HRP20200307T1 - Novi derivati pirolidina - Google Patents

Novi derivati pirolidina Download PDF

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Publication number
HRP20200307T1
HRP20200307T1 HRP20200307TT HRP20200307T HRP20200307T1 HR P20200307 T1 HRP20200307 T1 HR P20200307T1 HR P20200307T T HRP20200307T T HR P20200307TT HR P20200307 T HRP20200307 T HR P20200307T HR P20200307 T1 HRP20200307 T1 HR P20200307T1
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HR
Croatia
Prior art keywords
compound according
diabetes
trifluoromethyl
treatment
compound
Prior art date
Application number
HRP20200307TT
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English (en)
Inventor
Wolfgang Haap
Bernd Kuhn
Thomas Luebbers
Jens-Uwe Peters
Original Assignee
F. Hoffmann - La Roche Ag
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
Application filed by F. Hoffmann - La Roche Ag filed Critical F. Hoffmann - La Roche Ag
Publication of HRP20200307T1 publication Critical patent/HRP20200307T1/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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41921,2,3-Triazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)

Claims (5)

1. Spoj, naznačen time, da je predstavljen formulom (1-cijano ciklopropil)-amid (2S, 4R)-4-[4-(5-metil-tetrazol-2-il)-2-trifluorometil-benzensulfonil]-1-(1-trifluorometil-ciklopropankarbonil)-pirolidin-2-karboksilne kiseline ili njegova farmaceutski prihvatljiva sol ili njegov ester.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da je za uporabu kao terapeutski aktivna tvar.
3. Farmaceutski pripravak, naznačen time, da sadrži spoj prema patentnom zahtjevu 1 i terapeutski inertni nosač.
4. Spoj prema patentnom zahtjevu 1, naznačen time, da se upotrebljava za liječenje ili profilaksu dijabetesa, ateroskleroze, aneurizme trbušne aorte, periferne arterijske bolesti, raka, smanjenja kardiovaskularnih događaja u kroničnoj bolesti bubrega, dijabetičke nefropatije, dijabetičke retinopatije ili senilne makularne degeneracije.
5. Spoj prema patentnom zahtjevu 1, naznačen time, da se upotrebljava u liječenju bolesti posredovanih imunološkim mehanizmima, posebice reumatoidnog artritisa, multiple skleroze, Sjorgen sindroma, eritematoznog lupusa, neuropatske boli, dijabetesa tipa I, astme te alergija i kožnih imunoloških bolesti.
HRP20200307TT 2016-02-26 2020-02-24 Novi derivati pirolidina HRP20200307T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16157679 2016-02-26
EP17705662.9A EP3419970B1 (en) 2016-02-26 2017-02-22 Novel pyrrolidine derivatives
PCT/EP2017/053967 WO2017144483A1 (en) 2016-02-26 2017-02-22 Novel pyrrolidine derivatives

Publications (1)

Publication Number Publication Date
HRP20200307T1 true HRP20200307T1 (hr) 2020-06-12

Family

ID=55443159

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20200307TT HRP20200307T1 (hr) 2016-02-26 2020-02-24 Novi derivati pirolidina

Country Status (31)

Country Link
US (1) US10689339B2 (hr)
EP (1) EP3419970B1 (hr)
JP (1) JP6952044B2 (hr)
KR (1) KR20180111862A (hr)
CN (1) CN108699044B (hr)
AR (1) AR107717A1 (hr)
AU (1) AU2017224343B2 (hr)
CA (1) CA3011652C (hr)
CL (1) CL2018002347A1 (hr)
CO (1) CO2018007756A2 (hr)
CR (1) CR20180404A (hr)
DK (1) DK3419970T3 (hr)
ES (1) ES2775781T3 (hr)
HR (1) HRP20200307T1 (hr)
HU (1) HUE047842T2 (hr)
IL (1) IL260130B (hr)
LT (1) LT3419970T (hr)
MA (1) MA43667B1 (hr)
MX (1) MX2018009638A (hr)
MY (1) MY196560A (hr)
PH (1) PH12018501585B1 (hr)
PL (1) PL3419970T3 (hr)
PT (1) PT3419970T (hr)
RS (1) RS59938B1 (hr)
RU (1) RU2736498C1 (hr)
SG (1) SG11201807074VA (hr)
SI (1) SI3419970T1 (hr)
TW (1) TWI740903B (hr)
UA (1) UA122084C2 (hr)
WO (1) WO2017144483A1 (hr)
ZA (1) ZA201804120B (hr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102553613B1 (ko) 2017-01-24 2023-07-07 아스테라스 세이야쿠 가부시키가이샤 페닐디플루오로메틸 치환 프롤린아미드 화합물
AR114732A1 (es) 2018-09-18 2020-10-07 Hoffmann La Roche Utilización de un inhibidor de catepsina s contra la formación de anticuerpos antifármaco

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20120911A1 (es) * 2009-04-20 2012-08-06 Hoffmann La Roche Derivados de prolina como inhibidores de catepsina
PL2776392T3 (pl) * 2011-11-11 2016-11-30 Sposób wytwarzania pochodnych 1-acylo-4-fenylosulfonyloprolinoamidu i nowe związki pośrednie
JP2014533707A (ja) * 2011-11-25 2014-12-15 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft カテプシンの阻害剤としての新規ピロリジン誘導体
CN104114068B (zh) * 2011-12-09 2017-07-11 W.C.布拉德利公司 具有可调整的加热特征的烹饪炉排
CA2859928A1 (en) * 2012-02-17 2013-08-22 F. Hoffmann-La Roche Ag Novel pyrrolidine derivatives
KR20150044947A (ko) * 2012-08-21 2015-04-27 에프. 호프만-라 로슈 아게 신규한 피리딘 유도체

Also Published As

Publication number Publication date
CL2018002347A1 (es) 2018-11-30
UA122084C2 (uk) 2020-09-10
IL260130B (en) 2020-08-31
MY196560A (en) 2023-04-19
HUE047842T2 (hu) 2020-05-28
PT3419970T (pt) 2020-02-28
DK3419970T3 (da) 2020-03-02
CA3011652A1 (en) 2017-08-31
AU2017224343A1 (en) 2018-07-05
JP6952044B2 (ja) 2021-10-20
CA3011652C (en) 2024-01-09
CO2018007756A2 (es) 2018-10-10
TWI740903B (zh) 2021-10-01
ES2775781T3 (es) 2020-07-28
MA43667B1 (fr) 2020-03-31
US10689339B2 (en) 2020-06-23
CN108699044B (zh) 2022-03-04
EP3419970A1 (en) 2019-01-02
PH12018501585A1 (en) 2019-04-08
JP2019506416A (ja) 2019-03-07
AU2017224343B2 (en) 2020-09-10
KR20180111862A (ko) 2018-10-11
PH12018501585B1 (en) 2019-04-08
ZA201804120B (en) 2020-07-29
SG11201807074VA (en) 2018-09-27
US20180362461A1 (en) 2018-12-20
RS59938B1 (sr) 2020-03-31
WO2017144483A1 (en) 2017-08-31
RU2736498C1 (ru) 2020-11-17
CR20180404A (es) 2018-10-18
IL260130A (en) 2018-07-31
SI3419970T1 (sl) 2020-04-30
LT3419970T (lt) 2020-03-10
AR107717A1 (es) 2018-05-23
TW201733981A (zh) 2017-10-01
MX2018009638A (es) 2018-09-11
CN108699044A (zh) 2018-10-23
PL3419970T3 (pl) 2020-06-01
EP3419970B1 (en) 2020-01-01

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