HRP20200119T1 - Azetidiniloksifenilpirolidinski spojevi - Google Patents
Azetidiniloksifenilpirolidinski spojevi Download PDFInfo
- Publication number
- HRP20200119T1 HRP20200119T1 HRP20200119TT HRP20200119T HRP20200119T1 HR P20200119 T1 HRP20200119 T1 HR P20200119T1 HR P20200119T T HRP20200119T T HR P20200119TT HR P20200119 T HRP20200119 T HR P20200119T HR P20200119 T1 HRP20200119 T1 HR P20200119T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- pharmaceutically acceptable
- salt
- acceptable salt
- compound according
- Prior art date
Links
- WVEMMKKRMPLVQC-UHFFFAOYSA-N 2-(azetidin-1-yloxy)-1-phenylpyrrolidine Chemical class C1CCN1OC1N(C=2C=CC=CC=2)CCC1 WVEMMKKRMPLVQC-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 9
- 206010020853 Hypertonic bladder Diseases 0.000 claims 2
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000020629 overactive bladder Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- IEHKWSGCTWLXFU-IIBYNOLFSA-N tadalafil Chemical compound C1=C2OCOC2=CC([C@@H]2C3=C([C]4C=CC=CC4=N3)C[C@H]3N2C(=O)CN(C3=O)C)=C1 IEHKWSGCTWLXFU-IIBYNOLFSA-N 0.000 claims 2
- 229960000835 tadalafil Drugs 0.000 claims 2
- JIEGENLGWZJCAL-XHGXUTKZSA-N COC1=C(OC2CN(C2)C2=NC=C(Cl)C=C2)C=C(C=C1)[C@@H]1CN(C[C@@]1(C)[C@@H](C)O)C(=O)[C@@H](O)CO Chemical compound COC1=C(OC2CN(C2)C2=NC=C(Cl)C=C2)C=C(C=C1)[C@@H]1CN(C[C@@]1(C)[C@@H](C)O)C(=O)[C@@H](O)CO JIEGENLGWZJCAL-XHGXUTKZSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (11)
1. Spoj formule
,
naznačen time što
R je
R1 je CH3, CD3, CN, Cl ili CF3;
uz uvjet da kada je R1 CH3 ili CD3, nije vezan na položaju 5;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj ili sol u skladu s patentnim zahtjevom 1, naznačen time što ima formulu
.
3. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je R
.
4. Spoj ili sol u skladu s patentnim zahtjevom 1, 2 ili 3, naznačen time što je R1 Cl.
5. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je R
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1-5, naznačen time što je (2S)-3-[(3S,4S)-3-[(1R)-1-hidroksietil]-4-(4-metoksi-3-{[1-(5-klorpiridin-2-il)azetidin-3-il]oksi}fenil)-3-metilpirolidin-1-il]-3-oksopropan-1,2-diol.
7. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivi nosač, razrjeđivač ili pomoćnu tvar.
8. Farmaceutski pripravak, naznačen time što sadrži prvu komponentu, koja je spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol, i drugu komponentu, koja je tadalafil, kao i farmaceutski prihvatljivi nosač, razrjeđivač ili pomoćnu tvar.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u terapiji.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenje hiperaktivnog mokraćnog mjehura.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time što je namijenjen istodobnoj, odvojenoj ili uzastopnoj upotrebi u kombinaciji s tadalafilom u liječenju hiperaktivnog mokraćnog mjehura.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462049485P | 2014-09-12 | 2014-09-12 | |
EP15763763.8A EP3191466B1 (en) | 2014-09-12 | 2015-09-03 | Azetidinyloxyphenylpyrrolidine compounds |
PCT/US2015/048267 WO2016040083A1 (en) | 2014-09-12 | 2015-09-03 | Azetidinyloxyphenylpyrrolidine compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20200119T1 true HRP20200119T1 (hr) | 2020-04-03 |
Family
ID=54140711
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20200119TT HRP20200119T1 (hr) | 2014-09-12 | 2020-01-24 | Azetidiniloksifenilpirolidinski spojevi |
Country Status (34)
Country | Link |
---|---|
US (2) | US10781202B2 (hr) |
EP (1) | EP3191466B1 (hr) |
JP (1) | JP6285610B2 (hr) |
KR (1) | KR101857931B1 (hr) |
CN (1) | CN106795137B (hr) |
AP (1) | AP2017009778A0 (hr) |
AR (1) | AR101696A1 (hr) |
AU (1) | AU2015315533B2 (hr) |
BR (1) | BR112017002852A2 (hr) |
CA (1) | CA2955634A1 (hr) |
CL (1) | CL2017000484A1 (hr) |
CO (1) | CO2017001389A2 (hr) |
CR (1) | CR20170050A (hr) |
DK (1) | DK3191466T3 (hr) |
EA (1) | EA030034B1 (hr) |
EC (1) | ECSP17014972A (hr) |
ES (1) | ES2770047T3 (hr) |
HR (1) | HRP20200119T1 (hr) |
HU (1) | HUE047551T2 (hr) |
IL (1) | IL250378A0 (hr) |
LT (1) | LT3191466T (hr) |
MX (1) | MX2017003138A (hr) |
NZ (1) | NZ729087A (hr) |
PE (1) | PE20170328A1 (hr) |
PH (1) | PH12017500459A1 (hr) |
PL (1) | PL3191466T3 (hr) |
PT (1) | PT3191466T (hr) |
RS (1) | RS59845B1 (hr) |
SG (1) | SG11201701225YA (hr) |
SI (1) | SI3191466T1 (hr) |
TN (1) | TN2017000047A1 (hr) |
TW (1) | TW201625591A (hr) |
WO (1) | WO2016040083A1 (hr) |
ZA (1) | ZA201700555B (hr) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108707140B (zh) | 2013-03-14 | 2022-07-22 | 勃林格殷格翰国际有限公司 | 蛋白酶c抑制剂 |
EA031376B1 (ru) | 2014-09-12 | 2018-12-28 | Бёрингер Ингельхайм Интернациональ Гмбх | Спироциклические ингибиторы катепсина с |
CN111333637B (zh) * | 2018-12-18 | 2022-07-29 | 武汉人福创新药物研发中心有限公司 | 苯基吡咯烷类衍生物及其制备方法 |
CN111333625B (zh) * | 2018-12-18 | 2022-10-18 | 武汉人福创新药物研发中心有限公司 | 苯基吡咯烷类化合物及其用途 |
CA3123995C (en) * | 2018-12-18 | 2023-05-23 | Wuhan Humanwell Innovative Drug Research and Development Center Limited Company | Phenylpyrrolidine compound and use thereof |
CN112409333A (zh) * | 2019-08-23 | 2021-02-26 | 湖北生物医药产业技术研究院有限公司 | 苯基吡咯烷类化合物 |
KR20240004495A (ko) | 2021-04-29 | 2024-01-11 | 쑤저우 선카디아 바이오파마수티컬즈 컴퍼니 리미티드 | 이소퀴놀론 화합물과 이의 용도 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6258833B1 (en) * | 1999-12-23 | 2001-07-10 | Icos Corporation | Cyclic AMP-specific phosphodiesterase inhibitors |
EE200300362A (et) * | 2001-01-31 | 2003-12-15 | Pfizer Products Inc. | PDE4 isosüümide inhibiitoritena kasutatavad tiasolüül-, oksasolüül-, pürrolüül- ja imidasolüülhappeamiidi derivaadid |
US20090186896A1 (en) | 2005-09-29 | 2009-07-23 | Bayer Healthcare Ag | PDE Inhibitors and Combinations Thereof for the Treatment of Urological Disorders |
TW201206440A (en) | 2010-04-28 | 2012-02-16 | Astellas Pharma Inc | Prophylactic or therapeutic agent for diseases associated with pains in urinary organs |
JO3264B1 (ar) * | 2013-03-13 | 2018-09-16 | Lilly Co Eli | مركبات ازيتيدينيل أوكسي فينيل بيروليدين |
WO2016033776A1 (en) * | 2014-09-04 | 2016-03-10 | Eli Lilly And Company | Crystalline (2s) -3- [ (3s, 4s) -3- [ (1r) -1-hydroxyethyl] -4- (4-methoxy-3- { [1- (5-methylpyridin-2-yl) azetidin-3-yl] oxy} phenyl) -3-methylpyrrolidin-1-yl] -3-oxopropane-1, 2-diol |
-
2015
- 2015-08-26 AR ARP150102734A patent/AR101696A1/es unknown
- 2015-08-26 TW TW104127990A patent/TW201625591A/zh unknown
- 2015-09-03 SI SI201531038T patent/SI3191466T1/sl unknown
- 2015-09-03 CA CA2955634A patent/CA2955634A1/en not_active Abandoned
- 2015-09-03 EA EA201790156A patent/EA030034B1/ru not_active IP Right Cessation
- 2015-09-03 MX MX2017003138A patent/MX2017003138A/es unknown
- 2015-09-03 SG SG11201701225YA patent/SG11201701225YA/en unknown
- 2015-09-03 PE PE2017000243A patent/PE20170328A1/es unknown
- 2015-09-03 CN CN201580046264.3A patent/CN106795137B/zh active Active
- 2015-09-03 AU AU2015315533A patent/AU2015315533B2/en not_active Ceased
- 2015-09-03 EP EP15763763.8A patent/EP3191466B1/en active Active
- 2015-09-03 DK DK15763763.8T patent/DK3191466T3/da active
- 2015-09-03 PL PL15763763T patent/PL3191466T3/pl unknown
- 2015-09-03 LT LTEP15763763.8T patent/LT3191466T/lt unknown
- 2015-09-03 NZ NZ729087A patent/NZ729087A/en not_active IP Right Cessation
- 2015-09-03 KR KR1020177006717A patent/KR101857931B1/ko active IP Right Grant
- 2015-09-03 HU HUE15763763A patent/HUE047551T2/hu unknown
- 2015-09-03 BR BR112017002852A patent/BR112017002852A2/pt not_active Application Discontinuation
- 2015-09-03 TN TN2017000047A patent/TN2017000047A1/en unknown
- 2015-09-03 CR CR20170050A patent/CR20170050A/es unknown
- 2015-09-03 JP JP2017513639A patent/JP6285610B2/ja active Active
- 2015-09-03 AP AP2017009778A patent/AP2017009778A0/en unknown
- 2015-09-03 RS RS20200096A patent/RS59845B1/sr unknown
- 2015-09-03 US US15/506,017 patent/US10781202B2/en active Active
- 2015-09-03 ES ES15763763T patent/ES2770047T3/es active Active
- 2015-09-03 WO PCT/US2015/048267 patent/WO2016040083A1/en active Application Filing
- 2015-09-03 PT PT157637638T patent/PT3191466T/pt unknown
-
2017
- 2017-01-24 ZA ZA2017/00555A patent/ZA201700555B/en unknown
- 2017-01-31 IL IL250378A patent/IL250378A0/en unknown
- 2017-02-13 CO CONC2017/0001389A patent/CO2017001389A2/es unknown
- 2017-03-01 CL CL2017000484A patent/CL2017000484A1/es unknown
- 2017-03-10 PH PH12017500459A patent/PH12017500459A1/en unknown
- 2017-03-14 EC ECIEPI201714972A patent/ECSP17014972A/es unknown
-
2019
- 2019-09-13 US US16/570,422 patent/US20200002318A1/en not_active Abandoned
-
2020
- 2020-01-24 HR HRP20200119TT patent/HRP20200119T1/hr unknown
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