HRP20110839T1 - Derivati cikloheksaminizokinolona kao inhibitori rho-kinaze - Google Patents
Derivati cikloheksaminizokinolona kao inhibitori rho-kinaze Download PDFInfo
- Publication number
- HRP20110839T1 HRP20110839T1 HR20110839T HRP20110839T HRP20110839T1 HR P20110839 T1 HRP20110839 T1 HR P20110839T1 HR 20110839 T HR20110839 T HR 20110839T HR P20110839 T HRP20110839 T HR P20110839T HR P20110839 T1 HRP20110839 T1 HR P20110839T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- alkylene
- aryl
- heterocyclyl
- halogen
- Prior art date
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- -1 Cyclohexylamin isoquinolone derivatives Chemical class 0.000 title claims 4
- 239000003590 rho kinase inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 153
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 64
- 150000001875 compounds Chemical class 0.000 claims abstract 57
- 229910052736 halogen Inorganic materials 0.000 claims abstract 46
- 150000002367 halogens Chemical class 0.000 claims abstract 46
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims abstract 36
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims abstract 24
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims abstract 20
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 16
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims abstract 8
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims abstract 5
- 125000000217 alkyl group Chemical group 0.000 claims abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims abstract 4
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 3
- 125000002947 alkylene group Chemical group 0.000 claims abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 3
- 229910052799 carbon Inorganic materials 0.000 claims abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 239000005977 Ethylene Substances 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 200000000007 Arterial disease Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010019663 Hepatic failure Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010020880 Hypertrophy Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010023421 Kidney fibrosis Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010030043 Ocular hypertension Diseases 0.000 claims 1
- 206010053159 Organ failure Diseases 0.000 claims 1
- 229910018828 PO3H2 Inorganic materials 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000005107 Premature Birth Diseases 0.000 claims 1
- 206010036590 Premature baby Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000001647 Renal Insufficiency Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 229910006069 SO3H Inorganic materials 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000001580 bacterial effect Effects 0.000 claims 1
- 230000017531 blood circulation Effects 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 208000019836 digestive system infectious disease Diseases 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000002124 endocrine Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000001286 intracranial vasospasm Diseases 0.000 claims 1
- 208000023589 ischemic disease Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 208000007903 liver failure Diseases 0.000 claims 1
- 231100000835 liver failure Toxicity 0.000 claims 1
- 238000002483 medication Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 230000008816 organ damage Effects 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 210000005259 peripheral blood Anatomy 0.000 claims 1
- 239000011886 peripheral blood Substances 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000004240 prostatic hypertrophy Diseases 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
Classifications
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- 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
- C07D217/24—Oxygen atoms
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- 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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
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- 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
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- C07D405/02—Heterocyclic 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
- C07D405/12—Heterocyclic 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
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- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- Oncology (AREA)
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- Hospice & Palliative Care (AREA)
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- Immunology (AREA)
Abstract
Spoj formule (I) ili formule (I') naznačen time štoR1 je H, (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, [(C1-C6)alkilen]0-1-(C3-C8)cikloalkil, [(C1-C6)alkilen]0-1-(C5-C10)heterociklil, [(C1-C6)alkilen]0-1-(C6-C10)aril, C(O)-(C1-C6)alkil, C(O)(C2-C6)alkenil, C(O)-(C2-C6)alkinil, C(O)-[(C1-C6)alkilen]0-1-(C3-C8)cikloalkil, C(O)-[(C1-C6)alkilen]0-1-(C5-C10)heterociklil ili C(O)-[(C1-C6)alkilen]0-1-(C6-C10)aril; R2 je H, (C1-C6)alkil, [(C1-C6)alkilen]0-1-R', [(C1-C6)alkilen]0-1-O-(C1-C6)alkil, [(C1-C6)alkilen]0-1-O-R', [(C1-C6)alkilen]0-1-NH2, [(C1-C6)alkilen]0-1-NH(C1-C6)alkil, [(C1-C6)alkilen]0-1-N[(C1-C6)alkil]2, [(C1-C6)alkilen]0-1-CH[R']2, [(C1-C6)alkilen]0-1-C(O)-R', [(C1-C6)alkilen]0-1-C(O)NH2, [(C1-C6)alkilen]0-1-C(O)NH-R' ili [(C1-C6)alkilen]0-1-C(O)N[R']2;R3 je H, halogen, CN, (C1-C6)alkil, (C1-C6)alkilen-R', OH, O-R'', NH2, NHR'', NR''R'' ili N H-C(O)-R''; R4 je H, halogen, hidroksi, CN, (C1-C6)alkil, (C3-C8)cikloalkil, (C1-C6)alkilen-R'; R5 je H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C1-C6)alkilen-(C6-C10)aril, (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-(C5-C10)heterociklil, NH2, NH-R', NH-SO2H, NH-SO2-(C1-C6)alkil, NH-SO2-R', NH-C(O)-(C1-C6)alkil, NH-C(O)-R', C(O)N[(C1-C6)alkil]2, C(O)OH ili C(O)O-(C1-C6)alkil; R6 i R6' su međusobno neovisno H, R', (C1-C8)alkil, (C1-C6)alkilen-R', (C1-C6)alkilen-O-(C1-C6)alkil, (C1-C6)alkilen-O-R', (C1-C6)alkilen-CH[R']2, (C1-C6)alkilen-C(O)-R', (C1-C6)alkilen-C(O)NH2, (C1-C6)alkilen-C(O)NH-R' ili (C1-C6)alkilen-C(O)N[R']2;R7 i R8 su međusobno neovisno H, halogen, CN, NO2, (C1-C6)alkil, O-(C1-C6)alkil, O-[(C1-C6)alkilen]0-1-R', (C2-C6)alkenil, R', (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-R', NH2, NH-R', NH-SO2H, NH-SO2-(C1-C6)alkil, NH-SO2-R', SO2-NH2, SO2-NHR', NH-C(O)-(C1-C6)alkil, NH-C(O)-R', C(O)N[(C1-C6)alkil]2, C(O)OH ili C(O)O-(C1-C6)alkil; R9 je halogen ili (C1-C6)alkil; n je 0, 1, 2, 3 ili 4; iL je O ili O-(C1-C6)alkilen; gdje R' je (C3-C8)cikloalkil, (C5-C10)heterociklil ili (C6-C10)aril; iR'' je (C3-C8)cikloalkil, (C5-C10)heterociklil, (C6-C10)aril, (C1-C6)alkil, (C1-C6)alkilen-R', (C1-C6)alkilen-O-(C1-C6)alkil, (C1-C6)alkilen-O-R' ili (C1-C6)alkilen-NRxRy; igdje Rx i Ry su međusobno neovisno (C1-C6)alkil, (C5-C10)heterociklil, (C6-C10)aril, (C1-C4)alkilen-(C5-C10)heterociklil, (C1-C4)alkilen-(C6-C10)aril, (C1-C4)alkilen-NH(C1-C6)alkil, (C1-C4)alkilen-N[(C1-C6)alkil]2, (C1-C4)alkilen-N[(C6-C10)aril]2 ili (C1-C4)alkilen-N[(C5-C10)heterociklil]2; igdje u ostacima R4, R5, R7 i R8 jedan alkilni ili alkilenski atom vodik može izborno biti zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 ili CON(CH3)2, ili alkil ili alkilen mogu biti jednostruko ili višestruko halogenirani; igdje (C3-C8)cikloalkilna skupina može sadržavati 1 ili 2 dvostruke veze, a (C6-C10)arilna i (C5-C10)heterociklilna skupina su nesupstituirane ili jednostruko ili višestruko supstituirane pogodnim skupinama, koje se neovisno bira između halogena, CF3, NO2, N3, CN, C(O)-(C1-C6)alkil
Claims (52)
1. Spoj formule (I)
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ili formule (I')
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naznačen time što
R1 je H, (C1-C6)alkil, (C2-C6)alkenil, (C2-C6)alkinil, [(C1-C6)alkilen]0-1-(C3-C8)cikloalkil, [(C1-C6)alkilen]0-1-(C5-C10)heterociklil, [(C1-C6)alkilen]0-1-(C6-C10)aril, C(O)-(C1-C6)alkil, C(O)(C2-C6)alkenil, C(O)-(C2-C6)alkinil, C(O)-[(C1-C6)alkilen]0-1-(C3-C8)cikloalkil, C(O)-[(C1-C6)alkilen]0-1-(C5-C10)heterociklil ili C(O)-[(C1-C6)alkilen]0-1-(C6-C10)aril;
R2 je H, (C1-C6)alkil, [(C1-C6)alkilen]0-1-R', [(C1-C6)alkilen]0-1-O-(C1-C6)alkil, [(C1-C6)alkilen]0-1-O-R', [(C1-C6)alkilen]0-1-NH2, [(C1-C6)alkilen]0-1-NH(C1-C6)alkil, [(C1-C6)alkilen]0-1-N[(C1-C6)alkil]2, [(C1-C6)alkilen]0-1-CH[R']2, [(C1-C6)alkilen]0-1-C(O)-R', [(C1-C6)alkilen]0-1-C(O)NH2, [(C1-C6)alkilen]0-1-C(O)NH-R' ili [(C1-C6)alkilen]0-1-C(O)N[R']2;
R3 je H, halogen, CN, (C1-C6)alkil, (C1-C6)alkilen-R', OH, O-R'', NH2, NHR'', NR''R'' ili N H-C(O)-R'';
R4 je H, halogen, hidroksi, CN, (C1-C6)alkil, (C3-C8)cikloalkil, (C1-C6)alkilen-R';
R5 je H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C1-C6)alkilen-(C6-C10)aril, (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-(C5-C10)heterociklil, NH2, NH-R', NH-SO2H, NH-SO2-(C1-C6)alkil, NH-SO2-R', NH-C(O)-(C1-C6)alkil, NH-C(O)-R', C(O)N[(C1-C6)alkil]2, C(O)OH ili C(O)O-(C1-C6)alkil;
R6 i R6' su međusobno neovisno H, R', (C1-C8)alkil, (C1-C6)alkilen-R', (C1-C6)alkilen-O-(C1-C6)alkil, (C1-C6)alkilen-O-R', (C1-C6)alkilen-CH[R']2, (C1-C6)alkilen-C(O)-R', (C1-C6)alkilen-C(O)NH2, (C1-C6)alkilen-C(O)NH-R' ili (C1-C6)alkilen-C(O)N[R']2;
R7 i R8 su međusobno neovisno H, halogen, CN, NO2, (C1-C6)alkil, O-(C1-C6)alkil, O-[(C1-C6)alkilen]0-1-R', (C2-C6)alkenil, R', (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-R', NH2, NH-R', NH-SO2H, NH-SO2-(C1-C6)alkil, NH-SO2-R', SO2-NH2, SO2-NHR', NH-C(O)-(C1-C6)alkil, NH-C(O)-R', C(O)N[(C1-C6)alkil]2, C(O)OH ili C(O)O-(C1-C6)alkil;
R9 je halogen ili (C1-C6)alkil;
n je 0, 1, 2, 3 ili 4; i
L je O ili O-(C1-C6)alkilen;
gdje R' je (C3-C8)cikloalkil, (C5-C10)heterociklil ili (C6-C10)aril; i
R'' je (C3-C8)cikloalkil, (C5-C10)heterociklil, (C6-C10)aril, (C1-C6)alkil, (C1-C6)alkilen-R', (C1-C6)alkilen-O-(C1-C6)alkil, (C1-C6)alkilen-O-R' ili (C1-C6)alkilen-NRxRy; i
gdje Rx i Ry su međusobno neovisno (C1-C6)alkil, (C5-C10)heterociklil, (C6-C10)aril, (C1-C4)alkilen-(C5-C10)heterociklil, (C1-C4)alkilen-(C6-C10)aril, (C1-C4)alkilen-NH(C1-C6)alkil, (C1-C4)alkilen-N[(C1-C6)alkil]2, (C1-C4)alkilen-N[(C6-C10)aril]2 ili (C1-C4)alkilen-N[(C5-C10)heterociklil]2; i
gdje u ostacima R4, R5, R7 i R8 jedan alkilni ili alkilenski atom vodik može izborno biti zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 ili CON(CH3)2, ili alkil ili alkilen mogu biti jednostruko ili višestruko halogenirani; i
gdje (C3-C8)cikloalkilna skupina može sadržavati 1 ili 2 dvostruke veze, a (C6-C10)arilna i (C5-C10)heterociklilna skupina su nesupstituirane ili jednostruko ili višestruko supstituirane pogodnim skupinama, koje se neovisno bira između halogena, CF3, NO2, N3, CN, C(O)-(C1-C6)alkila, C(O)-(C6-C10)arila, COOH, COO(C1-C6)alkila, CONH2, CONH(C1-C6)alkila, CON[(C1-C6)alkil]2, (C3-C8)cikloalkila, (C1-C6)alkila, (C1-C6)alkilen-OH, (C1-C6)alkilen-NH2, (C1-C6)alkilen-NH(C1-C6)alkila, (C1-C6)alkilen-N[(C1-C6)alkil]2, (C2-C6)alkenila, (C2-C6)alkinila, O-(C1-C6)alkila, O-C(O)-(C1-C6)alkila, O-C(O)-(C6-C10)arila, O-C(O)-(C5-C10)heterociklila, PO3H2, SO3H, SO2-NH2, SO2NH(C1-C6)alkila, SO2N[(C1-C6)alkil]2, S-(C1-C6)alkila, S-(C1-C6)alkilen-(C6-C10)arila, S-(C1-C6)alkilen-(C5-C10)heterociklila, SO-(C1-C6)alkila, SO-(C1-C6)alkilen-(C6-C10)arila, SO-(C1-C6)alkilen-(C5-C10)heterociklila, SO2-(C1-C6)alkila, SO2-(C1-C6)alkilen-(C6-C10)arila, SO2-(C1-C6)alkilen-(C5-C10)heterociklila, SO2-NH(C1-C6)alkilen-(C1-C10)arila, SO2-NH(C1-C6)alkilen-(C5-C10)heterociklila, SO2-N[(C1-C6)alkil][(C1-C6)alkilen-(C6-C10)arila], SO2-N[(C1-C6)alkil][(C1-C6)alkilen-(C5-C10)heterociklila], SO2-N[(C1-C6)alkilen-(C6-C10)aril]2, SO2-N[(C1-C6)alkilen-(C5-C10)heterociklil]2, C(NH)(NH2), NH2, NH-(C1-C6)alkila, N[(C1-C6)alkil]2, NH-C(O)-(C1-C6)alkila, NH-C(O)O-(C1-C6)alkila, NH-C(O)-(C6-C10)arila, NH-C(O)-(C5-C10)heterociklila, NH-C(O)O-(C6-C10)arila, NH-C(O)O-(C5-C10)heterociklila, NH-C(O)-NH-(C1-C6)alkila, NH-C(O)-NH-(C6-C10)arila, NH-C(O)-NH-(C5-C10)heterociklila, NH-SO2-(C1-C6)alkila, NH-SO2-(C6-C10)arila, NH-SO2-(C5-C10)heterociklila, N(C1-C6)alkil-C(O)-(C1-C6)alkila, N(C1-C6)alkil-C(O)O-(C1-C6)alkila, N(C1-C6)alkil-C(O)-(C6-C10)arila, N(C1-C6)alkil-C(O)-heterociklila, N(C1-C6)alkil-C(O)O-(C6-C10)arila, N(C1-C6)alkil-C(O)O-(C5-C10)heterociklila, N(C1-C6)alkil-C(O)-NH-(C1-C6)alkila], N(C1-C6)alkil-C(O)-NH-(C6-C10)arila, N(C1-C6)alkil-C(O)-NH-(C5-C10)heterociklila, N[(C1-C6)alkil]-C(O)-N[(C1-C6)alkil]2, N[(C1-C6)alkil]-C(O)-N[(C1-C6)alkil]-(C6-C10)arila, N[(C1-C6)alkil]-C(O)-N[(C1-C6)alkil]-(C5-C10)heterociklila, N[(C1-C6)alkil]-C(O)-N[(C6-C10)aril]2, N[(C1-C6)alkil]-C(O)-N[(C5-C10)heterociklil]2, N[(C6-C10)aril]-C(O)-(C1-C6)alkila, N[(C5-C10)heterociklil]-C(O)-(C1-C6)alkila, N[(C6-C10)aril]-C(O)O-(C1-C6)alkila, N[(C5-C10)heterociklil]-C(O)O-(C1-C6)alkila, N(aril)-C(O)-(C6-C10)arila, N[(C5-C10)heterociklil]-C(O)-(C6-C10)arila, N[(C6-C10)aril]-C(O)O-(C6-C10)arila, N[(C5-C10)heterociklil]-C(O)O-(C6-C10)arila, N[(C6-C10)arila]-C(O)-NH-(C1-C6)alkila, N[(C5-C10)heterociklil]-C(O)-NH-(C1-C6)alkila, N(aril)-C(O)-NH-(C6-C10)arila, N[(C5-C10)heterociklil]-C(O)-NH-(C6-C10)arila, N[(C6-C10)aril]-C(O)-N[(C1-C6)alkil]2, N[(C5-C10)heterociklil]-C(O)-N[(C1-C6)alkil]2, N[(C6-C10)aril]-C(O)-N[(C1-C6)alkil]-(C6-C10)arila, N[(C5-C10)heterociklil]-C(O)-N[(C1-C6)alkil]-(C6-C10)arila, N[(C6-C10)aril]-C(O)-N[(C6-C10)aril]2, N[(C5-C10)heterociklil]-C(O)-N[(C6-C10)aril]2, (C6-C10)arila, (C1-C6)alkilen-(C6-C10)arila, O-(C1-C6)alkilen-(C6-C10)arila, (C5-C10)heterociklila, (C1-C6)alkilen-(C5-C10)heterociklila, O-(C1-C6)alkilen-(C5-C10)heterociklila, gdje (C6-C10)aril ili (C5-C10)heterociklil mogu biti 1 do 3 puta supstituirani s halogenom, OH, NO2, CN, O-(C1-C6)alkilom, (C1-C6)alkilom, NH2, NH(C1-C6)alkilom, N[(C1-C6)alkil]2, SO2CH3, COOH, C(O)O-(C1-C6)alkilom, CONH2, (C1-C6)alkilen-O-(C1-C6)alkilom, (C1-C6)alkilen-O-(C6-C10)arilom, O-(C1-C6)alkilen-(C6-C10)arilom; ili gdje (C6-C10)aril je vicinalno supstituiran s O-(C1-C4)alkilen-O skupinom, gdje 5-8-eročlani prsten zajedno s atomima ugljika tvore na njih vezani atomi kisika, te gdje arilni ili heterociklilni supstituenti (C6-C10)arilne i (C5-C10)heterociklilne skupine ne mogu biti dodatno supstituirani arilom ili heterociklilom koji nosi neku skupinu;
ili njihove farmaceutski prihvatljive soli i/ili stereoizomerni oblici.
2. Spoj formule (I) u skladu s patentni zahtjev 1, naznačen time što ga karakterizira spoj formule (II)
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3. Spoj formule (I') u skladu s patentni zahtjev 1, naznačen time što ga karakterizira spoj formule (II')
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4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što R6 i R6' su međusobno neovisno H, (C1-C6)alkil, R', (C1-C4)alkilen-(C3-C8)cikloalkil, (C1-C4)alkilen-(C5-C10)heterociklil, (C1-C4)alkilen-C(O)-(C5-C10)heterociklil, (C1-C4)alkilen-C(O)-(C6-C10)aril ili (C1-C6)alkilen-(C6-C10)aril.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što R6 i R6' su međusobno neovisno H, (C1-C6)alkil, (C5-C10)heterociklil, (C3-C8)cikloalkil, (C1-C4)alkilen-(C3-C8)cikloalkil, (C1-C4)alkilen-(C5-C10)heterociklil ili (C1-C6)alkilen-(C6-C10)aril.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što R6 je H, (C1-C6)alkil, (C3-C6)cikloalkil ili (C1-C4)alkilen-(C3-C6)cikloalkil, a R6' je H, (C1-C6)alkil, (C3-C8)cikloalkil, (C1-C4)alkilen-(C3-C8)cikloalkil, (C5-C10)heterociklil, (C1-C4)alkilen-(C5-C10)heterociklil ili (C1-C6)alkilen-(C6-C10)aril.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time što R6 je H, (C1-C6)alkil, a R6' je H, (C1-C6)alkil, (C3-C8)cikloalkil, (C1-C4)alkilen-(C3-C8)cikloalkil, (C5-C10)heterociklil, (C1-C4)alkilen-(C5-C10)heterociklil ili (C1-C6)alkilen-(C6-C10)aril.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što R6 je H, (C1-C6)alkil, a R6' je H, (C1-C6)alkil, (C3-C8)cikloalkil, (C1-C4)alkilen-(C3-C8)cikloalkil, (C1-C4)alkilen-(C5-C10)heterociklil u kojem je heterociklil nesupstituiran ili supstituiran s (C1-C4)alkilom ili halogenom, ili je (C1-C6)alkilen-(C6-C10)aril, u kojem je aril nesupstituiran ili supstituiran s halogenom, (C1-C4)alkilom, O-(C1-C4)alkilom ili SO2-(C1-C4)alkilom.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time što R6 je H, (C1-C6)alkil, a R6' je H, (C1-C6)alkil, (C3-C8)cikloalkil.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što R6 je H, a R6' je H, (C1-C6)alkil, (C3-C8)cikloalkil.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što R6 i R6' su H.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 11, naznačen time što R5 je H, halogen, CN, (C1-C6)alkil, R', NH-(C6-C10)aril, (C1-C6)alkilen-(C6-C10)aril ili (C1-C6)alkilen-(C5-C10)heterociklil.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, naznačen time što R5 je H, halogen, (C1-C6)alkil, R', NH-(C6-C10)aril, (C1-C6)alkilen-(C6-C10)aril ili (C1-C6)alkilen-(C5-C10)heterociklil.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 13, naznačen time što R5 je H, halogen, (C1-C6)alkil, (C6-C10)aril, (C5-C10) heteroaril, NH-(C6-C10)aril ili (C -C2)alkilen-(C6-C 10)aril.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14, naznačen time što R5 je H, halogen, (C1-C6)alkil, fenil ili (C5-C6)heteroaril.
16. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 15, naznačen time što R5 je H, halogen ili (C1-C6)alkil.
17. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 16, naznačen time što R5 je H ili halogen.
18. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 17, naznačen time što R5 je H.
19. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 18, naznačen time što R4 je H, halogen, CN, (C1-C6)alkil ili (C1-C6)alkilen-R'.
20. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 19, naznačen time što R4 je H, halogen, (C1-C6)alkil ili (C1-C6)alkilen-R'.
21. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 20, naznačen time što R4 je H, halogen, (C1-C6)alkil ili (C1-C2)alkilen-(C6-C10)aril.
22. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 21, naznačen time što R4 je H, halogen ili (C1-C6)alkil.
23. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 22, naznačen time što R4 je H ili (C1-C6)alkil.
24. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 20, naznačen time što R4 je H.
25. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 24, naznačen time što R7 i R8 su međusobno neovisno H, halogen, CN, (C1-C6)alkil, O-(C1-C6)alkil, (C2-C6)alkenil, R' ili (C1-C6)alkilen-(C3-C8)cikloalkil.
26. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 25, naznačen time što R7 i R8 su međusobno neovisno H, halogen, CN, (C1-C4)alkil, O-(C1-C4)alkil, (C2-C4)alkenil, fenil, (C5-C6)heteroaril, (C3-C6)cikloalkil ili (C1-C4)alkilen-(C3-C6)cikloalkil.
27. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 26, naznačen time što R7 i R8 su međusobno neovisno H, halogen, (C1-C4)alkil, O-(C1-C4)alkil ili (C3-C6)cikloalkil.
28. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, naznačen time što R7 je H, halogen, (C1-C4)alkil ili (C3-C6)cikloalkil, a R8 je H.
29. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 28, naznačen time što R7 i R8 su H.
30. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 29, naznačen time što R9 je halogen ili (C1-C4)alkil.
31. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 30, naznačen time što R9 je Cl, F, metil ili etil.
32. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 31, naznačen time što n je 0, 1, 2 ili 3.
33. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 32, naznačen time što n je 0 ili 1.
34. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 29, naznačen time što n je 0.
35. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 34, naznačen time što R3 je H, halogen, (C1-C6)alkil, (C1-C4)alkilen-R', O-R'' ili NHR''.
36. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 35, naznačen time što R3 je H, (C1-C6)alkil ili NHR''.
37. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 36, naznačen time što R3 je H, (C1-C4)alkil, NH-(C5-C6)heterociklil ili NH-fenil.
38. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 37, naznačen time što R3 je H, (C1-C4)alkil, NH-(C5-C6)heteroaril koji sadrži jedan ili više N atoma ili NH-fenil.
39. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 38, naznačen time što R3 je H.
40. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 39, naznačen time što L je vezan na položaju 4 u cikloheksilnom prstenu
[image]
ili
L je vezan na položaju 3 u cikloheksilnom prstenu
[image]
.
41. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 40, naznačen time što L je vezan na položaju 4 u cikloheksilnom prstenu.
42. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 41, naznačen time što L je O-metilen, O-etilen ili O.
43. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 42, naznačen time što L je O-metilen, O-etilen ili O vezan na položaju 4 u cikloheksilnom prstenu.
44. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 43, naznačen time što L je O.
45. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što
R3 je H, halogen, CN, (C1-C6)alkil, (C1-C6)alkilen-R', OH, O-R'', NH2 ili NHR'';
R4 je H, halogen, hidroksi, CN, (C1-C6)alkil, (C3-C8)cikloalkil, (C1-C6)alkilen-R';
R5 je H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C1-C6)alkilen-(C6-C10)aril, (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-(C5-C10)heterociklil, NH2, NH-R', NH-SO2H, NH-SO2-(C1-C6)alkil, NH-SO2-R', NH-C(O)-(C1-C6)alkil, NH-C(O)-R', C(O)N[(C1-C6)alkil]2, C(O)OH ili C(O)O-(C1-C6)alkil;
R6 i R6' su međusobno neovisno H, (C3-C8)cikloalkil, (C1-C8)alkil, (C1-C6)alkilen-R', (C1-C6)alkilen-O-(C1-C6)alkil, (C1-C6)alkilen-O-R', (C1-C6)alkilen-CH[R']2, (C1-C6)alkilen-C(O)NH2, (C1-C6)alkilen-C(O)NH-R' ili (C1-C6)alkilen-C(O)N[R']2;
R7 i R8 su međusobno neovisno H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-R', NH2, NH-R', NH-SO2-(C1-C6)alkil, NH-SO2-R', SO2-NH2, SO2-NHR', NH-C(O)-(C1-C6)alkil, NH-C(O)-R', C(O)N[(C1-C6)alkil]2, C(O)OH ili C(O)O-(C1-C6)alkil;
R9 je halogen ili (C1-C6)alkil;
n je 0, 1, 2; i
L je O ili O-(C1-C3)alkilen;
ili njegove farmaceutski prihvatljive soli i/ili stereoizomerni oblici.
46. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što
R3 je H, halogen, CN, (C1-C6)alkil, (C1-C2)alkilen-R' ili NHR'';
R4 je H, halogen, CN, (C1-C6)alkil, (C3-C8)cikloalkil, (C1-C2)alkilen-R';
R5 je H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C1-C6)alkilen-(C6-C10)aril, (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-(C5-C10)heterociklil, NH2, NH-R', NH-C(O)-(C1-C6)alkil ili C(O)N[(C1-C6)alkil]2;
R6 i R6' su međusobno neovisno H, (C3-C8)cikloalkil, (C1-C8)alkil ili (C1-C3)alkilen-R';
R7 i R8 su međusobno neovisno H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C2-C3)alkenilen-(C6-C10)aril, (C1-C3)alkilen-R', NH-R', NH-SO2-(C1-C6)alkil ili SO2-NH2;
R9 je halogen ili (C1-C6)alkil;
n je 0 ili 1; i
L je O ili O-metilen;
ili njegove farmaceutski prihvatljive soli i/ili stereoizomerni oblici.
47. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što
R3 je H, halogen, CN, (C1-C6)alkil, (C1-C2)alkilen-R' ili NHR'';
R4 je H, halogen, CN, (C1-C4)alkil, (C3-C6)cikloalkil, (C1-C2)alkilen-R';
R5 je H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C1-C6)alkilen-(C6-C10)aril, (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-(C5-C10)heterociklil, NH-R';
R6 je H, (C3-C6)cikloalkil ili (C1-C4)alkil;
R6' je H, (C3-C8)cikloalkil, (C1-C8)alkil ili (C1-C3)alkilen-R';
R7 i R8 su međusobno neovisno H, halogen, CN, NO2, (C1-C6)alkil, (C2-C6)alkenil, R', (C2-C3)alkenilen-(C6-C10)aril, (C1-C3)alkilen-R', NH-SO2-(C1-C6)alkil ili SO2-NH2;
R9 je halogen ili (C1-C4)alkil;
n je 0; i
L je O;
ili njegove farmaceutski prihvatljive soli i/ili stereoizomerni oblici.
48. Spoj u skladu s patentni zahtjev 1, naznačen time što ga se bira iz skupine koju čine
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili njihove farmaceutski prihvatljive soli i/ili stereoizomerni oblici.
49. Spoj formula (I) ili (I'), i/ili njegove fiziološki prihvatljive soli i/ili stereoizomerni oblici, u skladu s bilo kojim od patentnih zahtjeva 1 do 48, naznačen time što je namijenjen upotrebi kao medikament.
50. Upotreba najmanje jednog spoja formule (I) ili (I'), i/ili njegovih fizioloških prihvatljivih soli i/ili stereoizomernih oblika, u skladu s bilo kojim od patentnih zahtjeva 1 do 48, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta.
51. Upotreba najmanje jednog spoja formula (I) ili (I'), i/ili njegovih fiziološki prihvatljivih soli i/ili njegovih stereoizomernih oblika, u skladu s bilo kojim od patentnih zahtjeva 1 do 48, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta za liječenje i/ili sprječavanje hipertenzije, plućne hipertenzije, očne hipertenzije, retinopatije, glaukoma, poremećaja perifernog krvotoka, periferne okluzivne arterijske bolesti (PAOD), koronarne bolesti srca, angine pektoris, hipertrofije srca, srčane insuficijencije, ishemičnih bolesti, ishemične insuficijencija organa (konačnog oštećivanja organa), plućne fibroze, fibroze jetre, insuficijencije jetre, nefropatije, insuficijencije bubrega, fibroze bubrega, glomeruloskleroze bubrega, hipertrofije organa, astme, kronične opstruktivne plućne bolesti (COPD), sindroma dišnog distresa kod odraslih, trombotičnih poremećaja, inzulta, cerebralnog vazospazma, cerebralne ishemije, boli, neuronske degeneracije, ozljede kralježnične moždine, Alzheimerove bolesti, prijevremenog poroda, erektilne disfunkcije, endokrinih disfunkcija, arterioskleroze, hipertrofije prostate, dijabetesa i komplikacija dijabetesa, metaboličkog sindroma, restenoze krvnih žila, ateroskleroze, upale, autoimunih bolesti, AIDS-a, osteopatije, infekcije probavnog sustava bakterija, sepse ili razvoja i napredovanja raka.
52. Medikament, naznačen time što sadrži djelotvornu količinu najmanje jednog spoja formula (I) ili (I'), i/ili njegovih fiziološki prihvatljivih soli i/ili njegovih stereoizomernih oblika, u skladu s bilo kojim od patentnih zahtjeva 1 do 48, fiziološki podnošljive pomoćne tvari i podloge, te, gdje je to prikladno, dodatne aditive i/ili druge aktivne sastojke.
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