HRP20160100T1 - Razgranati derivati 3-fenilpropionske kiseline i njihova uporaba - Google Patents
Razgranati derivati 3-fenilpropionske kiseline i njihova uporaba Download PDFInfo
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- HRP20160100T1 HRP20160100T1 HRP20160100TT HRP20160100T HRP20160100T1 HR P20160100 T1 HRP20160100 T1 HR P20160100T1 HR P20160100T T HRP20160100T T HR P20160100TT HR P20160100 T HRP20160100 T HR P20160100T HR P20160100 T1 HRP20160100 T1 HR P20160100T1
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- Prior art keywords
- fluorine
- methyl
- formula
- solvates
- represents hydrogen
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- XMIIGOLPHOKFCH-UHFFFAOYSA-N 3-phenylpropionic acid Chemical class OC(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-N 0.000 title 1
- 229910052731 fluorine Inorganic materials 0.000 claims 20
- 239000011737 fluorine Substances 0.000 claims 20
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 19
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000002431 hydrogen Chemical group 0.000 claims 11
- 150000003839 salts Chemical group 0.000 claims 10
- 239000012453 solvate Chemical group 0.000 claims 10
- 229910052801 chlorine Inorganic materials 0.000 claims 9
- 239000000460 chlorine Chemical group 0.000 claims 9
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 8
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 8
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 7
- 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
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 4
- -1 cyano, methyl Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 3
- FEIACFYXEWBKHU-UHFFFAOYSA-N (2-aminopyridin-3-yl)methanol Chemical group NC1=NC=CC=C1CO FEIACFYXEWBKHU-UHFFFAOYSA-N 0.000 claims 2
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 claims 2
- 206010002383 Angina Pectoris Diseases 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000001647 Renal Insufficiency Diseases 0.000 claims 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 2
- 230000003176 fibrotic effect Effects 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 201000006370 kidney failure Diseases 0.000 claims 2
- 230000004089 microcirculation Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims 2
- 230000009424 thromboembolic effect Effects 0.000 claims 2
- 208000019553 vascular disease Diseases 0.000 claims 2
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- OBYVIVUJQDGTKI-RIUYPTKQSA-N 2-[[(2R,3S,4S,5R,6R)-3,5-dihydroxy-2-(hydroxymethyl)-6-methoxyoxan-4-yl]oxymethyl]quinoline-7-carboxylic acid Chemical group CO[C@H]1[C@@H]([C@H]([C@H]([C@H](O1)CO)O)OCC2=NC3=C(C=CC(=C3)C(=O)O)C=C2)O OBYVIVUJQDGTKI-RIUYPTKQSA-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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- YGYAWVDWMABLBF-UHFFFAOYSA-N Phosgene Chemical compound ClC(Cl)=O YGYAWVDWMABLBF-UHFFFAOYSA-N 0.000 claims 1
- LIUMDGLYGBIKBM-SFYKDHMMSA-N [(2s)-3-[[(2s)-1-[[(2s)-1-amino-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-[[3-[4-(3-chlorophenyl)phenyl]-1,2-oxazol-5-yl]methyl]-3-oxopropyl]-(4-bromophenyl)phosphinic acid Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(N)=O)CP(O)(=O)C=1C=CC(Br)=CC=1)C(ON=1)=CC=1C(C=C1)=CC=C1C1=CC=CC(Cl)=C1 LIUMDGLYGBIKBM-SFYKDHMMSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 230000002785 anti-thrombosis Effects 0.000 claims 1
- 238000010420 art technique Methods 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 239000003119 guanylate cyclase activator Substances 0.000 claims 1
- 238000007327 hydrogenolysis reaction Methods 0.000 claims 1
- 239000012442 inert solvent Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 230000037356 lipid metabolism Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- GCVFCUPRTZORNH-UHFFFAOYSA-N n,n-dimethyl-3-[4-(1,10-phenanthrolin-4-yl)butoxy]aniline;2-pyridin-2-ylpyridine;ruthenium Chemical compound [Ru].N1=CC=CC=C1C1=CC=CC=N1.N1=CC=CC=C1C1=CC=CC=N1.CN(C)C1=CC=CC(OCCCCC=2C3=C(C4=NC=CC=C4C=C3)N=CC=2)=C1 GCVFCUPRTZORNH-UHFFFAOYSA-N 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
- 239000002904 solvent Substances 0.000 claims 1
- 238000003797 solvolysis reaction Methods 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/14—Preparation of carboxylic acid amides by formation of carboxamide groups together with reactions not involving the carboxamide groups
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
- C07C233/53—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C07C233/55—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
Claims (10)
1. Spoj s formulom (I)
[image]
naznačen time da
R1, R2 i R3 međusobno neovisno predstavljaju vodik ili metil,
L predstavlja vezu ili predstavlja -CH2-,
R4A i R4B međusobno neovisno predstavljaju metil, trifluorometil ili etil
ili
R4A i R4B su spojeni jedan na drugi i zajedno s atomom ugljika na koji su vezani tvore ciklopropilni ili ciklobutilni prsten koji može biti supstituiran do dva puta sa fluorom,
R5 predstavlja vodik, fluor, metil ili metoksi,
R6 predstavlja vodik, fluor, klor, brom, cijano, metil, trifluorometil, etil, metoksi ili trifluorometoksi,
R7 predstavlja vodik, fluor, klor ili metil,
R8A predstavlja metil ili etil,
R8B predstavlja trifluorometil,
ili
R8A i R8B su spojeni jedan na drugi i zajedno s atomom ugljika na koji su vezani tvore proizvoljno difluoro-supstituiran ciklopentilni prsten s formulom
[image]
R9 predstavlja fluor, klor, brom, cijano, (C1-C4)-alkil, (C2-C4)-alkenil, ciklopropil ili ciklobutil, gdje (C1-C4)-alkil i (C2-C4)-alkenil mogu biti supstituirani do tri puta sa fluorom i ciklopropil i ciklobutil mogu biti supstituirani do dva puta sa fluorom,
i
R10 predstavlja vodik, fluor, klor, metil, trifluorometil, etil ili metoksi,
i soli, solvati i solvati njihovih soli.
2. Spoj s formulom (I) prema zahtjevu 1 naznačen time da
R1 predstavlja vodik ili metil,
R2 predstavlja vodik,
R3 predstavlja vodik ili metil,
L predstavlja vezu ili predstavlja -CH2-,
R4A i R4B oba predstavljaju metil ili su spojeni jedan na drugi i zajedno s atomom ugljika na koji su vezani tvore ciklopropilni ili ciklobutilni prsten koji može biti supstituiran do dva puta sa fluorom,
R5 predstavlja vodik, fluor, metil ili metoksi,
R6 predstavlja fluor, klor, metil ili etil,
R7 predstavlja vodik ili fluor,
R8A predstavlja metil,
R8B predstavlja trifluorometil,
ili
R8A i R8B su spojeni jedan na drugi i zajedno s atomom ugljika na koji su vezani tvore difluoro-supstituiran ciklopentilni prsten s formulom
[image]
R9 predstavlja fluor, klor, (C1-C4)-alkil, (C2-C3)-alkenil, ciklopropil ili ciklobutil, gdje (C1-C4)-alkil i (C2-C3)-alkenil mogu biti supstituirani do tri puta sa fluorom i ciklopropil i ciklobutil mogu biti supstituirani do dva puta sa fluorom,
i
R10 predstavlja vodik, fluor, klor, metil ili metoksi,
i soli, solvati i solvati njihovih soli.
3. Spoj s formulom (I) prema zahtjevu 1 ili 2 naznačen time da
R1 i R2 oba predstavljaju vodik,
R3 predstavlja vodik ili metil,
L predstavlja vezu ili predstavlja -CH2-,
R4A i R4B oba predstavljaju metil ili su spojeni jedan na drugi i zajedno s atomom ugljika na koji su vezani tvore ciklopropilni ili ciklobutilni prsten koji može biti supstituiran do dva puta sa fluorom,
R5 predstavlja vodik, fluor ili metil,
R6 predstavlja klor,
R7 predstavlja vodik,
R8A predstavlja metil,
R8B predstavlja trifluorometil,
R9 predstavlja fluor, klor, metil, trifluorometil, etil, 2,2,2-trifluoroetil, izopropil, tert-butil, ciklopropil ili 2,2-difluorociklopropil,
i
R10 predstavlja vodik, fluor, metil ili metoksi,
i soli, solvati i solvati njihovih soli.
4. Spoj prema zahtjevu 1 naznačen time da odgovara slijedećoj formuli
[image]
i soli, solvati i solvati njihovih soli.
5. Postupak za pripremanje spoja s formulom (I) kako je definirano u bilo kojem od zahtjeva 1 do 4, naznačen time da je karboksilna kiselina s formulom (II)
[image]
u kojoj R8A, R8B, R9 i R10 imaju značenja navedena u bilo kojem od zahtjeva 1 do 4,
vezana u inertnom otapalu pomoću sredstva za kondenzaciju ili putem intermedijera odgovarajućeg karbonil klorida u prisutnosti baze s aminom s formulom (III)
[image]
u kojoj L, R1, R2, R3, R4A, R4B, R5, R6 i R7 imaju značenja navedena u zahtjevima 1 do 4
i
T1 predstavlja (C1-C4)-alkil ili benzil, da se dobije karboksamid s formulom (IV)
[image]
u kojoj L, R1, R2, R3, R4A, R4B, R5, R6, R7, R8A, R8B, R9, R10 i T1 imaju gore navedena značenja,
i radikal estera T1 se zatim uklanja pomoću bazične ili kisele solvolize ili, u slučaju da T1 predstavlja benzil, također pomoću hidrogenolize da se dobije karboksilna kiselina s formulom (I) i spojevi s formulom (I) su proizvoljno odvojeni postupcima poznatim stručnjaku u ovom području tehnike u njihove enantiomere i/ili diastereomere i/ili reagiraju s odgovarajućim (i) otapalima i/ili (ii) bazama da se dobiju njihovi solvati, soli i/ili solvati soli.
6. Spoj kako je definirano u bilo kojem od zahtjeva 1 do 4 naznačen time da je za liječenje i/ili sprječavanje bolesti.
7. Uporaba spoja kako je definirano u bilo kojem od zahtjeva 1 do 4 naznačen time da je za pripremanje lijeka za liječenje i/ili sprječavanje zatajenja srca, angine pektoris, hipertenzije, plućne hipertenzije, tromboembolijskih poremećaja, ishemija, vaskularnih poremećaja, poremećaja mikrocirkulacije, insuficijencije bubrega, fibroznih poremećaja i arterioskleroze.
8. Lijek naznačen time da sadrži spoj kako je definirano u bilo kojem od zahtjeva 1 do 4 u kombinaciji s jednim ili inertnim, ne-toksičnim, farmaceutski prikladnim pomoćnim sredstvima.
9. Lijek naznačen time da sadrži spoj kako je definirano u bilo kojem od zahtjeva 1 do 4 u kombinaciji s jednim ili više dodatnih aktivnih spojeva odabranim iz skupine koja sadrži organske nitrate, donore NO, inhibitore cGMP-PDE, stimulatore gvanilatciklaze, sredstva koja imaju antitromboznu aktivnost, sredstva za snižavanje krvnog tlaka, te sredstva koja mijenjaju metabolizam lipida.
10. Lijek prema zahtjevu 8 ili 9 naznačen time da je za liječenje i/ili sprječavanje zatajenja srca, angine pektoris, hipertenzije, plućne hipertenzije, tromboembolijskih poremećaja, ishemija, vaskularnih poremećaja, poremećaja mikrocirkulacije, insuficijencije bubrega, fibroznih poremećaja i arterioskleroze.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102011007272A DE102011007272A1 (de) | 2011-04-13 | 2011-04-13 | Verzweigte 3-Phenylpropionsäure-Derivate und ihre Verwendung |
PCT/EP2012/055474 WO2012139888A1 (de) | 2011-04-13 | 2012-03-28 | Verzweigte 3-phenylpropionsäure-derivate und ihre verwendung |
EP12711861.0A EP2697191B1 (de) | 2011-04-13 | 2012-03-28 | Verzweigte 3-phenylpropionsäure-derivate und ihre verwendung |
Publications (1)
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