SI2861579T1 - Benzamidni derivati za inhibiranje aktivnosti ABL1, ABL2 in BCR-ABL1 - Google Patents
Benzamidni derivati za inhibiranje aktivnosti ABL1, ABL2 in BCR-ABL1 Download PDFInfo
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- SI2861579T1 SI2861579T1 SI201330997T SI201330997T SI2861579T1 SI 2861579 T1 SI2861579 T1 SI 2861579T1 SI 201330997 T SI201330997 T SI 201330997T SI 201330997 T SI201330997 T SI 201330997T SI 2861579 T1 SI2861579 T1 SI 2861579T1
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- 230000002401 inhibitory effect Effects 0.000 title claims abstract 3
- 150000003936 benzamides Chemical class 0.000 title claims 2
- 230000000694 effects Effects 0.000 title abstract 2
- 101100268645 Caenorhabditis elegans abl-1 gene Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 23
- 206010028980 Neoplasm Diseases 0.000 claims abstract 3
- -1 hydroxy, methyl Chemical group 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 9
- 125000003226 pyrazolyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 229920003083 Kollidon® VA64 Polymers 0.000 claims 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 3
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- VOVZXURTCKPRDQ-CQSZACIVSA-N n-[4-[chloro(difluoro)methoxy]phenyl]-6-[(3r)-3-hydroxypyrrolidin-1-yl]-5-(1h-pyrazol-5-yl)pyridine-3-carboxamide Chemical compound C1[C@H](O)CCN1C1=NC=C(C(=O)NC=2C=CC(OC(F)(F)Cl)=CC=2)C=C1C1=CC=NN1 VOVZXURTCKPRDQ-CQSZACIVSA-N 0.000 claims 3
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 3
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 3
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000003784 fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229960001346 nilotinib Drugs 0.000 claims 2
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 239000003840 Bafetinib Substances 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 1
- 101000823316 Homo sapiens Tyrosine-protein kinase ABL1 Proteins 0.000 claims 1
- 101000823271 Homo sapiens Tyrosine-protein kinase ABL2 Proteins 0.000 claims 1
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 1
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 1
- 239000002145 L01XE14 - Bosutinib Substances 0.000 claims 1
- 239000002137 L01XE24 - Ponatinib Substances 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 102100022596 Tyrosine-protein kinase ABL1 Human genes 0.000 claims 1
- 102100022651 Tyrosine-protein kinase ABL2 Human genes 0.000 claims 1
- 229950002365 bafetinib Drugs 0.000 claims 1
- ZGBAJMQHJDFTQJ-DEOSSOPVSA-N bafetinib Chemical compound C1[C@@H](N(C)C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=NC=3)C(C)=CC=2)C=C1C(F)(F)F ZGBAJMQHJDFTQJ-DEOSSOPVSA-N 0.000 claims 1
- 229960003736 bosutinib Drugs 0.000 claims 1
- UBPYILGKFZZVDX-UHFFFAOYSA-N bosutinib Chemical compound C1=C(Cl)C(OC)=CC(NC=2C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=CC=2C#N)=C1Cl UBPYILGKFZZVDX-UHFFFAOYSA-N 0.000 claims 1
- 229960002448 dasatinib Drugs 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960002411 imatinib Drugs 0.000 claims 1
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229960001131 ponatinib Drugs 0.000 claims 1
- PHXJVRSECIGDHY-UHFFFAOYSA-N ponatinib Chemical compound C1CN(C)CCN1CC(C(=C1)C(F)(F)F)=CC=C1NC(=O)C1=CC=C(C)C(C#CC=2N3N=CC=CC3=NC=2)=C1 PHXJVRSECIGDHY-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
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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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- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
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- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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Claims (18)
- EP 2861579 BI Benzamidni derivati za inhibiranje aktivnosti ABL1, ABL2 in BCR-ABL1 Patentni zahtevki1. Spojina s formulo (I): v kateri:Ri je pirazolil; kjer je pirazolil nesubstituiran ali substituiran z 1-2 skupinama R^ R2 je pirolidinil; kjer je pirolidinil substituiran z eno skupino R7; R3 je izbran izmed vodika in halo; Rt je izbran izmed -SF5 in -Y2-CF2-Y3; R<5 je vsakokrat, kadar se pojavi, neodvisno izbran izmed vodika, hidroksi, metila, metoksi, ciano, trifluorometila, hidroksi-metila, halo, amino, fluoro-etila, etila in ciklopropila; R7 je izbran izmed hidroksi, metila, halo, metoksi, hidroksi-metila, amino, metil-amino, amino-metila, trifluorometila, 2-hidroksipropan-2-ila, metil-karbonil-amino, dimetil-amino, 2-amino-3-metilbutanoil)oksi, karboksi, metoksi-karbonila, fosfonooksi, ciano in amino-karbonila; Y je izbran izmed CH in N; Yi je izbran izmed CH in N; Y2 je izbran izmed CF2, O in S(O)0.2; in Y3 je izbran izmed vodika, kloro, fluoro, metila, difluorometila in trifluorometila; ali farmacevtsko sprejemljive soli le-te.
- 2. Spojina po zahtevku 1 s formulo (Ib): v kateri:R3 je izbran izmed vodika in halo; R4 je izbran izmed -SF5 in -Y2-CF2-Y3; Rg je, kadar je vezan na dušik pirazolilnega obroča, izbran izmed vodika, metila, fluoro-etila, etila in ciklopropila; in R$ je, kadar je vezan na atom ogljika pirazolilnega obroča, izbran izmed vodika, hidroksi, metila, metoksi, dano, trifluorometila, hidroksi-metila, halo, amino, fluoro-etila, etila in ciklopropila; R7 je izbran izmed hidroksi, metila, halo, metoksi, hidroksi-metila, amino, metil-amino, amino-metila, trifluorometila, 2-hidroksipropan-2-ila, metil-karbonil-amino, dimetil-amino, 2-amino-3-metilbutanoil)oksi, karboksi metoksi-karbonila, fosfonooksi, ciano in aminokarbonila; Yi je izbran izmed CH in N; Y2 je izbran izmed CF2,0 in S(0)o-2; Y3 je izbran izmed vodika, fluoro, kloro, metila, difluorometila in trifluorometila; ali farmacevtsko sprejemljive soli le-te.
- 3. Spojina po zahtevku 2 s formulo (Ic):v kateri: R3 je izbran izmed vodika in halo; R4 je izbran izmed -SF5 in -Y2-CF2-Y3; R$ je, kadar je vezan na dušik pirazolilnega obroča, izbran izmed vodika, metila, fluoro-etila, etila in ciklopropila; in je, kadar je vezan na atom ogljika pirazolilnega obroča, izbran izmed vodika, hidroksi, metila, metoksi, ciano, trifluorometila, hidroksi-metila, halo, amino, fluoro-etila, etila in ciklopropila; R7 je izbran izmed hidroksi, metila, halo, metoksi, hidroksi-metila, amino, metil-amino, amino-metila, trifluorometila, 2-hidroksipropan-2-ila, metil-karbonil-amino, dimetil-amino, 2-amino-3-metilbutanoil)oksi, karboksi, metoksi-karbonila, fosfonooksi, ciano in amino-karbonila; Yi je izbran izmed CH in N; Y2 je izbran izmed CF2, O in S(O)0.2; Y3 je izbran izmed vodika, fluoro, kloro, metila, difluorometila in trifluorometila; ali farmacevtsko sprejemljive soli le-te.
- 4. Spojina po zahtevku 3 ali farmacevtsko sprejemljiva sol le-te, izbrana izmed:
- 5. Spojina po zahtevku 3 ali farmacevtsko sprejemljiva sol le-te, izbrana izmed:
- 6. Spojina po zahtevku 3 ali farmacevtsko sprejemljiva sol le-te, izbrana izmed:
- 7. Spojina po zahtevku 1 ali farmacevtsko sprejemljiva sol le-te, kije:
- 8. Spojina, izbrana izmed:
- 9. Spojina po zahtevku 1, ki je (R)-N-(4-(klorodifluorometoksi)fenil)-6-(3-hidroksipirolidin-l-il)-5-(lH-pirazol-5-il)nikotinamid ali farmacevtsko sprejemljiva sol le-tega.
- 10. Farmacevtski sestavek, ki obsega amorfno disperzijo (R)-N-(4-(klorodifluorometoksi)fenil)-6-(3-hidroksipirolidin-l-il)-5-(lH-pirazol-5-il)nikotinamida in 1-2 ekscipienta, izbrana izmed PVP VA64 in Pharmacoat 603.
- 11. Sestavek po zahtevku 10, kjer je delež Pharmacoat 603 v območju 30-45 %, delež PVP VA64 je v območju 30-45 % in delež (R)-N-(4-(klorodifluorometoksi)fenil)-6-(3-hidroksipirolidin-l-il)-5-(lH-pirazol-5-il)nikotinamida je v območju 20-30 %.
- 12. Sestavek po zahtevku 11, kjer je delež Pharmacoat 603 37,5 %, delež PVP VA64 je 37,5 % in delež (R)-N-(4-(klorodifluorometoksi)fenil)-6-(3-hidroksipirolidin-l-il)- 5-(lH-pirazol-5-il)nikotinamida je 25 %.
- 13. Spojina s formulo (I) ali farmacevtsko sprejemljiva sol le-te po katerem koli od zahtevkov 1-9 za uporabo pri zdravljenju raka.
- 14. Spojina s formulo (I) ali farmacevtsko sprejemljiva sol le-te za uporabo po zahtevku 13, kjer je rak levkemija, izbrana izmed kronične mieloične levkemije in akutne limfoblastne levkemije.
- 15. Spojina s formulo (I) ali farmacevtsko sprejemljiva sol le-te za uporabo po zahtevku 13 ali 14 skupaj z dodatno spojino, izbrano izmed imatiniba, nilotiniba, dasatiniba, bosutiniba, ponatiniba in bafetiniba.
- 16. Spojina s formulo (I) ali farmacevtsko sprejemljiva sol le-te za uporabo po zahtevku 15 pri zaporednem ali sočasnem dajanju z dodatno spojino, kjer je dodatna spojina nilotinib.
- 17. Spojina s formulo (I) ali farmacevtsko sprejemljiva sol le-te za uporabo po katerem koli od zahtevkov 13-16, kjer je spojina (R)-N-(4-(klorodifluorometoksi)fenil)-6-(3-hidroksipirolidin-l-il)-5-(lH-pirazol-5-il)nikotinamid ali farmacevtsko sprejemljiva sol le-tega.
- 18. Farmacevtski sestavek, ki obsega spojino ali farmacevtsko sprejemljivo sol le-te po katerem koli od zahtevkov 1-9 skupaj z enim ali več farmacevtsko sprejemljivimi nosilci.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261647174P | 2012-05-15 | 2012-05-15 | |
US201361790967P | 2013-03-15 | 2013-03-15 | |
PCT/IB2013/053768 WO2013171639A1 (en) | 2012-05-15 | 2013-05-09 | Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1 |
EP13730652.8A EP2861579B9 (en) | 2012-05-15 | 2013-05-09 | Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1 |
Publications (1)
Publication Number | Publication Date |
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SI2861579T1 true SI2861579T1 (sl) | 2018-05-31 |
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Families Citing this family (63)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20200127273A (ko) | 2012-04-26 | 2020-11-10 | 브리스톨-마이어스 스큅 컴퍼니 | 혈소판 응집을 치료하기 위한 프로테아제 활성화 수용체 4 (par4) 억제제로서의 이미다조티아디아졸 및 이미다조피라진 유도체 |
MX2014013373A (es) * | 2012-05-15 | 2015-08-14 | Novartis Ag | Derivados de benzamida para inhibir la actividad de abl1, abl2 y bcr-abl1. |
CA2868958C (en) * | 2012-05-15 | 2020-09-01 | Novartis Ag | Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1 |
JP6080947B2 (ja) | 2012-05-15 | 2017-02-15 | ノバルティス アーゲー | Abl1、abl2およびbcr−abl1の活性を阻害するための化合物および組成物 |
WO2013171642A1 (en) * | 2012-05-15 | 2013-11-21 | Novartis Ag | Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1 |
TWI568722B (zh) | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲mPGES-1抑制劑之三唑酮化合物 |
WO2014110574A1 (en) | 2013-01-14 | 2014-07-17 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
PE20160532A1 (es) | 2013-08-23 | 2016-05-21 | Incyte Corp | Compuesto de carboxamida de furo y tienopiridina utiles como inhibidores de cinasas pim |
US9682931B2 (en) * | 2013-11-01 | 2017-06-20 | Ube Industries, Ltd. | Aryloyl(oxy or amino)pentafluorosulfanylbenzene compound, pharmaceutically acceptable salt thereof, and prodrugs thereof |
JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
EP3105238A4 (en) | 2014-02-13 | 2017-11-08 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and their uses |
CU24481B1 (es) | 2014-03-14 | 2020-03-04 | Immutep Sas | Moléculas de anticuerpo que se unen a lag-3 |
WO2016003812A1 (en) | 2014-07-02 | 2016-01-07 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and uses therof |
US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
CR20170143A (es) | 2014-10-14 | 2017-06-19 | Dana Farber Cancer Inst Inc | Moléculas de anticuerpo que se unen a pd-l1 y usos de las mismas |
CN104478911A (zh) * | 2014-12-19 | 2015-04-01 | 成都安斯利生物医药有限公司 | 一种制备3-三氟甲基吡咯硼酸的方法 |
WO2016100882A1 (en) | 2014-12-19 | 2016-06-23 | Novartis Ag | Combination therapies |
EP3789027A1 (en) * | 2015-01-13 | 2021-03-10 | Kyoto University | Bosutinib, sunitinib, tivozanib, imatinib, nilotinib, rebastinib or bafetinib for preventing and/or treating amyotrophic lateral sclerosis |
TN2017000375A1 (en) | 2015-03-10 | 2019-01-16 | Aduro Biotech Inc | Compositions and methods for activating "stimulator of interferon gene" -dependent signalling |
US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
WO2017019896A1 (en) | 2015-07-29 | 2017-02-02 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
PT3317301T (pt) | 2015-07-29 | 2021-07-09 | Novartis Ag | Terapias de associação compreendendo moléculas de anticorpo contra lag-3 |
US20180207273A1 (en) | 2015-07-29 | 2018-07-26 | Novartis Ag | Combination therapies comprising antibody molecules to tim-3 |
TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
TW201718546A (zh) | 2015-10-02 | 2017-06-01 | 英塞特公司 | 適用作pim激酶抑制劑之雜環化合物 |
SG11201803520PA (en) | 2015-11-03 | 2018-05-30 | Janssen Biotech Inc | Antibodies specifically binding pd-1 and their uses |
AU2016369537B2 (en) | 2015-12-17 | 2024-03-14 | Novartis Ag | Antibody molecules to PD-1 and uses thereof |
US9931342B2 (en) | 2016-02-02 | 2018-04-03 | Duke University | Compositions and methods for the treatment of cancer |
EP3448852A4 (en) * | 2016-04-29 | 2019-04-10 | Astar Biotech LLC | NOVEL HETEROCYCLIC COMPOUNDS AS INHIBITORS OF TYROSINE KINASE BCR-ABL |
WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
WO2018060843A1 (en) * | 2016-09-27 | 2018-04-05 | Novartis Ag | Surfactant systems for crystallization of organic compounds |
US20190240176A1 (en) * | 2016-10-26 | 2019-08-08 | The University Of Georgia Research Foundation, Inc. | Methods of treatment for myeloid leukemia |
JP7234128B2 (ja) * | 2017-03-15 | 2023-03-07 | サン・ファーマ・アドバンスド・リサーチ・カンパニー・リミテッド | シクロプロパンカルボン酸(5-{5-[n’-(2-クロロ-6-メチルベンゾイル)ヒドラジノカルボニル]-2-メチル-フェニルエチニル}-ピリジン-2イル)アミドの新規非晶質分散体 |
UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
JPWO2018216705A1 (ja) * | 2017-05-23 | 2020-03-26 | 国立大学法人京都大学 | 神経変性疾患の予防及び/又は治療剤 |
WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | ANTIBODY MOLECULES DIRECTED AGAINST CD73 AND CORRESPONDING USES |
WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
CN111788196A (zh) | 2018-01-09 | 2020-10-16 | 配体药物公司 | 缩醛化合物及其治疗用途 |
CN112312904A (zh) * | 2018-04-16 | 2021-02-02 | C4医药公司 | 螺环化合物 |
AR126019A1 (es) | 2018-05-30 | 2023-09-06 | Novartis Ag | Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación |
KR102618168B1 (ko) * | 2018-07-06 | 2023-12-27 | 일양약품주식회사 | 프리온 질환의 예방 또는 치료를 위한 약제학적 조성물 |
KR102119150B1 (ko) | 2018-10-23 | 2020-06-04 | 한국원자력의학원 | N-1h-벤지미다졸-2-일-3-(1h-피롤-1-일) 벤자미드를 유효성분으로 함유하는 암 예방 또는 치료용 약학적 조성물 |
US11236070B2 (en) | 2019-05-16 | 2022-02-01 | Novartis Ag | Chemical process |
US11407735B2 (en) | 2019-05-16 | 2022-08-09 | Novartis Ag | Crystalline forms of N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide |
GB201913110D0 (en) * | 2019-09-11 | 2019-10-23 | Benevolentai Bio Ltd | New compounds and methods |
EP4031578A1 (en) | 2019-09-18 | 2022-07-27 | Novartis AG | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
CN114728943A (zh) * | 2020-01-19 | 2022-07-08 | 正大天晴药业集团股份有限公司 | 作为bcr-abl抑制剂的化合物 |
EP4353230A3 (en) | 2020-01-28 | 2024-06-19 | Teva Pharmaceuticals International GmbH | Solid state forms of asciminib and process for preparation thereof |
WO2021156360A1 (en) | 2020-02-05 | 2021-08-12 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for discontinuing a treatment with a tyrosine kinase inhibitor (tki) |
CN111321200A (zh) * | 2020-02-28 | 2020-06-23 | 广州安镝声生物医药科技有限公司 | 一种细胞外abl1激酶活性检测试剂盒及其应用 |
CN115124551B (zh) * | 2021-03-24 | 2024-04-30 | 奥锐特药业(天津)有限公司 | 一种高纯度米哚妥林的制备方法 |
WO2022206937A1 (zh) * | 2021-04-01 | 2022-10-06 | 苏州晶云药物科技股份有限公司 | 一种吡唑取代的烟酰胺类化合物的盐酸盐新晶型及其制备方法 |
EP4337205A1 (en) | 2021-05-11 | 2024-03-20 | Novartis AG | Dosing regimens |
KR20240014478A (ko) | 2021-05-28 | 2024-02-01 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | Bcr-abl 억제제로 사용되는 화합물 |
CN114149409B (zh) * | 2021-11-16 | 2024-03-22 | 中国药科大学 | 一种具有蛋白激酶抑制活性的(杂)芳基酰胺类化合物 |
CN116135851A (zh) * | 2021-11-17 | 2023-05-19 | 武汉众诚康健生物医药科技有限公司 | 一种芳香胺化合物及其应用 |
WO2023114759A2 (en) * | 2021-12-13 | 2023-06-22 | The Regents Of The University Of California | Abl inhibitors and uses thereof |
CN115109048B (zh) * | 2022-08-10 | 2023-12-08 | 中国药科大学 | 一种(杂)芳基酰胺类化合物 |
WO2024100212A1 (en) | 2022-11-10 | 2024-05-16 | Synthon B.V. | Crystalline form of asciminib hydrochloride |
Family Cites Families (60)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CH445129A (fr) | 1964-04-29 | 1967-10-15 | Nestle Sa | Procédé pour la préparation de composés d'inclusion à poids moléculaire élevé |
US3459731A (en) | 1966-12-16 | 1969-08-05 | Corn Products Co | Cyclodextrin polyethers and their production |
US3426011A (en) | 1967-02-13 | 1969-02-04 | Corn Products Co | Cyclodextrins with anionic properties |
US3453257A (en) | 1967-02-13 | 1969-07-01 | Corn Products Co | Cyclodextrin with cationic properties |
US3453259A (en) | 1967-03-22 | 1969-07-01 | Corn Products Co | Cyclodextrin polyol ethers and their oxidation products |
US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
DE2845997A1 (de) | 1978-10-23 | 1980-04-30 | Bayer Ag | Pflanzenwachstumsregulierende mittel, verfahren zu ihrer herstellung und ihre verwendung zur regulierung des pflanzenwachstums |
US4737323A (en) | 1986-02-13 | 1988-04-12 | Liposome Technology, Inc. | Liposome extrusion method |
US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
EP0333791A1 (de) | 1987-09-23 | 1989-09-27 | Ciba-Geigy Ag | Heterocyclische verbindungen |
US5010099A (en) | 1989-08-11 | 1991-04-23 | Harbor Branch Oceanographic Institution, Inc. | Discodermolide compounds, compositions containing same and method of preparation and use |
KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
US5395855A (en) | 1990-05-07 | 1995-03-07 | Ciba-Geigy Corporation | Hydrazones |
IL115849A0 (en) | 1994-11-03 | 1996-01-31 | Merz & Co Gmbh & Co | Tangential filtration preparation of liposomal drugs and liposome product thereof |
NZ334821A (en) | 1996-08-30 | 2000-12-22 | Novartis Ag | Method for producing epothilones |
DE69724269T2 (de) | 1996-09-06 | 2004-06-09 | Obducat Ab | Verfahren für das anisotrope ätzen von strukturen in leitende materialien |
DK1367057T3 (da) | 1996-11-18 | 2009-01-19 | Biotechnolog Forschung Gmbh | Epothiloner E og F |
US6441186B1 (en) | 1996-12-13 | 2002-08-27 | The Scripps Research Institute | Epothilone analogs |
GB9721069D0 (en) | 1997-10-03 | 1997-12-03 | Pharmacia & Upjohn Spa | Polymeric derivatives of camptothecin |
US6194181B1 (en) | 1998-02-19 | 2001-02-27 | Novartis Ag | Fermentative preparation process for and crystal forms of cytostatics |
CA2322157C (en) | 1998-02-25 | 2012-05-29 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
BR9912938B1 (pt) | 1998-08-11 | 2011-06-28 | derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos. | |
EP1135470A2 (en) | 1998-11-20 | 2001-09-26 | Kosan Biosciences, Inc. | Recombinant methods and materials for producing epothilone and epothilone derivatives |
CA2397493A1 (en) | 2000-01-27 | 2001-08-02 | Cytovia, Inc. | Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof |
PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
WO2003039529A1 (en) | 2001-11-07 | 2003-05-15 | 4Sc A.G. | Selective antibacterial agents |
AU2002367087A1 (en) | 2001-12-21 | 2003-07-15 | 7Tm Pharma A/S | Method for the treatment of mc receptor related disorders with a chelate and/or a chelator |
GB0215676D0 (en) * | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
US8030336B2 (en) | 2002-12-13 | 2011-10-04 | Ym Biosciences Australia Pty Ltd | Nicotinamide-based kinase inhibitors |
AR043633A1 (es) | 2003-03-20 | 2005-08-03 | Schering Corp | Ligandos de receptores de canabinoides |
US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
US20080167347A1 (en) | 2005-01-20 | 2008-07-10 | Shiongi & Co., Ltd. | Ctgf Expression Inhibitor |
EP1881961A1 (en) | 2005-05-11 | 2008-01-30 | Novo Nordisk A/S | New haloalkylsulfone substituted compounds useful for treating obesity and diabetes |
WO2007002441A1 (en) | 2005-06-24 | 2007-01-04 | Emory University | Methods of use for non-atp competitive tyrosine kinase inhibitors to treat pathogenic infection |
DK1746097T3 (da) | 2005-07-20 | 2010-05-25 | Aventis Pharma Sa | 1,4-dihydropyridin-kondenserede heterocykliske ringe, fremgangsmåde til fremstilling af disse, anvendelse og sammensætninger, der indeholder dem |
KR20080109068A (ko) * | 2006-04-05 | 2008-12-16 | 노파르티스 아게 | 암을 치료하기 위한 bcr-abl/c-kit/pdgf-r tk 억제제를 포함하는 조합물 |
WO2008021725A2 (en) | 2006-08-11 | 2008-02-21 | Smithkline Beecham Corporation | Chemical compounds |
CA2667010A1 (en) | 2006-10-20 | 2008-05-02 | Irm Llc | Compositions and methods for modulating c-kit and pdgfr receptors |
EP2097380A1 (en) * | 2006-11-15 | 2009-09-09 | High Point Pharmaceuticals, LLC | New haloalkylsulfone substituted compounds useful for treating obesity and diabetes |
JP5286281B2 (ja) * | 2007-01-05 | 2013-09-11 | ブリストル−マイヤーズ スクイブ カンパニー | アミノピラゾールキナーゼ阻害剤 |
WO2008112695A2 (en) | 2007-03-12 | 2008-09-18 | Irm Llc | Pyrazolo [3,4-d] pyrimidines and 1, 2, 5, 6-tetraaza- as- indacenes as protein kinase inhibitors for cancer treatment |
WO2008124393A1 (en) | 2007-04-04 | 2008-10-16 | Irm Llc | Benzothiazole derivatives and their use as protein kinase inhibitors |
WO2008144253A1 (en) | 2007-05-14 | 2008-11-27 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
BRPI0815038A2 (pt) | 2007-08-02 | 2015-03-17 | Hoffmann La Roche | Uso de derivados de benzamida para o tratamento de transtornos do cns |
WO2009039127A1 (en) | 2007-09-17 | 2009-03-26 | Abbott Laboratories | Uracil or thymine derivative for treating hepatitis c |
EA201001847A1 (ru) | 2008-06-11 | 2011-08-30 | Айрм Ллк | Соединения и композиции, применяемые для лечения малярии |
BRPI0920608A2 (pt) | 2008-09-29 | 2019-09-24 | Boehringer Ingelheim Int | compostos quimicos |
CN102548987B (zh) | 2009-07-14 | 2014-04-16 | 江苏迈度药物研发有限公司 | 作为激酶抑制剂的氟取代化合物及其使用方法 |
JP2011057661A (ja) | 2009-08-14 | 2011-03-24 | Bayer Cropscience Ag | 殺虫性カルボキサミド類 |
KR101663637B1 (ko) | 2009-11-13 | 2016-10-07 | 제노스코 | 키나아제 억제제 |
JO3634B1 (ar) * | 2009-11-17 | 2020-08-27 | Novartis Ag | طريقة لعلاج اضطرابات تكاثرية وحالات مرضية أخرى متوسطة بنشاط كيناز bcr-abl، c-kit، ddr1، ddr2، أو pdgf-r |
WO2011082400A2 (en) | 2010-01-04 | 2011-07-07 | President And Fellows Of Harvard College | Modulators of immunoinhibitory receptor pd-1, and methods of use thereof |
SG182361A1 (en) | 2010-01-29 | 2012-08-30 | Hanmi Science Co Ltd | THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES |
US9464065B2 (en) | 2011-03-24 | 2016-10-11 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
CN102276500A (zh) * | 2011-05-05 | 2011-12-14 | 西安交通大学 | 水杨酰胺类抗肿瘤化合物及其合成方法和用途 |
US9278910B2 (en) | 2011-05-31 | 2016-03-08 | Receptos, Inc. | GLP-1 receptor stabilizers and modulators |
JP6080947B2 (ja) | 2012-05-15 | 2017-02-15 | ノバルティス アーゲー | Abl1、abl2およびbcr−abl1の活性を阻害するための化合物および組成物 |
CA2868958C (en) | 2012-05-15 | 2020-09-01 | Novartis Ag | Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1 |
MX2014013373A (es) * | 2012-05-15 | 2015-08-14 | Novartis Ag | Derivados de benzamida para inhibir la actividad de abl1, abl2 y bcr-abl1. |
WO2013171642A1 (en) * | 2012-05-15 | 2013-11-21 | Novartis Ag | Benzamide derivatives for inhibiting the activity of abl1, abl2 and bcr-abl1 |
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