HRP20180009T1 - Agonisti receptora vazopresina-2 - Google Patents
Agonisti receptora vazopresina-2 Download PDFInfo
- Publication number
- HRP20180009T1 HRP20180009T1 HRP20180009TT HRP20180009T HRP20180009T1 HR P20180009 T1 HRP20180009 T1 HR P20180009T1 HR P20180009T T HRP20180009T T HR P20180009TT HR P20180009 T HRP20180009 T HR P20180009T HR P20180009 T1 HRP20180009 T1 HR P20180009T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound according
- alkyl
- compound
- image
- halogen
- Prior art date
Links
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 208000008967 Enuresis Diseases 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 201000010064 diabetes insipidus Diseases 0.000 claims 2
- 206010029446 nocturia Diseases 0.000 claims 2
- SZUVGFMDDVSKSI-WIFOCOSTSA-N (1s,2s,3s,5r)-1-(carboxymethyl)-3,5-bis[(4-phenoxyphenyl)methyl-propylcarbamoyl]cyclopentane-1,2-dicarboxylic acid Chemical compound O=C([C@@H]1[C@@H]([C@](CC(O)=O)([C@H](C(=O)N(CCC)CC=2C=CC(OC=3C=CC=CC=3)=CC=2)C1)C(O)=O)C(O)=O)N(CCC)CC(C=C1)=CC=C1OC1=CC=CC=C1 SZUVGFMDDVSKSI-WIFOCOSTSA-N 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- UNILWMWFPHPYOR-KXEYIPSPSA-M 1-[6-[2-[3-[3-[3-[2-[2-[3-[[2-[2-[[(2r)-1-[[2-[[(2r)-1-[3-[2-[2-[3-[[2-(2-amino-2-oxoethoxy)acetyl]amino]propoxy]ethoxy]ethoxy]propylamino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-[(2r)-2,3-di(hexadecanoyloxy)propyl]sulfanyl-1-oxopropan-2-yl Chemical compound O=C1C(SCCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CSC[C@@H](COC(=O)CCCCCCCCCCCCCCC)OC(=O)CCCCCCCCCCCCCCC)C(=O)NCC(=O)N[C@H](CO)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O)CC(=O)N1CCNC(=O)CCCCCN\1C2=CC=C(S([O-])(=O)=O)C=C2CC/1=C/C=C/C=C/C1=[N+](CC)C2=CC=C(S([O-])(=O)=O)C=C2C1 UNILWMWFPHPYOR-KXEYIPSPSA-M 0.000 claims 1
- -1 2 - cyclopropyl Chemical group 0.000 claims 1
- 229940126639 Compound 33 Drugs 0.000 claims 1
- PNUZDKCDAWUEGK-CYZMBNFOSA-N Sitafloxacin Chemical compound C([C@H]1N)N(C=2C(=C3C(C(C(C(O)=O)=CN3[C@H]3[C@H](C3)F)=O)=CC=2F)Cl)CC11CC1 PNUZDKCDAWUEGK-CYZMBNFOSA-N 0.000 claims 1
- 229940125773 compound 10 Drugs 0.000 claims 1
- 229940126543 compound 14 Drugs 0.000 claims 1
- 229940125898 compound 5 Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- ZLVXBBHTMQJRSX-VMGNSXQWSA-N jdtic Chemical compound C1([C@]2(C)CCN(C[C@@H]2C)C[C@H](C(C)C)NC(=O)[C@@H]2NCC3=CC(O)=CC=C3C2)=CC=CC(O)=C1 ZLVXBBHTMQJRSX-VMGNSXQWSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/16—Oxytocins; Vasopressins; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Cell Biology (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Epidemiology (AREA)
Claims (16)
1. Spoj formule I:
[image]
ili njegova farmaceutski prihvatljiva sol, naznačen time da:
R2 je H, C1-C4 alkil, halogen, -OH ili -O-C1-C4 alkil;
R3 je H ili -CH2-OH ili -C(O)-NR5R6;
R4 je H ili -C(=NH)-NH2;
R5 i R6 su neovisno H, C1-C6 alkil, -CH2- ciklopropil, - ciklopropil ili arilalkil pod uvjetom da R5 i R6 nisu oba H;
X i Y su neovisno -CH2- ili -S- pod uvjetom da X je -CH2-, Y nije -CH2-;
Z je -CHR7- ili S i R7 je H ili C1-C4 alkil, halogen, -OH ili -O-C1-C4 alkil;
R8 je H ili -CH3; i
Ar je heteroaril ili fenil proizvoljno supstituiran s jednim C1-C4 alkilom, halogenom, -OH ili -O-C1-C4 alkilom.
2. Spoj prema patentnom zahtjevu 1 naznačen time da su R5 i R6 neovisno H, C1-C6 alkil ili arilalkil.
3. Spoj prema patentnom zahtjevu 1 naznačen time da samo X ili samo Y su -S-.
4. Spoj prema patentnom zahtjevu 1 naznačen time da X je -CH2-.
5. Spoj prema patentnom zahtjevu 1 naznačen time da su X i Y oba -S-.
6. Spoj prema bilo kojem od patentnih zahtjeva 1-5 naznačen time da Ar je tiofen.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-6 naznačen time da R8 je -CH3.
8. Spoj prema bilo kojem od patentnih zahtjeva 1-7 naznačen time da R3 je -C(O)-NR5R6.
9. Spoj prema bilo kojem od patentnih zahtjeva 1-8 naznačen time da R5 je H i R6 je C1-C4 alkil.
10. Spoj prema bilo kojem od patentnih zahtjeva 1-8 naznačen time da oba od R5 i R6 su -CH2CH3.
11. Spoj prema bilo kojem od patentnih zahtjeva 1-10 naznačen time da R2 je halogen.
12. Spoj prema patentnom zahtjevu 11 naznačen time da R2 je -Cl.
13. Spoj prema patentnom zahtjevu 11 naznačen time da R2 je -F.
14. Spoj prema patentnom zahtjevu 1 naznačen time da je:
spoj 5
[image]
spoj 10
[image]
spoj 13
[image]
spoj 14
[image]
spoj 21
[image]
ili spoj 33
[image]
15. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1-14 naznačen time da je za upotrebu za liječenje dijabetes insipidusa, primarne noćne enureze ili nokturije.
16. Upotreba spoja prema bilo kojem od patentnih zahtjeva 1-14 naznačena time da je za proizvodnju lijekova za liječenje dijabetes insipidusa, primarne noćne enureze ili nokturije.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361859024P | 2013-07-26 | 2013-07-26 | |
| US201461952073P | 2014-03-12 | 2014-03-12 | |
| PCT/US2014/048317 WO2015013690A1 (en) | 2013-07-26 | 2014-07-25 | Vasopressin-2 receptor agonists |
| EP14755464.6A EP3024829B1 (en) | 2013-07-26 | 2014-07-25 | Vasopressin-2 receptor agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20180009T1 true HRP20180009T1 (hr) | 2018-02-09 |
Family
ID=51398870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20180009TT HRP20180009T1 (hr) | 2013-07-26 | 2018-01-04 | Agonisti receptora vazopresina-2 |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US10131692B2 (hr) |
| EP (1) | EP3024829B1 (hr) |
| JP (1) | JP6387095B2 (hr) |
| KR (1) | KR102198130B1 (hr) |
| CN (1) | CN105492441B (hr) |
| AU (1) | AU2014292860B2 (hr) |
| BR (1) | BR112016000436B1 (hr) |
| CA (1) | CA2919208A1 (hr) |
| DK (1) | DK3024829T3 (hr) |
| EA (1) | EA029392B1 (hr) |
| ES (1) | ES2656039T3 (hr) |
| HK (1) | HK1218647A1 (hr) |
| HR (1) | HRP20180009T1 (hr) |
| HU (1) | HUE035252T2 (hr) |
| IL (1) | IL243730B (hr) |
| JO (1) | JO3371B1 (hr) |
| LT (1) | LT3024829T (hr) |
| MX (1) | MX363355B (hr) |
| MY (1) | MY183429A (hr) |
| PH (1) | PH12016500044B1 (hr) |
| PL (1) | PL3024829T3 (hr) |
| PT (1) | PT3024829T (hr) |
| RS (1) | RS56604B1 (hr) |
| SG (1) | SG11201600031RA (hr) |
| SI (1) | SI3024829T1 (hr) |
| TW (1) | TWI640542B (hr) |
| WO (1) | WO2015013690A1 (hr) |
| ZA (1) | ZA201600145B (hr) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0918652B1 (pt) | 2008-09-17 | 2021-10-19 | Chiasma, Inc. | Composição farmacêutica compreendendo um meio hidrofóbico e uma forma sólida que compreende polipeptídeo e sal de ácido graxo de cadeia média, processo de produção da mesma e forma de dosagem oral |
| US10993984B2 (en) | 2016-10-21 | 2021-05-04 | Chiasma, Inc. | Terlipressin compositions and their methods of use |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE399252B (sv) * | 1976-05-24 | 1978-02-06 | Ferring Ab | Forfarande for framstellnign av antidiuretiskt verkande desamino-asparagin 4-d-arginin8-vasopressin |
| CA1246055A (en) * | 1980-03-24 | 1988-12-06 | Joseph H. Cort | N-.omega.-substituted hormonogens of vasopressin and its synthetic analogs |
| DK153883A (da) | 1982-04-20 | 1983-10-21 | Ceskoslovenska Akademie Ved | Vasopressin-analoge |
| SE501677C2 (sv) | 1993-06-18 | 1995-04-10 | Ferring Bv | Biologiskt aktiva vasopressinanaloger, farmaceutiska preparat innehållande dem samt deras användning för framställning av läkemedel |
| US5500413A (en) * | 1993-06-29 | 1996-03-19 | Ferring Ab | Process for manufacture of 1-deamino-8-D-arginine vasopressin |
| CZ292131B6 (cs) | 2000-02-16 | 2003-08-13 | Ústav organické chemie a biochemie AV ČR | Synthetické analogy Desmopressinu chráněné v C-terminální sekvenci proti karboxyamidasovému štěpení |
-
2014
- 2014-07-24 JO JOP/2014/0234A patent/JO3371B1/ar active
- 2014-07-25 LT LTEP14755464.6T patent/LT3024829T/lt unknown
- 2014-07-25 HU HUE14755464A patent/HUE035252T2/en unknown
- 2014-07-25 ES ES14755464.6T patent/ES2656039T3/es active Active
- 2014-07-25 CA CA2919208A patent/CA2919208A1/en not_active Abandoned
- 2014-07-25 PT PT147554646T patent/PT3024829T/pt unknown
- 2014-07-25 EP EP14755464.6A patent/EP3024829B1/en active Active
- 2014-07-25 KR KR1020167003247A patent/KR102198130B1/ko active IP Right Grant
- 2014-07-25 BR BR112016000436-1A patent/BR112016000436B1/pt active IP Right Grant
- 2014-07-25 PL PL14755464T patent/PL3024829T3/pl unknown
- 2014-07-25 MX MX2016000525A patent/MX363355B/es unknown
- 2014-07-25 CN CN201480041380.1A patent/CN105492441B/zh active Active
- 2014-07-25 MY MYPI2016700251A patent/MY183429A/en unknown
- 2014-07-25 JP JP2016530091A patent/JP6387095B2/ja active Active
- 2014-07-25 US US14/647,357 patent/US10131692B2/en active Active
- 2014-07-25 TW TW103125533A patent/TWI640542B/zh active
- 2014-07-25 SI SI201430496T patent/SI3024829T1/en unknown
- 2014-07-25 AU AU2014292860A patent/AU2014292860B2/en active Active
- 2014-07-25 DK DK14755464.6T patent/DK3024829T3/en active
- 2014-07-25 EA EA201690219A patent/EA029392B1/ru not_active IP Right Cessation
- 2014-07-25 SG SG11201600031RA patent/SG11201600031RA/en unknown
- 2014-07-25 WO PCT/US2014/048317 patent/WO2015013690A1/en active Application Filing
- 2014-07-25 RS RS20171214A patent/RS56604B1/sr unknown
-
2016
- 2016-01-07 PH PH12016500044A patent/PH12016500044B1/en unknown
- 2016-01-08 ZA ZA2016/00145A patent/ZA201600145B/en unknown
- 2016-01-22 IL IL243730A patent/IL243730B/en active IP Right Grant
- 2016-06-08 HK HK16106599.4A patent/HK1218647A1/zh unknown
-
2018
- 2018-01-04 HR HRP20180009TT patent/HRP20180009T1/hr unknown
- 2018-09-27 US US16/145,073 patent/US10745443B2/en active Active
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