HRP20100705T1 - Cikloalkilaminski supstituirani izokinolinski i izokinolinonski derivati - Google Patents
Cikloalkilaminski supstituirani izokinolinski i izokinolinonski derivati Download PDFInfo
- Publication number
- HRP20100705T1 HRP20100705T1 HR20100705T HRP20100705T HRP20100705T1 HR P20100705 T1 HRP20100705 T1 HR P20100705T1 HR 20100705 T HR20100705 T HR 20100705T HR P20100705 T HRP20100705 T HR P20100705T HR P20100705 T1 HRP20100705 T1 HR P20100705T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- alkylene
- aryl
- isoquinolin
- compound according
- Prior art date
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- AWJUIBRHMBBTKR-UHFFFAOYSA-N iso-quinoline Natural products C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 title 1
- VDBNYAPERZTOOF-UHFFFAOYSA-N isoquinolin-1(2H)-one Chemical class C1=CC=C2C(=O)NC=CC2=C1 VDBNYAPERZTOOF-UHFFFAOYSA-N 0.000 title 1
- 150000002537 isoquinolines Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 189
- 150000001875 compounds Chemical class 0.000 claims abstract 61
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 50
- 229910052736 halogen Inorganic materials 0.000 claims abstract 39
- 150000002367 halogens Chemical class 0.000 claims abstract 39
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims abstract 19
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 18
- 125000002947 alkylene group Chemical group 0.000 claims abstract 18
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims abstract 17
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 16
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 10
- 229910052799 carbon Inorganic materials 0.000 claims abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 8
- 125000000217 alkyl group Chemical group 0.000 claims abstract 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 6
- 239000001257 hydrogen Substances 0.000 claims abstract 6
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 6
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims abstract 5
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 3
- 125000003118 aryl group Chemical group 0.000 claims abstract 3
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 2
- 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 claims 19
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 17
- -1 (C1-C6)alkylene-R' Chemical group 0.000 claims 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 10
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 201000010260 leiomyoma Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical group NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 2
- 229920002554 vinyl polymer Polymers 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- VQRVPAVBZKORPH-UHFFFAOYSA-N 6-(4-amino-4-benzylcyclohexyl)oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(N)CC1=CC=CC=C1 VQRVPAVBZKORPH-UHFFFAOYSA-N 0.000 claims 1
- KIFSYDCZKXYTBM-UHFFFAOYSA-N 6-(4-amino-4-phenylcyclohexyl)oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(N)C1=CC=CC=C1 KIFSYDCZKXYTBM-UHFFFAOYSA-N 0.000 claims 1
- KHXBQZITYUJRMU-UHFFFAOYSA-N 6-[(1-amino-4-bicyclo[2.2.2]octanyl)oxy]-7-chloro-2h-isoquinolin-1-one Chemical compound C1=CNC(=O)C(C=C2Cl)=C1C=C2OC1(CC2)CCC2(N)CC1 KHXBQZITYUJRMU-UHFFFAOYSA-N 0.000 claims 1
- DRIVXCAUALAPCG-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-(3,4-dichlorophenyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(CN)C1=CC=C(Cl)C(Cl)=C1 DRIVXCAUALAPCG-UHFFFAOYSA-N 0.000 claims 1
- YQTHQGAWGJYBQU-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-(3,4-dimethoxyphenyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1=C(OC)C(OC)=CC=C1C1(CN)CCC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CC1 YQTHQGAWGJYBQU-UHFFFAOYSA-N 0.000 claims 1
- GITGRQCWFHTEGH-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-(3-chlorophenyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(CN)C1=CC=CC(Cl)=C1 GITGRQCWFHTEGH-UHFFFAOYSA-N 0.000 claims 1
- YHFSMARAKOSCAV-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-(3-methylphenyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound CC1=CC=CC(C2(CN)CCC(CC2)OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)=C1 YHFSMARAKOSCAV-UHFFFAOYSA-N 0.000 claims 1
- XDQASUXTOJJMCZ-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-(4-chlorophenyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(CN)C1=CC=C(Cl)C=C1 XDQASUXTOJJMCZ-UHFFFAOYSA-N 0.000 claims 1
- JQBDVFMSMFKFIU-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-(4-fluorophenyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(CN)C1=CC=C(F)C=C1 JQBDVFMSMFKFIU-UHFFFAOYSA-N 0.000 claims 1
- JJKIFVWUOCEGCD-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-(4-methoxyphenyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1=CC(OC)=CC=C1C1(CN)CCC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CC1 JJKIFVWUOCEGCD-UHFFFAOYSA-N 0.000 claims 1
- AOMYLCRSEQEVCW-UHFFFAOYSA-N 6-[4-(aminomethyl)-4-phenylcyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(CN)C1=CC=CC=C1 AOMYLCRSEQEVCW-UHFFFAOYSA-N 0.000 claims 1
- CONJEOHHKBJXHM-UHFFFAOYSA-N 6-[4-amino-4-(2,3-dihydroxypropyl)cyclohexyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CC(N)(CC(O)CO)CCC1OC(C(=C1)Cl)=CC2=C1C(=O)NC=C2 CONJEOHHKBJXHM-UHFFFAOYSA-N 0.000 claims 1
- BPZATNXUWRXOFR-UHFFFAOYSA-N 6-[5-amino-5-(2,3-dihydroxypropyl)cyclooctyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CCC(N)(CC(O)CO)CCCC1OC(C(=C1)Cl)=CC2=C1C(=O)NC=C2 BPZATNXUWRXOFR-UHFFFAOYSA-N 0.000 claims 1
- QLBYVJQLFXDTAY-UHFFFAOYSA-N 6-[5-amino-5-(3-hydroxypropyl)cyclooctyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CCC(N)(CCCO)CCCC1OC(C(=C1)Cl)=CC2=C1C(=O)NC=C2 QLBYVJQLFXDTAY-UHFFFAOYSA-N 0.000 claims 1
- RSDBMUXVVFBHFP-UHFFFAOYSA-N 6-[5-amino-5-(3-methoxypropyl)cyclooctyl]oxy-7-chloro-2h-isoquinolin-1-one Chemical compound C1CCC(CCCOC)(N)CCCC1OC(C(=C1)Cl)=CC2=C1C(=O)NC=C2 RSDBMUXVVFBHFP-UHFFFAOYSA-N 0.000 claims 1
- WPSDTAMLHYYWJL-UOYQGRGCSA-N 6-[[(1r,5r)-2-amino-6-bicyclo[3.3.1]nonanyl]oxy]-4-benzyl-7-methyl-2h-isoquinolin-1-one Chemical compound C([C@]1(C(CC[C@]2([H])C1)N)[H])CC2OC(C(=CC=1C(=O)NC=2)C)=CC=1C=2CC1=CC=CC=C1 WPSDTAMLHYYWJL-UOYQGRGCSA-N 0.000 claims 1
- XCNFSJZIYIUKAZ-CPWXYTRJSA-N 6-[[(1r,5r)-2-amino-6-bicyclo[3.3.1]nonanyl]oxy]-7-chloro-2h-isoquinolin-1-one Chemical compound C1=CNC(=O)C(C=C2Cl)=C1C=C2OC1CC[C@@]2([H])C(N)CC[C@]1([H])C2 XCNFSJZIYIUKAZ-CPWXYTRJSA-N 0.000 claims 1
- ODGPSQQDTKODQC-QBBMROGASA-N 6-[[(1r,5r)-2-amino-6-bicyclo[3.3.1]nonanyl]oxy]-7-methyl-2h-isoquinolin-1-one Chemical compound C1=CNC(=O)C(C=C2C)=C1C=C2OC1CC[C@@]2([H])C(N)CC[C@]1([H])C2 ODGPSQQDTKODQC-QBBMROGASA-N 0.000 claims 1
- VPSYCISPBILXNB-UHFFFAOYSA-N 7-chloro-6-[4-cyclopropyl-4-(ethylamino)cyclohexyl]oxy-2h-isoquinolin-1-one Chemical compound C1CC(OC=2C(=CC=3C(=O)NC=CC=3C=2)Cl)CCC1(NCC)C1CC1 VPSYCISPBILXNB-UHFFFAOYSA-N 0.000 claims 1
- 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
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 241000894006 Bacteria Species 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
- 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
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010056677 Nerve degeneration 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
- 208000030831 Peripheral arterial occlusive disease 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
- SOYBTBPSATWLBZ-UHFFFAOYSA-N [4-(7-chloroisoquinolin-6-yl)oxy-1-phenylcyclohexyl]methanamine Chemical compound C1CC(OC=2C(=CC3=CN=CC=C3C=2)Cl)CCC1(CN)C1=CC=CC=C1 SOYBTBPSATWLBZ-UHFFFAOYSA-N 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
- 230000017531 blood circulation Effects 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 230000035606 childbirth Effects 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 210000002249 digestive system Anatomy 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
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000015181 infectious disease 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
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 208000007903 liver failure Diseases 0.000 claims 1
- 231100000835 liver failure Toxicity 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 229940126601 medicinal product Drugs 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 150000002825 nitriles Chemical class 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 230000008816 organ damage Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 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
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002028 premature Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000004240 prostatic hypertrophy Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical group 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
- 150000001721 carbon Chemical group 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A61P11/06—Antiasthmatics
-
- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P27/06—Antiglaucoma agents or miotics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Abstract
Spoj formule (I) naznacen time stoR1 je H, OH ili NH2;R2 jeR', (C7-C8)alkil, (C1-C6)alkilen-R', (C2-C6)alkenil, (C2-C6)alkinil, (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', (C1-C6)alkilen-C(O)NH-(C1-C6)alkil, (C1-C6)alkilen-C(O)N[(C1-C6)alkil]2, (C1-C6)alkilen-C(O)N[R']2; (C1-C6)alkilen-C(O)O-(C1-C6)alkil, C(O)O-(C1-C6)alkil, C(O)OR', C(O)(C1-C6)alkil, C(O)R', C(O)-NH-(C2-C6)alkenil, C(O)-NH-(C2-C6)alkinil, C(O)NH-(C1-C6)alkil, C(O)NHR', C(O)-NH(C1-C6)alkilen-R', C(O)N[(C1-C6)alkil]R', C(O)N[(C1-C6)alkil]2,C(O)-(C1-C6)alkilen-R', C(O)O(C1-C6)alkilen-R'; ili R2 je (C1-C6)alkil, uz uvjet da u navedenom alkilnom ostatku najmanje jedan vodik je zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 ili CON(CH3)2;ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na razliciti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eroclani prsten; R3 jeH, halogen, (C1-C6)alkil, (C1-C6)alkilen-R', OH, O-R'', NH2,NHR'', NR''R'' iliNH-C(O)-R'', R4 jeH, halogen, hidroksi, CN, (C1-C6)alkil, R', (C1-C6)alkilen-R'; R5 jeH, 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, CH(OH)-(C1-C6)alkil, 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, iliC(O)O-(C1-C6)alkil; R6 i R6' su, medusobno 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', (C1-C6)alkilen-C(O)NH-(C1-C6)alkil, (C1-C6)alkilen-C(O)N[(C1-C6)alkil]2, (C1-C6)alkilen-C(O)N[R']2; (C1-C6)alkilen-C(O)O-(C1-C6)alkil, C(O)O-(C1-C6)alkil, C(O)OR', C(O)(C1-C6)alkil, C(O)R', C(O)NH-(C1-C6)alkil, C(O)NHR', C(O)N[(C1-C6)alkil]R', C(O)N[(C1-C6)alkil]2,C(O)-(C1-C6)alkilen-R', C(O)O(C1-C6)alkilen-R', iliR6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C10)heterociklilnu skupinu; R7 jeH, halogen, CN, NO2, (C1-C6)alkil, O-(C1-C6)alkil, (C2-C6)alkenil, R', (C2-C6)alkenilen-(C6-C10)aril, (C1-C6)alkilen-R', CH(OH)-(C1-C6)alkil, 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, iliC(O)O-(C1-C6)alkil; R8 je H, halogen ili (C1-C6)alkil; n je 1, 2, 3 ili 4; m je 1, 2, 3, 4 ili 5; r je 0, 1 ili 2 iL je O(CH2)p, S(CH2)p, S(O)(CH2)p, SO2(CH2)p NH(CH2)p, N(C1-C6)alkil-(CH2)p, N(C3-C6)cikloalkil-(CH2)p, N[CO(C1-C6)alkil]-(CH2)p ili N[(C1-C3)alkilen-R']-(CH2)p;p je 0, 1, 2, 3 ili 4; gdjeR' je (C3-C8)cikloalkil, (C5-C10)heterociklil, (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, medusobno neovisno
Claims (58)
1. Spoj formule (I)
[image]
naznačen time što
R1 je H, OH ili NH2;
R2 je
R',
(C7-C8)alkil,
(C1-C6)alkilen-R',
(C2-C6)alkenil,
(C2-C6)alkinil,
(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',
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
(C1-C6)alkilen-C(O)N[(C1-C6)alkil]2,
(C1-C6)alkilen-C(O)N[R']2;
(C1-C6)alkilen-C(O)O-(C1-C6)alkil,
C(O)O-(C1-C6)alkil,
C(O)OR',
C(O)(C1-C6)alkil,
C(O)R',
C(O)-NH-(C2-C6)alkenil,
C(O)-NH-(C2-C6)alkinil,
C(O)NH-(C1-C6)alkil,
C(O)NHR',
C(O)-NH(C1-C6)alkilen-R',
C(O)N[(C1-C6)alkil]R',
C(O)N[(C1-C6)alkil]2,
C(O)-(C1-C6)alkilen-R',
C(O)O(C1-C6)alkilen-R';
ili R2 je (C1-C6)alkil, uz uvjet da u navedenom alkilnom ostatku najmanje jedan vodik je zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 ili CON(CH3)2;
ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na različiti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eročlani prsten;
R3 je
H,
halogen,
(C1-C6)alkil,
(C1-C6)alkilen-R',
OH,
O-R'',
NH2,
NHR'',
NR''R'' ili
NH-C(O)-R'',
R4 je
H,
halogen,
hidroksi,
CN,
(C1-C6)alkil,
R',
(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,
CH(OH)-(C1-C6)alkil,
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',
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
(C1-C6)alkilen-C(O)N[(C1-C6)alkil]2,
(C1-C6)alkilen-C(O)N[R']2;
(C1-C6)alkilen-C(O)O-(C1-C6)alkil,
C(O)O-(C1-C6)alkil,
C(O)OR',
C(O)(C1-C6)alkil,
C(O)R',
C(O)NH-(C1-C6)alkil,
C(O)NHR',
C(O)N[(C1-C6)alkil]R',
C(O)N[(C1-C6)alkil]2,
C(O)-(C1-C6)alkilen-R',
C(O)O(C1-C6)alkilen-R', ili
R6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C10)heterociklilnu skupinu;
R7 je
H,
halogen,
CN,
NO2,
(C1-C6)alkil,
O-(C1-C6)alkil,
(C2-C6)alkenil,
R',
(C2-C6)alkenilen-(C6-C10)aril,
(C1-C6)alkilen-R',
CH(OH)-(C1-C6)alkil,
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;
R8 je H, halogen ili (C1-C6)alkil;
n je 1, 2, 3 ili 4;
m je 1, 2, 3, 4 ili 5;
r je 0, 1 ili 2 i
L je O(CH2)p, S(CH2)p, S(O)(CH2)p, SO2(CH2)p NH(CH2)p, N(C1-C6)alkil-(CH2)p, N(C3-C6)cikloalkil-(CH2)p, N[CO(C1-C6)alkil]-(CH2)p ili N[(C1-C3)alkilen-R']-(CH2)p;
p je 0, 1, 2, 3 ili 4;
gdje
R' je
(C3-C8)cikloalkil,
(C5-C10)heterociklil,
(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;
gdje u ostacima R2, R4, R5, R6, R6', R7 i R8 alkil, alkilen ili cikloalkil mogu jednom ili više puta biti izborno supstituirani s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH CONHCH3 ili CON(CH3)2;
gdje u ostacima R2 do R8 alkil ili alkilen mogu jednom ili više puta biti izborno supstituirani s halogenom;
gdje u ostacima R2 do R8 (C6-C10)aril i (C5-C10)heterociklil su nesupstituirani ili su jednom ili više puta supstituirani s pogodnim skupinama, koje se neovisno bira između halogena, OH, 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, PO3H2, SO3H, SO2-NH2, SO2NH(C1-C6)alkila, SO2N[(C1-C6)alkil]2, S-(C1-C6)alkila; SO-(C1-C6)alkila, SO2-(C1-C6)alkila, SO2-N=CH-N[(C1-C6)alkil]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-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)-NH-(C1-C6)alkil], (C6-C10)arila, (C1-C6)alkilen-(C6-C10)arila, O-(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 jedom do tri puta biti supstituirani sa skupinom koju se neovisno bira između halogena, OH, NO2, CN, O-(C1-C6)alkila, (C1-C6)alkila, NH2, NH(C1-C6)alkila, N[(C1-C6)alkil]2, SO2CH3, COOH, C(O)O-(C1-C6)alkila, CONH2, (C1-C6)alkilen-O-(C1-C6)alkila, (C1-C6)alkilen-O-(C6-C10)arila ili O-(C1-C6)alkilen-(C6-C10)arila;
ili gdje (C6-C10)aril je vicinalno supstituiran s O-(C1-C4)alkilen-O skupinom, gdje 5-8-eročlani prsten se tvori zajedno s atomima ugljika na koje su vezani atomi kisika;
te gdje arilni ili heterociklilni supstituenti (C6-C10)arilnih i (C5-C10)heterociklilnih skupina ne mogu biti daljnje supstituirani sa skupinom koja sadrži aril ili heterociklil;
ili njihovi stereoizomerni i/ili tautomerni oblici i/ili njihove farmaceutski prihvatljive soli.
2. Spoj formule (I) u skladu s patentnim zahtjevom 1, gdje R1 je H, naznačen time što ima formulu (II)
[image]
3. Spoj formule (I) u skladu s patentnim zahtjevom 1, gdje R1 je OH, naznačen time što ima formulu (III)
[image]
4. Spoj formule (I) u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 3, gdje R1 je OH, naznačen time što ima formulu (III')
[image]
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R1 je NH2.
6. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što R3 je H, halogen, (C1-C4)alkilen-R', O-R'' ili NHR''.
7. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time što R3 je H ili NHR''.
8. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što R3 je H; NH-(C5-C6)heterociklil, ili NH-fenil.
9. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time što R3 je H.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što R8 je H, halogen ili (C1-C4)alkil.
11. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačen time što R8 je H, Cl, F, metil ili etil.
12. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 11, naznačen time što R8 je H.
13. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 12, naznačen time što R4 je H, halogen ili (C1-C6)alkil.
14. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 13, naznačen time što R4 je H, halogen ili (C1-C4)alkil.
15. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 14, naznačen time što R4 je H.
16. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 15, naznačen time što R5 je H, halogen, CN, (C1-C6)alkil, (C2-C6)alkenil, R', NH-(C6-C10)aril, (C1-C6)alkilen-(C6-C10)aril ili (C1-C6)alkilen-(C5-C10)heterociklil.
17. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 16, naznačen time što R5 je H, halogen, (C1-C6)alkil, (C2-C6)alkenil, R', NH-(C6-C10)aril, (C1-C6)alkilen-(C6-C10)aril ili (C1-C6)alkilen-(C5-C10)heterociklil.
18. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 17, naznačen time što R5 je H, halogen, (C1-C6)alkil, (C2-C6)alkenil, (C6-C10) aril, NH-(C6-C10)aril, (C1-C2)alkilen-(C6-C10)aril ili (C5-C10)heteroaril.
19. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 18, naznačen time što R5 je H, halogen, (Cl-C6)alkil, (C2-C6)alkenil, (C6-C10)aril ili (C5-C10)heteroaril.
20. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 19, naznačen time što R5 je H, halogen, metil, etil, vinil, fenil, tienil ili piridil.
21. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 20, naznačen time što R5 je H, halogen, metil, ili etil.
22. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 21, naznačen time što R5 je H.
23. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 22, naznačen time što R7 je H, halogen, CN, (C1-C6)alkil, O-(C1-C6)alkil, (C2-C6)alkenil, R' ili (C1-C6)alkilen-(C3-C8)cikloalkil.
24. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 23, naznačen time što R7 je H, halogen, CN, (C1-C4)alkil, O-(C1-C4)alkil, (C2-C4)alkenil, fenil, ciklopropil ili (C5-C6)heteroaril.
25. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 24, naznačen time što R7 je H, fluor, klor, brom, metil, etil, metoksi, fenil, nitril, ciklopropil, tienil ili vinil.
26. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 25, naznačen time što R7 je H, fluor, klor, brom, metil ili metoksi.
27. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 26, naznačen time što R7 je H.
28. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 27, naznačen time što m je 2, 3, ili 4.
29. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 28, naznačen time što m je 3.
30. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 29, naznačen time što R2 je
R',
(C7-C8)alkil, (C1-C6)alkilen-R', (C2-C6)alkenil, (C1-C6)alkilen-C(O)NH2,
(C1-C6)alkilen-C(O)NH-R', (C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
(C1-C6)alkilen-C(O)N[(C1-C6)alkil]2,
(C1-C6)alkilen-C(O)N[R']2;
(C1-C6)alkilen-C(O)O-(C1-C6)alkil,
C(O)NH-(C1-C6)alkil,
C(O)NHR',
C(O)-NH-(C2-C6)alkenil,
C(O)-NH-(C2-C6)alkinil,
C(O)-NH(C1-C6)alkilen-R',
C(O)N[(C1-C6)alkil]R',
C(O)N[(C1-C6)alkil]2,
C(O)-(C1-C6)alkilen-R',
C(O)O(C1-C6)alkilen-R';
ili R2 je (C1-C6)alkil, uz uvjet da u navedenom alkilnom ostatku najmanje jedan vodik je zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 ili CON(CH3)2;
ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na različiti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eročlani prsten.
31. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 30, naznačen time što R2 je
R',
(C1-C6)alkilen-R',
(C2-C6)alkenil,
(C1-C6)alkilen-C(O)NH2,
(C1-C6)alkilen-C(O)NH-R',
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
C(O)NH-(C1-C6)alkil,
C(O)NHR',
C(O)-NH-(C2-C6)alkinil,
C(O)-NH(C1-C6)alkilen-R',
ili R2 je (C1-C3)alkil, uz uvjet da u navedenom alkilnom ostatku najmanje jedan vodik je zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH ili CON(CH3)2;
ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na različiti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eročlani prsten.
32. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 31, naznačen time što R2 je
R',
(C1-C6)alkilen-R',
(C2-C6)alkenil,
(C1-C6)alkilen-C(O)NH-R',
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
C(O)NH-(C1-C6)alkil,
C(O)NHR',
C(O)-NH-(C2-C6)alkinil,
C(O)-NH(C1-C6)alkilen-R',
ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na različiti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eročlani prsten;
33. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 32, naznačen time što n je 1, 2 ili 3.
34. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 33, naznačen time što n je 1 ili 2.
35. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 34, naznačen time što n je 1.
36. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 35, naznačen time što r je 0 ili 1.
37. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 36, naznačen time što
R6 i R6' su, međusobno neovisno,
H, (C1-C6)alkil,
R', (C1-C4)alkilen-(C3-Cg)cikloalkil,
(C1-C4)alkilen-(C5-C10)heterociklil,
C1-C4)alkilen-(C6-C10)aril,
(C1-C6)alkilen-O-(C1-C6)alkil,
(C1-C4)alkilen-C(O)-(C5-C10)heterociklil,
(C1-C4)alkilen-C(O)-(C6-C10)aril,
(C1-C6)alkilen-C(O)N[(C1-C6)alkil]2,
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
(C1-C6)alkilen-C(O)O-(C1-C6)alkil,
C(O)O-(C1-C6)alkil,
C(O)(C1-C6)alkil,
C(O)R',
C(O)NH-(C1-C6)alkil,
C(O)N[(C1-C6)alkil]2, ili
C(O)(C1-C6)alkilen-R',
ili R6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C10)heterociklilnu skupinu.
38. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 37, naznačen time što R6 i R6' su, međusobno neovisno,
H,
(C1-C6)alkil,
(C5-C10)heterociklil,
(C3-C8)cikloalkil,
(C6-C10)aril,
(C1-C4)alkilen-(C3-C8)cikloalkil,
(C1-C4)alkilen-(C5-C10)heterociklil,
(C1-C4)alkilen-(C6-C10)aril,
(C1-C6)alkilen-O-(C1-C6)alkil,
(C1-C6)alkilen-C(O)N[(C1-C6)alkil]2,
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
(C1-C6)alkilen-C(O)O-(C1-C6)alkil,
C(O)O-(C1-C6)alkil,
C(O)(C1-C6)alkil,
C(O)(C3-C8)cikloalkil,
C(O)NH-(C1-C6)alkil.
C(O)N[(C1-C6)alkil]2,
C(O)(C1-C6)alkilen-(C3-C8)cikloalkil,
C(O)(C1-C6)alkilen-(C5-C10)heterociklil,
C(O)(C1-C6)alkilen-(C6-C10)aril,
ili R6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C10)heterociklilnu skupinu.
39. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 38, naznačen time što
R6 je H, (C1-C6)alkil, (C3-C6)cikloalkil ili (C1-C4)alkilen-(C3-C6)cikloalkil, i
R6' je H,
(C1-C6)alkil,
(C3-C8)cikloalkil,
(C5-C10)heterociklil,
(C6-C10)aril,
(C1-C4)alkilen-(C3-C8)cikloalkil,
(C1-C4)alkilen-(C5-C10)heterociklil,
(C1-C4)alkilen-(C6-C10)aril,
(C1-C6)alkilen-O-(C1-C6)alkil,
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
(C1-C6)alkilen-C(O)N[(C1-C6)alkil]2,
(C1-C6)alkilen-C(O)O-(C1-C6)alkil,
C(O)O-(C1-C6)alkil,
C(O)(C1-C6)alkil,
C(O)(C3-C8)cikloalkil,
C(O)NH-(C1-C6)alkil,
C(O)N[(C1-C6)alkil]2,
C(O)(C1-C6)alkilen-(C3-C8)cikloalkil,
C(O)(C1-C6)alkilen-(C5-C10)heterociklil,
C(O)(C1-C6)alkilen-(C6-C10)aril, ili
R6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C10)heterociklilnu skupinu.
40. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 39, naznačen time što
R6 je H, (C1-C6)alkil i
R6' je H,
(C1-C6)alkil,
(C3-C8)cikloalkil,
(C6-C10)aril,
(C5-C10)heterociklil,
(C1-C4)alkilen-(C3-C8)cikloalkil,
(C1-C4)alkilen-(C5-C10)heterociklil,
(C1-C6)alkilen-(C6-C10)aril,
(C1-C4)alkilen-O-(C1-C4)alkil,
(C1-C4)alkilen-C(O)N[(C1-C4)alkil]2,
(C1-C6)alkilen-C(O)NH-(C1-C6)alkil,
C(O)(C1-C6)alkil,
C(O)(C1-C6)alkilen-(C5-C10)heterociklil, ili
R6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C10)heterociklilnu skupinu.
41. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 40, naznačen time što
R6 je H, (C1-C6)alkil i
R6' je
H,
(C1-C6)alkil;
(C3-C8)cikloalkil;
(C1-C4)alkilen-(C3-C8)cikloalkil;
(C1-C4)alkilen-O-(C1-C4)alkil;
(C1-C4)alkilen-C(O)N[(C1-C4)alkil]2;
(C1-C4)alkilen-(C5-C10)heterociklil, ili (C1-C4)alkilen-(C6-C10)aril;
C(O)(C1-C4)alkil;
C(O)(C1-C4)alkilen-(C5-C10)heterociklil;
ili R6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C6)heterociklilnu skupinu.
42. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 41, naznačen time što R6 je H, (C1-C6)alkil, a R6' je H, (C1-C6)alkil ili (C3-C8) cikloalkil.
43. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 42, naznačen time što R6 je H i R6' je H, (C1-C6)alkil ili (C3-C8)cikloalkil.
44. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 43, naznačen time što R6 i R6' su H.
45. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 44, naznačen time što m je 3, a L je vezan na položaj 3 ili na položaj 4 u aminocikloheksanskom prstenu.
46. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 45, naznačen time što m je 3, a L je vezan na položaj 4 u aminocikloheksanskom prstenu.
47. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 46, naznačen time što L je S(CH2)p, S(O)(CH2)p, ili SO2(CH2)p.
48. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 46, naznačen time što L je NH(CH2)p ili N(C1-C6)alkil)-(CH2)p.
49. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 46, naznačen time što L je O(CH2)p.
50. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 49, naznačen time što p je 0.
51. Spoj u skladu s patentnim zahtjevom 1, naznačen time što
R1 je H ili OH,
R2 je R', (C7-C8)alkil, (C1-C6)alkilen-R', (C1-C6)alkenil, (C1-C6)alkilen-C(O)NH2, (C1-C6)alkilen-C(O)NH-R', (C1-C6)alkilen-C(O)NH-(C1-C6)alkil,(C1-C6)alkilen-C(O)N[(C1-C6)alkil]2, (C1-C6)alkilen-C(O)N[R']2, (C1-C6)alkilen-C(O)O-(C1-C6)alkil, C(O)NH-(C1-C6)alkil, C(O)NHR', C(O)-NH-(C2-C6)alkenil, C(O)-NH-(C2-C6)alkinil, C(O)-NH(C1-C6)alkilen-R', C(O)N[(C1-C6)alkil]R', C(O)N[(C1-C6)alkil]2, C(O)-(C1-C6)alkilen-R', C(O)O(C1-C6)alkilen-R';
ili R2 je (C1-C6)alkil, uz uvjet da u navedenom alkilnom ostatku najmanje jedan vodik je zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 ili CON(CH3)2;
ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na različiti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eročlani prsten;
R3 je H, halogen, (C1-C4)alkilen-R', O-R'' ili NHR''
R4 je H, halogen ili (C1-C6)alkil;
R5 je H, (C1-C6)alkil, halogen, CN, (C2-C6)alkenil, (C6-C10)aril, NH-(C6-C10)aril, (C1-C6)alkilen-(C6-C10)aril, (C5-C10)heterociklil ili (C1-C6)alkilen-(C5-C10)heterociklil;
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)NH2, (C1-C6)alkilen-C(O)NH-R', (C1-C6)alkilen-C(O)N[(C1-C4)alkil]2, (C1-C6)alkilen-C(O)N[R']2, C(O)O-(C1-C6)alkil, C(O)(C1-C6)alkil, C(O)(C3-C8)cikloalkil, C(O)(C5-C10)heterociklil, C(O)NH-(C1-C6)alkil, C(O)N[(C1-C6)alkil]2, C(O)(C1-C6)alkilen-C3-C8)cikloalkil, C(O)(C1-C6)alkilen-(C5-C10)heterociklil, C(O)(C1-C6)alkilen-(C6-C10)aril, ili R6 i R6', zajedno s N-atomom na kojeg su vezani, tvore (C5-C6)heterociklilnu skupinu;
R7 je H, halogen, CN, (C1-C6)alkil, O-(C1-C6)alkil, (C2-C6)alkenil ili R';
R8 je H, halogen ili (C1-C6)alkil;
m je 2, 3 ili 4,
n je 1, 2 ili 3,
r je 0, 1 ili 2,
L je O(CH2)p, S(CH2)p, NH(CH2)p ili N(C1-C2)alkil-(CH2)p, i
p je 0, 1 ili 2.
52. Spoj u skladu s patentnim zahtjevom 1, naznačen time što
R1 je H ili OH;
R2 je R', (C1-C6)alkilen-R', (C1-C6)alkenil, (C1-C6)alkilen-C(O)NH2, (C1-C6)alkilen-C(O)NH-R', (C1-C6)alkilen-C(O)NH-(C1-C6)alkil, C(O)NH-(C1-C6)alkil, C(O)NHR', C(O)-NH-(C2-C6)alkinil, C(O)-NH(C1-C6)alkilen-R',
ili R2 je (C1-C3)alkil, uz uvjet da u navedenom alkilnom ostatku najmanje jedan vodik je zamijenjen s OH, OCH3, COOH, COOCH3, NH2, NHCH3, N(CH3)2, CONH2, CONHCH3 ili CON(CH3)2;
ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na različiti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eročlani prsten;
R3 je H, halogen ili NHR'', gdje R'' je definiran kao gore;
R4 je H, halogen ili (C1-C4)alkil;
R5 je H, (C1-C6)alkil, halogen, (C2-C4)alkenil, (C6-C10)aril, (C1-C6)alkilen-(C6-C10)aril ili (C5-C10)heterociklil;
R6 i R6' su, međusobno neovisno, H, (C3-C8)cikloalkil, (C1-C8)alkil, (C1-C6)alkilen-O-(C1-C6)alkil, (C1-C3)alkilen-R', C(O)(C1-C6)alkil, C(O)(C3-C8)cikloalkil, C(O)(C5-C6)heterociklil, C(O)(C1-C6)alkilen-(C3-C8)cikloalkil, C(O)(C1-C6)alkilen-(C5-C6)heterociklil ili C(O)(C1-C6)alkilen-(C6-C10)aril;
R7 je H, halogen, CN, (C1-C6)alkil, O(C1-C6)alkil, (C2-C6)alkenil ili R';
R8 je H, halogen ili (C1-C6)alkil;
m je 2, 3 ili 4;
n je 1, 2 ili 3;
r je 0 ili 1;
L je O(CH2)p, S(CH2)p ili NH(CH2)p; i
p je 0 ili 1.
53. Spoj u skladu s patentnim zahtjevom 1, naznačen time što
R1 je H ili OH;
R2 je R', (C1-C6)alkilen-R', (C1-C6)alkenil, (C1-C6)alkilen-C(O)NH-R', (C1-C6)alkilen-C(O)NH-(C1-C6)alkil, C(O)NH-(C1-C6)alkil, C(O)NHR', C(O)-NH-(C2-C6)alkinil, C(O)-NH(C1-C6)alkilen-R',
ili R2 je (C1-C4)alkilen, vezan na cikloalkilamin, gdje (C1-C4)alkilen tvori drugu vezu na različiti atom ugljika u cikloalkilaminskom prstenu, te, zajedno s atomima ugljika u cikloalkilaminu, tvori drugi, 4-8-eročlani prsten;
R3 je H, NH-(C5-C6)heteroaril ili NH-fenil;
R4 je H, halogen ili (C1-C4)alkil;
R5 je H, (C1-C4)alkil, halogen, (C2-C4)alkenil, (C6-C10)aril, (C1-C2)alkil-(C6-C10)aril ili (C5-C6)heteroaril;
R6 je H, (C3-C6)cikloalkil ili (C1-C4)alkil;
R6' je H, (C3-C8)cikloalkil, (C1-C8)alkil, (C1-C3)alkilen-R', C(O)O-(C1-C6)alkil, C(O)(C1-C6)alkil, C(O)(C3-C6)cikloalkil, C(O)(C5-C6)heterociklil, C(O)(C1-C3)alkilen-(C3-C6)cikloalkil, C(O)(C1-C3)alkilen-(C5-C6)heterociklil ili C(O)(C1-C3)alkilen-fenil;
R7 je H, halogen, CN, (C1-C4)alkil, O(C1-C4)alkil, (C2-C4)alkenil, fenil, ciklopropil, (C5-C6)heteroaril;
R8 je H, halogen ili (C1-C4)alkil;
m je 3,
n je 1;
r je 0 ili 1 i
L je O, S ili NH;
ili njihovi stereoizomerni i/ili tautomerni oblici i/ili njihove farmaceutski prihvatljive soli.
54. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira iz skupine koju čine
6-(4-Alil-4-aminocikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-(4-Alil-4-aminocikloheksiloksi)-2H-izokinolin-1-on,
6-(4-amino-4-benrilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-(4-Amino-4-fenilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-(4-Aminometil-4-fenilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-[4-Aminometil-4-(4-klorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-Aminometil-4-(3-klorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-Aminometil-4-(3-metilfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-Aminometil-4-(3,4-dimetoksi-fenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-Aminometil-4-(4-fluorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-Aminometil-4-(4-metoksi-fenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-Amlinometil-4-(4-metilfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-Aminometil-4-(3,4-diklorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on, ili
([4-(7-Klorizokinolin-6-iloksi)-1-fenilcikloheksil]metilamin),
ili njihovi stereoizomerni i/ili tautomerni oblici i/ili njihove farmaceutski prihvatljive soli.
55. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira iz skupine koju čine
6-(4-Alil-4-aminocikloheksiloksi)-4,7-dimetil-2H-izokinolin-1-on,
6-(cis-4-Alil-4-aminocikloheksiloksi)-7-metil-2H-izokinolin-1-on ,
6-(cis-4-Amino-4-ciklopropilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-(trans-4-Amino-4-ciklopropilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-(trans-4-Amino-4-ciklopropilcikloheksiloksi)-7-metil-2H-izokinolin-1-on,
6-(cis-1-Aminobicikloheksil-4-iloksi)-7-klor-2H-izokinolin-1-on,
6-(trans-1-Aminobicikloheksil-4-iloksi)-7-klor-2H-izokinolin-1-on,
6-(5-Alil-5-aminociklooktiloksi)-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(3-metoksipropil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[trans-4-Amino-4-(3-metoksipropil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-(trans-4-Benzilamino-4-ciklopropilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
7-Klor-6-(trans-4-ciklopropil-4-isopropilaminocikloheksiloksi)-2H-izokinolin-1-on,
7-Klor-6-(4-ciklopropil-4-etilaminocikloheksiloksi)-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(3-hidroksipropil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[trans-4-amino-4-(3-hidroksipropil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[4-amino-4-(2,3-dihidroksipropil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[5-Amino-5-(3-hidroksipropil)ciklooktiloksi]-7-klor-2H-izokinolin-1-on,
6-[5-Amino-5-(3-metoksipropil)ciklooktiloksi]-7-klor-2H-izokinolin-1-on,
6-[5-Amino-5-(2,3-dihidroksipropil)ciklooktiloksi]-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(4-fluorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-(cis-4-Amino-4-fenilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-(trans-4-Amino-4-fenilcikloheksiloksi)-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(4-trifluormetilfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(4-fluorfenil)cikloheksiloksi]-4-benzil-7-metil-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(3,5-dimetilfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(3,5-dimetilfenil)cikloheksiloksi]-7-metil-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(2,4-difluorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(2,6-difluorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(2,6-difluorfenil)cikloheksiloksi]-7-metil-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(4-fluorfenil)cikloheksiloksi]-7-metil-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(2,6-difluorfenil)cikloheksiloksi]-4-benzil-7-metil-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(2,4-difluorfenil)cikloheksiloksi]-7-metil-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(2-fluorfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(2-fluorfenil)cikloheksiloksi]-7-metil-2H-izokinolin-1-on,
6-[cis-4-Amino-4-(3,5-dimetilfenil)cikloheksiloksi]-7-klor-2H-izokinolin-1-on,
6-((1R,5R)-6-Aminobiciklo[3.3.1]non-2-iloksi)-7-klor-2H-izokinolin-1-on,
6-((1R,5R)-6-Aminobiciklo[3.3.1]non-2-iloksi)-7-metil-2H-izokinolin-1-on,
6-((1R,5R)-6-Aminobiciklo[3.3.1]non-2-iloksi)-4-benzil-7-metil-2H-izokinolin-1-on,
6-(4-Aminobiciklo[2.2.2]okt-1-iloksi)-7-klor-2H-izokinolin-1-on,
6-{[(3-endo)-3-Aminobiciklo[3.3.1]non-9-il]oksi}-7-klorizokinolin-1(2H)-on,
6-{[(3-exo)-3-Aminobiciklo[3.3.1]non-9-il]oksi}-7-klorizokinolin-1(2H)-on,
6-{[(3-endo,8-syn)-3-Aminobiciklo[3.2.1]okt-8-il]oksi}-7-klorizokinolin-1(2H)-on, ili
6-{[(3-endo,8-anti)-3-Aminobiciklo[3.2.1]okt-8-il]oksi}-7-klorizokinolin-1(2H)-on,
ili njihovi stereoizomerni i/ili tautomerni oblici i/ili njihove farmaceutski prihvatljive soli.
56. Upotreba najmanje jednog spoja formule (I), i/ili njegove farmaceutski prihvatljive soli, u skladu s bilo kojim od patentnih zahtjeva 1 do 55, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta.
57. Upotreba najmanje jednog spoja formule (I), i/ili njegove farmaceutski prihvatljive soli, u skladu s bilo kojim od patentnih zahtjeva 1 do 55, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta za liječenje i/ili sprječavanje hipertenzije, plućne hipertenzije, očne hipertenzije, retinopatije, glaukoma, poremećaja perifernog krvotoka, bolesti začepljenja perifernih arterija (PAOD), koronarne bolesti srca, angine pektoris, hipertrofije srca, insuficijencije srca, ishemičnih bolesti, ishemične insuficijencije organa (oštećenja krajnjeg organa), fibroidnih pluća, fibroidne jetre, insuficijencije jetre, nefropatije, insuficijencije bubrega, fibroidnog bubrega, glomeruloskleroze bubrega, hipertrofije organa, astme, kronične opstruktivne plućne bolesti (COPD), sindroma dišnog distresa kod odraslih, trombotičkih poremećaja, inzulta, cerebralnog vazospazma, cerebralne ishemije, boli, degeneracije nerurona, ozljede kralježnične moždine, Alzheimerove bolesti, prijevremenog porođaja, 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 bakterijama, sepse ili razvoja i napredovanja raka.
58. Medikament, naznačen time što sadrži djelotvornu količinu najmanje jednog spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 55, i/ili njegove farmakološki prihvatljive soli, farmaceutski prihvatljive pomoćne tvari i podloge, te, gdje je to prikladno, dodatne aditive i/ili druge aktivne sastojke.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06026897 | 2006-12-27 | ||
| PCT/EP2007/011169 WO2008077556A1 (en) | 2006-12-27 | 2007-12-19 | Cycloalkylamine substituted isoquinoline and isoquinolinone derivatives |
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