EA032104B1 - Морфолин- и 1,4-оксазепан-амиды в качестве агонистов соматостатинового рецептора подтипа 4 (sstr4) - Google Patents

Морфолин- и 1,4-оксазепан-амиды в качестве агонистов соматостатинового рецептора подтипа 4 (sstr4) Download PDF

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Publication number
EA032104B1
EA032104B1 EA201791058A EA201791058A EA032104B1 EA 032104 B1 EA032104 B1 EA 032104B1 EA 201791058 A EA201791058 A EA 201791058A EA 201791058 A EA201791058 A EA 201791058A EA 032104 B1 EA032104 B1 EA 032104B1
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Eurasian Patent Office
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mmol
hplc
group
compound according
compound
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EA201791058A
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English (en)
Russian (ru)
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EA201791058A1 (ru
Inventor
Рокко Маццаферро
Марко Феррара
Риккардо Джованнини
Айан Лингард
Клаус Рудольф
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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Publication of EA201791058A1 publication Critical patent/EA201791058A1/ru
Publication of EA032104B1 publication Critical patent/EA032104B1/ru

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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
EA201791058A 2014-11-14 2015-11-12 Морфолин- и 1,4-оксазепан-амиды в качестве агонистов соматостатинового рецептора подтипа 4 (sstr4) EA032104B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14193185 2014-11-14
PCT/EP2015/076440 WO2016075240A1 (en) 2014-11-14 2015-11-12 Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (sstr4) agonists

Publications (2)

Publication Number Publication Date
EA201791058A1 EA201791058A1 (ru) 2017-11-30
EA032104B1 true EA032104B1 (ru) 2019-04-30

Family

ID=51904765

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201791058A EA032104B1 (ru) 2014-11-14 2015-11-12 Морфолин- и 1,4-оксазепан-амиды в качестве агонистов соматостатинового рецептора подтипа 4 (sstr4)

Country Status (14)

Country Link
US (2) US10071974B2 (Direct)
EP (1) EP3218372B1 (Direct)
JP (1) JP6641367B2 (Direct)
KR (1) KR20170082632A (Direct)
CN (1) CN107108592B (Direct)
AU (1) AU2015345070A1 (Direct)
BR (1) BR112017009595A2 (Direct)
CA (1) CA2965566A1 (Direct)
CL (1) CL2017001181A1 (Direct)
EA (1) EA032104B1 (Direct)
IL (1) IL251465A0 (Direct)
MX (1) MX370366B (Direct)
PH (1) PH12017500821A1 (Direct)
WO (1) WO2016075240A1 (Direct)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2699580T3 (Direct) 2014-01-24 2018-02-24
EP3053452A1 (en) * 2015-01-16 2016-08-10 Interquim, S.A. Naturally derived colour stabilizer
WO2018022978A1 (en) * 2016-07-29 2018-02-01 Insmed Incorporated Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating bronchiectasis
US20200087390A1 (en) 2016-12-21 2020-03-19 Amgen Inc. Anti-tnf alpha antibody formulations
US11912687B2 (en) 2017-05-12 2024-02-27 Board of Trustees of the Southern Illinois University 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
EP3634406B1 (en) 2017-05-12 2023-09-06 Board of Trustees of The Southern Illinois University on behalf of Southern Illinois University Edwardsville 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
FI3758708T3 (fi) 2018-03-01 2025-02-18 Astrazeneca Ab (2s)-{(1s)-1-syano-2-[4-(3-metyyli-2-okso-2,3-dihydro-1,3-bentsoksatsol-5-yyli)fenyyli]etyyli}-1,4-oksatsepaani-2-karboksamidia käsittäviä farmaseuttisia koostumuksia
TWI834637B (zh) * 2018-03-01 2024-03-11 日商武田藥品工業有限公司 六氫吡啶基-3-(芳氧基)丙醯胺及丙酸酯
KR20210032431A (ko) 2018-07-17 2021-03-24 인스메드 인코포레이티드 루푸스 신염을 치료하기 위한 특정 (2s)-n-[(1s)-1-시아노-2-페닐에틸]-1,4-옥사제판-2-카복스아미드
AR121683A1 (es) * 2020-03-31 2022-06-29 Takeda Pharmaceuticals Co Derivados de n-heteroarilalquil-2-(heterociclil y heterociclilmetil)acetamida como agonistas de sstr4
CN113717161B (zh) * 2020-05-21 2023-06-09 广州费米子科技有限责任公司 含氮饱和杂环化合物及其制备方法、药物组合物和应用
WO2022012534A1 (zh) * 2020-07-13 2022-01-20 广州费米子科技有限责任公司 含氮杂环化合物、药物组合物和应用
AR127055A1 (es) 2021-09-14 2023-12-13 Lilly Co Eli Sales agonistas de sstr4
EP4646265A1 (en) 2023-01-06 2025-11-12 Insmed Incorporated Novel, reversible dpp1 inhibitors and uses thereof
WO2025027049A1 (en) 2023-08-02 2025-02-06 Boehringer Ingelheim International Gmbh (2s,5r)-5-(hydroxymethyl)morpholine-2-carboxamides as agonists of sstr4
WO2025247982A1 (en) 2024-05-29 2025-12-04 Grünenthal GmbH Piperazines which act as sstr4 modulators

Citations (1)

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WO2010059922A1 (en) * 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds

Family Cites Families (2)

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ES2377758T3 (es) * 2004-11-12 2012-03-30 Bristol-Myers Squibb Company Compuestos tricíclicos basados en tiazolo[4,5-b]piridina imidazo-fusionada y composiciones farmacéuticas que los comprenden
WO2012120476A1 (en) 2011-03-10 2012-09-13 Lupin Limited Substituted morpholines as modulators for the calcium sensing receptor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010059922A1 (en) * 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CRIDER A MICHAEL; WITT KEN A: "Somatostatin sst4 ligands: chemistry and pharmacology.", MINI REVIEWS IN MEDICINAL CHEMISTRY, BENTHAM SCIENCE PUBL, NL, vol. 7, no. 3, 1 March 2007 (2007-03-01), NL, pages 213 - 220, XP009129242, ISSN: 1389-5575 *

Also Published As

Publication number Publication date
JP2017533930A (ja) 2017-11-16
JP6641367B2 (ja) 2020-02-05
US10577336B2 (en) 2020-03-03
AU2015345070A1 (en) 2017-04-20
US20180339971A1 (en) 2018-11-29
MX2017006231A (es) 2017-07-31
CN107108592B (zh) 2021-01-29
KR20170082632A (ko) 2017-07-14
CL2017001181A1 (es) 2018-02-02
EP3218372B1 (en) 2020-05-20
US10071974B2 (en) 2018-09-11
MX370366B (es) 2019-12-11
CN107108592A (zh) 2017-08-29
EA201791058A1 (ru) 2017-11-30
WO2016075240A1 (en) 2016-05-19
EP3218372A1 (en) 2017-09-20
BR112017009595A2 (pt) 2017-12-19
PH12017500821A1 (en) 2017-10-02
CA2965566A1 (en) 2016-05-19
IL251465A0 (en) 2017-05-29
US20170320838A1 (en) 2017-11-09

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU