HRP20161010T1 - C5ar antagonisti - Google Patents
C5ar antagonisti Download PDFInfo
- Publication number
- HRP20161010T1 HRP20161010T1 HRP20161010TT HRP20161010T HRP20161010T1 HR P20161010 T1 HRP20161010 T1 HR P20161010T1 HR P20161010T T HRP20161010T T HR P20161010TT HR P20161010 T HRP20161010 T HR P20161010T HR P20161010 T1 HRP20161010 T1 HR P20161010T1
- Authority
- HR
- Croatia
- Prior art keywords
- group
- alkyl
- heteroaryl
- independently selected
- aryl
- Prior art date
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- 239000005557 antagonist Substances 0.000 title 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 46
- 229910052757 nitrogen Inorganic materials 0.000 claims 45
- 150000001875 compounds Chemical class 0.000 claims 40
- 125000003118 aryl group Chemical group 0.000 claims 33
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 30
- 125000005842 heteroatom Chemical group 0.000 claims 29
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 28
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 28
- 229910052736 halogen Inorganic materials 0.000 claims 27
- 229910052760 oxygen Inorganic materials 0.000 claims 27
- 229910052717 sulfur Inorganic materials 0.000 claims 27
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 26
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 20
- 229910003827 NRaRb Inorganic materials 0.000 claims 17
- 125000005843 halogen group Chemical group 0.000 claims 17
- -1 hydroxy, methyl Chemical group 0.000 claims 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 16
- 125000001931 aliphatic group Chemical group 0.000 claims 15
- 125000003282 alkyl amino group Chemical group 0.000 claims 15
- 125000004122 cyclic group Chemical group 0.000 claims 15
- 125000004663 dialkyl amino group Chemical group 0.000 claims 15
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 208000027866 inflammatory disease Diseases 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 6
- 125000003386 piperidinyl group Chemical group 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 125000002837 carbocyclic group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000002757 morpholinyl group Chemical group 0.000 claims 5
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 5
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 5
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims 4
- 206010061218 Inflammation Diseases 0.000 claims 4
- 208000026106 cerebrovascular disease Diseases 0.000 claims 4
- 230000002526 effect on cardiovascular system Effects 0.000 claims 4
- 230000004054 inflammatory process Effects 0.000 claims 4
- 230000001575 pathological effect Effects 0.000 claims 4
- 102000005590 Anaphylatoxin C5a Receptor Human genes 0.000 claims 3
- 108010059426 Anaphylatoxin C5a Receptor Proteins 0.000 claims 3
- 206010018364 Glomerulonephritis Diseases 0.000 claims 3
- 208000005777 Lupus Nephritis Diseases 0.000 claims 3
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 3
- 239000008280 blood Substances 0.000 claims 3
- 238000006243 chemical reaction Methods 0.000 claims 3
- 208000010247 contact dermatitis Diseases 0.000 claims 3
- 208000017169 kidney disease Diseases 0.000 claims 3
- 206010025135 lupus erythematosus Diseases 0.000 claims 3
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 201000008383 nephritis Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 206010047115 Vasculitis Diseases 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 208000035408 type 1 diabetes mellitus 1 Diseases 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
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000010718 Multiple Organ Failure Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 206010038563 Reocclusion Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 1
- 206010052568 Urticaria chronic Diseases 0.000 claims 1
- 206010053648 Vascular occlusion Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 230000035605 chemotaxis Effects 0.000 claims 1
- 208000024376 chronic urticaria Diseases 0.000 claims 1
- 230000024203 complement activation Effects 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002949 hemolytic effect Effects 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 208000012947 ischemia reperfusion injury Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 210000000265 leukocyte Anatomy 0.000 claims 1
- 231100000516 lung damage Toxicity 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000000897 modulatory effect Effects 0.000 claims 1
- 208000029744 multiple organ dysfunction syndrome Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000004235 neutropenia Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 230000003582 thrombocytopenic effect Effects 0.000 claims 1
- 230000008736 traumatic injury Effects 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 208000021331 vascular occlusion disease Diseases 0.000 claims 1
Classifications
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
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Claims (27)
1. Spoj formule
[image]
ili njegova farmaceutski prihvatljiva sol, hidrat ili rotomer; naznačen time, da
C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R1;
C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenata R2;
C3 je odabran iz skupine koja se sastoji od C1-8 alkila, C3-8 cikloalkila, C3-8 cikloalkil-C1-4 alkila, arila, aril-C1-4 alkila, heteroarila, heteroaril-C1-4 alkila, heterocikloalkila ili heterocikloalkil-C1-4 alkila, pri čemu heterocikloalkilna skupina ili dio skupine sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, a svaki C3 prema potrebi je supstituiran s 1 do 3 supstituenta R3; svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, -CO2Ra, -CONRaRb, -C(O)Ra, OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa, -S(O)2NRaRb; pri čemu je svaki Ra i Rb neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika, mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane među N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, a pri čemu su alifatski i ciklički dijelovi Ra, Rb i Rc prema potrebi dodatno supstituirani sa jednim do tri halogena, hidroksi, metil, amino, alkilamino i dialkilamino skupinama; i po želji, kada se dva R1 supstituenta na susjednim atomima kombiniraju tako da tvore kondenzirani peteročlani ili šesteročlani karbociklični prsten; svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, -CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, - NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki od Rd i Re neovisno odabran iz skupine koju čine vodik, C1-8 alkil i C1-8 haloalkil,
ili kada je spojen na isti atom dušika, može se kombinirati s dušikovim atomom tako da tvori peteročlani ili šesteročlani prsten sa 0 do 2 dodatna heteroatoma kao članova prstena, odabranih iz niza N, O ili S; svaki Rf neovisno je odabran iz skupine koju čine C1-8 alkil, C1-8 haloalkil, C3-6 cikloalkil, heterocikloalkil, aril i heteroaril, pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s jednim do tri halogena, hidroksi, metil, amino, alkilamino i dialkilamino skupinom; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, -CO2Rg, -CONRgRh, - C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, -NRgC(O)NRgRh, -NRgRh, - ORg, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh , -X4-CONRgRh, -X4-NRhC(O)Rg, -NHRj i - NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koju čine vodik, C1-8 alkil, C3-6 cikloalkil i C1-8 haloalkil, ili kada su spojeni na isti atom dušika, mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena, koji su odabrani među N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki R1 neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; a svaki Rj odabran je iz skupine koju čine C3-6cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i Rj prema potrebi dodatno supstituirani s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino; i
X je vodik ili CH3.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da:X je vodik.
3. Spoj u skladu s patentnim zahtjevom 1 naznačen time, da spoj ima formulu:
[image]
ili spoj ima formulu:
[image]
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da spoj ima formulu:
[image]
ili
[image]
pri čemu
X1 je odabran iz skupine koja sadržava N, CH i CR1; indeks n je cijeli broj od 0 do 2; X2 je odabran iz skupine koja sadržava N, CH i CR2; a indeks m je cijeli broj od 0 do 2,
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da spoj ima formulu:
[image]
pri čemu je indeks p cijeli broj od 0 do 3.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da spoj ima formulu:
[image]
pri čemu je R3 odabran iz skupine koju čine -NRgRh, -NHRj -NHCH2Rj, -X4-NRgRh, -X4- Rj i -X4-NRhCORg.
7. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C1 odabran iz skupine koju čine fenil, piridil, indolil i tiazolil, od kojih je svaki prema potrebi supstituiran s od 1 do 3 supstituenta R1; i pri čemu je svaki R1 neovisno odabran iz skupine koja se sastoji od halogena, -CN, - Rc, -NRaRb i -ORa, i pri čemu je svaki Ra i Rb neovisno odabran iz skupine koju čine vodik, C1-8 alkil i C1-8 haloalkil, ili kada su vezani na isti atom dušika, mogu se kombinirati s dušikovim atomom i tvoriti pirolidinski prsten; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila i C3-6 cikloalkila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i Rc prema potrebi dodatno supstituirani s jednom do tri hidroksi, metil amino, alkilamino i dialkilamino skupine; i po želji, kada su dva supstituenta R1 na susjednim atomima, kombiniraju se tako da tvore peteročlani ili šesteročlani kaRbociklički prsten.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C2 odabran iz skupine koja sadržava fenil, naftil, piridil i indolil, od kojih je svaki prema potrebi supstituiran sa 1 do 3 R2 supstituenta; i
pri čemu je svaki R2 neovisno odabran iz skupine koja se sastoji od halogena, Rf i - ORd; pri čemu je svaki Rd neovisno odabran od vodika, C1-8 alkila i C1-8 haloalkila; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd i Rf prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino.
9. Spoj u skladu s patentnim zahtjevom 7, naznačen time, da je C1 odabran iz skupine koju čine
[image]
10. Spoj u skladu s patentnim zahtjevom 8, naznačen time, da je C2 odabran iz skupine koju čine:
[image]
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C3 odabran iz skupine koju čine C3-6 alkil, C3-6 cikloalkil, C3-6 cikloalkilC1-2alkil, fenil, piridinil, pirazolil, piperidinil, pirolidinil, piperidinilmetil i pirolidinilmetil, od kojih je svaki prema potrebi supstituiran sa 1 do 3 supstituenta R3, pri čemu je svaki R3 neovisno odabran iz skupine koja se sastoji od halogena, -Ri -CO2Rg, -CONRgRh, -NRhC(O)Rg, - NRhC(O)2Ri, -NRgRh , -ORg, -X4-Rj -X4-NRgRh, -X4-CONRgRh, -X4-NRhC(O)Rg,, -NHRj i - NHCH2Rj, pri čemu je X4 C1-3 alkilen; svaki od Rg i Rh neovisno je odabran iz skupine koju čine vodik, C1-8 alkil, C3-6 cikloalkil i C1-8 haloalkil, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji sadržava od 0 do 1 dodatnog heteroatoma kao članove prstena odabrane iz skupine koju čine N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj odabran je iz skupine koju čine C3-6cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil, i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i RJ prema potrebi dodatno supstituirani s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C3 odabran iz skupine koju čine:
[image]
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je C3 odabran iz skupine koju čine:
[image]
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je spoj odabran iz skupine koju čine:
[image]
[image]
[image]
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[image]
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i
15. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je navedeni spoj
[image]
ili njegova farmaceutski prihvatljiva sol.
16. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je navedeni spoj
[image]
ili njegova farmaceutski prihvatljiva sol.
17. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je navedeni spoj
[image]
ili njegova farmaceutski prihvatljiva sol.
18. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 17, naznačen time, da se rabi u terapijskom liječenju ljudskog ili životinjskog tijela.
19. Farmaceutski pripravak, naznačen time, da sadržava farmaceutski prihvatljivi nosač i spoj formule
[image]
ili njegova farmaceutski prihvatljiva sol, hidrat ili rotomer; pri čemu
C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R1;
C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R2;
C3 je odabran iz skupine koja se sastoji od C1-8 alkila, C3-8 cikloalkila, C3-8 cikloalkil-C1-4 alkila, arila, aril-C1-4 alkila, heteroarila, heteroaril-C1-4 alkila, heterocikloalkila ili heterocikloalkil-C1-4 alkila, pri čemu je heterocikloalkil skupina ili njezin dio sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, a svaki C3 prema potrebi je supstituiran s 1 do 3 supstituenta R3; svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, -CO2Ra, -CONRaRb, -C(O)Ra, -OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa i -S(O)2NRaRb; pri čemu je svaki Ra i Rb neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao člana prstena iz niza N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i RC prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; i po želji, kada su dva supstituenta R1 na susjednim atomima, kombiniraju se tako da tvore peteročlani ili šesteročlani karbociklični prsten;
svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, -CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, - NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki Rd i Re neovisno odabran iz skupine koja se sastoji od vodika, C1-8 alkila, i C1-8
haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima 0 do 2 dodatna heteroatoma kao članove prstena odabrane od N, O ili S; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, -CO2R9, -CONRgRh, -C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, - NRgC(O)NRgRh, -NRgRh, -ORg, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh, -X4-CONRg Rh, - X4-NRhC(O)Rg, -NHRj i -NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koja se sastoji od vodika, C1-8 alkila, C3-6 cikloalkila i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane između N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj je odabran iz skupine koju čine C3-6 cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil, i pri čemu su alifatski i ciklički dijelovi RG, Rh, R1 i RJ prema potrebi dodatno supstituirani s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino; i
X je vodik ili CH3.
20. Spoj za uporabu u postupku liječenja sisavca koji pati od ili je sklon bolestima ili poRemećajima koji uključuju patološku aktivaciju C5a receptora, naznačen time, da je bolest ili poRemećaj upalna bolest ili poRemećaj; kardiovaskularni ili cerebrovaskularni poRemećaj; autoimuni poRemećaj; ili
patološka posljedica povezane sa skupinom koju čine dijabetes ovisan o inzulinu, mellitus, lupus nefropatija, Heymann nefritis, membranski nefritis, glomerulonefritis, Reakcija na osjetljivost na kontakt i upala koje su posljedica kontakta krvi s umjetnim površinama;
navedeni postupak uključuje primjenu djelotvorne količine spoja na sisavcu, pri čemu
navedeni spoj ima formulu:
[image]
ili je njegova farmaceutski prihvatljiva sol, hidrat ili rotomer; pri čemu
C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 supstituenta R1;
C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S; i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa 1 do 3 R2 supstituenta;
C3 je odabran iz skupine koja se sastoji od C1-8 alkil, C3-8 cikloalkil, C3-8 cikloalkil-C1-4 alkil, aril, aril-C1-4 alkil, heteroaril, heteroaril-C1-4 alkil, heterocikloalkil ili heterocikloalkil-C1-4 alkil, pri čemu heterocikloalkil skupina ili njezin dio sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, i svaki C3 prema potrebi je supstituiran s 1 do 3 R3 supstituenta;
svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, -CO2Ra, -CONRaRb, -C(O)Ra, -OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa, -S(O)2NRaRb; pri čemu je svaki Ra i Rb neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma, kao članove prstena iz niza N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i RC prema potrebi dodatno supstituirani sa jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; i po želji, kada se dva supstituenta R1 na susjednim atomima kombiniraju tako da tvore petero ili šesteročlani karbociklični prsten;
svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, -CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, - NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki Rd i Re neovisno odabran od vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena, odabranih od N, O ili S; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, -CO2R9, -CONRgRh, - C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, -NRgC(O)NRgRh, -NRgRh, - ORg, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh, -X4-CONR9 Rh, -X4-NRhC(O)Rg, -NHRj i - NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koja se sastoji od vodika, C1-8 alkila, C3-6 cikloalkila i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane između N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj odabran je iz skupine koju čine C3-6cikloalkil, pirolinil, piperidinil, moRfolinil, tetrahidrofuranil i tetrahidropiranil i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i Rj prema potrebi dodatno supstituiran s jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino i dialkilamino ; i X je vodik ili CH3.
21. Spoj za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da je upalna bolest ili poRemećaj odabran iz skupine koju čine neutropenija, sepsa, septički šok, Alzheimerova bolest, multipla skleroza, moždani udar, upalne bolesti crijeva, kronična opstruktivna plućna bolest, upala povezana s opeklinama, oštećenja pluća, osteoartritis, atopični dermatitis, kronična urtikarija, ishemijsko-RepeRfuzijske ozljede, sindrom akutnog Respiratornog distResa, sindrom sistemskog upalnog odgovora, sindrom višestruke disfunkcije oRgana, odbacivanje transplantata tkiva i hiperakutno odbacivanja transplantiranih oRgana;
kaRdiovaskularni ili ceRebrovaskularni poRemećaj bira se iz skupine koju čine infarkt miokaRda, koronarna tromboza, vaskularna okluzija, postoperativna vaskularna Reokluzija, ateroskleroza, traumatska ozljeda sRedišnjeg živčanog sustava i ishemijske srčane bolesti; i
autoimuni poRemećaj odabran je iz skupine koju čine Reumatoidni artritis, sistemski eritematozni lupus, Guillain-BarRe sindrom, pankReatitis, lupus nefritis, lupus glomerulonefritis, psorijaza, Crohnova bolest, vaskulitis, sindrom iritabilnog crijeva, dermatomiozitis, multipla skleroza, bronhijalna astma, pemfigus, pemfigoid, skleroderma, mijastenija gravis, autoimuna hemolitička i trombocitopenična stanja, GoodpastuReov sindrom, immunovasculitis, odbacivanje tkivnih transplantata i hiperakutno odbacivanja transplantiranih oRgana.
22. Spoj za uporabu u skladu s patentnim zahtjevom 20 ili 21, naznačen time, da je bolest ili poRemećaj upalna bolest ili poRemećaj.
23. Spoj za uporabu u skladu s patentnim zahtjevom 20 ili 21, naznačen time, da je bolest ili poRemećaj kaRdiovaskularni ili ceRebrovaskularni poRemećaj.
24. Spoj za uporabu u skladu s patentnim zahtjevom 20 ili 21, naznačen time, da je bolest ili poRemećaj autoimuni poRemećaj.
25. Spoj za uporabu u skladu s patentnim zahtjevom 20, naznačen time, da je bolest ili poRemećaj patološka posljedica povezana sa skupinom koju čine dijabetes uvjetovan inzulinom, šećerna bolest, lupus nefropatija, Heymann nefritis, membranski nefritis, glomerulonefritis, Reakcija osjetljivosti na kontakt te upala uslijed kontakta krvi s umjetnim površinama.
26. Spoj za uporabu u metodi inhibiranja stanične kemotaksije posRedovane Receptorom C5a u liječenju stanja koje je autoimuni poRemećaj, upalni poRemećaj,
patološka posljedica povezana s diabetes mellitusom ovisnomo inzulinu (uključujući dijabetičku Retinopatiju), lupus nefropatija, Heymann nefritis, membranski nefritis ili drugi oblik glomerulonefritisa, Reakcije osjetljivosti na kontakt, odnosno upala uslijed kontakta krvi s umjetnim površinama koje mogu izazvati aktivaciju komplementa; bolesti povezane s ishemijskim / RepeRfuzijskim ozljedama; makularna degeneracija; kaRdiovaskularne ili ceRebrovaskularne bolesti; bolest vaskulitisa; infekcija HIV-om ili AIDS; neurodegenerativni poRemećaj;
naznačen time, da podrazumijeva dovođenje u kontakt bijelih krvnih stanica sisavaca s količinom spoja koja ima modulacijski učinak na Receptor C5a, a spoj ima formulu
[image]
ili je njegova farmaceutski prihvatljiva sol, hidrat ili rotomer istih; pri čemu
C1 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna
skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N,
0 i S i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa
1 do 3 supstituenta R1;
C2 je odabran iz skupine koja se sastoji od arila i heteroarila, pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N,
0 i S i pri čemu su navedene aril i heteroaril skupine prema potrebi supstituirane sa
1 do 3 supstituenta R2;
C3 je odabran iz skupine koja se sastoji od C1-8 alkila, C3-8 cikloalkila, C3-8 cikloalkil- C1-4 alkila, arila, aril-C1-4 alkila, heteroarila, heteroaril-C1-4 alkila, heterocikloalkila ili heterocikloalkil C1-4 alkila, pri čemu heterocikloalkil skupina ili dio sadržava od 1 do 3 heteroatoma odabrana iz skupine koja se sastoji od N, O i S, te pri čemu heteroarilna skupina ima 1 do 3 heteroatoma u prstenu odabrana iz skupine koja se sastoji od N, O i S, i svaki C3 prema potrebi je supstituiran s 1 do 3 supstituenta R3; svaki R1 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rc, - CO2Ra, -CONRaRb, -C(O)Ra, -OC(O)NRaRb, -NRbC(O)Ra, -NRbC(O)2Rc, -NRa- C(O)NRaRb, -NRaC(O)NRaRb, -NRaRb, -ORa, -S(O)2NRaRb; pri čemu je svaki Ra i Rb
neovisno odabran između vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s atomom dušika kako bi tvorili petero ili šestero člani prsten koji ima od 0 do 2 dodatna heteroatoma kao članova prstena odabrana iz skupine koja se sastoji od N, O ili S; svaki Rc neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Ra, Rb i Rc prema potrebi dodatno supstituirani sa jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; i po želji, kada se dva supstituenta R1 na susjednim atomima kombiniraju tako da tvore kondenzirani peteročlani ili šesteročlani karbociklični prsten;
svaki R2 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Rf, - CO2Rd, -CONRdRe, -C(O)Rd, -OC(O)NRdRe, -NReC(O)Rd, -NReC(O)2Rf, -NRdC(O)NRdRe, -NRdC(O)NRdRe, -NRdRe, -ORd, i -S(O)2NRdRe; pri čemu je svaki od Rd i Re neovisno odabran od vodika, C1-8 alkila, i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena, odabranih od N, O ili S; svaki Rf neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila, i pri čemu su alifatski i ciklički dijelovi Rd, Re i Rf prema potrebi dodatno supstituirani s od jednom do tri skupine halogen, hidroksi, metil, amino, alkilamino i dialkilamino; svaki R3 neovisno je odabran iz skupine koja se sastoji od halogena, -CN, -Ri, - CO2R9, -CONRgRh, -C(O)Rg, -OC(O)NRgRh, -NRhC(O)Rg, -NRhC(O)2Ri, -NRgC(O)NRgRh, -NRgRh, -OR9, -S(O)2NRgRh, -X4-Rj, -X4-NRgRh, -X4-CONR9 Rh, -X4-NRhC(O)Rg, -NHRj i -NHCH2Rj, pri čemu je X4 C1-4 alkilen; svaki Rg i Rh neovisno je odabran iz skupine koja se sastoji od vodika, C1-8 alkila, C3-6 cikloalkila i C1-8 haloalkila, ili kada su spojeni na isti atom dušika mogu se kombinirati s dušikovim atomom tako da tvore peteročlani ili šesteročlani prsten koji ima od 0 do 2 dodatna heteroatoma kao članove prstena odabrane između N, O ili S, i prema potrebi je supstituiran s jednim ili dva okso; svaki Ri neovisno je odabran iz skupine koja se sastoji od C1-8 alkila, C1-8 haloalkila, C3-6 cikloalkila, heterocikloalkila, arila i heteroarila; i svaki Rj je odabran iz skupine koju čine C3-6 cikloalkil, pirolinil, piperidinil, morfolinil, tetrahidrofuranil i tetrahidropiranil, i pri čemu su alifatski i ciklički dijelovi Rg, Rh, Ri i RJ prema potrebi dodatno supstituirani sa jednom do tri skupine halogen, metil, CF3, hidroksi, amino, alkilamino, i dialkilamino; i X je vodik ili CH3.
27. Spoj za uporabu u skladu s patentnim zahtjevom 26 za liječenje bolesti, naznačen time, da je bolest odabrana iz skupine koju čine sepsa kronične opstruktivne plućne bolesti (KOPB), Reumatski artritis, lupus nefritis i multipla skleroza.
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