ME01284B - Organska jedinjenja - Google Patents
Organska jedinjenjaInfo
- Publication number
- ME01284B ME01284B MEP-2011-21A MEP2111A ME01284B ME 01284 B ME01284 B ME 01284B ME P2111 A MEP2111 A ME P2111A ME 01284 B ME01284 B ME 01284B
- Authority
- ME
- Montenegro
- Prior art keywords
- amide
- thiazol
- methyl
- dicarboxylic acids
- amid
- Prior art date
Links
- 150000002894 organic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 28
- 108091007960 PI3Ks Proteins 0.000 claims abstract 15
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims abstract 15
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims abstract 15
- 201000010099 disease Diseases 0.000 claims abstract 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 11
- 150000003839 salts Chemical class 0.000 claims abstract 11
- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical class OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 claims 22
- 125000001424 substituent group Chemical group 0.000 claims 20
- 239000002253 acid Substances 0.000 claims 16
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 14
- 150000007513 acids Chemical class 0.000 claims 14
- 229910052805 deuterium Inorganic materials 0.000 claims 14
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 10
- -1 cyano, aminocarbonyl Chemical group 0.000 claims 10
- 125000001153 fluoro group Chemical group F* 0.000 claims 10
- 230000001404 mediated effect Effects 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- OAWXZFGKDDFTGS-UHFFFAOYSA-N pyrrolidine-1,2-dicarboxylic acid Chemical class OC(=O)C1CCCN1C(O)=O OAWXZFGKDDFTGS-UHFFFAOYSA-N 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 206010069754 Acquired gene mutation Diseases 0.000 claims 2
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000009621 actinic keratosis Diseases 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 230000009826 neoplastic cell growth Effects 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 2
- 230000037439 somatic mutation Effects 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000012609 Cowden disease Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 101000605639 Homo sapiens Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Proteins 0.000 claims 1
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 1
- 208000034578 Multiple myelomas 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
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 claims 1
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims 1
- 102100038332 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Human genes 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 230000003213 activating effect Effects 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 230000003321 amplification Effects 0.000 claims 1
- 210000000013 bile duct Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000000621 bronchi Anatomy 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- WBLIXGSTEMXDSM-UHFFFAOYSA-N chloromethane Chemical group Cl[CH2] WBLIXGSTEMXDSM-UHFFFAOYSA-N 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002357 endometrial effect Effects 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical group F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000003747 lymphoid leukemia Diseases 0.000 claims 1
- 210000005075 mammary gland Anatomy 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- 208000025440 neoplasm of neck Diseases 0.000 claims 1
- 238000003199 nucleic acid amplification method Methods 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 210000004197 pelvis Anatomy 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 210000003800 pharynx Anatomy 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 201000010700 sporadic breast cancer Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
- 230000005945 translocation Effects 0.000 claims 1
- WCYWZMWISLQXQU-FIBGUPNXSA-N trideuteriomethane Chemical group [2H][C]([2H])[2H] WCYWZMWISLQXQU-FIBGUPNXSA-N 0.000 claims 1
- 230000003827 upregulation Effects 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 230000002485 urinary effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
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Abstract
Dati pronalazak odnosi se na jedinjenje formule (I) ili njegovu so, gde su supstituenti đeifnisani u opisu, na kompozicije i na upotrebu jeđinjenja u lečenju oboljenja koje se može poboljšati inbibiranjem fosfatidilinozitol 3-kinasa.
Claims (17)
1. Jedinjenje formule (I) ili njegova so, naznačen time, što A predstavlja heteroaril koji je odabran iz grupe koju čine: gde R1 predstavlja jedan od sledećih supstituenata: (1) nesupstituisani ili supstituisani, najbolje supstituisani C1-C7-alkil, gde su pomenuti supstituenti svaki za sebe odabrani izmedju jedne ili više, najbolje od jedne do devet sledećih grupa C3-C5-cikloalkil; (2) po slobodnom izboru supstituisani C3-C5-cikloalkil, gde su pomenuti supstituenti svaki za sebe odabrani od jedne ili više, najbolje jedne do četiri od sledećih grupa: deuterijum, C1-C4-alkil (najbolje metil), fluoro, cijano, aminokarbonil; (3) po slobodnom izboru supstituisani fenil, gde su pomenuti supstituenti svaki za sebe odabrani od jedne ili više, najbolje od jedne do dve od sledećih grupa: deuterijum, halo, cijano, C1-C7-alkil, C1-C7-alkllamino, di(C1-C7-alkil)amino, C1-C7-alkilaminokarbonil, di(C1-C7-alkil)aminokarbonil, C1-C7-alkoksi; (4) po slobodnom izboru supstituisani mono- ih di- supstituisani amin; gde su pomenuti supstituenti nezavisno odabrani od sledećih grupa: deuterijum, C1-C7 alkil (koja može da bude nesupstituisana ili supstituisana sa jednim ili više supstituenata odabranih iz grupe koju čine deuterijum, fluoro, hloro, hidroksi), fenilsulfonil (koji može da bude nesupstituisan ili supstituisan sa jednom ili više, najbolje jednom grupom, poput C1-C7-alkil, C1-C7-alkoksi, di(C1-C7-alkil)amino-C1-C7-alkoksi); (5) supstituisani sulfonil; gde je pomenuti supstituent nezavisno odabran od sledećih grupa: C1-C7-alkil (koji može da bude nesupstituisan ili supstituisan sa jedjnim ili više supstituenata, koji su odabrani iz grupe koju čine deuterijum, fluoro), pirolidino, (koji može da bude nesupstituisan ili supstituisan sa jednim ili više supstituenata, koji su odabrani iz grupe koju čine deuterijum, hidroksi, okso; naročito jedna okso), (6) fluoro, chloro; gde R2 predstavlja vodonik; R3 predstavlja (1) vodonik, (2) fluoro, hloro, (3) po slobodnom supstituisani metil, gde su pomenuti supstituenti svaki za sebenezavisno odabrani od jedne ili više, najbolje od jedne do triod sledećih grupa: deuterijum, fluoro, hloro, dimetilamino; sa izuzetkom 2-amiđ l-({5-[2-(terc-butil)-pirimidin-4-il]-4-metil-tiazol-2-il}-amid) (S)-Pirohd±n-l,2-dikarboksilne kiseline.
2. Jedinjenje prema bilo kojem od predhodnih patentnih zahteva, naznačen time, što A predstavlja heteroaril koji je odabran iz grupe koju čine: gde R1 predstavlja: (1) ciklopropilmetil ili po slobodnom izboru supstituisani, razgranati C3-C7-alkil, gde pomenuti supstituenti po slobodnom izboru mogu da budu svaki za sebe odabrani od jedne ili više, najbolje od jedne do devet od sledećih grupa: deuterijum, fluoro; (2) po slobodnom izboru supstituisani ciklopropil ili ciklobutil, gde su pomenuti supstituenti svaki za sebe odabrani iz grupe koja je nezavisno odabrana izmedju jedne ili više, najbolje jedne do četiri od sledećih grupa: metil, deuterijum, fluoro, cijano, aminokarbonil; (3) po slobodnom izboru supstituisani fenil, gde su supstituenti svaki za sebe odabrani od jedne ih više, najbolje jedne do dve od sledećih grupa: deuterijum, halo, cijano, C1-C7-alkil, C1-C7-alkilamino, di(C1-C7-alkil)aniino, C1-C7-alkilaminokarbonil, di(C1-C7-alkil)aminokarbonil, C1-C7-alkoksi; (4) po slobodnom izboru mono- ih di- supstituisani amin; gde su pomenuti supstituenti svaki za sebe odabrani od sledećih grupa: deuterijum, C1-C7-alkil (koji može da bude nesupstituisan ih supstituisan sa jednim ih više supstituenata koji su odabrani iz grupe koju čine deuterijum, fluoro, hloro, hidroksi), fenilsulfonil (koja može da bude nesupstituisana ili supstituisana sa jednom ili sa više, najbolje jednom od grupa kao što su C1-C7-alkil, C1-C7-alkoksi, di(C1-C7-alkil)amino-C1-C7-alkoksi); (6) supsittuisani sulfonil; gde je pomenuti supstituent odabran od sledećih grupa: C1-C7-alkil (koja može da bude nesupstituisana ili supstituisana sa jednim ili više supstituenata koji su odabrani iz grupe koju čine deuterijum, fluoro), pirolidino, (koja može da bude nesupstituisana ili supstituisana sa jednim ili više supstituenata koji su odabrani iz grupe koju čine deuterijum, hidroksi, okso; naročito jedna okso), (6) fluoro, hloro; R3 predstavlja vodonik; R3 predstavlja vodonik, metil, CD3, CH2Cl, CH2F, CH3N(CH3)3; sa izuzetkom 2-amid l-({S-[2-(terc-butil)-pirimidin-4-il]-4-metil-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikarboksilne kiseline.
3. Jedinjenje prema patentnom zahtevu 1 ili 2, naznačen time, što A predstavlja heteroarilkojije odabran iz grupe koju čine:
4. Jedinjenje prema patentnom zahtevu 1 ili 2, naznačen time, što je jedinjenje formule (I) ima formulu (IB) sa izuzetkom 2-amid l-({S-[2-(terc-butil)-pirimidin-4-il]-4-metil-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikarboksilne kiseline.
5. Jedinjenje prema bilo kojem od patentnih zahteva 1 do 3, naznačen time, što jedinjenje formule (I) ima formulu (IA)
6. Jedinjenje, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, naznačen time, stoje odabrano iz grupe koju čine, 2-amid 1 - {[5-(2- fcerc-butil-piridin-4-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin- 1.2- dikarboksilne kiseline; 2-amid 1- {[5-(2-ciklopropil-piridin-4-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin- 1.2- dikarboksilne kiseline; 2-amid l-({5-[2-(2-fluoro-fenil)-piridin-4-il]-4-metil-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{ [5-(2-ciklobutil-piridin-4-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin- 1.2- dikarboksilne kiseline; 2-amid 1 -({4-metil-5-[2-(l-metil-ciklopropil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Piro]idin-l,2-dikarboksilne kiseline; 2-amid l-({4-metil-5-[2-(l-metil-ciklobutil)-piridin-4-il]-tiazol-2-il}-amid) (S> Pirolidin-1,2- dikarboksilne kiseline; 2-amid l-{[5-(2-fcerc-butil-piridin-4-il)-tiazol-2-il]-amid} (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(2-izopropil-piridin-4-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin-l,2 dikarboksilne kiseline; 2-amid 1-{[5-(2-ciklobutil-piridin-4-il)-tiazol-2-il]-amid} (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-({5-[2-(l-metil-ciklopropil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin 1.2- dikarboksilne kiseline; 2-amid l-({5-[2-(l-trifluorometil-ciklopropil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin-1,2-dikarboksilne kiseline; 2-amid l-({5-[2-(2,2,2-trifluoro-l,l-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidln-l,2- dikarboksilne kiseline; 2-amid 1 -({5-[2-(1 -trifluorometil-ciklobutil)-piridin-4-il] -tiazol-2-ii} -amid) (S) -PiroUdin-l,2-dikart>oksilne kiseline; 2-amid l-({4-metil-5-[2-(l-trifluorometil-ciklopropil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikart)oksilne kiseline; (S)-Pirolidin-l,2-dikart)Oksilne kiseline 2-amid l-({4-metil-5-[2-(2,2,2-trifluoro-1,1 -dimetil-etil)-piridin-4-il] -tiazol-2-il} -amid); (S)-Pirolidin-l,2-dikartioksilne kiseline 2-amid l-({4-metil-5-[2-(l-trifluorometil-ciklobutil)-piriđin-4-il] -tiazol-2-il} -amid); 2-amid 1 -({5-[2-(l-metil-ciklobutil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin- 1.2- đikarboksilne kiseline; 2-amid l-({5-[2-(l-cijano-ciklopropil)-piridin-4-il]-4-metil-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikart)oksilne kiseline; 2-amid 1 -({5-[2-(l-cijano-ciklo'butil)-piridin-4-il]-4-metil-tiazol-2-il}-amid) (S)-Pirolidin-1,2-dikartioksilne kiseline 2-amid 1 -({5- [2-( 1 -karbamoil-ciklobutil) -piridin-4-il] -4-metil-tiazol-2-il} -amid) (S)-Pirolidin-l,2-dikart)oksilne kiseline; 2-amid 1 -({5-[2-(2-dimetilamino-1,1 -dimetiI-etiI)-piridin-4-il]-4-metil-tiazol-2- il}-amid) (S)- Pirolidin-l,2-dikart)Oksilne kiseline; 2-amid l-{[5-(2-dietilajnino-piridin-4-il)-4-metil-tiazol-2-il]-amid] (S)-Pirolidin- 1.2- dikarboksilne kiseline; 2-amid l-{[5-(2-dietilamino-piridin-4-il)-tiazol-2-il]-amid} (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(3-fcerc-butil-3H-'benzoimidazol-5-il)-tiazol-2-iI]-amid} (S)-Pirolidin- 1.2- dikarboksilne kiseline; 2-amid l-{[5-(3-fcerc-butil-2-metil-3H-'benzoimidazol-5-il)-tiazol-2-il]-amid} (S)-Pirolidin-l,2-dikart)oksilne kiseline; 2-amid l-{[5-(3-etil-3H-t)enzoimidazol-5-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin-1,2-dikarboksilne kiseline; 2-amid 1 - [(5- {2-[ 1 -(4-metoksi-fenil)-1 -metil-etil]-piridin-4-iI} -4-metil-tiazol-2-il)-amid] (S)-Pirolidin-l,2-dikart)oksilne kiseline; 2-amid 1 - [ (5- {2- [ 1 -(4-metoksi-fenil)-1 -metil-etil] -piridin-4-il} -tiazol-2-il) -amid] (S)-Pirolidin-l,2-dikartioksilne kiseline; 2-amid l-[(5-{2-[l-(4-metoksi-fenil)-ciklopropil]-piridin-4-il}-4-metil-tiazol-2-il> amid] (S)-Pirobdin-l,2-dikarboksilne kiseline; 2-amid 1 -[(5- {2-[ 1 -(4-metoksi-fenil)-ciklopropil]-piridin-4-il} -tiazol-2-il)-amid] (S)-Pirolidin-1,2-dikarboksilne kiseline; 2-amid l-{[5-(2-{l-[4-(3-dimetilamino-propoksi)-fenil]-l-metil-etil}-piridin-4-il> 4-metil-tiazol-2-il]-amid} (S)-PiroUdin-l,2-dikarboksilne kiseline; 2-amid 1 -({4-metil-5-[2-( 1 -d^-metil-ciklobutil)-piridin-4-il]-tiazol-2-il}-amid) (S> Pirolidin-l,2-dikarboksilne kiseline; 2-amid 1 -({5-[2-( 1 -d3-metil-ciklobutil)-piriđin-4-il] -tiazol-2-il} -amid) (S> Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-({4-đ3-metil-5-[2-(l-metil-ciklopropil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin-l ,2-dikarboksilne kiseline; 2-amid 1 -({4-d3-metil-5-[2-(2,2,2-trifluoro-1,1 -dimetil-etil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-({4-dimetilaminometil-5-[2-(l-d3-metil-ciklobutil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-({4-hloro-5-[2-(2,2,2-trifluoro-l,l-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-({4-fluorometil-5-[2-(2,2,2-trifluoro-l,l-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(5-benzenes'ulfonilamino-6-hloro-piridin-3-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(5-benzensulfonilamino-6-hloro-piridin-3-il)-tiazol-2-il]-amid} (S> Pirolidin-l,2-dikarboksilne kiseline; 2-amid 1 - {[5-(6-amino-5-trifluorometil-piridin-3-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid 1 -({4-metil-5-[2-(l -metil-ciklopropil)-pirimidin-4-il]-tiazol-2-il} -amid) (S> Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(2-izopropil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S)- Pirolidin- 1.2- dikarboksilne kiseline; 2-amid l-{[5-(2-benzil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S)- Pirolidin- 1.2- dikarboksilne kiseline; 2-amid l-{ [5-(2-etil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(2-metoksimetil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S)- Pirolidin-l,2-dikart)oksilne kiseline; 2-amid l-({5-[2-(2,6-diMoro-benzil)-pMmidin-4-il]-4-metil-tiazol-2-il}-amid) (S)-Pirolidin-l,2-dikartioksilne kiseline; 2-amid l-{ [5-(2-izobutil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S)-Pirolidin- 1,2-dikarboksilne kiseline; 2-amid l-({5-[2-(4-metoksi-fenoksimetil)-pirimidin-4-iI]-4-metiI-tiazol-2-il}- amid) (S)-Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-({5-[2-(3-metoksi-fenoksimetil)-pirimidin-4-il]-4-metil-tiazol-2-il}- amid) (S)-Pirolidin-l,2-dikart)oksilne kiseline; 2-amid l-({5-[2-(2-fluoro-fenil)-pirimidin-4-il]-4-metil-tiazol-2-il}-amid) (S)- Piroliđin-1,2-dikarboksilne kiseline; 2-amid l-{ [5-(2-trifluorometiI-pirimidin-4-il)-4-metiI-tiazol-2-il]-amid} (S)- PiroUdin-l,2-dikartioksilne kiseline; 2-amid 1 -({4-metil-5- [2-( 1,1,2-trimetil-propil) -pirimiđin-4-iI] -tiazol-2-il} -amid) (S)-Pirolidin-l,2-dikartioksilne kiseline; 2-amid 1 -[(5- {2-[ 1 -(4-metoksi-feniI)-l -metil-etil]-pirimidin-4-il} -4-metil-tiazol-2-il)-amid] (S)-Pirolidin-l,2-dikarboksiIne kiseline; 2-amid 1 -({4-metil-5-[2-( 1,1 -dimetil-propil)-pirimidin-4-iI]-tiazol-2-il} -amid) (S)-Pirolidin-l,2-dikartioksilne kiseline; 2-amid 1 -({4-metil-5- [2-( 1 -metil-1 -p-toUl-etil)-pirimidin-4-il] -tiazol-2-il} -amid) (S)-Pirolidin-l,2-dikartioksiIne kiseline; 2-amid l-({4-metiI-5-[2-(l-fenil-ciklopentil)-pirimidin-4-il]-tiazol-2-il}-amid) (S)- Pirolidin-l,2-dikartioksilne kiseline; 2-amid l-({4-metil-5-[2-ciklopropil-pirimidin-4-iI]-tiazol-2-il}-amid) (S)- Pirolidin-l,2-dikart)oksilne kiseline; 2-amid l-({4-metil-5-[2-ciklobutil-pirimidin-4-il]-tiazol-2-il}-amid) (S)-Pirolidin- 1,2-dikarboksilne kiseline; 2-amid l-{[5-(2-d9-terc-butil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S)- Pirolidin-l,2-dikartioksilne kiseline; 2-amid 1 -({4-metil-5-[2-(2-metil-ciklopropil)-pirimidin-4-iI] -tiazol-2-il} -amid) (S)-PiroUdin-l,2-dikartioksilne kiseline; 2-amid l-{[5-(2-dietilamino-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S)- Pirolidin-l,2-dikartioksilne kiseline; 2-amid l-({4-metil-5-[2-(2,2,2-trifluoro-l,l-dimetil-etil)-pirimidin-4-il]-tiazol-2-il}-amid) (S)-Pirohdin-l,2-dikarboksilne kiseline; 2-amid l-({5-[2-(etil-metil-amino)-pirimidin-4-il]-4-metil-tiazol-2-il}-amid) (S> Pirohdin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(6-ciklopropil-pirazin-2-il)-4-metil-tiazol-2-il]-amid} (S)- Pirolidin- 1.2- dikarboksilne kiseline; 2-amid l-{ [4-metil-5-(5-trifluorometil-piridin-3-il)-tiazol-2-il]-amid} (S> Pirohdin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(6-dio-dietilamino-pirazin-2-il)-4-metil-tiazol-2-il]-amid} (S> Pirohdin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(6-dietilamino-pirazin-2-il)-4-metil-tiazol-2-il]-amid} (S)- Pirolidin- 1.2- dikarboksilne kiseline; 2-amid l-{ [5-(2-ciklopropilmetil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S> Pirolidin-l,2-dikarboksilne kiseline; 2-amid 1 -({5-[2-(2-fluoro-1,1 -dimetil-etil)-pirimidin-4-il]-4-metil-tiazol-2-il} - amid) (S)- Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-{[5-(2-terc-butil-6-metil-pirimidin-4-il)-4-metil-tiazol-2-il]-amid} (S> Pirolidin-l,2-dikarboksilne kiseline; 2-amid 1 -({5-[2-(2-fluoro-1,1 -dimetil-etil)-piridin-4-il]-4-metil-tiazol-2-il} -amid) (S)- Pirolidin-l,2-dikarboksilne kiseline; 2-amid l-({5-[2-(2-fluoro-l-fluorometil-l-metil-etil)-piridin-4-il]-4-metil-tiazol-2-il}-amid (S)-Pirolidin-l,2-dikarboksilne kiseline.
7. Jedinjenje formule (I) prema bilo kojem od patentnih zahteva 1 do 6, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, za upotrebu kao farmaceutskog sredstva.
8. Jedinjenje formule (I) prema bilo kojem od patentnih zahteva 1 do 6, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, za upotrebu u lečenju jednog ih više oboljenja posredovanih fosfatidilinozitol 3-kinazom (PI3K).
9. Upotreba jedinjenja formule (I) prema bilo kojem od patentnih zahteva 1 do 6, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, za proizvodnju leka za lečenje jednog ili više oboljenja posredovanih fosfatidilinozitol 3-kinazom (PI3K).
10. Postupak lečenja oboljenja posredstvom fosfatidilinozitol 3-kinaze (PI3K) naznačen time, što obuhvata davanje terapijski efikasne količine jedinjenja formule (I) prema bilo kojem od patentnih zahteva od 1 do 6, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, ispitanicima za potrebe njihovog lečenja.
11. Farmaceutska kompozicija naznačena time, što obuhvata terapijski efikasnu količinu jedinjenja formule (I) prema bilo kojem od patentnih zahteva 1 do 6, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli.
12. Kombinovana farmaceutska kompozicija, prilagodjena za istovremenu ih uzastopnu primenu, naznačen time, što obuhvata terapijski efikasnu količinu jedinjenja formule (I) prema bilo kojem od patentnih zahteva 1 do 6 u slobodnom ih u obliku farmaceutski prihvatljive soh i terapijski efikasnu količinu jednog ih više kombinacionih partnera; i jedan ih više farmaceutski prihvatljivih ekscepijenata.
13. Farmaceutska kompozicija prema patentnom zahtevu 11 hi kombinovana farmaceutska kompozicija prema patentnom zahtevu 12 za upotrebu u lečenju oboljenja posredovanih Protein tirosine kinazom, naročito oboljenja posredovanih fosfatidilinozitol 3-kinazom (PI3K).
14. Jedinjenje prema patentnom zahtevu 8, upotreba jedinjenja prema patentnom zahtevu 9, hi postupak lečenja prema patentnom zahtevu 10, naznačen time, što je oboljenje posredovano fosfatidilinozitol 3-kinazom (PI3K), oboljenje posredovano PI3K alfa.
15. Jedinjenje prema patentnom zahtevu 8, upotreba jedinjenja prema patentnom zahtevu 9, hi postupak lečenja prema patentnom zahtevu 10, naznačen time, što je pomenuto oboljenje posredovano fosfatidilinozitol 3-kinazom (PI3K) zavisno odprekomernog ispoljavanja ih amplifikacije PI3K alfa, somatske mutacije PIK3CA hi germinativne mutacije ili somatske mutacije PTEN ili mutacije i translokacije p85a koje dovode do ushodne regulacije p85-pl 10 kompleksa.
16. Jedinjenje prema bilo kojem od patentnih zahteva 1 do 6ili njegove farmaceutski prihvatljive soli, za upotrebu u lečenju proliferativnih oboljenja; benignih ili malignih tumora; kancera odabranih od sarkoma, pluća i bronhije; kancera prostate; grudi (uključujući sporadične karcinome dojke i tegobe od Cowden-ove bolesti); pankreasa; kancer gastrointestinalnog trakta; debelog creva i rektuma; kolorektalni kancer, tiroidne kancere; jetre i žučnog kanala unutar jetre; hepatocelularne; nadbubrežna žlezda; kancere stomaka, kancere želuca; gliome/glioblastome; endometrijalne; melanoma; bubrežne i mokraćne karlice; mokraćne bešike; tela materice; grhća materice; jajnika; multipli mijeloma; ezofagusa; leukemije, akutne mijelogene leukemije; hronične mijelogene leukemije, limfocitne leukemije; mijeloidne leukemije; mozga; oralne duplje i farinksa; larinksa; tankog creva; ne-Hočkinove limfome; melanoma; i dlakavog adenoma kolona, neoplazije; neoplazije epitelijalnog karaktera; limfomi; karcinom mlečne žlezde; bazocelularni karcinom; skvamocelularni karcinom; aktinska keratoza (solarna keratoza); tumori, uključujući soldine tumore; tumor glave ili vrata; pohcitemija vera; esencijalna trombocitopenija; mijelofibroza sa mijeloidnom metaplazijom; i Valdenštromovu (Waldenstroem) bolest.
17. Postupak za proizvodnju jedinjenja formule (I) prema bilo kojem od patentnih zahteva od 1 to 6, naznačen time, što obuhvata reakciju jedinjenja formule II i gde su supstituenti definisani za bilo koji od patentnih zahteva 1 do 6, u prisustvu aktivacionog sredstva (“ postupak A”) ili jedinjenja formule (IIIB) u kojoj su supstituenti definisani prema jednom od patentnih zahteva od 1 do 6 ; gde RG predstavlja reaktivnu grupu, (kao stoje imidazolilkarbonil), (“ postupak B”); u svakom slučaju opciono u prisusustvu diluenta i po slobodnom izboru u prisustvu pomoćnog sredstva za reakciju; i po slobodnom izboru rekuperovanjem rezultujućeg jedinjenja formule (I) dobijenog prema postpuku A ili postupku B, različito jedinjenje formule (I), i/ ili prevodjenje dobijene soli jedinjenja formule (I) u njenuu različitu so, i/ ili rekuperovanje dobijenog slobodnog jedinjenja formule (I) u njegovu so, i/ ili odvajanje izomera jedinjenja formule (I) od jednog ili više različitih izomera koji se mogu dobiti iz jedinjenja formule (I)
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| US9667408P | 2008-09-12 | 2008-09-12 | |
| PCT/EP2009/061644 WO2010029082A1 (en) | 2008-09-10 | 2009-09-08 | Organic compounds |
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