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
Links
- -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
-
- 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
- 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
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P11/16—Central respiratory analeptics
-
- 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
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- A61P5/00—Drugs for disorders of the endocrine 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
-
- 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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Gynecology & Obstetrics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Reproductive Health (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Molecular Biology (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)
[image]
ili formule (I')
[image]
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)
[image]
3. Spoj formule (I') u skladu s patentni zahtjev 1, naznačen time što ga karakterizira spoj formule (II')
[image]
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.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05016153 | 2005-07-26 | ||
| PCT/EP2006/007140 WO2007012422A1 (en) | 2005-07-26 | 2006-07-20 | Cyclohexylamin isoquinolone derivatives as rho-kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20110839T1 true HRP20110839T1 (hr) | 2011-12-31 |
Family
ID=35115842
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20110839T HRP20110839T1 (hr) | 2005-07-26 | 2011-11-14 | Derivati cikloheksaminizokinolona kao inhibitori rho-kinaze |
Country Status (37)
| Country | Link |
|---|---|
| US (2) | US8609691B2 (hr) |
| EP (1) | EP1912949B1 (hr) |
| JP (1) | JP5049970B2 (hr) |
| KR (1) | KR101336678B1 (hr) |
| CN (1) | CN101228132B (hr) |
| AR (1) | AR057082A1 (hr) |
| AT (1) | ATE521595T1 (hr) |
| AU (1) | AU2006274246B2 (hr) |
| BR (1) | BRPI0614063A2 (hr) |
| CA (1) | CA2615663C (hr) |
| CR (1) | CR9604A (hr) |
| CY (1) | CY1112085T1 (hr) |
| DK (1) | DK1912949T3 (hr) |
| DO (1) | DOP2006000177A (hr) |
| EC (1) | ECSP088136A (hr) |
| ES (1) | ES2372067T3 (hr) |
| GT (1) | GT200600327A (hr) |
| HK (1) | HK1123036A1 (hr) |
| HN (1) | HN2008000130A (hr) |
| HR (1) | HRP20110839T1 (hr) |
| IL (1) | IL188949A (hr) |
| MA (1) | MA29639B1 (hr) |
| MX (1) | MX2008000956A (hr) |
| MY (1) | MY146644A (hr) |
| NI (1) | NI200800024A (hr) |
| NO (1) | NO20080965L (hr) |
| NZ (1) | NZ565669A (hr) |
| PE (1) | PE20070181A1 (hr) |
| PL (1) | PL1912949T3 (hr) |
| PT (1) | PT1912949E (hr) |
| RS (1) | RS52241B (hr) |
| RU (1) | RU2440988C2 (hr) |
| SI (1) | SI1912949T1 (hr) |
| TN (1) | TNSN08038A1 (hr) |
| TW (1) | TWI412521B (hr) |
| WO (1) | WO2007012422A1 (hr) |
| ZA (1) | ZA200710952B (hr) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006264043B2 (en) | 2005-06-28 | 2012-04-26 | Sanofi-Aventis | Isoquinoline derivatives as inhibitors of Rho-kinase |
| CN101228132B (zh) | 2005-07-26 | 2012-10-10 | 塞诺菲-安万特股份有限公司 | 作为Rho-激酶抑制剂的环己基胺异喹啉酮衍生物 |
| UA93882C2 (ru) | 2005-07-26 | 2011-03-25 | Санофи-Авентис | Пиперидинил-замещенные производные изохинолона kak ингибиторы rho-киназы |
| US7893088B2 (en) * | 2006-08-18 | 2011-02-22 | N.V. Organon | 6-substituted isoquinoline derivatives |
| JP5271909B2 (ja) * | 2006-09-11 | 2013-08-21 | エム・エス・ディー・オス・ベー・フェー | ２−（１−オキソ−１ｈ−イソキノリン−２−イル）アセトアミド誘導体 |
| BRPI0720862A2 (pt) | 2006-12-27 | 2014-02-25 | Sanofi Aventis | Derivados de isoquinolina e isoquinolinona substituídos como inibidores de rho-cinase |
| WO2008077555A2 (en) | 2006-12-27 | 2008-07-03 | Sanofi-Aventis | Substituted isoquinolines and their use as rho-kinase inhibitors |
| CN101611012B (zh) * | 2006-12-27 | 2012-11-14 | 塞诺菲-安万特股份有限公司 | 环烷基胺取代的异喹啉衍生物 |
| KR101494452B1 (ko) | 2006-12-27 | 2015-02-16 | 사노피 | 사이클로알킬아민 치환된 이소퀴놀린 및 이소퀴놀리논 유도체 |
| MY155009A (en) | 2006-12-27 | 2015-08-28 | Sanofi Aventis | Cycloalkylamine substituted isoquinolone derivatives |
| KR20090094338A (ko) | 2006-12-27 | 2009-09-04 | 사노피-아벤티스 | 치환된 이소퀴놀린 및 이소퀴놀리논 유도체 |
| CL2008000973A1 (es) | 2007-04-05 | 2009-01-02 | Astrazeneca Ab | Compuestos derivados de 1-oxo-isoquinolina; procedimiento de preparación; composición farmacéutica; y su uso en el tratamiento de enfermedades pulmonares obstructvas crónicas (epoc) y asma. |
| JP5524071B2 (ja) * | 2007-10-24 | 2014-06-18 | メルク・シャープ・アンド・ドーム・コーポレーション | 複素環フェニルアミドｔ型カルシウムチャネルアンタゴニスト |
| RU2532481C2 (ru) | 2008-06-24 | 2014-11-10 | Санофи-Авентис | Би- и полициклические замещенные производные изохинолина и изохинолинона, полезные в качестве ингибиторов rho-киназы |
| PL2313374T3 (pl) * | 2008-06-24 | 2014-03-31 | Sanofi Sa | 6-podstawione izochinoliny i izochinolinony |
| KR101638326B1 (ko) * | 2008-06-24 | 2016-07-12 | 사노피 | Ｒｈｏ 키나제 억제제로서의 치환된 이소퀴놀린 및 이소퀴놀리논 |
| BRPI0917936A2 (pt) * | 2008-08-25 | 2017-07-11 | Irm Llc | Moduladores de via hedgehog |
| AR073711A1 (es) | 2008-10-01 | 2010-11-24 | Astrazeneca Ab | Derivados de isoquinolina |
| TW201443023A (zh) * | 2013-01-18 | 2014-11-16 | 必治妥美雅史谷比公司 | 作爲ｒｏｃｋ抑制劑之酞□酮及異喹啉酮 |
| FI3640241T3 (fi) | 2013-10-18 | 2023-01-13 | Bromodomeeni-inhibiittorit | |
| CA2927830A1 (en) * | 2013-10-23 | 2015-04-30 | Chugai Seiyaku Kabushiki Kaisha | Quinazolinone and isoquinolinone derivative |
| FR3017868A1 (fr) | 2014-02-21 | 2015-08-28 | Servier Lab | Derives d'isoquinoleine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| CN105085478B (zh) * | 2014-04-28 | 2019-04-12 | 南京明德新药研发股份有限公司 | 异喹啉磺胺衍生物及其药物组合物和制药用途 |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| WO2016180918A1 (en) | 2015-05-12 | 2016-11-17 | Platod | Combination of pharmacological and microfluidic features for improved platelets production |
| WO2017003723A1 (en) | 2015-07-01 | 2017-01-05 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| AU2017252276A1 (en) | 2016-04-18 | 2018-11-15 | Celgene Quanticel Research, Inc. | Therapeutic compounds |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| WO2019023278A1 (en) | 2017-07-25 | 2019-01-31 | Crinetics Pharmaceuticals, Inc. | MODULATORS OF SOMATOSTATIN AND USES THEREOF |
| WO2019236879A1 (en) * | 2018-06-07 | 2019-12-12 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| CN114874236B (zh) * | 2022-06-24 | 2023-05-05 | 中国工程物理研究院化工材料研究所 | 一种五元氮杂稠环骨架及其制备方法 |
Family Cites Families (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2485537B2 (fr) | 1977-04-13 | 1986-05-16 | Anvar | Dipyrido(4,3-b)(3,4-f)indoles, procede d'obtention, application therapeutique et compositions pharmaceutiques les contenant |
| WO1992002476A1 (en) | 1990-07-31 | 1992-02-20 | E.I. Du Pont De Nemours And Company | Catalytic equilibration of selected halocarbons |
| US5480883A (en) * | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| GB9516709D0 (en) | 1995-08-15 | 1995-10-18 | Zeneca Ltd | Medicament |
| ZA9610741B (en) | 1995-12-22 | 1997-06-24 | Warner Lambert Co | 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists |
| DE69737631T3 (de) | 1996-08-12 | 2011-08-18 | Mitsubishi Tanabe Pharma Corp. | MEDIKAMENTE ENTHALTEND Rho-KINASE INHIBITOREN |
| JPH1087629A (ja) | 1996-09-18 | 1998-04-07 | Fujisawa Pharmaceut Co Ltd | 新規イソキノリン誘導体、およびその医薬用途 |
| AU8872198A (en) | 1997-08-29 | 1999-03-22 | Zeneca Limited | Aminometyl oxooxazolidinyl benzene derivatives |
| TW575567B (en) | 1998-10-23 | 2004-02-11 | Akzo Nobel Nv | Serine protease inhibitor |
| US6541456B1 (en) | 1999-12-01 | 2003-04-01 | Isis Pharmaceuticals, Inc. | Antimicrobial 2-deoxystreptamine compounds |
| US6784192B2 (en) | 2000-01-20 | 2004-08-31 | Eisai Co., Ltd. | Piperidine compound and pharmaceutical composition thereof |
| US7217722B2 (en) * | 2000-02-01 | 2007-05-15 | Kirin Beer Kabushiki Kaisha | Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same |
| AU2001239947A1 (en) | 2000-02-29 | 2001-09-12 | Curis, Inc. | Methods and compositions for regulating adipocytes |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| AR033517A1 (es) | 2000-04-08 | 2003-12-26 | Astrazeneca Ab | Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos |
| GB0013060D0 (en) | 2000-05-31 | 2000-07-19 | Astrazeneca Ab | Chemical compounds |
| AU2001296008A1 (en) | 2000-10-27 | 2002-05-06 | Takeda Chemical Industries Ltd. | Process for preparing substituted aromatic compounds and intermediates therefor |
| WO2002055496A1 (en) | 2001-01-15 | 2002-07-18 | Glaxo Group Limited | Aryl piperidine and piperazine derivatives as inducers of ldl-receptor expression |
| SE0101038D0 (sv) | 2001-03-23 | 2001-03-23 | Astrazeneca Ab | Novel compounds |
| WO2002088101A2 (en) | 2001-04-27 | 2002-11-07 | Vertex Pharmaceuticals Incorporated | Inhibitors of bace |
| US7199147B2 (en) * | 2001-06-12 | 2007-04-03 | Dainippon Sumitomo Pharma Co., Ltd. | Rho kinase inhibitors |
| GB0117899D0 (en) | 2001-07-23 | 2001-09-12 | Astrazeneca Ab | Chemical compounds |
| WO2003024450A1 (en) | 2001-09-20 | 2003-03-27 | Eisai Co., Ltd. | Methods for treating prion diseases |
| SE0104340D0 (sv) | 2001-12-20 | 2001-12-20 | Astrazeneca Ab | New compounds |
| KR20050019918A (ko) * | 2002-07-22 | 2005-03-03 | 아사히 가세이 파마 가부시키가이샤 | 5-치환 이소퀴놀린 유도체 |
| WO2004009555A1 (ja) * | 2002-07-22 | 2004-01-29 | Asahi Kasei Pharma Corporation | ５−置換イソキノリン誘導体 |
| WO2004024717A1 (ja) | 2002-09-12 | 2004-03-25 | Kirin Beer Kabushiki Kaisha | キナーゼ阻害活性を有するイソキノリン誘導体およびそれを含む医薬 |
| ATE421324T1 (de) * | 2003-03-11 | 2009-02-15 | Novartis Ag | Verwendung von isochinolin-derivaten zur behandlung von krebs und erkrankungen im zusammenhang mit map kinase |
| US20040225116A1 (en) | 2003-05-08 | 2004-11-11 | Payne Mark S. | Nucleic acid fragments encoding nitrile hydratase and amidase enzymes from comamonas testosteroni 5-MGAM-4D and recombinant organisms expressing those enzymes useful for the production of amides and acids |
| US20040266755A1 (en) | 2003-05-29 | 2004-12-30 | Schering Aktiengesellschaft | Prodrugs of 1-(1-hydroxy-5-isoquinolinesulfonyl) homopiperazine |
| EP1638939A2 (en) | 2003-06-24 | 2006-03-29 | Neurosearch A/S | Aza-ring derivatives and their use as monoamine neurotransmitter re-uptake inhibitors |
| US7826566B2 (en) | 2003-08-22 | 2010-11-02 | 4Links Limited | Communication system |
| WO2005030791A2 (en) | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Isoquinolinone potassium channel inhibitors |
| JP4794446B2 (ja) | 2003-09-23 | 2011-10-19 | メルク・シャープ・エンド・ドーム・コーポレイション | イソキノリン系カリウムチャンネル阻害薬 |
| US20050067037A1 (en) | 2003-09-30 | 2005-03-31 | Conocophillips Company | Collapse resistant composite riser |
| JPWO2005035516A1 (ja) * | 2003-10-10 | 2006-12-21 | 小野薬品工業株式会社 | 新規縮合複素環化合物およびその用途 |
| EP1689719A1 (en) | 2003-11-25 | 2006-08-16 | Eli Lilly And Company | 7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b) |
| WO2005074535A2 (en) | 2004-01-30 | 2005-08-18 | Eisai Co., Ltd. | Cholinesterase inhibitors for spinal cord disorders |
| US20080312189A1 (en) | 2004-03-05 | 2008-12-18 | Eisai Co., Ltd. | Cadasil Treatment with Cholinesterase Inhibitors |
| SE0400850D0 (sv) | 2004-03-30 | 2004-03-31 | Astrazeneca Ab | Novel Compounds |
| JP4969049B2 (ja) * | 2004-04-06 | 2012-07-04 | 株式会社アマダ | 曲げ加工装置 |
| US7517991B2 (en) * | 2004-10-12 | 2009-04-14 | Bristol-Myers Squibb Company | N-sulfonylpiperidine cannabinoid receptor 1 antagonists |
| EP1741525A1 (de) | 2005-07-06 | 2007-01-10 | Trumpf Werkzeugmaschinen GmbH + Co. KG | Vorrichtung zur Aufnahme von plattenförmigen Materialien |
| UA93882C2 (ru) | 2005-07-26 | 2011-03-25 | Санофи-Авентис | Пиперидинил-замещенные производные изохинолона kak ингибиторы rho-киназы |
| CN101228132B (zh) | 2005-07-26 | 2012-10-10 | 塞诺菲-安万特股份有限公司 | 作为Rho-激酶抑制剂的环己基胺异喹啉酮衍生物 |
| TW200745101A (en) | 2005-09-30 | 2007-12-16 | Organon Nv | 9-Azabicyclo[3.3.1]nonane derivatives |
| JP4033221B2 (ja) | 2005-12-02 | 2008-01-16 | ダイキン工業株式会社 | 冷媒加熱装置 |
| US7618985B2 (en) | 2005-12-08 | 2009-11-17 | N.V. Organon | Isoquinoline derivatives |
| TW200738682A (en) | 2005-12-08 | 2007-10-16 | Organon Nv | Isoquinoline derivatives |
| US7893088B2 (en) | 2006-08-18 | 2011-02-22 | N.V. Organon | 6-substituted isoquinoline derivatives |
| KR101494452B1 (ko) | 2006-12-27 | 2015-02-16 | 사노피 | 사이클로알킬아민 치환된 이소퀴놀린 및 이소퀴놀리논 유도체 |
| WO2008077555A2 (en) | 2006-12-27 | 2008-07-03 | Sanofi-Aventis | Substituted isoquinolines and their use as rho-kinase inhibitors |
-
2006
- 2006-07-20 CN CN2006800271401A patent/CN101228132B/zh not_active Expired - Fee Related
- 2006-07-20 NI NI200800024A patent/NI200800024A/es unknown
- 2006-07-20 CA CA2615663A patent/CA2615663C/en not_active Expired - Fee Related
- 2006-07-20 PT PT06776307T patent/PT1912949E/pt unknown
- 2006-07-20 ES ES06776307T patent/ES2372067T3/es active Active
- 2006-07-20 WO PCT/EP2006/007140 patent/WO2007012422A1/en active Application Filing
- 2006-07-20 NZ NZ565669A patent/NZ565669A/en not_active IP Right Cessation
- 2006-07-20 RU RU2008106926/04A patent/RU2440988C2/ru not_active IP Right Cessation
- 2006-07-20 RS RS20110494A patent/RS52241B/en unknown
- 2006-07-20 MX MX2008000956A patent/MX2008000956A/es active IP Right Grant
- 2006-07-20 KR KR1020087002147A patent/KR101336678B1/ko not_active IP Right Cessation
- 2006-07-20 PL PL06776307T patent/PL1912949T3/pl unknown
- 2006-07-20 DK DK06776307.8T patent/DK1912949T3/da active
- 2006-07-20 SI SI200631175T patent/SI1912949T1/sl unknown
- 2006-07-20 AT AT06776307T patent/ATE521595T1/de active
- 2006-07-20 EP EP06776307A patent/EP1912949B1/en active Active
- 2006-07-20 AU AU2006274246A patent/AU2006274246B2/en not_active Ceased
- 2006-07-20 BR BRPI0614063-7A patent/BRPI0614063A2/pt active Search and Examination
- 2006-07-20 JP JP2008523189A patent/JP5049970B2/ja not_active Expired - Fee Related
- 2006-07-24 GT GT200600327A patent/GT200600327A/es unknown
- 2006-07-24 MY MYPI20063516A patent/MY146644A/en unknown
- 2006-07-24 TW TW095126883A patent/TWI412521B/zh not_active IP Right Cessation
- 2006-07-25 PE PE2006000895A patent/PE20070181A1/es not_active Application Discontinuation
- 2006-07-25 DO DO2006000177A patent/DOP2006000177A/es unknown
- 2006-07-25 AR ARP060103200A patent/AR057082A1/es unknown
-
2007
- 2007-12-18 CR CR9604A patent/CR9604A/es not_active Application Discontinuation
- 2007-12-18 ZA ZA200710952A patent/ZA200710952B/xx unknown
-
2008
- 2008-01-21 MA MA30586A patent/MA29639B1/fr unknown
- 2008-01-22 IL IL188949A patent/IL188949A/en not_active IP Right Cessation
- 2008-01-25 EC EC2008008136A patent/ECSP088136A/es unknown
- 2008-01-25 TN TNP2008000038A patent/TNSN08038A1/en unknown
- 2008-01-25 US US12/019,799 patent/US8609691B2/en not_active Expired - Fee Related
- 2008-01-28 HN HN2008000130A patent/HN2008000130A/es unknown
- 2008-02-22 NO NO20080965A patent/NO20080965L/no not_active Application Discontinuation
- 2008-12-29 HK HK08114022.5A patent/HK1123036A1/xx not_active IP Right Cessation
-
2011
- 2011-06-15 US US13/161,003 patent/US8796458B2/en not_active Expired - Fee Related
- 2011-11-14 HR HR20110839T patent/HRP20110839T1/hr unknown
- 2011-11-24 CY CY20111101153T patent/CY1112085T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20110839T1 (hr) | Derivati cikloheksaminizokinolona kao inhibitori rho-kinaze | |
| HRP20100705T1 (hr) | Cikloalkilaminski supstituirani izokinolinski i izokinolinonski derivati | |
| RU2009128693A (ru) | Замещенные производные изохинолина и изохинолинона | |
| HRP20090589T1 (hr) | Izokinolinski derivati kao inhibitori ro-kinaze | |
| RU2009128645A (ru) | Замещенные изохинолиновые и изохинолиноновые производные в качестве ингибиторов rho-киназы | |
| RU2009128688A (ru) | Замещенные циклоалкиламином производные изохинолина и изохинолинона | |
| RU2009128653A (ru) | Замещенные циклоалкиламином производные изохинолона | |
| RU2008106950A (ru) | Пиперидинилзамещенные производные изохинолона как ингибиторы rho-киназы | |
| JP2009502829A5 (hr) | ||
| JP2009502830A5 (hr) | ||
| ES2285151T3 (es) | Derivados de 1-amido-4-fenil-4-benciloximetil-piperidina y compuestos relacionados como antagonistas de neurocinina-1 (nk-1) para el tratamiento de vomitos, depresion ansiedad y tos. | |
| JP2010514721A5 (hr) | ||
| AR036604A1 (es) | Derivados de 4-pirimidona 3-sustituida | |
| JP2018537533A5 (hr) | ||
| AR087301A1 (es) | Derivados de carboxamida y urea que contienen pirazol heteroaromatico sustituido como ligandos del receptor de vanilloide | |
| NO20074698L (no) | Pyrazinylsubstituerte piperazinpiperidiner med CXCR3-antagonistaktivitet | |
| WO2010115836A4 (en) | Substituted piperidines as ccr3 antagonists | |
| IS7709A (is) | Pýrasóló[3,4-b]pýridín efnasambönd, og notkun þeirra sem fosfórdíesterasa hindrar | |
| CO6821946A2 (es) | Derivados de piridin-2(1h)-ona útiles como medicamentos para el tramiento de trastornos mieloproliferativos, rechazo de trasplantes, enfermedades mediadas por el sistema inmune y enfermedades inflamatorias | |
| WO2012107498A4 (en) | Lysine demethylase inhibitors for myeloproliferative disorders | |
| AR058287A1 (es) | Derivados de isoquinolina y composicion farmaceutica | |
| WO2007084560A8 (en) | INHIBITORS OF TNFα, PDE4 AND B-RAF, COMPOSITIONS THEREOF AND METHODS OF USE THEREWITH | |
| JP2010514718A5 (hr) | ||
| JO2676B1 (en) | Derivatives of second-aza-spiro- (5,4) -dikan and their use as antihistamines | |
| TW200603797A (en) | Substituted 4-alkyl- and 4-alkanoyl-piperidine derivatives and their use as neurokinin antagonists |