HRP20210402T1 - Spojevi - Google Patents
Spojevi Download PDFInfo
- Publication number
- HRP20210402T1 HRP20210402T1 HRP20210402TT HRP20210402T HRP20210402T1 HR P20210402 T1 HRP20210402 T1 HR P20210402T1 HR P20210402T T HRP20210402T T HR P20210402TT HR P20210402 T HRP20210402 T HR P20210402T HR P20210402 T1 HRP20210402 T1 HR P20210402T1
- Authority
- HR
- Croatia
- Prior art keywords
- hydrogen
- compound
- halogen
- alkyl
- substituted
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 208000004554 Leishmaniasis Diseases 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000030852 Parasitic disease Diseases 0.000 claims 2
- 206010047505 Visceral leishmaniasis Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 208000029080 human African trypanosomiasis Diseases 0.000 claims 2
- -1 hydroxy, methoxy Chemical group 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- GJVFBWCTGUSGDD-UHFFFAOYSA-L pentamethonium bromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCC[N+](C)(C)C GJVFBWCTGUSGDD-UHFFFAOYSA-L 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000000230 African Trypanosomiasis Diseases 0.000 claims 1
- 206010001935 American trypanosomiasis Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 208000024699 Chagas disease Diseases 0.000 claims 1
- 241000222727 Leishmania donovani Species 0.000 claims 1
- 241000223105 Trypanosoma brucei Species 0.000 claims 1
- 241000223109 Trypanosoma cruzi Species 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000002612 sleeping sickness Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- 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
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/14—Ectoparasiticides, e.g. scabicides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (15)
1. Spoj Formule (I),
[image]
,
ili njegova sol,
naznačen time što
A1 je CH;
A2 se bira između CR13 i N;
R1 se bira između C1-C6alkila, C3-C7cikloalkila, C4-C7heterocikloalkila, fenila, C5-C6heteroarila, C1-C6alkoksi, -OC3-C7cikloalkila i NR10aR10b; gdje C3-C7cikloalkil, C4-C7heterocikloalkil, fenil, C5-C6heteroaril i -OC3-C7cikloalkil mogu biti supstituirani s jednom do tri skupine, koje se neovisno bira između hidroksi, metoksi, C1-C3alkila i halogena;
L1 je povezujuća skupina, koju se bira između -C(O)- i -S(O)n-, gdje n predstavlja 1 do 2;
R3 se bira između vodika, halogena, metil, metoksi i cijano;
R4 se bira između vodika, halogena, metil, metoksi i cijano;
R2 se bira između vodika, halogena, Ar, Cy, X, NR5aR5b i -C(O)-R15;
Ar se bira između fenila i C5-C6heteroarila, od kojih svaki može biti supstituiran s jednom do tri skupine, koje se neovisno bira između halogena i -L2-R7;
L2 je povezujuća skupina, koju se bira između veze, -(CH2)m-, -O(CH2)m-, -C2-C4alkenil-, -OC2-C4alkenil-, -(CH2)p-NH-(CH2)q-, te -(CH2)p-C(O)-(CH2)q-; gdje m predstavlja 1 do 4, a p i q neovisno predstavljaju 0 do 4;
R7 se bira između vodika; hidroksi; NR8aR8b; C4-C7heterocikloalkila, koji može biti supstituiran s jednom ili dvije C1-C3alkilne skupine; C3-C7cikloalkila; C1-C6alkoksi, koji može biti supstituiran s jednom skupinom NR14aR14b; te fenila, koji može biti supstituiran s jednom do tri skupine, koje se neovisno bira između halogena, metoksi i metila;
Cy se bira između C3-C7cikloalkila, C4-C7heterocikloalkila, C5-C7cikloalkenila i C5-C7heterocikloalkenila, od kojih svaki može biti supstituiran s jednom do tri skupine, koje se neovisno bira između C1-C3alkila, C1-C3alkoksi, C4-C7heterocikloalkila, NR11aR11b, =O, -C(O)-R15 i -C(O)O-R15;
X se bira između C1-C6alkila, C2-C6alkenila i C1-C6alkoksi, od kojih svaki može biti supstituiran s jednom do tri skupine, koje se neovisno bira između hidroksi, metoksi, halogena, NR13aR13b i C4-C7heterocikloalkila, gdje C4-C7heterocikloalkil može biti supstituiran s jednim do tri C1-C3alkilne skupine;
R5a se bira između vodika; C1-C6alkila, koji može biti supstituiran s jednim skupina koju se bira između Ar i Cy; -C(O)-R9; -C(O)-OR9; te -SO2-R9;
R5b se bira između vodika i C1-C3alkila;
R8a i R8b se neovisno bira između vodika i C1-C3alkila;
R9 se bira između C1-C6alkila, C3-C7cikloalkila, C4-C7heterocikloalkila, fenila i C5-C6heteroarila;
R10a i R10b se neovisno bira između vodika i C1-C3alkila;
R11a i R11b se neovisno bira između vodika i C1-C3alkila;
R12 se bira između vodika, halogena i metila;
R13 se bira između vodika, C1-C3alkila, -C(O)-C4-C7heterocikloalkila, -C(O)-C1-C3alkila i -C(O)-C3-C7cikloalkila;
R13a i R13b se neovisno bira između vodika i C1-C3alkila;
R14a i R14b se neovisno bira između vodika i C1-C3alkila; i
R15 se bira između C1-C6alkila, Ar, C3-C7cikloalkila i C4-C7heterocikloalkila.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R1 C4-C7heterocikloalkil, koji može biti supstituiran s jednim C1-C3alkilom ili s jednim ili dva halogena.
3. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što L1 je -C(O)-.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što se R2 bira između vodika, halogena, Ar, Cy, te X.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što je R2 Cy, gdje je Cy izborno supstituirani C4-C7heterocikloalkil.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je R3 vodik ili halogen, a R4 je vodik, halogen ili metil.
7. Spoj Formule (I) u skladu s patentnim zahtjevom 1, naznačen time što je
[image]
.
8. Spoj Formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili njegova farmaceutski prihvatljiva sol.
9. Farmaceutski pripravak, naznačen time što sadrži (a) spoj Formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegovu farmaceutski prihvatljivu sol, i (b) farmaceutski prihvatljivi nosač.
10. Kombinacija, naznačena time što sadrži (a) spoj Formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegovu farmaceutski prihvatljivu sol, i (b) najmanje jedno dodatno terapijsko sredstvo.
11. Spoj Formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u terapiji.
12. Spoj Formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju ili sprječavanje parazitarne bolesti koju se bira između Chagasove bolesti, ljudske afričke tripanosomijaze, životinjske afričke tripanosomijaze i lišmanijaze.
13. Spoj Formule (I), ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 12, naznačen time što je parazitarna bolest lišmanijaza.
14. Spoj Formule (I), ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 12 ili 13, naznačen time što je lišmanijaza visceralna lišmanijaza.
15. Spoj Formule (I), ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 14, naznačen time što visceralnu lišmanijazu uzrokuje Leishmania donovani.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15382418 | 2015-08-07 | ||
| EP16747519.3A EP3331885B1 (en) | 2015-08-07 | 2016-08-03 | Compounds |
| PCT/EP2016/068592 WO2017025416A1 (en) | 2015-08-07 | 2016-08-03 | Compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20210402T1 true HRP20210402T1 (hr) | 2021-04-16 |
Family
ID=53887051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20210402TT HRP20210402T1 (hr) | 2015-08-07 | 2021-03-09 | Spojevi |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US10479792B2 (hr) |
| EP (1) | EP3331885B1 (hr) |
| JP (1) | JP6838045B2 (hr) |
| KR (1) | KR102652898B1 (hr) |
| CN (1) | CN108137599B (hr) |
| AR (1) | AR105606A1 (hr) |
| AU (1) | AU2016307230B2 (hr) |
| BR (1) | BR112018002597B1 (hr) |
| CA (1) | CA2994997C (hr) |
| CY (1) | CY1124151T1 (hr) |
| DK (1) | DK3331885T3 (hr) |
| ES (1) | ES2856899T3 (hr) |
| HR (1) | HRP20210402T1 (hr) |
| HU (1) | HUE052932T2 (hr) |
| IL (1) | IL257336B (hr) |
| LT (1) | LT3331885T (hr) |
| MY (1) | MY197042A (hr) |
| PL (1) | PL3331885T3 (hr) |
| PT (1) | PT3331885T (hr) |
| RS (1) | RS61434B1 (hr) |
| RU (1) | RU2734877C2 (hr) |
| SI (1) | SI3331885T1 (hr) |
| TW (1) | TWI746454B (hr) |
| WO (1) | WO2017025416A1 (hr) |
| ZA (1) | ZA201800733B (hr) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190278A1 (ar) * | 2017-05-31 | 2019-11-28 | Novartis Ag | مركبات 5، 6-ثنائية الحلقة مندمجة وتركيبات لعلاج الأمراض الطفيلية |
| EA039324B1 (ru) * | 2017-11-06 | 2022-01-13 | Новартис Аг | 5,6–конденсированные бициклические соединения и композиции для лечения паразитарных заболеваний |
| RU2717960C1 (ru) * | 2019-08-05 | 2020-03-27 | Федеральное Государственное бюджетное учреждение "27 Научный центр" Министерства обороны Российской Федерации | СПОСОБ ПОЛУЧЕНИЯ ЗАМЕЩЕННЫХ α-БРОМАРИЛАЦЕТАЛЬДЕГИДОВ С ИСПОЛЬЗОВАНИЕМ БРОМИДА МЕДИ (II) |
| WO2024077273A2 (en) * | 2022-10-07 | 2024-04-11 | Denali Therapeutics Inc. | Compounds, compositions, and methods |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010059418A1 (en) * | 2008-11-19 | 2010-05-27 | The Government Of The U.S.A. As Represented By The Secretary Of The Dept. Of Health & Human Services | Substituted triazine and purine compounds, methods of inhibiting cruzain and rhodesain and methods of treating chagas disease and african trypanosomiasis |
| PL2448939T3 (pl) * | 2009-07-02 | 2017-08-31 | Sanofi | Pochodne 2,3-dihydro-1h-imidazo {1,2-a} pirymidyn-5-onu, ich wytwarzanie i ich zastosowanie farmaceutyczne |
| WO2014151630A2 (en) * | 2013-03-15 | 2014-09-25 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| UY35400A (es) * | 2013-03-15 | 2014-10-31 | Novartis Ag | Compuestos y composiciones para el tratamiento de enfermedades parasitarias |
| US9186361B2 (en) * | 2013-03-15 | 2015-11-17 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| US9296754B2 (en) | 2013-03-15 | 2016-03-29 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| HUE040254T2 (hu) * | 2013-12-19 | 2019-02-28 | Novartis Ag | Protozoa proteaszóma inhibitor [1,2,4]triazolo[1,5-a]pirimidinszármazékok paraziták által okozott betegségek, például leishmaniasis kezelésére |
-
2016
- 2016-08-03 EP EP16747519.3A patent/EP3331885B1/en active Active
- 2016-08-03 BR BR112018002597-6A patent/BR112018002597B1/pt active IP Right Grant
- 2016-08-03 AU AU2016307230A patent/AU2016307230B2/en active Active
- 2016-08-03 HU HUE16747519A patent/HUE052932T2/hu unknown
- 2016-08-03 JP JP2018506295A patent/JP6838045B2/ja active Active
- 2016-08-03 PL PL16747519T patent/PL3331885T3/pl unknown
- 2016-08-03 SI SI201631098T patent/SI3331885T1/sl unknown
- 2016-08-03 CA CA2994997A patent/CA2994997C/en active Active
- 2016-08-03 WO PCT/EP2016/068592 patent/WO2017025416A1/en active Application Filing
- 2016-08-03 RS RS20210152A patent/RS61434B1/sr unknown
- 2016-08-03 RU RU2018107657A patent/RU2734877C2/ru active
- 2016-08-03 CN CN201680057096.2A patent/CN108137599B/zh active Active
- 2016-08-03 LT LTEP16747519.3T patent/LT3331885T/lt unknown
- 2016-08-03 ES ES16747519T patent/ES2856899T3/es active Active
- 2016-08-03 US US15/750,896 patent/US10479792B2/en active Active
- 2016-08-03 PT PT167475193T patent/PT3331885T/pt unknown
- 2016-08-03 KR KR1020187005944A patent/KR102652898B1/ko active IP Right Grant
- 2016-08-03 MY MYPI2018700471A patent/MY197042A/en unknown
- 2016-08-03 DK DK16747519.3T patent/DK3331885T3/da active
- 2016-08-04 TW TW105124717A patent/TWI746454B/zh active
- 2016-08-04 AR ARP160102392A patent/AR105606A1/es unknown
-
2018
- 2018-02-04 IL IL257336A patent/IL257336B/en active IP Right Grant
- 2018-02-05 ZA ZA2018/00733A patent/ZA201800733B/en unknown
-
2021
- 2021-03-09 HR HRP20210402TT patent/HRP20210402T1/hr unknown
- 2021-03-11 CY CY20211100209T patent/CY1124151T1/el unknown
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