CA2965566A1 - Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (sstr4) agonists - Google Patents

Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (sstr4) agonists Download PDF

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Publication number
CA2965566A1
CA2965566A1 CA2965566A CA2965566A CA2965566A1 CA 2965566 A1 CA2965566 A1 CA 2965566A1 CA 2965566 A CA2965566 A CA 2965566A CA 2965566 A CA2965566 A CA 2965566A CA 2965566 A1 CA2965566 A1 CA 2965566A1
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CA
Canada
Prior art keywords
mmol
group
alkyl
hplc
acid
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2965566A
Other languages
English (en)
French (fr)
Inventor
Rocco Mazzaferro
Marco Ferrara
Riccardo Giovannini
Iain Lingard
Klaus Rudolf
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim International GmbH
Original Assignee
Boehringer Ingelheim International GmbH
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.)
Filing date
Publication date
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of CA2965566A1 publication Critical patent/CA2965566A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CA2965566A 2014-11-14 2015-11-12 Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (sstr4) agonists Abandoned CA2965566A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14193185 2014-11-14
EP14193185.7 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 (1)

Publication Number Publication Date
CA2965566A1 true CA2965566A1 (en) 2016-05-19

Family

ID=51904765

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2965566A Abandoned CA2965566A1 (en) 2014-11-14 2015-11-12 Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (sstr4) agonists

Country Status (14)

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

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2699580T3 (enExample) 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
EP3824906A1 (en) 2016-12-21 2021-05-26 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
WO2018209267A2 (en) 2017-05-12 2018-11-15 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
PT3758708T (pt) 2018-03-01 2025-02-13 Astrazeneca Ab Composições farmacêuticas compreendendo (2s)-{(1,s)-1-ciano-2-[4-(3-metil-2-oxo-2,3-di-hidro-1,3-benzoxazol-5-il)fenil]etil}-1,4-oxazepano-2-carboxamida
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
CA3106269A1 (en) 2018-07-17 2020-01-23 Insmed Incorporated Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating lupus nephritis
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
TWI910192B (zh) * 2020-07-13 2026-01-01 大陸商廣州費米子科技有限責任公司 含氮雜環化合物、藥物組合物和應用
TWI860849B (zh) 2021-09-14 2024-11-01 美商美國禮來大藥廠 Sstr4促效劑鹽
CN117209492B (zh) * 2022-12-21 2026-06-30 睿辰康达生物医药(武汉)有限公司 一种制备苯并五元含氮杂环类化合物的方法
JP2026503035A (ja) 2023-01-06 2026-01-27 インスメッド インコーポレイテッド 新規な可逆性ｄｐｐ１阻害剤及びその用途
IL326196A (en) 2023-08-02 2026-03-01 Boehringer Ingelheim Int (2S, 5R)-5-(hydroxymethyl)morpholine-2-carboxamides as SSTR4 agonists
WO2025162472A1 (en) 2024-01-31 2025-08-07 Insmed Incorporated Linear dipeptidyl peptidase 1 inhibitors and uses thereof
WO2025247982A1 (en) 2024-05-29 2025-12-04 Grünenthal GmbH Piperazines which act as sstr4 modulators

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE538124T1 (de) * 2004-11-12 2012-01-15 Bristol Myers Squibb Co Imidazokondensierte tricyclische verbindungen auf thiazoloä4,5-büpyridin-basis und pharmazeutische zusammensetzungen damit
WO2010059922A1 (en) 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds
AU2012226375B2 (en) 2011-03-10 2017-04-13 Lupin Atlantis Holdings Sa Substituted morpholines as modulators for the calcium sensing receptor

Also Published As

Publication number Publication date
EA201791058A1 (ru) 2017-11-30
CN107108592B (zh) 2021-01-29
BR112017009595A2 (pt) 2017-12-19
CN107108592A (zh) 2017-08-29
US10577336B2 (en) 2020-03-03
EP3218372B1 (en) 2020-05-20
JP6641367B2 (ja) 2020-02-05
MX370366B (es) 2019-12-11
WO2016075240A1 (en) 2016-05-19
AU2015345070A1 (en) 2017-04-20
US20170320838A1 (en) 2017-11-09
CL2017001181A1 (es) 2018-02-02
JP2017533930A (ja) 2017-11-16
EA032104B1 (ru) 2019-04-30
PH12017500821A1 (en) 2017-10-02
US10071974B2 (en) 2018-09-11
IL251465A0 (en) 2017-05-29
KR20170082632A (ko) 2017-07-14
US20180339971A1 (en) 2018-11-29
EP3218372A1 (en) 2017-09-20
MX2017006231A (es) 2017-07-31

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20220203