HRP20210607T1 - Izokinolin-3-il karboksamidi i njihova priprema i upotreba - Google Patents
Izokinolin-3-il karboksamidi i njihova priprema i upotreba Download PDFInfo
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- HRP20210607T1 HRP20210607T1 HRP20210607TT HRP20210607T HRP20210607T1 HR P20210607 T1 HRP20210607 T1 HR P20210607T1 HR P20210607T T HRP20210607T T HR P20210607TT HR P20210607 T HRP20210607 T HR P20210607T HR P20210607 T1 HRP20210607 T1 HR P20210607T1
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- KKSZSACCVDIWIE-UHFFFAOYSA-N isoquinoline-3-carboxamide Chemical class C1=CC=C2C=NC(C(=O)N)=CC2=C1 KKSZSACCVDIWIE-UHFFFAOYSA-N 0.000 title 1
- 125000002947 alkylene group Chemical group 0.000 claims 29
- 150000004820 halides Chemical class 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 17
- 125000003342 alkenyl group Chemical group 0.000 claims 15
- 125000000304 alkynyl group Chemical group 0.000 claims 15
- 125000001188 haloalkyl group Chemical group 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 208000035475 disorder Diseases 0.000 claims 7
- 206010016654 Fibrosis Diseases 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 230000004761 fibrosis Effects 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 230000003176 fibrotic effect Effects 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000002158 Proliferative Vitreoretinopathy Diseases 0.000 claims 2
- 206010038934 Retinopathy proliferative Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 208000021971 neovascular inflammatory vitreoretinopathy Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 230000006785 proliferative vitreoretinopathy Effects 0.000 claims 2
- 230000037390 scarring Effects 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000006468 Adrenal Cortex Neoplasms Diseases 0.000 claims 1
- 206010061424 Anal cancer Diseases 0.000 claims 1
- 208000007860 Anus Neoplasms Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000010392 Bone Fractures Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010007279 Carcinoid tumour of the gastrointestinal tract Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 206010061246 Intervertebral disc degeneration Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010023421 Kidney fibrosis Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010027452 Metastases to bone Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010048654 Muscle fibrosis Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 1
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims 1
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 208000001164 Osteoporotic Fractures Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims 1
- 206010061934 Salivary gland cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010050207 Skin fibrosis Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 201000009365 Thymic carcinoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010067269 Uterine fibrosis Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 201000002454 adrenal cortex cancer Diseases 0.000 claims 1
- 201000011165 anus cancer Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000015100 cartilage disease Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000018180 degenerative disc disease Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000024519 eye neoplasm Diseases 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 1
- 210000004392 genitalia Anatomy 0.000 claims 1
- 208000003884 gestational trophoblastic disease Diseases 0.000 claims 1
- 206010061989 glomerulosclerosis Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 230000001969 hypertrophic effect Effects 0.000 claims 1
- 210000003026 hypopharynx Anatomy 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 208000021600 intervertebral disc degenerative disease Diseases 0.000 claims 1
- 208000023589 ischemic disease Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 208000025854 malignant tumor of adrenal cortex Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008106 ocular cancer Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000003899 penis Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 206010062261 spinal cord neoplasm Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 208000037965 uterine sarcoma Diseases 0.000 claims 1
Classifications
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- 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
- C07D401/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (17)
1. Spoj, ili njegova farmaceutski prihvatljiva sol, s Formulom I:
[image]
naznačen time što:
R1, R2, R4, i R5 su neovisno odabrani iz skupine koja sadrži H, halogenid, amino, nesupstituiran -(C1-3 haloalkil), i nesupstituiran -(C1-3 alkil);
R3 je 5-eročalni heteroaril po izboru supstituiran s 1-4 R45;
R6 je odabran iz skupine koja sadrži -fenil supstituiran s 1-5 R36, -(C1-3 alkilen)ppiridinil po izboru supstituiran s 1-6 R37, i 6-10 člani heteroaril po izboru supstituiran s 1-6 R37; pri čemu je karbonil s Formulom I vezan na aromatski prsten heteroarila; pri čemu je -(C1-3 alkilen) po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, -C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R' neovisno odabrana od H i -(C1-6 alkil);
svaki R36 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-9 alkil), nesupstituiran -(C2-9 alkenil), nesupstituiran -(C2-9 alkinil), nesupstituiran -(C1-9 haloalkil), -XR42,-C(=O)N(R47)2, -(C1-4 alkilen)pN(R50)2, -(C1-4 alkilen)pheterociklil po izboru supstituiran s 1-10 R43, i -(C1-4 alkilen)pkarbociklil po izboru supstituiran s 1-12 R44; pri čemu je svaki -(C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, - C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R' neovisno odabrana od H i -(C1-6 alkil);
svaki R37 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-9 alkil), nesupstituiran -(C2-9 alkenil), nesupstituiran -(C2-9 alkinil), nesupstituiran -(C1-9 haloalkil), -XR42, - C(=O)N(R47)2, -(C1-4 alkilen)pN(R50)2, -(C1-4 alkilen)pheterociklil po izboru supstituiran s 1-10 R43, i —(C1-4 alkilen)pkarbociklil po izboru supstituiran s 1-12 R44; pri čemu je svaki -(C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, - C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R’ neovisno odabrana od H i -(C1-6 alkil);
svaki R38 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5 alkenil), nesupstituiran -(C2-5 alkinil), nesupstituiran -(C1-5 haloalkil), -CN, i - (C1-4 alkilen)pkarbociklil po izboru supstituiran s 1-12 R44; pri čemu je svaki -(C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, - C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R' neovisno odabrana od H i -(C1-6 alkil);
svaki R39 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5 alkenil), nesupstituiran -(C2-5 alkinil), nesupstituiran -(C1-5 haloalkil), -CN, i - (C1-4 alkilen)pkarbociklil po izboru supstituiran s 1-12 R44; pri čemu je svaki -(C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, - C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem svaka pojava R i R' je neovisno odabrana od H i -(C1-6 alkil);
svaki R40 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5 alkenil), nesupstituiran -(C2-5 alkinil), nesupstituiran -(C1-5 haloalkil), -CN, i - (C1-4 alkilen)pkarbociklil po izboru supstituiran s 1-12 R44; pri čemu je svaki -(C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, - C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R’ neovisno odabrana od H i -(C1-6 alkil);
svaki R41 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5 alkenil), nesupstituiran -(C2-5 alkinil), nesupstituiran -(C1-5 haloalkil), i -CN;
svaki R42 je neovisno odabran iz skupine koja sadrži H, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5 alkenil), nesupstituiran -(C2-5 alkinil), nesupstituiran -(C1-5 haloalkil), -(C1-4 alkilen)N(R48)2, -(C1-4 alkilen)paril po izboru supstituiran s 1-10 R46, -(C1-4 alkilen)pheterociklil po izboru supstituiran s 1-12 R43, i -(C1-4 alkilen)pkarbociklil po izboru supstituiran s 1-12 R44; pri čemu je svaki -(C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, -C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R’ neovisno odabrana od H i -(C1-6 alkil);
svaki R43 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5 alkenil), nesupstituiran -(C2-5 alkinil), nesupstituiran -(C1-5 haloalkil), -CN, -OH, - C(=O)R51, -N(R50)2, i -(C1-4 alkilen)pkarbociklil po izboru supstituiran s 1-12 R44; pri čemu je svaki - (C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, -C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R’ neovisno odabrana od H i -(C1-6 alkil);
svaki R44 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5 alkenil), nesupstituiran -(C2-5 alkinil), nesupstituiran -(C1-5 haloalkil), i -CN;
svaki R45 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-9 alkil), nesupstituiran -(C2-9 alkenil), nesupstituiran -(C2-9 alkinil), nesupstituiran -(C1-9 haloalkil), -(C1-4 alkilen)pN(R48)2, -(C1-4 alkilen)pOR49, -C(=O)N(R48)2, -(C1-4 alkilen)pheterociklil po izboru supstituiran s 1-10 R38, i -karbociklil po izboru supstituiran s 1-12 R39; pri čemu je svaki -(C1-4 alkilen), neovisno, po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, -C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R’ neovisno odabrana od H i -(C1-6 alkil);
alternativno, dva susjedna R45 uzeta zajedno tvore prsten koji je odabran iz skupine koja sadrži -heterociklil po izboru supstituiran s 1-10 R40 i -karbociklil po izboru supstituiran s 1-12 R41;
svaki R46 je neovisno odabran iz skupine koja sadrži halogenid, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5alkenil), nesupstituiran -(C2-5alkinil), nesupstituiran -(C1-5haloalkil), i -CN;
svaki R47 je neovisno odabran iz skupine koja sadrži H, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5alkenil), nesupstituiran -(C2-5alkinil), i nesupstituiran -(C1-5haloalkil);
svaki R48 je neovisno odabran iz skupine koja sadrži H, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5alkenil), nesupstituiran -(C2-5alkinil), i nesupstituiran -(C1-5haloalkil);
svaki R49 je neovisno odabran iz skupine koja sadrži H, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5alkenil), nesupstituiran -(C2-5alkinil), i nesupstituiran -(C1-5 haloalkil);
svaki R50 je neovisno odabran iz skupine koja sadrži H, nesupstituiran -(C1-5 alkil), nesupstituiran -(C2-5alkenil), nesupstituiran -(C2-5alkinil), nesupstituiran -(C1-5 haloalkil), i -(C1-4 alkilen)N(R48)2; pri čemu je -(C1-4 alkilen) po izboru supstituiran s -(C1-6 alkil), -(C1-6 haloalkil), halogenidom, hidroksilom, -C(O)OR, -C(O)R, -(C1-6 alkoksil), -NRR', -C(O)NRR', i cijano, u kojem je svaka pojava R i R’ neovisno odabrana od H i -(C1-6 alkil);
svaki R51 je heteroaril po izboru supstituiran s 1-6 R52;
svaki R52 je -heterociklil po izboru supstituiran s 1-10 R46;
svaki X je odabran iz skupine koja sadrži O, S, i NR48; i
svaki p je neovisno 0 ili 1.
2. Spoj prema patentnom zahtjevu 1, naznačen time što R1, R2, R4, i R5 su H.
3. Spoj prema bilo kojem od patentnih zahtjeva 1-2, naznačen time što R3 je pirazolil supstituiran s jednim -(C1-3 alkilom).
4. Spoj prema bilo kojem od patentnih zahtjeva 1-2, naznačen time što R3 je imidazolil supstituiran s jednim -(C1-3 alkilom).
5. Spoj prema bilo kojem od patentnih zahtjeva 1-2, naznačen time što R3 je triazolil supstituiran s jednim -(C1-3 alkilom).
6. Spoj prema bilo kojem od patentnih zahtjeva 1-5, naznačen time što R6 je -fenil supstituiran s jednim R36.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-6, naznačen time što R36 je odabran iz skupine koja sadrži halogenid, -heterociklil po izboru supstituiran s 1-2 R43, -CH2heterociklil po izboru supstituiran s 1-2 R43, -Oheterociklil po izboru supstituiran s 1-2 R43, -NHheterociklil po izboru supstituiran s 1-2 R43, -O(C1-4 alkil), i -O(C1-4 haloalkil).
8. Spoj prema bilo kojem od patentnih zahtjeva 1-5, naznačen time što R6 je -piridinil po izboru supstituiran s 1-6 R37.
9. Spoj prema bilo kojem od patentnih zahtjeva 1-5 i 8, naznačen time što R6 je -piridin-4-il po izboru supstituiran s jednim R37.
10. Spoj prema bilo kojem od patentnih zahtjeva 1-5 i 8-9, naznačen time što je R37 odabran iz skupine koja sadrži halogenid, -(C1-3 alkil), -heterociklil po izboru supstituiran s 1-2 R43, - CH2heterociklil po izboru supstituiran s 1-2 R43, -Oheterociklil po izboru supstituiran s 1-2 R43, - NHheterociklil po izboru supstituiran s 1-2 R43, -O(C1-4 alkil), i -O(C1-4 haloalkil).
11. Spoj prema bilo kojem od patentnih zahtjeva 1-10, naznačen time što je R43 odabran iz skupine koja sadrži nesupstituiran -(C1-3 alkil), nesupstituiran -(C1-3 haloalkil), i -karbociklil po izboru supstituiran s 1-12 R44.
12. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj s formulom I odabran iz skupine koja sadrži:
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i
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ili njihova farmaceutski prihvatljiva sol.
13. Farmaceutski pripravak naznačen time što sadrži terapeutski učinkovitu količinu spoja prema bilo kojem od zahtjeva 1-12, ili njegovu farmaceutski prihvatljivu sol, te farmaceutski prihvatljivo pomoćno sredstvo.
14. Spoj prema bilo kojem od patentnih zahtjeva 1-12, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema zahtjevu 13, naznačen time što se koristi u liječenju poremećaja ili bolesti kod pacijenta, pri čemu je poremećaj ili bolest odabran od: raka, plućne fibroze, idiopatske plućne fibroze (IPF), degenerativne bolesti diska, prijeloma kosti/osteoporotskih prijeloma, bolesti kostiju ili hrskavice, osteoartritisa, plućne bolesti, i fibroznog poremećaja, pri čemu je pacijent čovjek.
15. Spoj za uporabu prema patentnom zahtjevu 14, naznačen time što je bolest ili poremećaj rak, pri čemu je rak odabran iz skupine koja sadrži: hepatocelularni karcinom, rak debelog crijeva, rak dojke, rak gušterače, kroničnu mijeloičnu leukemiju (CML), kroničnu mijelomonocitna leukemiju, kroničnu limfocitnu leukemiju (CLL), akutnu mijeloičnu leukemiju, akutnu limfocitnu leukemiju, Hodgkinov limfom, limfom, sarkom, rak jajnika, rak pluća ne malih stanica, rak pluća malih stanica, multipli mijelom, rak nazofarinksa, neuroblastom, osteosarkom, rak penisa, tumori hipofize, rak prostate, retinoblastom, rabdomiosarkom, rak žlijezda slinovnica, rak kože - bazalnih i pločastih stanica, rak kože - melanom, rak tankog crijeva, rak želuca, rak testisa, karcinom timusa, rak štitnjače, sarkom maternice, rak rodnice, rak vulve, rak grkljana ili hipofarinksa, rak bubrega, Kaposijev sarkom, gestacijska trofoblastična bolest, gastrointestinalni stromalni tumor, gastrointestinalni karcinoidni tumor, rak žučnog mjehura, rak oka (melanom i limfom), Ewingov tumor, rak jednjaka, rak endometrija, kolorektalni karcinom, rak vrata maternice, tumor mozga ili leđne moždine, metastaze kostiju, rak kostiju, rak mokraćnog mjehura, rak žučnog kanala, analni rak, i rak korteksa nadbubrežne žlijezde.
16. Spoj za uporabu prema bilo kojem od patentnih zahtjeva 14-15, naznačen time što je rak, rak gušterače.
17. Spoj za uporabu prema patentnom zahtjevu 14, naznačen time što je poremećaj ili bolest fibrotični poremećaj, pri čemu je fibrotični poremećaj odabran iz skupine koja sadrži: kožnu fibrozu; sklerodermiju; progresivnu sistemsku fibrozu; plućnu fibrozu; mišićnu fibrozu; fibrozu bubrega; glomerulosklerozu; glomerulonefritis; hipertrofično stvaranje ožiljaka; fibrozu maternice; bubrežnu fibrozu; cirozu jetre, fibrozu jetre; adhezije; kroničnu opstruktivnu plućnu bolest; fibrozu nakon infarkta miokarda; plućnu fibrozu; fibrozu i ožiljke povezane s difuznom/intersticijskom bolesti pluća; fibrozu središnjeg živčanog sustava; fibrozu povezanu s proliferativnom vitreoretinopatijom (PVR); restenozu; endometriozu; ishemijsku bolest, i fibrozu zbog zračenja.
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