ME02603B - Nove 5 - aminotetrahidrohinolin-2-karbonske kiseline i njihova upotreba - Google Patents
Nove 5 - aminotetrahidrohinolin-2-karbonske kiseline i njihova upotrebaInfo
- Publication number
- ME02603B ME02603B MEP-2017-30A MEP201730A ME02603B ME 02603 B ME02603 B ME 02603B ME P201730 A MEP201730 A ME P201730A ME 02603 B ME02603 B ME 02603B
- Authority
- ME
- Montenegro
- Prior art keywords
- formula
- compound
- salts
- solvates
- fluorine
- Prior art date
Links
- YCTMSIGDGYEBRJ-UHFFFAOYSA-N 5-amino-1,2,3,4-tetrahydroquinoline-2-carboxylic acid Chemical class N1C(C(O)=O)CCC2=C1C=CC=C2N YCTMSIGDGYEBRJ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 17
- 150000003839 salts Chemical group 0.000 claims 14
- 239000012453 solvate Chemical group 0.000 claims 13
- 229910052731 fluorine Chemical group 0.000 claims 11
- 239000011737 fluorine Chemical group 0.000 claims 11
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 10
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 8
- 229910052801 chlorine Inorganic materials 0.000 claims 8
- 239000000460 chlorine Chemical group 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 4
- 206010002383 Angina Pectoris Diseases 0.000 claims 3
- 206010003210 Arteriosclerosis Diseases 0.000 claims 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 3
- 206010019280 Heart failures Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 208000001647 Renal Insufficiency Diseases 0.000 claims 3
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- -1 cyano, methyl Chemical group 0.000 claims 3
- 230000003176 fibrotic effect Effects 0.000 claims 3
- 208000028867 ischemia Diseases 0.000 claims 3
- 230000004089 microcirculation Effects 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 208000002815 pulmonary hypertension Diseases 0.000 claims 3
- 230000009424 thromboembolic effect Effects 0.000 claims 3
- 208000019553 vascular disease Diseases 0.000 claims 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 201000006370 kidney failure Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 2
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 claims 2
- HFCWZVGKWGOBKV-UHFFFAOYSA-N 5-[2-(4-carboxyphenyl)ethyl-[2-[2-[[2-chloro-4-[4-(trifluoromethyl)phenyl]phenyl]methoxy]phenyl]ethyl]amino]-5,6,7,8-tetrahydroquinoline-2-carboxylic acid Chemical compound C1=CC(C(=O)O)=CC=C1CCN(C1C2=CC=C(N=C2CCC1)C(O)=O)CCC1=CC=CC=C1OCC1=CC=C(C=2C=CC(=CC=2)C(F)(F)F)C=C1Cl HFCWZVGKWGOBKV-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 102000010180 Endothelin receptor Human genes 0.000 claims 1
- 229940118365 Endothelin receptor antagonist Drugs 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 229940123333 Phosphodiesterase 5 inhibitor Drugs 0.000 claims 1
- 108091006335 Prostaglandin I receptors Proteins 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 230000003055 anti-obstructive effect Effects 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 229960004676 antithrombotic agent Drugs 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- MAPRDOKILZKGDP-UHFFFAOYSA-N bromo-chloro-iodomethanesulfonic acid Chemical compound OS(=O)(=O)C(Cl)(Br)I MAPRDOKILZKGDP-UHFFFAOYSA-N 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 239000003119 guanylate cyclase activator Substances 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- 229940125721 immunosuppressive agent Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 229940082615 organic nitrates used in cardiac disease Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000002590 phosphodiesterase V inhibitor Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003815 prostacyclins Chemical class 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Quinoline Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (13)
1.Jedinjenje sa formulom (I) naznačeno time što R1 predstavlja vodonik ili fluor, L1 predstavlja etan-1,2-diil ili 1,4-fenilen, i A predstavlja grupu sa formulom u kojoj * označava odgovarajuću tačku vezivanja na ostatak molekula, L3 predstavlja vezu, -O-, -CH2-, -CH2-CH2- ili -CH=CH-, i R3C predstavlja supstituent izabran iz grupe koju čine fluor, hlor, brom, cijano, (C1-C4)-alkil, difluormetil, trifluormetil, (C1-C4)-alkoksi, difluormetoksi i trifluormetoksi, i R3D predstavlja supstituent izabran iz grupe koju čine vodonik, fluor, hlor, brom, cijano, (C1-C4)-alkil, difluormetil, trifluormetil, (C1-C4)-alkoksi, difluormetoksi i trifluormetoksi, i soli, solvati i solvati njihovih soli.
2.Jedinjenje sa formulom (I) prema zahtevu 1 naznačeno time što R1 predstavlja vodonik ili fluor, L1 predstavlja etan-1,2-diil ili 1,4-fenilen, i A predstavlja grupu sa formulom u kojoj * označava odgovarajuću tačku vezivanja na ostatak molekula, L3 predstavlja vezu, -CH2-CH2- ili -CH=CH-, R3C predstavlja fluor, hlor, metil ili trifluormetil, i R3D predstavlja vodonik, fluor, hlor, cijano, metil, trifluormetil, metoksi ili trifluormetoksi, i soli, solvati i solvati njihovih soli.
3.Jedinjenje sa formulom (I) prema zahtevu 1 ili 2 naznačeno time što R1 predstavlja vodonik ili fluor, L1 predstavlja etan-1,2-diil ili 1,4-fenilen, i A predstavlja grupu sa formulom u kojoj * označava odgovarajuću tačku vezivanja na ostatak molekula, L3 predstavlja vezu, -CH2-CH2- ili -CH=CH-, R3C predstavlja fluor, hlor, metil ili trifluormetil, i R3D predstavlja vodonik, fluor, hlor, cijano, metil, trifluormetil ili trifluormetoksi, i soli, solvati i solvati njihovih soli.
4.Jedinjenje sa formulom (I) prema zahtevu 1, 2 ili 3 naznačeno time što R1 predstavlja vodonik ili fluor, L1 predstavlja etan-1,2-diil ili 1,4-fenilen, i A predstavlja grupu sa formulom u kojoj * označava odgovarajuću tačku vezivanja na ostatak molekula, L3 predstavlja vezu ili -CH2-CH2-, R3C predstavlja hlor, i R3D predstavlja vodonik, fluor ili trifluormetil, i soli, solvati i solvati njihovih soli.
5.5-{[2-(4-karboksifenil)etil][2-(2-{[3-hlor-4'-(trifluormetil)bifenil-4-il]metoksi}fenil)etil]amino}-5,6,7,8-tetrahidrokinolin-2-karboksilna kiselina prema formuli u nastavku i soli, solvati i solvati njihovih soli.
6.5-{(4-karboksibutil)[2-(2-{[3-hlor-4'-(trifluormetil)bifenil-4-il]metoksi}fenil)etil]amino}-5,6,7,8-tetrahidrokinolin-2-karboksilna kiselina prema formuli u nastavku i soli, solvati i solvati njihovih soli.
7.Postupak za pripremanje jedinjenja sa formulom (I) kako je definisano u bilo kom od zahteva 1 do 6, naznačen time što ili [A] jedinjenje sa formulom (II) u kojoj R1 i L1 imaju značenja data u bilo kom od zahteva 1 do 6 i T1 i T2 su identični ili različiti i predstavljaju (C1-C4)-alkil, reaguje u prisustvu baze sa jedinjenjem sa formulom (III) u kojoj A ima značenja data u bilo kom od zahteva 1 do 6 i X1 predstavlja odlazeću grupu kao što je, na primer, hlor, brom, jod, mesilat, triflat ili tosilat, ili [B] jedinjenje sa formulom (IV) u kojoj R1 i A imaju značenja data u bilo kom od zahteva 1 do 6 i T2 predstavlja (C1-C4)-alkil, reaguje u prisustvu baze sa jedinjenjem sa formulom (V) u kojoj L1 ima značenja data u bilo kom od zahteva 1 do 6, T1 predstavlja (C1-C4)-alkil, i X2 predstavlja odlazeću grupu kao što je, na primer, hlor, brom, jod, mesilat, triflat ili tosilat, i odgovarajuće dobijeno jedinjenje sa formulom (VI) u kojoj R1, A, L1, T1 i T2 imaju gore navedena značenja, se zatim konvertuje hidrolizom grupa estra -C(O)OT1 i -C(O)OT2 u odgovarajuću dikarboksilnu kiselinu sa formulom (I) i na ovaj način dobivena jedinjenja sa formulom (I) se opciono rastavljaju na njihove enantiomere i/ili dijastereomere i/ili se opciono konvertuju sa odgovarajućim (i) rastvaračima i/ili (ii) bazama ili kiselinama u njihove solvate, soli i/ili solvate soli.
8.Jedinjenje kako je definisano u bilo kom od zahteva 1 do 6 naznačeno time što je za lečenje i/ili prevenciju bolesti.
9.Jedinjenje kako je definisano u bilo kom od zahteva 1 do 6 naznačeno time što je za upotrebu u postupku lečenja i/ili prevencije primarnih i sekundarnih oblika plućne hipertenzije, zatajenja srca, angine pektoris, hipertenzije, tromboembolijskih poremećaja, ishemija, vaskularnih poremećaja, oštećenja mikrocirkulacije, insuficijencije bubrega, fibroznih poremećaja i arterioskleroze.
10.Upotreba jedinjenja kako je definisano u bilo kom od zahteva 1 do 6 naznačena time da je za dobivanje leka za lečenje i/ili prevenciju primarnih i sekundarnih oblika plućne hipertenzije, zatajenja srca, angine pektoris, hipertenzije, tromboembolijskih poremećaja, ishemija, vaskularnih poremećaja, oštećenja mikrocirkulacije, insuficijencije bubrega, fibroznih poremećaja i arterioskleroze.
11.Lek, naznačen time što sadrži jedinjenje kako je definisano u bilo kom od zahteva 1 do 6 u kombinaciji sa jednom ili više inertnih netoksičnih farmaceutski prihvatljivih pomoćnih supstanci.
12.Lek, naznačen time što sadrži jedinjenje kako je definisano u bilo kom od zahteva 1 do 6 u kombinaciji sa jednim ili više daljnjih aktivnih jedinjenja koja su izabrana iz grupe koju čine organski nitrati, donori NO, inhibitori PDE 5, analozi prostaciklina, agonisti IP receptora, antagonisti receptora endotelina, stimulatori gvanilat ciklaze, inhibitori tirozin kinaze, anti-opstruktivna sredstva, anti-inflamatorna i/ili imunosupresivna sredstva, antitrombotička sredstva, sredstva za snižavanje krvnog pritiska i sredstva koja menjaju metabolizam masti.
13. Lek prema zahtevu 11 ili 12 naznačen time što je za lečenje i/ili prevenciju primarnih i sekundarnih oblika plućne hipertenzije, zatajenja srca, angine pektoris, hipertenzije, tromboembolijskih poremećaja, ishemija, vaskularnih poremećaja, oštećenja mikrocirkulacije, insuficijencije bubrega, fibroznih poremećaja i arterioskleroze.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12177284 | 2012-07-20 | ||
| EP13167967 | 2013-05-16 | ||
| EP13744464.2A EP2875003B1 (de) | 2012-07-20 | 2013-07-16 | Neue 5-aminotetrahydrochinolin-2-carbonsäuren und ihre verwendung |
| PCT/EP2013/065017 WO2014012934A1 (de) | 2012-07-20 | 2013-07-16 | Neue 5-aminotetrahydrochinolin-2-carbonsäuren und ihre verwendung |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02603B true ME02603B (me) | 2017-06-20 |
Family
ID=48914233
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2017-30A ME02603B (me) | 2012-07-20 | 2013-07-16 | Nove 5 - aminotetrahidrohinolin-2-karbonske kiseline i njihova upotreba |
Country Status (40)
| Country | Link |
|---|---|
| US (3) | US8981104B2 (me) |
| EP (1) | EP2875003B1 (me) |
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| DE102011007272A1 (de) | 2011-04-13 | 2012-10-18 | Bayer Pharma Aktiengesellschaft | Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung |
| JP6118965B2 (ja) | 2012-04-16 | 2017-04-26 | トーアエイヨー株式会社 | 2環性化合物 |
| WO2014012935A1 (de) | 2012-07-20 | 2014-01-23 | Bayer Pharma Aktiengesellschaft | Substituierte aminoindan- und aminotetralin-carbonsäuren und ihre verwendung |
| BR112015001211B1 (pt) * | 2012-07-20 | 2020-12-15 | Bayer Pharma Aktiengesellschaft | Ácidos 5-aminotetra-hidroquinolina-2-carboxílicos, processos para a sua preparação, seus usos no tratamento e/ou prevenção de doenças e seus medicamentos |
| FR3000065A1 (fr) | 2012-12-21 | 2014-06-27 | Univ Lille Ii Droit & Sante | Composes bicycliques ayant une activite potentialisatrice de l'activite d'un antibiotique actif contre les mycobacteries-composition et produit pharmaceutiques comprenant de tels composes |
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| US20180169095A1 (en) | 2015-05-06 | 2018-06-21 | Bayer Pharma Aktiengesellschaft | The use of sgc stimulators, sgc activators, alone and combinations with pde5 inhibitors for the treatment of digital ulcers (du) concomitant to systemic sclerosis (ssc) |
| CN113750102A (zh) | 2015-07-23 | 2021-12-07 | 拜耳制药股份公司 | 可溶性鸟苷酸环化酶的刺激剂和/或活化剂及其用途 |
| SG11201900360TA (en) * | 2016-07-22 | 2019-02-27 | Toa Eiyo Ltd | Therapeutic agent for glaucoma |
| CN109890379A (zh) | 2016-10-11 | 2019-06-14 | 拜耳制药股份公司 | 包含sGC活化剂和盐皮质激素受体拮抗剂的组合产品 |
| WO2018153899A1 (de) | 2017-02-22 | 2018-08-30 | Bayer Pharma Aktiengesellschaft | Selektive partielle adenosin a1 rezeptor-agonisten in kombination mit stimulatoren und/oder aktivatoren der löslichen guanylatcyclase (sgc) |
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| CN108218770A (zh) * | 2018-02-28 | 2018-06-29 | 南京波普生物医药研发有限公司 | 2-氯-7,8-二氢-6h-喹啉-5-酮的制备方法 |
| WO2019211081A1 (en) | 2018-04-30 | 2019-11-07 | Bayer Aktiengesellschaft | The use of sgc activators and sgc stimulators for the treatment of cognitive impairment |
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| US11508483B2 (en) | 2018-05-30 | 2022-11-22 | Adverio Pharma Gmbh | Method of identifying a subgroup of patients suffering from dcSSc which benefits from a treatment with sGC stimulators and sGC activators in a higher degree than a control group |
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| WO2020216669A1 (de) | 2019-04-23 | 2020-10-29 | Bayer Aktiengesellschaft | Phenylsubstituierte imidazopyridinamide und ihre verwendung |
| EP3966226B1 (en) | 2019-05-07 | 2025-12-24 | Bayer Aktiengesellschaft | Masp inhibitory compounds and uses thereof |
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| CA3244896A1 (en) | 2021-12-29 | 2023-07-06 | Bayer Aktiengesellschaft | Pharmaceutical dry powder inhalation formulation |
| CA3244893A1 (en) | 2021-12-29 | 2023-07-06 | Bayer Aktiengesellschaft | PROCESS FOR PREPARING (5S)-{[2-(4-CARBOXYPHENYL)ETHYL] |2-(2-{|3-CHLORO-4'-(TRIFLUOROMETHYL)BIPHENYL-4-YL]METHOXY}PHENYL)ETHYL]AMINOL-5,6,7,8-TETRAHYDROQUINOLINE-2-CARBOXYLIC AND ITS CRYSTALLINE FORMS FOR USE AS A PHARMACEUTICALLY ACTIVE COMPOUND |
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