HRP20160350T1 - Heterociklički spojevi i njihove uporabe - Google Patents
Heterociklički spojevi i njihove uporabe Download PDFInfo
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- HRP20160350T1 HRP20160350T1 HRP20160350TT HRP20160350T HRP20160350T1 HR P20160350 T1 HRP20160350 T1 HR P20160350T1 HR P20160350T T HRP20160350T T HR P20160350TT HR P20160350 T HRP20160350 T HR P20160350T HR P20160350 T1 HRP20160350 T1 HR P20160350T1
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- Croatia
- Prior art keywords
- nrara
- 4alkyl
- ora
- 6alkyl
- 4haloalkyl
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- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 15
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 14
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- 230000002757 inflammatory effect Effects 0.000 claims 5
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000000464 thioxo group Chemical group S=* 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010027654 Allergic conditions Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000025324 B-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000030289 Lymphoproliferative disease Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002552 acute disseminated encephalomyelitis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000005243 lung squamous cell carcinoma Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
Classifications
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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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P27/00—Drugs for disorders of the senses
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A61P37/08—Antiallergic agents
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- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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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
- C07D471/04—Ortho-condensed systems
-
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/28—Oxygen atom
- C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
-
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Transplantation (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (13)
1. Spoj koje ima strukturu:
[image]
ili bilo koja njegova farmaceutski prihvatljiva sol, u kojem:
X1 je C(R9);
X2 je N;
Y je N(R11), O ili S;
Z je CR8 ili N;
n je 0, 1, 2 ili 3;
R1 je direktno vezan ili preko kisika vezan zasićen, djelomično zasićen ili nezasićen 5-, 6- ili 7-člani monociklični prsten koji sadrži 0, 1, 2, 3 ili 4 atoma izabrana od N, O i S, ali koji sadrži ne više od jednog O ili S, gdje su dostupni atomi ugljika u prstenu supstituirani sa 0, 1 ili 2 okso ili tiokso grupe, gdje je prsten supstituiran sa 0 ili 1 R2 supstituenta, i prsten je dodatno supstituiran sa 0, 1, 2 ili 3 supstituenta nezavisno izabrana od halo, nitro, cijano, C1-4alkil, OC1-4alkil, OC1-4haloalkil, NHC1-4alkil, N(C1-4alkil)C1-4alkil i C1-4haloalkil;
R2 je izabran od halo, C1-4haloalkil, cijano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, -OC2-6alkilNRaRa, -OC2-6alkilORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaC2-6alkilNRaRa i -NRaC2-6alkilORa; ili
R2 je izabran od C1-6alkil, fenil, benzil, heteroaril, heterociklus, -(C1-3alkil)heteroaril, -(C1-3alkil)heterociklus, -O(C1-3alkil)heteroaril, -O(C1-3alkil)heterociklus, -NRa(C1-3alkil)heteroaril, -NRa(C1-3alkil)heterociklus, -(C1-3alkil)fenil, -O(C1-3alkil)fenil i -NRa(C1-3alkil)fenil, od kojih su svi supstituirani sa 0, 1, 2 ili 3 supstituenta izabrana od C1-4haloalkil, OC1-4alkil, Br, Cl, F, I i C1-4alkil;
R3 je izabran od H, halo, C1-4haloalkil, cijano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, -OC2-6alkilNRaRa, -OC2-6alkilORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaC2-6alkilNRaRa, -NRaC2-6alkilORa, C1-6alkil, fenil, benzil, heteroaril i heterociklus, gdje su C1-6alkil, fenil, benzil, heteroaril i heterociklus dodatno supstituirani sa 0, 1, 2 ili 3 supstituenta izabrana od C1-6haloalkil, OC1-6alkil, Br, Cl, F, I i C1-6alkil;
R4 je, nezavisno, u svakom slučaju, halo, nitro, cijano, C1-4alkil, OC1-4alkil, OC1-4haloalkil, NHC1-4alkil, N(C1-4alkil)C1-4alkil ili C1-4haloalkil;
R5 je, nezavisno, u svakom slučaju, H, halo, C1-6alkil, C1-4haloalkil ili C1-6alkil supstituiran sa 1, 2 ili 3 supstituenta izabrana od halo, cijano, OH, OC1-4alkil, C1-4alkil, C1-3haloalkil, OC1-4alkil, NH2, NHC1-4alkil, N(C1-4alkil)C1-4alkil; ili obe R5 grupe zajedno formiraju C3-6spiroalkil supstituiran sa 0, 1, 2 ili 3 supstituenta izabrana od halo, cijano, OH, OC1-4alkil, C1-4alkil, C1-3haloalkil, OC1-4alkil, NH2, NHC1-4alkil, N(C1-4alkil)C1-4alkil;
R6 je izabran od H, halo, C1-6alkil, C1-4haloalkil, cijano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa;
R7 je izabran od H, halo, C1-6alkil, C1-4haloalkil, cijano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa;
R8 je izabran od H, C1-6haloalkil, Br, Cl, F, I, ORa, NRaRa, C1-6alkil, fenil, benzil, heteroaril i heterociklus, gdje su C1-6alkil, fenil, benzil, heteroaril i heterociklus dodatno supstituirani sa 0, 1, 2 ili 3 supstituenta izabrana od C1-6haloalkil, OC1-6alkil, Br, Cl, F, I i C1-6alkil;
R9 je izabran od H, halo, C1-4haloalkil, cijano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, -OC2-6alkilNRaRa, -OC2-6alkilORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaC2-6alkilNRaRa, -NRaC2-6alkilORa, C1-6alkil, fenil, benzil, heteroaril i heterociklus, gdje su C1-6alkil, fenil, benzil, heteroaril i heterociklus dodatno supstituirani sa 0, 1, 2 ili 3 supstituenta izabrana od halo, C1-4haloalkil, cijano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa,
-OC(=O)N(Ra)S(=O)2Ra, -OC2-6alkilNRaRa, -OC2-6alkilORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaC2-6alkilNRaRa, -NRaC2-6alkilORa; ili R9 je zasićeni, djelomično zasićeni ili nezasićeni 5-, 6- ili 7-člani monociklični prsten koji sadrži O, 1, 2, 3 ili 4 atoma izabrana od N, O i S, ali koji ne sadrži više od jednog O ili S, gdje su dostupni atomi ugljika u prstenu supstituirani sa 0, 1 ili 2 okso ili tiokso grupe, gdje je prsten supstituiran sa 0, 1, 2, 3 ili 4 supstituenta izabrana od halo, C1-4haloalkil, cijano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, -OC2-6alkilNRaRa, -OC2-6alkilORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaC2-6alkilNRaRa i -NRaC2-6alkilORa;
R11 je H ili C1-4alkil;
Ra je nezavisno, u svakom slučaju, H ili Rb; i
Rb je nezavisno, u svakom slučaju, fenil, benzil ili C1-6alkil, pri čemu su fenil, benzil i C1-6alkil supstituirani sa 0, 1, 2 ili 3 supstituenta izabrana od halo, C1-4alkil, C1-3haloalkil, -OC1-4alkil, -NH2, -NHC1-4alkil, -N(C1-4alkil)C1-4alkil.
2. Spoj prema patentnom zahtjevu 1, koji ima strukturu:
[image]
3. Spoj prema patentnom zahtjevu 1, koji ima strukturu:
[image]
4. Spoj prema patentnom zahtjevu 1, koji ima strukturu:
[image]
5. Spoj prema patentnom zahtjevu 1, naznačen time što R3 je F, Cl ili Br; i n je O.
6. Spoj prema patentnom zahtjevu 1, naznačen time što R1 je fenil supstituiran sa 0 ili 1 R2 supstituenta, i fenil je dodatno supstituiran sa 0, 1, 2 ili 3 supstituenta nezavisno izabrana od halo, nitro, cijano, C1-4alkil, OC1-4alkil, OC1-4haloalkil, NHC1-4alkil, N(C1-4alkil)C1-4alkil i C1-4haloalkil.
7. Spoj prema patentnom zahtjevu 1, naznačen time što R1 je direktno vezani ili kisikom vezani zasićeni, djelomično zasićeni ili nezasićeni 5-, 6- ili 7-člani monociklični prsten koji sadrži 1, 2, 3 ili 4 atoma izabrana od N, O i S, ali koji ne sadrži više od jednog O ili S, pri čemu su dostupni atomi ugljika u prstenu supstituirani sa 0, 1 ili 2 okso ili tiokso grupe, gdje je prsten supstituiran sa 0 ili 1 R2 supstituentom, i prsten je dodatno supstituiran sa 0, 1, 2 ili 3 supstituenta nezavisno izabrana od halo, nitro, cijano, C1-4alkil, OC1-4alkil, OC1-4haloalkil, NHC1-4alkil, N(C1-4alkil)C1-4alkil i C1-4haloalkil.
8. Spoj prema patentnom zahtjevu 1, koji ima strukturu:
[image]
[image]
ili
[image]
ili bilo koja farmaceutski prihvatljiva sol bilo kojeg od a) do c).
9. Spoj prema patentnom zahtjevu 8 kao slobodna baza.
10. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 9 i farmaceutski prihvatljiv razblaživač ili nosač.
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9 za uporabu u liječenju reumatoidnog artritisa, ankiloznog spondilitisa, osteoartritisa, psorijatičkog artritisa, psorijaze, inflamatornih bolesti i autoimunih bolesti, inflamatornih poremećaja crijeva, inflamatornih poremećaja oka, inflamatornih ili nestabilnih poremećaja bešike, problema sa kožom sa inflamatornim komponentama, kroničnih inflamatornih stanja, autoimunih bolesti, sustavnog lupus eritematodusa (SLE), mijastenije gravis, reumatoidnog artritisa, akutnog diseminiranog encefalomijelitisa, idiopatske trombocitopenije purpure, multiple skleroze, Sjoegren-ovog sindroma i autoimune hemolitičke anemije, alergijskih stanja i hipersenzitivnosti.
12. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9 za uporabu u liječenju kancera, koji su posredovani, ovisni od ili povezani sa aktivnošću p110δ.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 9, za uporabu u liječenju kancera debelog crijeva, glioblastoma, karcinoma endometrija, hepatostaničnog kancera, kancera pluća, melanoma, karcinoma renalnih stanica, karcinoma tireoidee, staničnog limfoma, limfoproliferativnih poremećaja, sitnoćelijskog kancera pluća, karcinoma skvamoznih stanica pluća, glioma, kancera dojke, kancera prostate, kancera jajnika, kancera grlića materice, leukemije, akutne mijeloidne leukemije, mijelodisplastičnog sindroma, mijeloproliferativnih bolesti, kronične mijeloidne leukemije, T-stanične akutne limfoblastične leukemije, B-stanične akutne limfoblastične leukemije, ne-Hodgkin-ovog limfoma, B-staničnog limfoma, solidnih tumora.
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