | CO6862155A2 (hr) |
CY (2) | CY1116994T1 (hr) |
DK (2) | DK3034497T3 (hr) |
EA (2) | EA023593B1 (hr) |
EC (1) | ECSP14013173A (hr) |
ES (2) | ES2778675T3 (hr) |
HK (1) | HK1226069A1 (hr) |
HR (2) | HRP20151346T1 (hr) |
HU (1) | HUE025856T2 (hr) |
IL (2) | IL229843A (hr) |
LT (1) | LT3034497T (hr) |
MA (1) | MA35608B1 (hr) |
MD (2) | MD20180023A2 (hr) |
MX (2) | MX349852B (hr) |
PE (1) | PE20140849A1 (hr) |
PL (2) | PL3034497T3 (hr) |
PT (2) | PT2723722E (hr) |
RS (2) | RS54445B1 (hr) |
SG (1) | SG10201605241PA (hr) |
SI (2) | SI2723722T1 (hr) |
SM (1) | SMT201600057B (hr) |
TW (3) | TW201730158A (hr) |
UA (1) | UA118169C2 (hr) |
UY (1) | UY34161A (hr) |
WO (1) | WO2013003386A1 (hr) |
ZA (1) | ZA201309337B (hr) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
US6858615B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
CA2810655C (en) | 2004-06-24 | 2013-12-10 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
BRPI0620960A2 (pt) | 2005-12-28 | 2011-11-29 | Vertex Pharmaceuticals Incorporated | formas sólidas de n-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-didro-4- oxiquinolina-3- carboxamida |
US8476442B2 (en) | 2009-03-20 | 2013-07-02 | Vertex Pharmaceutical Incorporated | Process for making modulators of cystic fibrosis transmembrane conductance regulator |
AR086745A1 (es) * | 2011-06-27 | 2014-01-22 | Parion Sciences Inc | 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida |
DK2723176T3 (en) | 2011-06-27 | 2017-07-31 | Parion Sciences Inc | CHEMICAL AND METABOLIC STABLE DIPEPTIDE WITH POTENT SODIUM CHANNEL BLOCK ACTIVITY |
LT2773633T (lt) | 2011-11-02 | 2017-11-10 | Boehringer Ingelheim International Gmbh | Heterocikliniai junginiai, vaistai, turintys minėtus junginius, jų panaudojimas ir jų gavimo būdai |
WO2013064451A1 (en) | 2011-11-02 | 2013-05-10 | Boehringer Ingelheim International Gmbh | Novel process for the preparation of acylguanidines and acylthioureas |
US8859559B2 (en) | 2011-12-20 | 2014-10-14 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
MX2014010253A (es) | 2012-02-27 | 2014-11-12 | Vertex Pharma | Composicion farmaceutica y administraciones de la misma. |
JP6204977B2 (ja) | 2012-05-25 | 2017-09-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 三級アミン、前記アミンを含む薬物、その使用及びその調製方法 |
JP6272312B2 (ja) | 2012-05-29 | 2018-01-31 | パリオン・サイエンシィズ・インコーポレーテッド | ドライアイおよび他の粘膜疾患の治療のためのナトリウムチャネル遮断活性を有するデンドリマー様アミノアミド |
US8841309B2 (en) | 2012-09-24 | 2014-09-23 | Boehringer Ingelheim International Gmbh | Substituted pyrazines and their use in the treatment of disease |
KR20150095870A (ko) | 2012-12-17 | 2015-08-21 | 패리온 사이언스 인코퍼레이티드 | 3,5-디아미노-6-클로로-n-(n-(4-페닐부틸)카르밤이미도일)피라진-2-카르복스아미드 화합물 |
MX2015007796A (es) * | 2012-12-17 | 2015-09-04 | Parion Sciences Inc | Derivados de cloro-pirazin carboxamida con actividad bloqueadora sobre los canales de sodio epiteliales. |
ES2674665T3 (es) * | 2012-12-17 | 2018-07-03 | Parion Sciences, Inc. | Compuestos de 3,5-diamino-6-cloro-N-(N-(4-fenilbutilo)carbamimidoilo)-pirazina-2-carboxamida |
MX368243B (es) | 2013-08-23 | 2019-09-25 | Parion Sciences Inc | Agentes mucolíticos de ditiol. |
US9102633B2 (en) | 2013-12-13 | 2015-08-11 | Parion Sciences, Inc. | Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds |
UY36034A (es) | 2014-03-18 | 2015-09-30 | Astrazeneca Ab | Derivados de 3,5-diamino-6-cloro-pirazina-2-carboxamida y sales farmaceuticamente aceptables de estos |
US20150376145A1 (en) | 2014-06-30 | 2015-12-31 | Parion Sciences, Inc. | Stable sodium channel blockers |
CN105588886B (zh) * | 2014-11-18 | 2020-01-31 | 重庆医药工业研究院有限责任公司 | 一种采用液相色谱法测定阿普斯特及其制剂中杂质的方法 |
CN107614480B (zh) * | 2015-01-30 | 2020-09-15 | 帕里昂科学公司 | 新型单硫醇粘液溶解剂 |
CN107708680A (zh) | 2015-04-30 | 2018-02-16 | 帕里昂科学公司 | 新的二硫醇粘液溶解剂的前药 |
GB201610854D0 (en) | 2016-06-21 | 2016-08-03 | Entpr Therapeutics Ltd | Compounds |
GB201619694D0 (en) | 2016-11-22 | 2017-01-04 | Entpr Therapeutics Ltd | Compounds |
GB201717051D0 (en) | 2017-10-17 | 2017-11-29 | Enterprise Therapeutics Ltd | Compounds |
IL277071B1 (en) | 2018-03-08 | 2024-03-01 | Incyte Corp | Aminopyrizine diol compounds as PI3K–y inhibitors |
EP3950057A4 (en) * | 2019-03-29 | 2022-12-28 | National University Corporation Kagawa University | OSMOTIC PRESSURE REGULATOR FOR PERITONEAL DIALYSATE WITH D-ALLOSE AND/OR D-ALLULOSE |
Family Cites Families (416)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3268406A (en) | 1961-10-12 | 1966-08-23 | Merck & Co Inc | Compositions and method of using (3-amino-pyrazinoyl) guanidines |
US3316266A (en) | 1964-03-31 | 1967-04-25 | Merck & Co Inc | 3-aminopyrazinoic acid derivatives and process for their preparation |
NL6409716A (hr) | 1962-10-30 | 1965-10-01 | ||
DK109779C (da) | 1962-10-30 | 1968-07-01 | Merck & Co Inc | Fremgangsmåde til fremstilling af 3-aminopyrazinamidoguanidinforbindelser eller syreadditionssalte heraf. |
NL299929A (hr) | 1962-10-30 | |||
NL6409714A (hr) | 1962-10-30 | 1965-10-01 | ||
NL299931A (hr) | 1962-10-30 | |||
US3274191A (en) | 1963-11-15 | 1966-09-20 | Merck & Co Inc | N-(3-aminopyrazinoyl) benzamidines and process for preparing |
US3240780A (en) | 1963-12-23 | 1966-03-15 | Merck & Co Inc | Amino-pyrazinoyl guanidines |
DE1245967B (de) | 1964-03-31 | 1967-08-03 | Merck &. Co., Inc., Rahway, N.J. (V. St. A.) | Verfahren zur Herstellung von S.S-Diamino-o-chlor-pyrazincarbonsäurealkylestern |
NL6501301A (hr) | 1964-04-03 | 1965-10-04 | ||
US3249610A (en) | 1964-09-08 | 1966-05-03 | Merck & Co Inc | Synthesis of 3-amino, 5-chloro, 6-substituted-pyrazinoates |
DE1281818B (de) | 1965-07-17 | 1968-10-31 | Rheinische Kalksteinwerke | Verfahren zum gleichzeitigen Mahlen mehrerer Rohstoffe unterschiedlicher Mahlbarkeit |
US3318813A (en) | 1965-08-16 | 1967-05-09 | Dow Chemical Co | Poly-alkylstyrene viscosity index improver |
US3274192A (en) | 1965-10-04 | 1966-09-20 | Merck & Co Inc | Derivatives of pyrazine and a method for their preparation |
US3341540A (en) | 1965-10-04 | 1967-09-12 | Merck & Co Inc | 3-amino-6-halopyrazinonitriles and their syntheses |
US3305552A (en) | 1965-11-22 | 1967-02-21 | Merck & Co Inc | 3-aminopyrazinoic acids and process for their preparation |
US3361748A (en) | 1965-11-22 | 1968-01-02 | Merck & Co Inc | Process for the preparation of pteridinones |
US3361306A (en) | 1966-03-31 | 1968-01-02 | Merck & Co Inc | Aerosol unit dispensing uniform amounts of a medically active ingredient |
NL6707564A (hr) | 1966-08-25 | 1968-02-26 | ||
IL27897A (en) | 1966-08-25 | 1972-02-29 | Merck & Co Inc | Preparation of pyrazinoalguanides and pyrazinoamidoguanidines |
FR1525670A (fr) | 1966-08-25 | 1968-05-17 | Merck & Co Inc | Procédé de fabrication de guanidines substituées |
FR1525671A (fr) | 1966-08-25 | 1968-05-17 | Merck & Co Inc | Procédé de préparation de (3, 5 - diamino - 6 - halogéno - pyrazinoyl) - guanidines et de (3, 5 - diamino - 6 - halogéno -pyrazinamido) guanidines |
US3660400A (en) | 1966-11-17 | 1972-05-02 | Merck & Co Inc | Lower alkyl 3-hydroxy and 3-mercaptopyrazinoates |
US3472848A (en) | 1966-11-17 | 1969-10-14 | Merck & Co Inc | 3-hydroxy and 3-mercapto-pyrazinoyl-guanidines,corresponding ethers and thioethers and processes for their preparation |
US3527758A (en) | 1967-04-13 | 1970-09-08 | Merck & Co Inc | Process for the preparation of pyrazinoylguanidines from a pyrazinoic azide and a guanidine |
US3507865A (en) | 1967-04-27 | 1970-04-21 | Merck & Co Inc | 3-hydroxy- and 3-mercaptopyrazinamidoguanidines the corresponding ethers and thioethers and processes for their preparation |
US3507866A (en) | 1967-08-08 | 1970-04-21 | Merck & Co Inc | 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation |
US3487082A (en) | 1967-09-28 | 1969-12-30 | Merck & Co Inc | 2,4 - diamino - 6 - halopteridines and processes for their preparation |
US3503973A (en) | 1967-11-07 | 1970-03-31 | Merck & Co Inc | Process for preparation of pyrazinoylguanidines |
US3515723A (en) | 1967-11-14 | 1970-06-02 | Merck & Co Inc | 2 - (5 - amino - 1h - 1,2,4 - triazol - 3 - yl)- 3-aminopyrazines and processes for their preparation |
US3531484A (en) | 1968-02-14 | 1970-09-29 | Merck & Co Inc | 1-(3-aminopyrazinoyl)-4,5,5-trisubstituted biguanide products |
US3461123A (en) | 1968-04-12 | 1969-08-12 | Merck & Co Inc | 1h-imidazo(4,5-b)pyrazin-2-ones and processes for their preparation |
US3506662A (en) | 1968-04-30 | 1970-04-14 | Merck & Co Inc | Process for preparation of pyrazinoyland pyrazinamidoguanidines |
US3625950A (en) | 1968-07-03 | 1971-12-07 | Merck & Co Inc | Certain halophenoxy alkanamides, hydrazides and derivatives thereof |
US3575975A (en) | 1968-07-25 | 1971-04-20 | Merck & Co Inc | Process for the preparation of 3-aminopyrazinoylureas |
US3539569A (en) | 1968-08-21 | 1970-11-10 | Merck & Co Inc | Preparation of pyrazinoylguanidines from pyrazinoylureas |
US3544571A (en) | 1968-09-04 | 1970-12-01 | Merck & Co Inc | Process for making pyrazinoylthiourea compounds |
US3555023A (en) | 1968-11-13 | 1971-01-12 | Merck & Co Inc | 1-(3 - aminopyrazinoyl) - 3 - substituted-3-thioisosemicarbazides and method for preparation |
US3555024A (en) | 1968-11-13 | 1971-01-12 | Merck & Co Inc | 1-(3-aminopyrazinoyl)semicarbazides,1-(3-aminopyrazinoyl) - thiosemicarbazides,and method for their preparation |
US3668241A (en) | 1968-11-25 | 1972-06-06 | Merck & Co Inc | Substituted 1-oxoinden-5-yloxy alkanoic acids |
US3586688A (en) | 1968-12-18 | 1971-06-22 | Merck & Co Inc | Certain aminopyridinecarbonyl guanidines |
US3573305A (en) | 1968-12-30 | 1971-03-30 | Merck & Co Inc | (3-amino-pyrazinoyl)sulfamides and their preparation |
US3577418A (en) | 1969-02-12 | 1971-05-04 | Merck & Co Inc | Pyrazinamide derivatives and processes for their preparation |
US3565070A (en) | 1969-02-28 | 1971-02-23 | Riker Laboratories Inc | Inhalation actuable aerosol dispenser |
US3573306A (en) | 1969-03-05 | 1971-03-30 | Merck & Co Inc | Process for preparation of n-substituted 3,5-diamino-6-halopyrazinamides |
US3544568A (en) | 1969-03-18 | 1970-12-01 | Merck & Co Inc | 3-amino-5,6-substituted pyrazinamides |
US3660397A (en) | 1970-04-17 | 1972-05-02 | Merck & Co Inc | Imidazo(4 5-b)pyrazines |
US3864401A (en) | 1970-12-23 | 1975-02-04 | Merck & Co Inc | Substituted 2-aminomethyl-4,6-dihalophenols |
US3794734A (en) | 1971-03-03 | 1974-02-26 | Merck & Co Inc | Methods of treating edema and hypertension using certain 2-aminoethylphenols |
US3935313A (en) | 1971-03-29 | 1976-01-27 | Jan Marcel Didier Aron-Samuel | Pharmaceutical composition containing N-(3-diethyl-aminopropyl)-4-nitro-1-oxide-pyridine-2-carboxamide and process for the treatment of hypertension therewith |
US3948895A (en) | 1971-09-28 | 1976-04-06 | E. I. Du Pont De Nemours And Company | Synthesis of 3,5-diaminopyrazinoic acid from 3,5-diamino-2,6-dicyanopyrazine and intermediates |
BE791201A (fr) | 1971-11-12 | 1973-05-10 | Merck & Co Inc | Indanyloxytetrazoles |
US3953476A (en) | 1971-12-27 | 1976-04-27 | Merck & Co., Inc. | 3-Amino-5-sulfonylbenzoic acids |
US3894085A (en) | 1972-09-19 | 1975-07-08 | Ciba Geigy Corp | New 2-halo nitrones, their manufacture and their use for the manufacture of N-substituted araliphatic aldehyde-nitrones |
US4085219A (en) | 1972-10-13 | 1978-04-18 | Merck & Co., Inc. | 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids |
US4081554A (en) | 1972-10-13 | 1978-03-28 | Merck & Co., Inc. | 1-oxo-2,2-disubstituted-5-indanyloxy(or thio)alkano acids |
US3976686A (en) | 1972-10-13 | 1976-08-24 | Merck & Co., Inc. | [1-Oxo-2,3-hydrocarbylene-5-indanyloxy(or thio)]alkanoic acids |
US3984465A (en) | 1972-10-13 | 1976-10-05 | Merck & Co., Inc. | 1-Oxo-2,2-disubstituted-5-indanyloxy(or thio)alkanoic acids |
US4091015A (en) | 1972-10-27 | 1978-05-23 | American Home Products Corporation | 15-Substituted prostanoic acids |
US4066692A (en) | 1972-10-30 | 1978-01-03 | Merck & Co., Inc. | 11,12-secoprostaglandins |
US4092356A (en) | 1972-10-30 | 1978-05-30 | Merck & Co., Inc. | 11,12-Secoprostaglandins |
US4055597A (en) | 1973-01-26 | 1977-10-25 | Merck & Co., Inc. | 10-Aza-11,12-secoprostaglandins |
US3987091A (en) | 1973-04-12 | 1976-10-19 | Merck & Co., Inc. | 11,12-secoprostaglandins |
US4091107A (en) | 1973-04-25 | 1978-05-23 | Merck & Co., Inc. | 8-Aza-9-oxo(and dioxo)-thia-11,12-secoprostaglandins |
US4033996A (en) | 1973-04-25 | 1977-07-05 | Merck & Co., Inc. | 8-Aza-9-oxo(and dioxo)-thia-11,12-secoprostaglandins |
US3894065A (en) | 1973-04-27 | 1975-07-08 | Merck & Co Inc | Aryl-oxo-alkanoic acids |
US4182764A (en) | 1973-10-11 | 1980-01-08 | Merck & Co., Inc. | Tetrazole derivatives of [1-oxo-2-aryl or thienyl-2-substituted-5-indanyloxy(or thio)]alkanoic acids |
US4177285A (en) | 1973-10-11 | 1979-12-04 | Merck & Co., Inc. | [1-Oxo-2-thienyl-2-substituted-5-indanyloxy (or thio)]alkanoic acids and derivatives thereof |
US4003927A (en) | 1973-10-12 | 1977-01-18 | Merck & Co., Inc. | (1-Oxo-7,8-disubstituted-1,2,3,4-tetrahydro-6-naphthyloxy)- and (3,4-disubstituted-5-oxo-6,7,8,9-tetrahydro-5H-benzocycloheptene-2-yloxy) acetic acids and derivatives |
US3966966A (en) | 1973-10-12 | 1976-06-29 | Merck & Co., Inc. | Pharmaceutical compositions and method of treatment employing 1,3-dioxo-2,2-disubstituted indanyloxy alkanoic acids |
US3929872A (en) | 1973-10-12 | 1975-12-30 | Merck & Co Inc | Indanacetic acid compounds |
US3976681A (en) | 1973-10-12 | 1976-08-24 | Merck & Co., Inc. | [1,3-Dioxo-2-substituted and 2,2-disubstituted- indanyloxy (or thio] alkanoic acids |
US4006180A (en) | 1973-10-12 | 1977-02-01 | Merck & Co., Inc. | [1,3-Dihydroxy-2-substituted and 2,2-disubstituted-indanyloxy(or thio)]alkanoic acids |
US4012524A (en) | 1973-10-12 | 1977-03-15 | Merck & Co., Inc. | [1-Hydroxy-5-indanyloxy (or thio)]-alkanoic acids |
US3989749A (en) | 1973-10-17 | 1976-11-02 | Merck & Co., Inc. | 11,12-Secoprostaglandins |
US3991087A (en) | 1973-12-13 | 1976-11-09 | Merck & Co., Inc. | 8-Halo-11,12-secoprostaglandins |
US3979361A (en) | 1974-02-20 | 1976-09-07 | Merck & Co., Inc. | 2-Aminomethyl-6-trihalo-methylphenols |
US3914253A (en) | 1974-03-04 | 1975-10-21 | Merck & Co Inc | 5-Oxo-6-substituted-cyclopent-{8 f{9 -indole-2-carboxylic acids |
US3931239A (en) | 1974-04-03 | 1976-01-06 | Merck & Co., Inc. | 6-Oxo-7-substituted-6H-indeno-[5,4-b]furan(and thiophene)-carboxylic acids |
US3958004A (en) | 1974-04-23 | 1976-05-18 | Merck & Co., Inc. | Phenoxyacetic acid derivatives as uricosuric agents |
US3928624A (en) | 1974-04-25 | 1975-12-23 | Merck & Co Inc | Phenol compounds in treating pain, fever and inflammation |
US3956374A (en) | 1974-05-03 | 1976-05-11 | Merck & Co., Inc. | Aryl-oxo-heptenoic acids |
US3974212A (en) | 1974-05-22 | 1976-08-10 | Merck & Co., Inc. | [1-Hydroximino-2,2-disubstituted-5-indanyloxy-(or thio)]alkanoic acids |
AT351182B (de) | 1974-06-25 | 1979-07-10 | Merck & Co Inc | Verfahren zur herstellung von neuen 9-thia-, 9-oxothia- und 9-dioxothia- 11,12-secoprosta- glandinen |
PL98342B1 (pl) | 1974-07-30 | 1978-04-29 | Sposob wytwarzania kwasu 1-keto-2-arylo-/lub tienylo/-2-podstawionego-indanyloksy-/lub tio/-5-alkanokarboksylowego | |
US4020177A (en) | 1974-08-30 | 1977-04-26 | Merck & Co., Inc. | Substituted phenoxy-tridecanoic acids |
US4055596A (en) | 1974-09-13 | 1977-10-25 | Merck & Co., Inc. | 11,12-Seco-prostaglandins |
US3991106A (en) | 1974-09-13 | 1976-11-09 | Merck & Co., Inc. | 16-Ethers of 8-aza-9-dioxothia-11,12-seco-prostaglandins |
US3984552A (en) | 1975-02-24 | 1976-10-05 | Merck & Co., Inc. | 6-Oxo-7-substituted and 7,7-disubstituted-6H-indeno-[5,4-b]furan (and thiophene) carboxylic acids |
JPS51116341A (en) | 1975-04-04 | 1976-10-13 | Automob Antipollut & Saf Res Center | Detection apparatus for oil pressure |
US4018802A (en) | 1975-04-09 | 1977-04-19 | Merck & Co., Inc. | 9-Thia- and oxothia- and 9-dioxothia-11,12-seco-prostaglandins and processes |
US4097504A (en) | 1975-04-23 | 1978-06-27 | Merck & Co., Inc. | 11,12-Secoprostaglandins |
US4092414A (en) | 1975-04-25 | 1978-05-30 | Merck & Co., Inc. | 3,4-Dihydrospiro-2H-1,3-benzoxazines and their use in treating edema, abnormal electrolyte retention, and inflammation |
US4059602A (en) | 1975-06-06 | 1977-11-22 | Merck & Co., Inc. | 8-Methyl-, phenyl-, or substituted phenyl-11,12-secoprostaglandins |
US4059601A (en) | 1975-06-06 | 1977-11-22 | Merck & Co., Inc. | 8-Halo-11,12-secoprostaglandins |
US4126629A (en) | 1975-06-18 | 1978-11-21 | Merck & Co., Inc. | Substituted phenoxy-tridecenoic acids/esters |
US4087542A (en) | 1975-07-09 | 1978-05-02 | Merck & Co., Inc. | 2,3-Dihydro-6,7-disubstituted-5-acyl benzofuran-2-carboxylic acids |
US4181727A (en) | 1975-07-09 | 1980-01-01 | Merck & Co., Inc. | 2,3-Dihydro-6,7-disubstituted-5-acyl benzofuran-2-carboxylic acids |
US4296122A (en) | 1975-07-09 | 1981-10-20 | Merck & Co., Inc. | 2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids |
US4044153A (en) | 1975-08-01 | 1977-08-23 | Merck & Co., Inc. | Antiinflammatory 2-aminomethyl-6-trihalomethylphenols |
US4203988A (en) | 1975-11-12 | 1980-05-20 | Merck & Co., Inc. | Pyridinyl ureas and pharmaceutical use |
US4029816A (en) | 1975-11-25 | 1977-06-14 | Merck & Co., Inc. | Substituted 2-aminomethyl-6-iodophenols |
US4085211A (en) | 1975-12-15 | 1978-04-18 | Merck & Co., Inc. | Pyrazinecarboxamides and processes for preparing same |
US4070464A (en) | 1976-02-19 | 1978-01-24 | Merck & Co., Inc. | Method of treating autoimmune diseases |
US4085125A (en) | 1976-03-22 | 1978-04-18 | Merck & Co., Inc. | 9-Thia-, 9-oxothia-, and 9-dioxothia-11,12-seco-prostaglandins and processes |
US4128564A (en) | 1976-03-22 | 1978-12-05 | Merck & Co., Inc. | 9-Thia- and oxothia- and 9-dioxothia-11,12-seco-prostaglandins |
US4181661A (en) | 1976-05-03 | 1980-01-01 | Merck & Co., Inc. | Derivatives of 2-iminothiazolidines and thiazolines |
US4029803A (en) | 1976-05-03 | 1977-06-14 | Merck & Co., Inc. | Method of treatment with 2-iminothiazolidines and thiazolines |
US4022794A (en) | 1976-05-24 | 1977-05-10 | Merck & Co., Inc. | Novel analogs of prostaglandins with 4-oxo-thiazolidinyl nucleus and method of preparation thereof |
US4059587A (en) | 1976-05-24 | 1977-11-22 | Merck & Co., Inc. | Certain thiazolidine compounds |
US4025625A (en) | 1976-06-15 | 1977-05-24 | Merck & Co., Inc. | Imidazothiazines |
US4054652A (en) | 1976-06-15 | 1977-10-18 | Merck & Co., Inc. | Dihydro- and tetrahydro- iminothiazines |
NL7705652A (nl) | 1976-06-15 | 1977-12-19 | Merck & Co Inc | 2-imino-3-aminothiazolidinen. |
US4087526A (en) | 1976-07-23 | 1978-05-02 | Merck & Co., Inc. | (3-Amino-5-substituted-6-fluoropyrazinoyl or pyrazamido)-guanidines and their derivatives bearing substituents on the guanidino nitrogens |
US4111877A (en) | 1976-07-29 | 1978-09-05 | Air Products & Chemicals, Inc. | Allyl esters of n-alkyl-omega-(alkyleneureido) amic acids and their synthesis and use in aqueous emulsion polymer systems |
US4067980A (en) | 1976-08-16 | 1978-01-10 | Merck & Co., Inc. | Spirobenzoxazinium salts, method of use and compositions thereof as antihypertensive agents |
US4085117A (en) | 1976-10-18 | 1978-04-18 | Merck & Co., Inc. | 6,7-Disubstituted-5-(acyl)benzofuran-2-carboxylic acids |
US4100294A (en) | 1976-12-06 | 1978-07-11 | Merck & Co., Inc. | 5-(Hydroxy (substituted) methyl)-2,3-dihydrobenzo furan-2-carboxylic acid and its derivatives |
US4150235A (en) | 1976-12-17 | 1979-04-17 | Merck & Co., Inc. | Interphenylene 11,12-secoprostaglandins |
US4175203A (en) | 1976-12-17 | 1979-11-20 | Merck & Co., Inc. | Interphenylene 11,12-secoprostaglandins |
US4105769A (en) | 1977-01-24 | 1978-08-08 | Merck & Co., Inc. | Inhibition of indoleamine-N-methyl transferase by 2-iminopyridines |
US4087435A (en) | 1977-02-17 | 1978-05-02 | Merck & Co., Inc. | 8-Aza-9-dioxothiaprostanoic acids |
US4115573A (en) | 1977-03-04 | 1978-09-19 | Merck & Co., Inc. | N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same |
US4208413A (en) | 1977-03-04 | 1980-06-17 | Merck & Co., Inc. | N-Pyrazinecarbonyl-N'-alkoxycarbonyl and N',N"-bis(alkoxycarbonyl)guanidines and processes for preparing same |
US4112236A (en) | 1977-04-04 | 1978-09-05 | Merck & Co., Inc. | Interphenylene 8-aza-9-dioxothia-11,12-secoprostaglandins |
US4108859A (en) | 1977-06-06 | 1978-08-22 | The Dow Chemical Company | Microbicidal (pyridinylamino) alkyl guanidines |
US4115402A (en) | 1977-06-17 | 1978-09-19 | Merck & Co., Inc. | 2,3-Dichloro-4-[(substituted-sulfonyl)-phenoxy]-acetic acids |
US4196292A (en) | 1977-06-29 | 1980-04-01 | Merck & Co., Inc. | 6-Substituted amiloride derivatives |
US4229456A (en) | 1977-07-18 | 1980-10-21 | Merck & Co., Inc. | Substituted naphthyridinones and processes for their preparations |
US4133885A (en) | 1977-07-18 | 1979-01-09 | Merck & Co., Inc. | Substituted naphthyridinones |
US4536507A (en) | 1977-07-26 | 1985-08-20 | Merck & Co., Inc. | Prostaglandin antagonists |
US4093728A (en) | 1977-08-18 | 1978-06-06 | E. R. Squibb & Sons, Inc. | Triazoloisoindoles |
US4140776A (en) | 1977-09-16 | 1979-02-20 | Merck & Co., Inc. | N-pyrazinecarbonyl-N'-acylguanidines |
US4130566A (en) | 1977-10-27 | 1978-12-19 | Sumitomo Chemical Company, Limited | Process for producing 5-carboxy-2-acetylthiophene |
US4127584A (en) | 1977-11-11 | 1978-11-28 | Merck & Co., Inc. | 2,3-Substituted-1,2,5-thiadiazolium salt antimicrobials |
US4159279A (en) | 1977-11-23 | 1979-06-26 | Merck & Co., Inc. | Nuclear substituted 2-hydroxyphenylmethanesulfamic acids |
US4292430A (en) | 1977-11-23 | 1981-09-29 | Merck & Co., Inc. | 2,3-Substituted-1,2-isothiazolium salt antimicrobials |
US4267341A (en) | 1977-11-23 | 1981-05-12 | Merck & Co., Inc. | Process for preparing 2,3-substituted-1,2,-isothiazolium salt antimicrobials |
US4166177A (en) | 1977-12-27 | 1979-08-28 | Merck & Co., Inc. | Substituted 2,2-dioxo-1,2,3-benzoxathiazines |
US4145551A (en) | 1978-01-09 | 1979-03-20 | Merck & Co., Inc. | Pyrazine-2-carbonyloxyguanidines |
US4401669A (en) | 1978-01-27 | 1983-08-30 | Merck & Co., Inc. | 2,3-Dihydro-substituted-5-benzoyl benzofuran-2-carboxylic acids and their use in treating hypertension |
US4189496A (en) | 1978-02-16 | 1980-02-19 | Merck & Co., Inc. | 2,3-Dihydro-5-thienylmethyl and furylmethyl-6-substituted and 6,7-disubstituted-benzofuran-2-carboxylic acid |
US4163781A (en) | 1978-04-17 | 1979-08-07 | Merck & Co., Inc. | 3-Amino-N-[(phosphonoamino)iminomethyl]-6-halopyrazinecarboxamide compounds, compositions and methods of use |
US4156005A (en) | 1978-06-21 | 1979-05-22 | Merck & Co., Inc. | Derivatives of 1,2-benzisoxazoles |
US4394515A (en) | 1978-06-23 | 1983-07-19 | Merck & Co., Inc. | 10,11-Dihydro-11-oxodibenzo[b,f]thiepin compounds |
US4263207A (en) | 1978-08-01 | 1981-04-21 | Merck & Co., Inc. | 10,11-Dihydrodibenzo[b,f][1,4]thiazepine carboxylic acids esters and amides thereof |
US4190655A (en) | 1978-08-28 | 1980-02-26 | Merck & Co., Inc. | Amiloride citrate |
US4226867A (en) | 1978-10-06 | 1980-10-07 | Merck & Co., Inc. | 3,3-Substituted spiro-1,2,4-benzothiadiazines |
US4187315A (en) | 1978-10-11 | 1980-02-05 | Merck & Co., Inc. | N-alkyl(and cycloalkyl)oxamic acid and derivatives as inhibitors of glycolic acid oxidase |
US4207329A (en) | 1978-10-11 | 1980-06-10 | Merck & Co., Inc. | Derivatives of glycolic and glyoxylic acid as inhibitors of glycolic acid oxidase |
US4178386A (en) | 1978-10-11 | 1979-12-11 | Merck & Co., Inc. | Inhibitors of glycolic acid oxidase |
US4390537A (en) | 1978-11-16 | 1983-06-28 | Merck & Co., Inc. | 1-(Substituted-aminoalkoxyphenyl)-2-methylene-1-alkanones, compositions and use |
US4342782A (en) | 1978-11-16 | 1982-08-03 | Merck & Co., Inc. | 1-(Substituted-aminoalkoxyphenyl)-2-methylene-1-alkanones, compositions and use thereof |
US4282365A (en) | 1978-11-24 | 1981-08-04 | Merck & Co., Inc. | Dibenz[b,e]oxepin compounds |
US4249021A (en) | 1979-02-26 | 1981-02-03 | Merck & Co., Inc. | Indanacetic acid compounds |
US4246406A (en) | 1979-03-27 | 1981-01-20 | Merck & Co., Inc. | Heterocyclic substituted pyrazinoylguanidines |
US4224447A (en) | 1979-03-27 | 1980-09-23 | Merck & Co., Inc. | Novel pyrazinecarboxamides and processes for preparing same |
US4221790A (en) | 1979-04-16 | 1980-09-09 | Merck & Co., Inc. | Substituted 2,2-dioxo-1,2,3-benzoxathiazines |
US4233452A (en) | 1979-05-03 | 1980-11-11 | Merck & Co., Inc. | Derivatives of glycolic and glyoxylic acid as inhibitors of glycolic acid oxidase |
US4220654A (en) | 1979-06-04 | 1980-09-02 | Merck & Co., Inc. | Cyclic imidazole cyanoguanidines |
US4256758A (en) | 1979-06-11 | 1981-03-17 | Merck & Co., Inc. | 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4537902A (en) | 1979-06-11 | 1985-08-27 | Merck & Co., Inc. | 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4431660A (en) | 1979-06-11 | 1984-02-14 | Merck & Co., Inc. | (4'-Biphenylyloxy and-thio-oxy)-3-hydroxy-3-pyrroline-2,5-diones and a method of treating calcium oxalate renal lithiasis therewith |
US4291050A (en) | 1979-06-21 | 1981-09-22 | Merck & Co., Inc. | 6,7-Disubstituted-2 or 2,2-substituted-5-substituted-1-indanones |
US4237144A (en) | 1979-06-21 | 1980-12-02 | Merck & Co., Inc. | 2,3-Dihydro-2,6,7-trisubstituted-5-acylbenzofurans |
US4237130A (en) | 1979-06-21 | 1980-12-02 | Merck & Co., Inc. | 2,3-Dihydro-6,7-disubstituted-5-(substituted sulfonyl)benzofuran-2-carboxylic acids |
JPS6034925B2 (ja) | 1979-07-31 | 1985-08-12 | 帝人株式会社 | 持続性鼻腔用製剤およびその製造法 |
US4710513A (en) | 1979-08-17 | 1987-12-01 | Merck & Co., Inc. | Substituted pyranone inhibitors of cholesterol synthesis |
US4459422A (en) | 1979-08-17 | 1984-07-10 | Merck & Co., Inc. | Substituted pyranone inhibitors of cholesterol synthesis |
US4567289A (en) | 1979-08-17 | 1986-01-28 | Merck & Co., Inc. | Substituted pyranone inhibitors of cholesterol synthesis |
US4375475A (en) | 1979-08-17 | 1983-03-01 | Merck & Co., Inc. | Substituted pyranone inhibitors of cholesterol synthesis |
US4298743A (en) | 1979-09-11 | 1981-11-03 | Merck & Co., Inc. | 4-(Substituted phenyl thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones |
US4296237A (en) | 1979-09-11 | 1981-10-20 | Merck & Co., Inc. | 4-(Pyridyl, piperazinyl and thiazolyl substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones |
US4379791A (en) | 1979-09-11 | 1983-04-12 | Merck & Co., Inc. | 4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4377588A (en) | 1979-09-11 | 1983-03-22 | Merck Sharp & Dohme (I.A.) Corp. | 4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4317922A (en) | 1979-10-19 | 1982-03-02 | Merck & Co., Inc. | [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids and their analogs, esters, salts and derivatives |
US4337354A (en) | 1979-10-19 | 1982-06-29 | Merck & Co., Inc. | [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids, their analogs, esters, salts, and derivatives |
US4356313A (en) | 1979-10-19 | 1982-10-26 | Merck & Co., Inc. | [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acid esters and their analogs, the parent acids and their salts |
US4432992A (en) | 1979-11-05 | 1984-02-21 | Merck & Co., Inc. | 4-[5(and 4)-Substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4342776A (en) | 1979-11-05 | 1982-08-03 | Merck & Co., Inc. | 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4349561A (en) | 1979-11-05 | 1982-09-14 | Merck & Co., Inc. | 4-Substituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4448786A (en) | 1979-11-05 | 1984-05-15 | Merck & Co., Inc. | 4-Naphthyl and substituted naphthyl-3-hydroxy-3-pyrroline-2,5-diones and their use as inhibitors of glycolic acid oxidase |
US4464363A (en) | 1979-12-20 | 1984-08-07 | Merck & Co., Inc. | Ajuvants for rectal delivery of drug substances |
US4260771A (en) | 1979-12-20 | 1981-04-07 | Merck & Co., Inc. | Interphenylene 9-thia-11-oxo-12-azaprostanoic acid compounds |
US4428959A (en) | 1980-04-04 | 1984-01-31 | Merck & Co., Inc. | 4-Alkylsubstituted-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase |
US4362724A (en) | 1980-05-19 | 1982-12-07 | Merck & Co., Inc. | Method of treating edema and hypertension and pharmaceutical composition therefor in which the active ingredient comprises a novel substituted pyrazinyl-1,2,4-oxadiazole and a kaliuretic diuretic |
US4309540A (en) | 1980-05-19 | 1982-01-05 | Merck & Co., Inc. | Substituted pyrazinyl-1,2,4-oxadiazoles |
US4356314A (en) | 1980-06-30 | 1982-10-26 | Merck & Co., Inc. | [5,6,9A-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids, their analogs, esters, salts, and derivatives |
US4317822A (en) | 1980-07-02 | 1982-03-02 | Merck & Co., Inc. | 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-triazin-2-yl)2-pyrazinecarboxamides |
US4272537A (en) | 1980-07-02 | 1981-06-09 | Merck & Co., Inc. | 3-Amino-5-substituted-6-halo-N-(4,4-disubstituted-6-substituted-1,3,5-triazin-2-yl)-2-pyrazinecarboxamides |
US4277602A (en) | 1980-07-02 | 1981-07-07 | Merck & Co., Inc. | 3-Amino-5-substituted-6-halo-N-(3,4-dihydro-6-substituted-1,3,5-truazin-2-yl)2-pyrazinecarboxamides |
US4465850A (en) | 1980-09-02 | 1984-08-14 | Merck & Co., Inc. | Treatment of brain injury due to gray matter edema with (indanyloxy) butanoic acids |
US4389417A (en) | 1980-09-05 | 1983-06-21 | Merck & Co., Inc. | Treatment of gray matter edema |
US4312860A (en) | 1980-10-24 | 1982-01-26 | Regents Of The University Of California | Lung surfactant compositions |
US4394385A (en) | 1980-11-21 | 1983-07-19 | Merck & Co., Inc. | Treatment of gray matter edema |
US4316043A (en) | 1980-12-19 | 1982-02-16 | Merck & Co., Inc. | [(5,6,9a-Substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoic and cycloalkanoic acids and their analogs, esters, salts and derivatives |
US4336397A (en) | 1980-12-29 | 1982-06-22 | Merck & Co., Inc. | 2,4-Dioxo-4-substituted-1-butanoic acid derivatives useful in treating urinary tract calcium oxalate lithiasis |
US4337258A (en) | 1980-12-29 | 1982-06-29 | Merck & Co., Inc. | 2,4-Dioxo-4-substituted-1-butanoic acid derivatives useful in treating urinary tract calcium oxalate lithiasis |
US4431652A (en) | 1980-12-29 | 1984-02-14 | Merck & Co., Inc. | 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis |
US4428956A (en) | 1980-12-29 | 1984-01-31 | Merck & Co., Inc. | 4-Hydroxy-5-substituted-3-(2H)-isothiazolone-1,1-dioxide derivatives useful in treating urinary tract calcium oxalate lithiasis |
US4778897A (en) | 1981-02-25 | 1988-10-18 | Merck & Co., Inc. | 6H-dibenz[b,e][1,4]oxathiepin compounds |
US4582842A (en) | 1981-02-25 | 1986-04-15 | Merck & Co., Inc. | Anti-asthmatic 6H-dibenz-[b,e] [1,4]oxathiepin derivatives, compositions, and method of use therefor |
US4454132A (en) | 1981-03-16 | 1984-06-12 | Merck & Co., Inc. | Pharmaceutical compositions of novel substituted pyrazinyl-1,2,4-oxadiazoles useful in the treatment of edema and hypertension |
US4510322A (en) | 1981-07-13 | 1985-04-09 | Merck & Co., Inc. | Indacrinone having enhanced uricosuric |
US4420615A (en) | 1981-08-24 | 1983-12-13 | Merck & Co., Inc. | Substituted pyridopyrimidines as gastric secretion inhibitors |
US4425337A (en) | 1981-12-30 | 1984-01-10 | Merck & Co., Inc. | Adjuvants for rectal delivery of drug |
US4463208A (en) | 1981-12-30 | 1984-07-31 | Merck & Co., Inc. | Treatment of gray matter edema |
US4952582A (en) | 1982-01-04 | 1990-08-28 | Beyer Jr Karl H | Pyrazinoylguanidine and derivatives thereof having few polar substituents and being useful as hyperuretic agents |
US4663322A (en) | 1982-01-04 | 1987-05-05 | Beyer Jr Karl H | Antihypertensive hyperuretic and saluretic agent combinations |
US4594349A (en) | 1982-01-04 | 1986-06-10 | Beyer Jr Karl H | Hyperuretic agents |
US4389393A (en) | 1982-03-26 | 1983-06-21 | Forest Laboratories, Inc. | Sustained release therapeutic compositions based on high molecular weight hydroxypropylmethylcellulose |
US4440740A (en) | 1982-04-26 | 1984-04-03 | Merck & Co., Inc. | α-Keto aldehydes as enhancing agents of gastro-intestinal drug absorption |
US4479932A (en) | 1982-05-18 | 1984-10-30 | University Of Florida | Brain-specific drug delivery |
US4540564A (en) | 1982-05-18 | 1985-09-10 | University Of Florida | Brain-specific drug delivery |
US4501729A (en) | 1982-12-13 | 1985-02-26 | Research Corporation | Aerosolized amiloride treatment of retained pulmonary secretions |
JPS6032714A (ja) | 1983-08-01 | 1985-02-19 | Teijin Ltd | 鼻腔粘膜に適用するための安定化された粉末状薬学的組成物 |
US4699917A (en) | 1983-09-26 | 1987-10-13 | Merck & Co., Inc. | Anti-asthmatic tetrazolyl 6H-dibenz-[B,E]-[1,4]-oxathiepin derivatives, compositions, and method of use therefor |
US4596821A (en) | 1984-05-01 | 1986-06-24 | Merck & Co., Inc. | Treatment of gray matter edema with 3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones |
US4680414A (en) | 1984-05-01 | 1987-07-14 | Merck & Co., Inc. | Substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones |
US4604403A (en) | 1984-05-01 | 1986-08-05 | Merck & Co., Inc. | Use of substituted-3(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones for treating grey matter edema |
US4634717A (en) | 1984-05-01 | 1987-01-06 | Merck & Co., Inc. | Substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, useful for treating persons with gray matter edema |
US4605664A (en) | 1984-05-01 | 1986-08-12 | Merck & Co., Inc. | Use of substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones for treatment of grey matter edema |
US4605663A (en) | 1984-05-01 | 1986-08-12 | Merck & Co., Inc. | Use of substituted-3-(2,3-dihydro-1H-inden-5-yl)-4-hydroxy-1H-pyrrole-2,5-diones, for treatment of grey matter edema |
US4604394A (en) | 1984-10-01 | 1986-08-05 | Merck & Co., Inc. | Antiarrhythmic compositions and method |
US4805811A (en) | 1985-03-29 | 1989-02-21 | Aktiebolaget Draco | Dosage device |
US4754061A (en) | 1985-06-04 | 1988-06-28 | Merck & Co., Inc. | Substituted (2,3-dihydro-1-oxo-1H-inden-5-yl)alkanoic acids, their derivatives and their salts |
US4579869A (en) | 1985-08-02 | 1986-04-01 | Merck & Co., Inc. | Substituted [(2,3-dihydro-1-oxo-1H-inden-5-yl)amino]alkanoic acids, their derivatives and their salts |
US4654365A (en) | 1985-09-26 | 1987-03-31 | Merck & Co., Inc. | 2,3-dihydro-5-(3-oxo-2-cyclohexen-1-yl)-2-benzofurancarboxylic acids, and their salts useful in the treatment of brain injury |
US4604396A (en) | 1985-09-26 | 1986-08-05 | Merck & Co., Inc. | [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]ethanimidamides and [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]ethanimidic acid hydrazides, their derivatives and their salts |
US4625047A (en) | 1985-12-23 | 1986-11-25 | Merck & Co., Inc. | Substituted (2,3-dihydro-4-(3-oxo-1-cyclohexen-1-yl)phenoxy) alkanoic acids, their derivatives and their salts |
US4719310A (en) | 1985-12-23 | 1988-01-12 | Merck & Co., Inc. | Ester and amide substituted (2,3-dihydro-4-(3-oxo-1-cyclohexen-1-yl)phenoxy)alkanoic acids and their salts |
US4777281A (en) | 1986-03-03 | 1988-10-11 | Merck & Co., Inc. | [3,4-dichloro-6,7,8,8a,9,10-hexahydro-6-oxo-8a-substituted-2-phenanthrenyl)oxy]-alkanoic acids and -ethanimidamides |
US4731472A (en) | 1986-03-03 | 1988-03-15 | Merck & Co., Inc. | (5,6-dichloro-3-oxo-9A-propyl-2,3,9,9A-tetrahydrofluoren-7-yl)alkanoic acids and alkanimidamides |
US4835313A (en) | 1986-03-03 | 1989-05-30 | Merck & Co., Inc. | (5,6-dichloro-3-oxo-9α-propyl-2,3,9,9α-tetrahydrofluoren-7-yl) alkanimidamides |
US4699926A (en) | 1986-04-04 | 1987-10-13 | Merck & Co., Inc. | Compounds useful in treating sickle cell anemia |
US4751244A (en) | 1986-04-04 | 1988-06-14 | Merck & Co., Inc. | Compounds useful in treating sickle cell anemia |
US4731473A (en) | 1986-04-04 | 1988-03-15 | Merck & Co., Inc. | Compounds useful in treating sickle cell anemia |
US4731381A (en) | 1986-04-04 | 1988-03-15 | Merck & Co., Inc. | Method of treating a person for sickle cell anemia |
US4675341A (en) | 1986-08-13 | 1987-06-23 | Merck & Co., Inc. | [(5,6-dichloro-3-oxo-9a-propyl-2,3,9,9a-tetrahydrofluoren-7-yl)oxy]ethanol and its derivatives |
US4937232A (en) | 1986-09-15 | 1990-06-26 | Duke University | Inhibition of protein kinase C by long-chain bases |
US4797391A (en) | 1986-09-24 | 1989-01-10 | Merck & Co., Inc. | ((5,6-dichloro-3-oxo-9,9a-disubstituted-2,3,9,9a-tetrahydrofluoren-7-yl)oxy)alkanoic acids and alkanimidamides |
US4769370A (en) | 1986-09-24 | 1988-09-06 | Merck & Co., Inc. | (1,2-dichloro-8-oxo-5a-substituted-5a,6,7,8-tetrahydrodibenzofuran-3-yl)alkanoic acids and alkanimidamides |
US4731471A (en) | 1986-11-03 | 1988-03-15 | Merck & Co., Inc. | (5,6-dichloro-3-oxo-2,3,9,9a-tetrahydrofluoren-7-yl)-alkanoic acids and alkanimidamides bearing novel functional 9a-substituents |
US4731470A (en) | 1986-11-03 | 1988-03-15 | Merck & Co., Inc. | [(5,6-dichloro-3-oxo-2,9a-alkano-2,3,9,9a-tetrahydro-1H-fluoren-7-yl)oxy]alkanoic acids and alkanimidamides |
US4782073A (en) | 1986-12-24 | 1988-11-01 | Merck & Co., Inc. | Amides of [(5,6-dichloro-3-oxo-9-alpha-substituted-2,3,9,9-alpha-tetrahydrofluoren-7-yl-oxyl]acetic acids, and pharmaceutical compositions thereof |
US4771076A (en) | 1987-06-01 | 1988-09-13 | Merck & Co., Inc. | [(2-substituted 1,2-dihydro-1-oxo-1H-inden-5-yl)oxy]alkanesulfonic acids and salts thereof |
US4775695A (en) | 1987-06-01 | 1988-10-04 | Merck & Co., Inc. | Substituted amidinoalkoxy and amidinoalkylamino indanones and salts thereof |
US5132296A (en) | 1987-08-14 | 1992-07-21 | Cherksey Bruce D | Membrane NA+ channel protein and related therapeutic compounds |
US5242947A (en) | 1988-02-10 | 1993-09-07 | New York University | Use of polyamines as ionic-channel regulating agents |
US4894376A (en) | 1988-02-26 | 1990-01-16 | Trustees Of The University Of Pennsylvania | Methods of treating diseases characterized by hyperexcitability of neurons |
US4923874A (en) | 1988-07-21 | 1990-05-08 | G. D. Searle & Co. | Use of 8-azapurin-6-one derivatives for control of hypertension |
US5100806A (en) | 1989-03-24 | 1992-03-31 | Macri James N | Method for detecting Edwards syndrome |
US4955371A (en) | 1989-05-08 | 1990-09-11 | Transtech Scientific, Inc. | Disposable inhalation activated, aerosol device for pulmonary medicine |
CA2063273C (en) | 1989-07-11 | 2002-09-24 | Bradley J. Benson | Surfactant compositions and methods |
US5707644A (en) | 1989-11-04 | 1998-01-13 | Danbiosyst Uk Limited | Small particle compositions for intranasal drug delivery |
US5215991A (en) | 1990-01-26 | 1993-06-01 | Allergan, Inc. | Combination of selective alpha-adrenergic agonists and Na+ /H+ ex |
DE4003272A1 (de) | 1990-02-03 | 1991-08-08 | Boehringer Ingelheim Kg | Neue treibgasmischungen und ihre verwendung in arzneimittelzubereitungen |
US5449682A (en) | 1990-02-13 | 1995-09-12 | Merck & Co., Inc. | Angiotensin II antagonists incorporating a substituted benzyl element |
US5182299A (en) | 1990-03-19 | 1993-01-26 | Brigham And Women's Hospital | Treatment of osmotic disturbance with organic osmolytes |
AU654979B2 (en) | 1990-10-05 | 1994-12-01 | University Of North Carolina At Chapel Hill, The | Method of administering amiloride |
US5614216A (en) | 1990-10-17 | 1997-03-25 | The Liposome Company, Inc. | Synthetic lung surfactant |
EP0517573A1 (fr) | 1991-06-05 | 1992-12-09 | Synthelabo | Compositions pharmaceutiques pour le traitement des affections des voies respiratoires |
US5292498A (en) | 1991-06-19 | 1994-03-08 | The University Of North Carolina At Chapel Hill | Method of treating lung disease with uridine triphosphates |
DE69233690T2 (de) | 1991-07-02 | 2008-01-24 | Nektar Therapeutics, San Carlos | Abgabevorrichtung für nebelförmige Medikamente |
DK1086688T3 (da) | 1991-12-18 | 2004-08-16 | Minnesota Mining & Mfg | Aerosolformuleringer til suspensioner |
US7105152B1 (en) | 1991-12-18 | 2006-09-12 | 3M Innovative Properties Company | Suspension aerosol formulations |
US5261538A (en) | 1992-04-21 | 1993-11-16 | Glaxo Inc. | Aerosol testing method |
US5312820A (en) | 1992-07-17 | 1994-05-17 | Merck & Co., Inc. | Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines |
DE4236237A1 (de) | 1992-10-27 | 1994-04-28 | Behringwerke Ag | Prodrugs, ihre Herstellung und Verwendung als Arzneimittel |
ATE157351T1 (de) | 1993-02-20 | 1997-09-15 | Hoechst Ag | Substituierte benzoylguanidine, verfahren zu ihrer herstellung, ihre verwendung als medikament, als inhibitoren des zellulären na+/h+-austauschs oder als diagnostikum sowie sie enthaltendes medikament |
US5384128A (en) | 1993-03-02 | 1995-01-24 | University Of Alabama Research Foundation | Method of and compounds for treatment for cystic fibrosis |
US5512269A (en) | 1993-06-09 | 1996-04-30 | Burroughs Wellcome, Co. | Method of treating retained pulmonary secretions |
US5466823A (en) | 1993-11-30 | 1995-11-14 | G.D. Searle & Co. | Substituted pyrazolyl benzenesulfonamides |
CA2276945C (en) | 1993-11-30 | 2006-08-01 | G.D. Searle & Co. | Tricyclic-substituted pyrazolyl benzenesulfonamides and pharmaceutical compositions thereof |
US6051576A (en) | 1994-01-28 | 2000-04-18 | University Of Kentucky Research Foundation | Means to achieve sustained release of synergistic drugs by conjugation |
AUPM411494A0 (en) | 1994-02-25 | 1994-03-24 | Central Sydney Area Health Service | Method and device for the provocation of upper or lower airway narrowing and/or the induction of sputum |
US6190691B1 (en) | 1994-04-12 | 2001-02-20 | Adolor Corporation | Methods for treating inflammatory conditions |
US5962477A (en) | 1994-04-12 | 1999-10-05 | Adolor Corporation | Screening methods for cytokine inhibitors |
US5538991A (en) | 1994-09-14 | 1996-07-23 | Merck & Co., Inc. | Endothelin antagonists bearing 5-membered heterocyclic amides |
US5522385A (en) | 1994-09-27 | 1996-06-04 | Aradigm Corporation | Dynamic particle size control for aerosolized drug delivery |
US5618557A (en) | 1994-11-22 | 1997-04-08 | E.R. Squibb & Sons, Inc. | Prophylactic treatment of allergic contact dermatitis |
US5544647A (en) | 1994-11-29 | 1996-08-13 | Iep Group, Inc. | Metered dose inhalator |
US5622163A (en) | 1994-11-29 | 1997-04-22 | Iep Group, Inc. | Counter for fluid dispensers |
US5656256A (en) | 1994-12-14 | 1997-08-12 | The University Of North Carolina At Chapel Hill | Methods of treating lung disease by an aerosol containing benzamil or phenamil |
HU219899B (hu) | 1995-04-14 | 2001-09-28 | Glaxo Wellcome Inc. | Inhalálóberendezés flutikaszon-propionát adagolására mért dózisban |
US5908611A (en) | 1995-05-05 | 1999-06-01 | The Scripps Research Institute | Treatment of viscous mucous-associated diseases |
US5635160A (en) | 1995-06-07 | 1997-06-03 | The University Of North Carolina At Chapel Hill | Dinucleotides useful for the treatment of cystic fibrosis and for hydrating mucus secretions |
US5994336A (en) | 1995-06-07 | 1999-11-30 | Magainin Pharmaceuticals Inc. | Method of inhibiting proliferation of cells by administering an aminosterol compound |
US5628984A (en) | 1995-07-31 | 1997-05-13 | University Of North Carolina At Chapel Hill | Method of detecting lung disease |
JPH11512435A (ja) | 1995-09-12 | 1999-10-26 | ジェネンテック インコーポレーテッド | 嚢胞性繊維症の治療 |
US6399585B1 (en) | 1996-05-15 | 2002-06-04 | Janet E. Larson | In Utero treatment of CFTR-related deficiencies |
US6015828A (en) | 1996-05-31 | 2000-01-18 | Cuppoletti; John | Chemical modification of chloride channels as a treatment for cystic fibrosis and other diseases |
US6071910A (en) | 1996-12-05 | 2000-06-06 | Mayo Foundation For Medical Education And Research | Use of agents to treat eosinophil-associated pathologies |
CA2279963C (en) | 1997-02-06 | 2008-04-22 | Inspire Pharmaceuticals, Inc. | Dinucleotides and their use |
US6818629B2 (en) | 1997-02-10 | 2004-11-16 | Inspire Pharmaceuticals, Inc. | Pharmaceutical formulation comprising P1-(2'-deoxycytidine 5'-)P4-(uridine 5'-) tetraphosphate |
US7223744B2 (en) | 1997-02-10 | 2007-05-29 | Inspire Pharmaceuticals, Inc. | Pharmaceutical formulation comprising dinucleoside polyphosphates and salts thereof |
US20010031244A1 (en) | 1997-06-13 | 2001-10-18 | Chiesi Farmaceutici S.P.A. | Pharmaceutical aerosol composition |
ZA987847B (en) | 1997-08-29 | 1999-06-28 | Univ North Carolina | Method of treating lung diseases with uridine 5'-diphosphate and analogs thereof |
US6153187A (en) | 1997-09-02 | 2000-11-28 | Insight Strategy & Marketing Ltd. | Use of glycosaminoglycans degrading enzymes for management of airway associated diseases |
US6159968A (en) | 1998-01-15 | 2000-12-12 | University Of Cincinnati | Activation of chloride channels for correction of defective chloride transport |
US6291514B1 (en) | 1998-02-09 | 2001-09-18 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors |
GB9807232D0 (en) | 1998-04-03 | 1998-06-03 | Univ Cardiff | Aerosol composition |
DE69905464T2 (de) | 1998-05-22 | 2004-01-15 | Inspire Pharmaceuticals Inc | Therapeutische dinucleotide und deren derivate |
US6294188B1 (en) | 1998-07-09 | 2001-09-25 | Aviana Biopharm Inc. | Methods involving changing the constitutive and stimulated secretions of the local reproductive system of women |
CN1150890C (zh) | 1998-08-04 | 2004-05-26 | 杰格研究股份公司 | 药用气溶胶制剂 |
US6136294C1 (en) | 1998-09-22 | 2002-09-24 | Aeropharm Technology Inc | Amino acid stabilized medical aerosol formulation |
US6458338B1 (en) | 1998-09-22 | 2002-10-01 | Aeropharm Technology Incorporated | Amino acid stabilized medicinal aerosol formulations |
DE69934435T2 (de) | 1998-10-20 | 2007-09-27 | University Of North Carolina At Chapel Hill | Methoden zum befeuchten der nasenschleimhaut |
EP1126832A2 (en) | 1998-10-27 | 2001-08-29 | Yale University | Conductance of improperly folded proteins through the secretory pathway |
US6926911B1 (en) | 1998-12-22 | 2005-08-09 | The University Of North Carolina At Chapel Hill | Compounds and methods for the treatment of airway diseases and for the delivery of airway drugs |
US6329034B1 (en) | 1999-01-18 | 2001-12-11 | Roger L. Pendry | Label having tab member and methods for forming, applying and using the same |
US6116234A (en) | 1999-02-01 | 2000-09-12 | Iep Pharmaceutical Devices Inc. | Metered dose inhaler agitator |
AR023088A1 (es) | 1999-02-26 | 2002-09-04 | Inspire Pharmaceuticals Inc | Uso de disfosfatos de uridina, adenina y citidina y analogos de los mismos para la manufactura de un medicamento para la estimulacion de la hidratacion delas mucosas. |
WO2000074754A2 (en) | 1999-06-05 | 2000-12-14 | Innovata Biomed Limited | Delivery system |
GB2353222B (en) | 1999-06-23 | 2001-09-19 | Cambridge Consultants | Inhalers |
US20040195160A1 (en) | 1999-07-12 | 2004-10-07 | Marine Desalination Systems, L.L.C. | Hydrate-based reduction of fluid inventories and concentration of aqueous and other water-containing products |
JP2004513870A (ja) | 1999-07-19 | 2004-05-13 | ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル | ナトリウムチャネルブロッカーの結合物及びその使用法 |
GB9920839D0 (en) | 1999-09-04 | 1999-11-10 | Innovata Biomed Ltd | Inhaler |
AU1068401A (en) | 1999-10-12 | 2001-04-23 | Shl Medical Ab | Inhaler |
AUPQ344799A0 (en) | 1999-10-15 | 1999-11-11 | University Of Sydney, The | Treatment of respiratory diseases and infections |
US6297226B1 (en) | 1999-10-15 | 2001-10-02 | Neotherapeutics, Inc. | Synthesis and methods of use of 9-substituted guanine derivatives |
JO2178B1 (en) | 1999-10-19 | 2003-04-23 | اف . هوفمان لاروش ايه جي | Treatment of invasive diseases, using selected anti-PAR materials |
ES2343124T3 (es) | 1999-10-29 | 2010-07-23 | Novartis Ag | Composiciones de polvo seco con dispersabilidad mejorada. |
US6204270B1 (en) | 1999-11-12 | 2001-03-20 | Eyal S. Ron | Ophthalmic and mucosal preparations |
GB9928265D0 (en) | 1999-12-01 | 2000-01-26 | Innovata Biomed Ltd | Inhaler |
US6476048B1 (en) | 1999-12-07 | 2002-11-05 | Inotek Pharamaceuticals Corporation | Substituted phenanthridinones and methods of use thereof |
SE9904706D0 (sv) | 1999-12-21 | 1999-12-21 | Astra Ab | An inhalation device |
WO2001055390A1 (en) | 2000-01-28 | 2001-08-02 | Human Genome Sciences, Inc. | Human serpin polynucleotides, polypeptides, and antibodies |
US7345051B2 (en) | 2000-01-31 | 2008-03-18 | Genaera Corporation | Mucin synthesis inhibitors |
US7171965B2 (en) | 2000-02-01 | 2007-02-06 | Valois S.A.S. | Breath actuated dry powder inhaler and tape dose strip |
GB0017839D0 (en) | 2000-07-21 | 2000-09-06 | Ici Plc | Hydrogenation catalysts |
US20040199456A1 (en) | 2000-08-01 | 2004-10-07 | Andrew Flint | Method and apparatus for explaining credit scores |
FR2813593B1 (fr) | 2000-09-07 | 2002-12-06 | Valois Sa | Dispositif de distribution de produit fluide de type multidose |
GB0026647D0 (en) | 2000-10-31 | 2000-12-13 | Glaxo Group Ltd | Medicament dispenser |
JP4204315B2 (ja) | 2000-11-20 | 2009-01-07 | ビオヴィトルム・アクチボラゲット(プブリクト) | セロトニン5−ht2レセプターのアンタゴニストとしてのピペラジニルピラジン化合物 |
DE10101440B4 (de) | 2001-01-15 | 2017-10-26 | REMS-WERK Christian Föll und Söhne GmbH & Co. | Preßzange |
GB2377532B (en) | 2001-07-11 | 2005-06-29 | Sendo Int Ltd | Communications devices operable to electronically process text data for representing characters of a text message, and methods for operating such devices |
US20030135716A1 (en) | 2002-01-14 | 2003-07-17 | Gil Vinitzky | Method of creating a high performance virtual multiprocessor by adding a new dimension to a processor's pipeline |
US6858614B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenolic guanidine sodium channel blockers |
US6858615B2 (en) | 2002-02-19 | 2005-02-22 | Parion Sciences, Inc. | Phenyl guanidine sodium channel blockers |
US6889690B2 (en) | 2002-05-10 | 2005-05-10 | Oriel Therapeutics, Inc. | Dry powder inhalers, related blister devices, and associated methods of dispensing dry powder substances and fabricating blister packages |
EP1542667B1 (en) | 2002-07-24 | 2012-03-07 | PTC Therapeutics, Inc. | Ureido substituted benzoic acid compounds and their use for nonsense suppression and the treatment of disease |
US20050227974A9 (en) | 2002-08-01 | 2005-10-13 | Euro-Celtique S.A. | Aminoalkyl-substituted aryl compounds and their use as sodium channel blockers |
US6903105B2 (en) | 2003-02-19 | 2005-06-07 | Parion Sciences, Inc. | Sodium channel blockers |
EP3345895B1 (en) | 2003-04-11 | 2019-12-04 | PTC Therapeutics, Inc. | 1,2,4-oxadiazole benzoic acid compound and its use for nonsense suppression and the treatment of disease |
EP1488819A1 (en) | 2003-06-16 | 2004-12-22 | Rijksuniversiteit te Groningen | Dry powder inhaler and method for pulmonary inhalation of dry powder |
WO2005016879A2 (en) | 2003-08-18 | 2005-02-24 | Parion Sciences, Inc. | Cyclic pyrazinoylguanidine sodium channel blockers |
PT1663235E (pt) | 2003-08-18 | 2013-10-29 | Parion Sciences Inc | Novos bloqueadores dos canais do sódio de pirazinoílguanidina protegida |
JP2007502827A (ja) * | 2003-08-18 | 2007-02-15 | パリオン・サイエンシィズ・インコーポレーテッド | 脂肪族ピラジノイルグアニジンナトリウムチャネルブロッカー |
US20050090505A1 (en) | 2003-08-18 | 2005-04-28 | Johnson Michael R. | Methods of reducing risk of infection from pathogens |
US7745442B2 (en) | 2003-08-20 | 2010-06-29 | Parion Sciences, Inc. | Methods of reducing risk of infection from pathogens |
US20090253714A1 (en) | 2003-08-20 | 2009-10-08 | Johnson Michael R | Methods of reducing risk of infection from pathogens |
DE10339710A1 (de) | 2003-08-22 | 2005-03-17 | Siemens Ag | Verfahren zur Zulassungsanfrage zu einem Datenzugriff auf Nutzungs- und Zustandsdaten von Mobilfunkteilnehmern in einem Mobilfunknetz |
US7499570B2 (en) | 2004-03-02 | 2009-03-03 | Siemens Corporate Research, Inc. | Illumination invariant change detection |
US6887597B1 (en) | 2004-05-03 | 2005-05-03 | Prestone Products Corporation | Methods and composition for cleaning and passivating fuel cell systems |
US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
US7375102B2 (en) | 2004-06-28 | 2008-05-20 | Amgen Sf, Llc | Tetrahydroquinazolin-4(3H)-one-related and tetrahydropyrido[2,3-D]pyrimidin-4(3H)-one-related compounds, compositions and methods for their use |
US7399766B2 (en) | 2004-08-18 | 2008-07-15 | Parion Sciences, Inc. | Soluble amide & ester pyrazinoylguanidine sodium channel blockers |
KR20070059063A (ko) | 2004-08-18 | 2007-06-11 | 마이클 알 존슨. | 지방족 아미드 및 에스테르 피라지노일구아니딘 나트륨채널 차단제 |
US20090324724A1 (en) | 2004-08-18 | 2009-12-31 | Parion Sciences, Inc. | Soluble amide & ester pyrazinoylguanidine sodium channel blockers |
WO2006023617A2 (en) * | 2004-08-18 | 2006-03-02 | Johnson Michael R | Cyclic amide & ester pyrazinoylguanidine sodium channel blockers |
WO2006044682A1 (en) | 2004-10-13 | 2006-04-27 | Ptc Therapeutics, Inc. | Compounds for nonsense suppression, and methods for their use |
JP2009221164A (ja) | 2008-03-17 | 2009-10-01 | Nitto Denko Corp | 肺線維症処置剤 |
US7507809B2 (en) | 2005-01-07 | 2009-03-24 | Alnylam Pharmaceuticals, Inc. | RNAi modulation of RSV and therapeutic uses thereof |
JP4964469B2 (ja) | 2005-01-14 | 2012-06-27 | ガジック・テクニカル・エンタープライゼス | 磁気ヘッド及びディスクをテストするための真空チャック・スピンスタンド |
US20070021439A1 (en) | 2005-07-25 | 2007-01-25 | Parion Sciences, Inc. | Methods of reducing risk of infection from pathogens with soluble amide and ester pyrazinoylguanidine sodium channel blockers |
US7807834B2 (en) | 2005-08-03 | 2010-10-05 | Parion Sciences, Inc. | Capped pyrazinoylguanidine sodium channel blockers |
WO2007065437A2 (en) | 2005-12-06 | 2007-06-14 | P2-Science Aps | Modulation of the p2y2 receptor pathway |
GB0526240D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
GB0526244D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
CA2635214A1 (en) | 2005-12-27 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Compounds useful in cftr assays and methods therewith |
KR101501780B1 (ko) | 2006-01-24 | 2015-03-16 | 넥스바이오, 인코퍼레이티드 | 고분자 미소 구체들의 조제를 위한 기술 |
US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
ATE534383T1 (de) | 2006-05-12 | 2011-12-15 | Vertex Pharma | Zusammensetzungen aus n-ä2,4-bis(1,1- dimethylethyl)-5-hydroxyphenylü-1,4-dihydro-4- oxochinolin-3-carboxamid |
WO2007146867A2 (en) | 2006-06-09 | 2007-12-21 | Parion Sciences Inc. | Aliphatic pyrazinoylguanidine sodium channel blockers with beta agonist activity |
PL2035004T3 (pl) | 2006-06-09 | 2013-01-31 | Parion Sciences Inc | Podstawione fenylem pirazynoiloguanidynowe blokery kanału sodowego o aktywności beta-agonistycznej |
CA2653773A1 (en) | 2006-06-09 | 2007-12-21 | Parion Sciences, Inc. | Cyclic substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity |
CN101534813A (zh) * | 2006-09-07 | 2009-09-16 | 帕里昂科学公司 | 通过使用钠通道阻断剂和渗透调节剂的治疗来增加粘膜水化和粘液清除的方法 |
US8058278B2 (en) | 2006-09-07 | 2011-11-15 | Parion Sciences, Inc. | Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes |
US7981898B2 (en) | 2006-09-07 | 2011-07-19 | Parion Sciences, Inc. | Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes |
US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
US7754739B2 (en) | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
WO2008124496A1 (en) | 2007-04-03 | 2008-10-16 | Parion Sciences, Inc. | Method of treating acid-sensing ion channel mediated pain, cough, and central nervous system disorders |
US8288391B2 (en) | 2007-04-03 | 2012-10-16 | Parion Sciences, Inc. | Pyrazinoylguanidine compounds for use as taste modulators |
EP2152316A4 (en) | 2007-04-26 | 2011-03-23 | Quark Pharmaceuticals Inc | THERAPEUTIC DELIVERY OF INHIBITORY NUCLEIC ACID MOLECULES IN THE RESPIRATORY SYSTEM |
PE20090733A1 (es) | 2007-05-07 | 2009-07-17 | Novartis Ag | Derivados de pirazina como bloqueadores de los canales de sodio epitelial |
EP1997502A1 (en) | 2007-06-01 | 2008-12-03 | CHIESI FARMACEUTICI S.p.A. | Reconstituted surfactants having improved properties |
US20090098207A1 (en) | 2007-07-24 | 2009-04-16 | Nexbio, Inc. | Technology for the Preparation of Microparticles |
WO2009049159A1 (en) | 2007-10-10 | 2009-04-16 | Parion Sciences, Inc. | Delivering osmolytes by nasal cannula |
US8410067B2 (en) | 2007-11-06 | 2013-04-02 | Benaroya Research Institute | Inhibition of versican with siRNA and other molecules |
BRPI0820669A2 (pt) | 2007-12-10 | 2020-08-04 | Novartis Ag | compostos orgânicos |
CN101951913A (zh) | 2008-02-26 | 2011-01-19 | 帕里昂科学公司 | 聚芳族钠通道阻断剂 |
CA2931134C (en) | 2008-02-28 | 2019-07-30 | Vertex Pharmaceuticals Incorporated | Heteroaryl derivatives as cftr modulators |
US8261047B2 (en) | 2008-03-17 | 2012-09-04 | Freescale Semiconductor, Inc. | Qualification of conditional debug instructions based on address |
ES2552990T3 (es) | 2008-03-31 | 2015-12-03 | Vertex Pharmaceuticals Incorporated | Derivados de piridilo como moduladores del CFTR |
KR20110011621A (ko) | 2008-05-13 | 2011-02-08 | 노파르티스 아게 | 3,5―디아미노―6―클로로―피라진―2―카르복실산 유도체 및 기도 질환의 치료를 위한 상피 나트륨 채널 차단제로서의 이들의 용도 |
ES2535736T3 (es) | 2008-06-10 | 2015-05-14 | Novartis Ag | Derivados de pirazina como bloqueadores de los canales de sodio epitelial |
US20100074881A1 (en) | 2008-07-11 | 2010-03-25 | Parion Sciences, Inc. | Multiple nebulizer systems |
JP5645835B2 (ja) | 2008-10-23 | 2014-12-24 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | N−(4−(7−アザビシクロ[2.2.1]ヘプタン−7−イル)−2−(トリフルオロメチル)フェニル)−4−オキソ−5−(トリフルオロメチル)−1,4−ジヒドロキノリン−3−カルボキサミドの固体形態 |
US20100316628A1 (en) | 2008-12-09 | 2010-12-16 | The General Hospital Corporation | Agents and methods for treating respiratory disorders |
EP2382197B1 (en) | 2008-12-30 | 2016-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
WO2011156355A1 (en) | 2010-06-09 | 2011-12-15 | Kainos Medicine, Inc. | Production method of phenyl guanidine salts and their intermediates |
KR20120017648A (ko) | 2010-08-19 | 2012-02-29 | 삼성전자주식회사 | 디스플레이장치와, 디스플레이 패널의 구동방법 |
AR086745A1 (es) | 2011-06-27 | 2014-01-22 | Parion Sciences Inc | 3,5-diamino-6-cloro-n-(n-(4-(4-(2-(hexil(2,3,4,5,6-pentahidroxihexil)amino)etoxi)fenil)butil)carbamimidoil)pirazina-2-carboxamida |
DK2723176T3 (en) | 2011-06-27 | 2017-07-31 | Parion Sciences Inc | CHEMICAL AND METABOLIC STABLE DIPEPTIDE WITH POTENT SODIUM CHANNEL BLOCK ACTIVITY |
JP6272312B2 (ja) | 2012-05-29 | 2018-01-31 | パリオン・サイエンシィズ・インコーポレーテッド | ドライアイおよび他の粘膜疾患の治療のためのナトリウムチャネル遮断活性を有するデンドリマー様アミノアミド |
WO2014036445A2 (en) | 2012-08-31 | 2014-03-06 | Johnson Michael R | Novel mucolytic agents |
KR20140047189A (ko) | 2012-10-04 | 2014-04-22 | 이영시 | 칼슘 함량이 높은 홍시 재배용 친환경 비료 및 이를 이용한 홍시의 제배방법 |
LT2928878T (lt) | 2012-11-15 | 2016-11-25 | Bayer Pharma Aktiengesellschaft | 5-fluor-n-(piridin-2-il)piridin-2-amino dariniai, turintys sulfoksimino grupę |
KR20150095870A (ko) | 2012-12-17 | 2015-08-21 | 패리온 사이언스 인코퍼레이티드 | 3,5-디아미노-6-클로로-n-(n-(4-페닐부틸)카르밤이미도일)피라진-2-카르복스아미드 화합물 |
MX2015007796A (es) | 2012-12-17 | 2015-09-04 | Parion Sciences Inc | Derivados de cloro-pirazin carboxamida con actividad bloqueadora sobre los canales de sodio epiteliales. |
MX368243B (es) | 2013-08-23 | 2019-09-25 | Parion Sciences Inc | Agentes mucolíticos de ditiol. |
US9102633B2 (en) | 2013-12-13 | 2015-08-11 | Parion Sciences, Inc. | Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds |
US20150376145A1 (en) | 2014-06-30 | 2015-12-31 | Parion Sciences, Inc. | Stable sodium channel blockers |
-
2012
- 2012-06-25 AR ARP120102267A patent/AR086745A1/es unknown
- 2012-06-26 CN CN201280040628.3A patent/CN103764633B/zh active Active
- 2012-06-26 DK DK15184092.3T patent/DK3034497T3/da active
- 2012-06-26 CA CA2838251A patent/CA2838251C/en active Active
- 2012-06-26 PL PL15184092T patent/PL3034497T3/pl unknown
- 2012-06-26 MD MDA20180023A patent/MD20180023A2/ro not_active Application Discontinuation
- 2012-06-26 PE PE2013002803A patent/PE20140849A1/es active IP Right Grant
- 2012-06-26 LT LTEP15184092.3T patent/LT3034497T/lt unknown
- 2012-06-26 EP EP19217140.3A patent/EP3693361A1/en active Pending
- 2012-06-26 EP EP15184092.3A patent/EP3034497B1/en active Active
- 2012-06-26 JP JP2014518934A patent/JP6010617B2/ja active Active
- 2012-06-26 MX MX2013015046A patent/MX349852B/es active IP Right Grant
- 2012-06-26 TW TW105136658A patent/TW201730158A/zh unknown
- 2012-06-26 MX MX2017010468A patent/MX371300B/es unknown
- 2012-06-26 ES ES15184092T patent/ES2778675T3/es active Active
- 2012-06-26 PT PT127333680T patent/PT2723722E/pt unknown
- 2012-06-26 US US13/533,911 patent/US8669262B2/en active Active
- 2012-06-26 EA EA201391730A patent/EA023593B1/ru not_active IP Right Cessation
- 2012-06-26 PT PT151840923T patent/PT3034497T/pt unknown
- 2012-06-26 RS RS20150832A patent/RS54445B1/en unknown
- 2012-06-26 CN CN201710088762.5A patent/CN108033921B/zh active Active
- 2012-06-26 KR KR1020147001729A patent/KR102120252B1/ko active IP Right Grant
- 2012-06-26 TW TW107130383A patent/TWI699356B/zh active
- 2012-06-26 SI SI201230384T patent/SI2723722T1/sl unknown
- 2012-06-26 SI SI201231750T patent/SI3034497T1/sl unknown
- 2012-06-26 TW TW101122796A patent/TWI564295B/zh active
- 2012-06-26 DK DK12733368.0T patent/DK2723722T3/en active
- 2012-06-26 HU HUE12733368A patent/HUE025856T2/en unknown
- 2012-06-26 SG SG10201605241PA patent/SG10201605241PA/en unknown
- 2012-06-26 RS RS20200299A patent/RS60243B1/sr unknown
- 2012-06-26 MD MDA20140008A patent/MD4574C1/ro not_active IP Right Cessation
- 2012-06-26 UY UY0001034161A patent/UY34161A/es not_active Application Discontinuation
- 2012-06-26 WO PCT/US2012/044272 patent/WO2013003386A1/en active Application Filing
- 2012-06-26 AU AU2012275502A patent/AU2012275502B2/en active Active
- 2012-06-26 UA UAA201314493A patent/UA118169C2/uk unknown
- 2012-06-26 AP AP2014007464A patent/AP2014007464A0/xx unknown
- 2012-06-26 EA EA201591978A patent/EA037741B1/ru not_active IP Right Cessation
- 2012-06-26 PL PL12733368T patent/PL2723722T3/pl unknown
- 2012-06-26 EP EP12733368.0A patent/EP2723722B1/en active Active
- 2012-06-26 ES ES12733368.0T patent/ES2553788T3/es active Active
- 2012-06-26 BR BR112013033511-4A patent/BR112013033511B1/pt active IP Right Grant
-
2013
- 2013-12-06 ZA ZA2013/09337A patent/ZA201309337B/en unknown
- 2013-12-08 IL IL229843A patent/IL229843A/en active IP Right Grant
- 2013-12-18 US US14/132,194 patent/US9586910B2/en active Active
- 2013-12-27 CL CL2013003759A patent/CL2013003759A1/es unknown
-
2014
- 2014-01-22 MA MA36704A patent/MA35608B1/fr unknown
- 2014-01-24 CO CO14014367A patent/CO6862155A2/es active IP Right Grant
- 2014-01-24 EC ECSP14013173 patent/ECSP14013173A/es unknown
-
2015
- 2015-12-03 CY CY20151101101T patent/CY1116994T1/el unknown
- 2015-12-08 HR HRP20151346TT patent/HRP20151346T1/hr unknown
-
2016
- 2016-02-24 SM SM201600057T patent/SMT201600057B/xx unknown
- 2016-03-25 JP JP2016061516A patent/JP2016117773A/ja not_active Withdrawn
- 2016-09-29 IL IL248124A patent/IL248124B/en active IP Right Grant
- 2016-12-20 HK HK16114465A patent/HK1226069A1/zh unknown
-
2017
- 2017-03-01 US US15/446,877 patent/US10752597B2/en active Active
- 2017-07-27 AU AU2017208308A patent/AU2017208308A1/en not_active Abandoned
-
2018
- 2018-03-06 JP JP2018039635A patent/JP2018087252A/ja not_active Withdrawn
-
2019
- 2019-05-01 AU AU2019203085A patent/AU2019203085A1/en not_active Abandoned
- 2019-12-16 JP JP2019226645A patent/JP2020055865A/ja active Pending
-
2020
- 2020-03-16 HR HRP20200429TT patent/HRP20200429T1/hr unknown
- 2020-03-17 CY CY20201100243T patent/CY1122860T1/el unknown
- 2020-08-11 US US16/990,176 patent/US11578042B2/en active Active
- 2020-11-20 AU AU2020273343A patent/AU2020273343A1/en not_active Abandoned
-
2021
- 2021-05-19 JP JP2021084641A patent/JP2021120408A/ja not_active Withdrawn
-
2023
- 2023-03-15 JP JP2023041166A patent/JP2023072065A/ja active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20200429T1 (hr) | 3,5-diamino-6-kloro-n-(n-(4-(4-(2-(heksil(2,3,4,5,6-penta-hidroksiheksil)amino)etoksi)fenil)butil)karbamimidoil)pirazin-2-karboksamid | |
JP2014518268A5 (hr) | ||
RU2018138195A (ru) | Соединения 3,5-диамино-6-хлор-n-(n-(4- фенилбутил)карбамимидоил)пиразин-2-карбоксамида | |
JP6392242B2 (ja) | 粘膜への水分付与が不十分であることが好都合である疾患の治療に有用なクロロ−ピラジンカルボキサミド誘導体 | |
ES2708218T3 (es) | Método y formulación para inhalación | |
HRP20171044T1 (hr) | Kemijski i metabolički stabilni dipeptid s potentnom aktivnošću blokatora natrijevog kanala | |
JP2018507914A5 (hr) | ||
JP2014525471A (ja) | 咳および咳発作の治療 | |
US20230113516A1 (en) | 5-amino-2,3-dihydro-1,4-phthalazinedione for treatment of acute lung injury | |
JP2018197263A (ja) | アリールアルキル及びアリールオキシアルキル置換の上皮ナトリウムチャネル遮断化合物 | |
EA201201393A1 (ru) | Ингалятор, разработанный для доставки лекарственного средства в виде сухого порошка | |
HRP20160420T1 (hr) | Kristalni oblik sukcinatne soli | |
CN116419754A (zh) | 用于治疗和预防肺部感染的葡萄糖苷酶抑制剂 | |
ES2647223T3 (es) | Vapendavir para el alivio de los síntomas del asma en un sujeto que tiene una infección por el VRH | |
JP2013522295A5 (hr) | ||
ES2615932T3 (es) | Composición farmacéutica para uso en inhalación que contiene un corticoide y una quinolona o ácido fusídico | |
EP3964207A1 (en) | Antiviral pharmaceutical composition for topical administration | |
RU2020111926A (ru) | Новые составы 2-(имидазол-4-ил)-этанамида пентандиовой-1,5 кислоты для лечения и профилактики вирусных заболеваний | |
JP2023524064A (ja) | ウイルス感染を治療又は予防するためのクロファジミン組成物及び方法 | |
AU2022338350A1 (en) | Formulation | |
WO2022212365A1 (en) | Pyrrolopyrimidine nucleosides for treating or preventing a sars-cov-2 infection | |
RU2019128667A (ru) | Новые составы 2-(имидазол-4-ил)-этанамида пентандиовой-1,5 кислоты для лечения и профилактики вирусных заболеваний |