HRP20200119T1 - Azetidiniloksifenilpirolidinski spojevi - Google Patents

Azetidiniloksifenilpirolidinski spojevi Download PDF

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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
Application number
HRP20200119TT
Other languages
English (en)
Inventor
Gary G. Deng
Danwen Huang
Cynthia Darshini Jesudason
Joshua O. Odingo
Original Assignee
Eli Lilly And Company
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=54140711&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20200119(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Eli Lilly And Company filed Critical Eli Lilly And Company
Publication of HRP20200119T1 publication Critical patent/HRP20200119T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • 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.
HRP20200119TT 2014-09-12 2020-01-24 Azetidiniloksifenilpirolidinski spojevi HRP20200119T1 (hr)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
LT3191466T (lt) 2020-02-25
MX2017003138A (es) 2017-05-23
ECSP17014972A (es) 2018-03-31
AU2015315533B2 (en) 2018-03-15
EA030034B1 (ru) 2018-06-29
PE20170328A1 (es) 2017-04-19
IL250378A0 (en) 2017-03-30
HUE047551T2 (hu) 2020-04-28
CN106795137A (zh) 2017-05-31
TW201625591A (zh) 2016-07-16
EP3191466A1 (en) 2017-07-19
US10781202B2 (en) 2020-09-22
TN2017000047A1 (en) 2018-07-04
DK3191466T3 (da) 2020-01-20
JP2017527587A (ja) 2017-09-21
SG11201701225YA (en) 2017-03-30
CN106795137B (zh) 2020-08-25
AP2017009778A0 (en) 2017-03-31
EA201790156A1 (ru) 2017-06-30
BR112017002852A2 (pt) 2017-12-26
SI3191466T1 (sl) 2020-02-28
CA2955634A1 (en) 2016-03-17
EP3191466B1 (en) 2019-12-04
US20200002318A1 (en) 2020-01-02
CL2017000484A1 (es) 2017-11-10
ES2770047T3 (es) 2020-06-30
AR101696A1 (es) 2017-01-04
PT3191466T (pt) 2020-02-17
NZ729087A (en) 2018-07-27
JP6285610B2 (ja) 2018-02-28
PL3191466T3 (pl) 2020-05-18
ZA201700555B (en) 2018-12-19
KR20170040803A (ko) 2017-04-13
CO2017001389A2 (es) 2017-05-10
US20170240532A1 (en) 2017-08-24
AU2015315533A1 (en) 2017-02-23
PH12017500459A1 (en) 2017-07-31
RS59845B1 (sr) 2020-02-28
KR101857931B1 (ko) 2018-05-14
CR20170050A (es) 2017-04-25
WO2016040083A1 (en) 2016-03-17

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