RU2003103603A - Производные колхинола в качестве ингибиторов ангиогенеза - Google Patents
Производные колхинола в качестве ингибиторов ангиогенезаInfo
- Publication number
- RU2003103603A RU2003103603A RU2003103603/04A RU2003103603A RU2003103603A RU 2003103603 A RU2003103603 A RU 2003103603A RU 2003103603/04 A RU2003103603/04 A RU 2003103603/04A RU 2003103603 A RU2003103603 A RU 2003103603A RU 2003103603 A RU2003103603 A RU 2003103603A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- hydroxy
- alkoxy
- pharmaceutically acceptable
- amino
- Prior art date
Links
- HSDSUBIABLFGDX-AWEZNQCLSA-N (7s)-7-amino-1,2,3-trimethoxy-6,7-dihydro-5h-dibenzo[5,3-b:1',2'-e][7]annulen-9-ol Chemical class C1C[C@H](N)C2=CC(O)=CC=C2C2=C1C=C(OC)C(OC)=C2OC HSDSUBIABLFGDX-AWEZNQCLSA-N 0.000 title 1
- 230000033115 angiogenesis Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 88
- -1 hydroxy, phosphoryloxy Chemical group 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 24
- 229910052757 nitrogen Inorganic materials 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 239000000651 prodrug Substances 0.000 claims 17
- 229940002612 prodrug Drugs 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 17
- 239000012453 solvate Substances 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 15
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 13
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 125000001589 carboacyl group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 229910000397 disodium phosphate Inorganic materials 0.000 claims 4
- 235000019800 disodium phosphate Nutrition 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 239000001488 sodium phosphate Substances 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 2
- IAGFPWUZTLVULW-KRWDZBQOSA-N 2-amino-n-[2-oxo-2-[[(7s)-1,2,3,9-tetramethoxy-6,7-dihydro-5h-dibenzo[5,3-b:1',2'-e][7]annulen-7-yl]amino]ethyl]acetamide Chemical compound NCC(=O)NCC(=O)N[C@H]1CCC2=CC(OC)=C(OC)C(OC)=C2C2=CC=C(OC)C=C21 IAGFPWUZTLVULW-KRWDZBQOSA-N 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
- 230000000254 damaging effect Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 238000001727 in vivo Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 230000002792 vascular Effects 0.000 claims 2
- MAHWPDWNBBRICZ-HNNXBMFYSA-N (7s)-1,2,3,9-tetramethoxy-6,7-dihydro-5h-dibenzo[5,3-b:1',2'-e][7]annulen-7-amine Chemical compound N[C@H]1CCC2=CC(OC)=C(OC)C(OC)=C2C2=CC=C(OC)C=C21 MAHWPDWNBBRICZ-HNNXBMFYSA-N 0.000 claims 1
- DZWFITHNVLGHJM-FQEVSTJZSA-N 1-(2-imidazol-1-ylethyl)-3-[(7s)-1,2,3,9-tetramethoxy-6,7-dihydro-5h-dibenzo[5,3-b:1',2'-e][7]annulen-7-yl]urea Chemical compound N([C@@H]1C=2C(C3=C(OC)C(OC)=C(OC)C=C3CC1)=CC=C(C=2)OC)C(=O)NCCN1C=CN=C1 DZWFITHNVLGHJM-FQEVSTJZSA-N 0.000 claims 1
- GJVYXMVWXNYWRD-NRFANRHFSA-N 2-morpholin-4-ylethyl n-[(7s)-1,2,3,9-tetramethoxy-6,7-dihydro-5h-dibenzo[5,3-b:1',2'-e][7]annulen-7-yl]carbamate Chemical compound N([C@@H]1C=2C(C3=C(OC)C(OC)=C(OC)C=C3CC1)=CC=C(C=2)OC)C(=O)OCCN1CCOCC1 GJVYXMVWXNYWRD-NRFANRHFSA-N 0.000 claims 1
- XOVLFBRDOGXOQR-QFIPXVFZSA-N 4-(4-methylpiperazin-1-yl)-4-oxo-n-[(7s)-1,2,3,9-tetramethoxy-6,7-dihydro-5h-dibenzo[5,3-b:1',2'-e][7]annulen-7-yl]butanamide Chemical compound N([C@@H]1C=2C(C3=C(OC)C(OC)=C(OC)C=C3CC1)=CC=C(C=2)OC)C(=O)CCC(=O)N1CCN(C)CC1 XOVLFBRDOGXOQR-QFIPXVFZSA-N 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 125000003275 alpha amino acid group Chemical group 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000008300 phosphoramidites Chemical class 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
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- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
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Claims (17)
1. Соединение формулы (I)
где R1, R2 и R3, каждый независимо, представляют гидрокси, фосфорилокси (-ОРО3Н2), С1-4алкокси или гидролизуемый in vivo сложный эфир гидроксигруппы, при условии, что, по меньшей мере, 2 из R1, R2 и R3 представляют С1-4алкокси;
А представляет –СО-, -С(О)О-, -CON(R8)-, -SO2- или –SO2N(R8)- (где R8 представляет водород, С1-4алкил, С1-3алкокси-С1-3-алкил, аминоС1-3алкил или гидроксиС1-3-алкил);
а является целым числом от 1 до 4 включительно;
Rа и Rb независимо выбраны из водорода, гидрокси и амино;
В представляет –О-, -СО-, -N(R9)СО-, -CON(R9)-, -С(О)О-, -N(R9)-, N(R9)С(О)О-, -N(R9)CON(R10)-, -N(R9)SO2-, -SO2N(R9)- или прямую одинарную связь (где R9 и R10 независимо выбраны из водорода, С1-4алкила, С1-3алкокси-С1-3-алкила, аминоС1-3алкила или гидроксиС1-3-алкила);
b является 0 или целым числом от 1 до 4 включительно (при условии, что когда b равно 0, В является одинарной прямой связью);
D представляет карбокси, сульфо, тетразолил, имидазолил, фосфорилокси, гидрокси, амино, N-(С1-4алкил)амино, N,N-ди(С1-3-алкил)амино или группу формулы –Y1-(СН2)сR11 или –NHCH(R12)СООН [где Y1 представляет прямую одинарную связь, -О-, -С(О)-, -N(R13)-, -N(R13)С(О)- или –С(О)N(R13)- (где R13 представляет водород, С1-4алкил, С1-3алкокси-С2-3алкил, аминоС2-3алкил или гидроксиС2-3алкил); с равно 0 или является целым числом от 1 до 4 включительно; R11 представляет 5-6-членную насыщенную гетероциклическую группу (связанную через углерод или азот), содержащую 1 или 2 гетероатома кольца, независимо выбранных из О, S и N, или 5-6-членную ненасыщенную или частично ненасыщенную гетероарильную группу (связанную через углерод или азот), содержащую 1 или 2 гетероатома кольца, независимо выбранных из О, S и N, причем данная гетероциклическая группа или гетероарильная группа может нести 1 или 2 заместителя, выбранных из оксо, гидрокси, галогена, С1-4алкила, С2-4алканоила, карбамоила, N-(С1-4алкил)карбамоила, N,N-ди-(С1-4алкил)-карбамоила, гидроксиС1-4алкила, С1-4алкокси, цианоС1-3алкила, карбамоилС1-3алкила, карбоксиС1-4алкила, аминоС1-4алкила, N-С1-4-алкиламиноС1-4алкила, ди-N,N-(С1-4-алкил)аминоС1-4алкила, С1-4алкоксиС1-4алкила, С1-4алкилсульфонилС1-4алкила и R14 (где R14 представляет 5-6-членную насыщенную гетероциклическую группу (связанную через углерод или азот), содержащую 1 или 2 гетероатома в кольце, независимо выбранных из О, S и N, причем данная гетероциклическая группа является необязательно замещенной 1 или 2 из заместителей, выбранных из оксо, гидрокси, галогена, С1-4-алкила, гидроксиС1-4-алкила, С1-4-алкокси, С1-4-алкоксиС1-4-алкила и С1-4-алкилсульфонилС1-4-алкила);
R12 является аминокислотной боковой цепью;
R5 представляет С1-4алкокси;
R4 и R6, каждый независимо, выбраны из:
водорода, фтора, нитро, амино, N-С1-4алкиламино, N,N-ди-(С1-4алкил)амино, гидрокси, С1-4-алкокси и С1-4-алкила;
R7 представляет водород, С1-4алкил, С1-3алкоксиС1-3алкил, аминоС1-3алкил или гидроксиС1-3алкил
или его фармацевтически приемлемые соль, сольват и пролекарство.
2. Соединение по п.1, где R1, R2 и R3, все представляют метокси, или его фармацевтически приемлемая соль, сольват или пролекарство.
3. Соединение по п.1,
где R1, R2 и R3, все представляют С1-4алкокси;
R4 и R6 независимо выбраны из водорода, гидрокси, С1-3алкокси и С1-3-алкила;
R5 представляет метокси;
А представляет –СО-, -С(О)О- или –CONH-;
а = 1, 2 или 3;
В представляет –СО-, -NHCO-, -CONH, -С(О)О-, -NH-,
-NHC(О)О-, NHCONH- или одинарную прямую связь;
b = 0, 1 или 2;
D представляет карбокси, сульфо, фосфорилокси, гидрокси, амино, N-С1-4алкиламино, N,N-ди(С1-4алкил)амино или группу формулы –Y1-(СН2)сR11 (где Y1 представляет –NHC(О)- или –CONH-; с = 1 или 2; R11 представляет 5-6-членную насыщенную гетероциклическую группу (связанную через азот), содержащую 1 или 2 гетероатома в кольце, выбранных независимо из О и N, причем гетероциклическая группа может нести 1 или 2 заместителя, выбранные из: С1-4алкила, С2-4алканоила, карбамоила, цианоС1-3алкила, гидроксиС1-3алкила, карбокси-С1-3алкила и аминоС1-3алкила);
R7 представляет водород;
или его фармацевтически приемлемая соль, сольват или пролекарство.
4. Соединение по п.1,
где R1, R2 и R3, все представляют метокси;
R4 и R6 независимо выбраны из водорода, гидрокси, метокси и метила;
R5 представляет метокси;
А представляет –СО-, -С(О)О- или –CONH-;
а = 2 или 3;
В представляет –СО-, -NHCO-, -CONH или одинарную прямую связь;
b = 0 или 1;
D представляет карбокси, фосфорилокси, гидрокси, амино, N-С1-4алкиламино, N,N-ди(С1-4алкил)амино или группу формулы –Y1(СН2)сR11 (где Y1 представляет –NHC(О)- или –С(О)NH-; с = 1 или 2; R11 представляет пиперазинил, морфолинил или пиперидинил, каждый из которых связан через атом азота в кольце, и каждое кольцо является необязательно замещенным 1 заместителем или 2 заместителями, выбранными из С1-4алкила, С2-4алканоила, карбамоила, цианоС1-3алкила, гидроксиС1-3алкила, карбоксиС1-3алкила и аминоС1-3алкила);
R7 представляет водород;
или его фармацевтически приемлемая соль, сольват или пролекарство.
5. Соединение по п.1 формулы (II)
где а, b, А, В и D имеют значения, указанные в п.1;
или его фармацевтически приемлемые соль, сольват или пролекарство.
6. Соединение по п.5,
где А представляет –СО-, -С(О)О- или –CONH-;
а = 2 или 3;
В представляет –СО-, -NHCO-, -CONH или одинарную прямую связь;
b = 0 или 1;
D представляет карбокси, фосфорилокси, гидрокси, амино, N-С1-4алкиламино, N,N-ди(С1-4алкил)амино или группу формулы –Y1(СН2)сR11 (где Y1 представляет –NHC(О)- или –С(О)NH-; с = 1 или 2; R11 представляет пиперазинил, морфолинил или пиперидинил, каждый из которых связан через атом азота в кольце, и каждое кольцо является необязательно замещенным 1 или 2 заместителями, выбранными из
С1-4алкила, С2-4алканоила, карбамоила, цианоС1-3алкила, гидроксиС1-3алкила, карбоксиС1-3алкила и аминоС1-3алкила);
или его фармацевтически приемлемые соль, сольват или пролекарство.
7. Соединение по п.1 формулы (III)
где R1, R2 и R3, каждый независимо, представляют гидрокси, фосфорилокси (-ОРО3Н2), С1-4алкокси или гидролизуемый in vivo сложный эфир гидроксигруппы, при условии, что, по меньшей мере, 2 из R1, R2 и R3 представляют С1-4алкокси;
А представляет –СО-, -С(О)О-, -CON(R8)-, -SO2- или –SO2N(R8)- (где R8 представляет водород, С1-4алкил, С1-3алкокси-С2-3алкил, аминоС2-3алкил или гидроксиС2-3-алкил);
а является целым числом от 1 до 4 включительно;
Rа и Rb независимо выбраны из водорода, гидрокси и амино;
В представляет –О-, -СО-, -N(R9)СО-, -CON(R9)-, -С(О)О-, -N(R9)-, N(R9)С(О)О-, -N(R9)CON(R10)-, -N(R9)SO2-, -SO2N(R9)- или прямую одинарную связь (где R9 и R10 независимо выбраны из водорода, С1-4алкила, С1-3алкоксиС2-3алкила, аминоС2-3алкила и гидроксиС2-3алкила);
b = 0 или является целым числом от 1 до 4 включительно;
D представляет 5-6-членную насыщенную гетероциклическую группу (связанную через углерод или азот), содержащую 1 гетероатом или 2 гетероатома в кольце, независимо выбранных из О и N, причем данная гетероциклическая группа является необязательно замещенной 1 или 2 заместителями, выбранными из оксо, гидрокси, галогена, С1-4алкила, С2-4алканоила, карбамоила, N-(С1-4алкил)карбамоила, N,N-ди-(С1-4алкил)карбамоила, гидроксиС1-4алкила, С1-4алкокси, цианоС1-3алкила, карбамоилС1-3алкила, карбоксиС1-4алкила, аминоС1-4алкила, N-С1-4-алкиламиноС1-4алкила, ди-N,N-(С1-4алкил)аминоС1-4алкила, С1-4-алкоксиС1-4алкила и С1-4алкилсульфонилС1-4алкила и R14 (когда R14 является 5-6-членной насыщенной гетероциклической группой (связанной через углерод или азот), содержащей 1 или 2 гетероатома в кольце, независимо выбранных из О и N, причем данная гетероциклическая группа является необязательно замещенной 1 или 2 заместителями, выбранными из оксо, гидрокси, галогена, С1-4алкила, гидроксиС1-4алкила, С1-4алкокси, С1-4алкоксиС1-4алкила и С1-4алкилсульфонилС1-4алкила);
R5 представляет С1-4алкокси;
R4 и R6, каждый независимо, выбраны из водорода, галогена, нитро, амино, N-С1-4алкиламино, N,N-ди(С1-4алкил)амино, гидрокси, С1-4алкокси и С1-4алкила;
R7 представляет водород, С1-4алкил, С1-3алкоксиС1-3алкил, аминоС1-3алкил или гидроксиС1-3алкил;
или его фармацевтически приемлемые соль, сольват и пролекарство.
8. Соединение по п.7,
где R1, R2 и R3, все представляют С1-4алкокси;
R4 и R6 независимо выбраны из водорода, гидрокси, С1-3-алкокси и С1-3-алкила;
R5 представляет метокси;
А представляет –СО-, -С(О)О- или –CONH;
а = 1, 2 или 3;
В представляет -СО-, -NHCO-, -CONH, -С(О)О-, -NH-, -NHC(O)O-, -NHCONH- или прямую одинарную связь;
b = 0, 1 или 2;
D представляет пиперазинил или морфолинил или пиперидинил, причем каждое кольцо является необязательно замещенным 1 или 2 заместителями, выбранными из С1-4алкила, С2-4алканоила, карбамоила, цианоС1-3алкила, гидроксиС1-3алкила, карбоксиС1-3-алкила и аминоС1-3алкила;
R7 представляет водород;
или его фармацевтически приемлемые соли, сольваты или пролекарства.
9. Соединение по п.7,
где R1, R2 и R3, все представляют метокси;
R4 и R6 независимо выбраны из водорода, гидрокси, метокси и метила;
R5 представляет метокси;
А представляет –СО-, -С(О)О- или –CONH;
а = 2 или 3;
В представляет -СО-, -NHCO-, -CONH или прямую одинарную связь;
b = 0 или 1;
D представляет пиперазино или морфолино, причем каждое кольцо является необязательно замещенным 1 или 2 заместителями, выбранными из метила, этила, ацетила, пропионила, карбамоила и 2-гидроксиэтила;
R7 представляет водород;
или его фармацевтически приемлемые соли, сольваты или пролекарства.
10. Соединение по п.7, формулы
где а, b, А, В и D имеют значения, представленные выше в пункте 7;
или его фармацевтически приемлемые соли, сольват или пролекарство.
11. Соединение по п.10,
где А представляет –СО-, -С(О)О- или –CONH-;
а = 2 или 3;
В представляет –СО-, -NHCO-, –CONH или одинарную прямую связь;
b = 0 или 1;
D представляет пиперазино или морфолино, причем каждое кольцо является необязательно замещенным 1 или 2 заместителями, выбранными из метила, этила, ацетила, пропионила, карбамоила и 2-гидроксиэтила;
или его фармацевтически приемлемые соль, сольват или пролекарство.
12. Соединение по п.10, где
А представляет –СО-, -С(О)О- или –CONH-;
а = 2 или 3;
В представляет –СО-, -NHCO-, –CONH или одинарную прямую связь;
b = 0 или 1;
D представляет морфолино, 4-метилпиперазин-1-ил или 4-ацетилпиперазин-1-ил;
или их фармацевтически приемлемые соль, сольват или пролекарство.
13. Соединение по п.1, выбранное из группы, включающей
N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо-[а,с]циклогептен-5-ил]-2-[2-аминоацетиламино]ацетамид;
4-оксо-4-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]амино]бутилдинатрий фосфат;
N-{ N-[2-(имидазол-1-ил)этил]карбамоил} -(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-иламин и
2-{ N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]карбамоилокси} этил-динатрийфосфат;
2-морфолиноэтил-N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]карбамат;
3-(1-метилпиперазин-4-ил)пропил-N-[(5S)-3,9,10,11-тетра-метокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]карбамат;
N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо-[а,с]циклогептен-5-ил]-2-[2-аминоацетиламино]ацетамид;
2-(1-ацетилпиперазин-4-ил)этил-N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]карбамат;
N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]-4-(1-метилпиперазин-4-ил)-4-оксобутан-1-амид;
4-оксо-4-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]аминобутилдинатрийфосфат;
N-{ N-[2-(имидазол-1-ил)этил]карбамоил} -5(S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-иламин;
3-(1-ацетилпиперазин-4-ил)пропил-N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]карбамат;
N-1-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо-[а,с]циклогептен-5-ил]карбамоилокси]этилдинатрийфосфат;
4-морфолино-4-оксобутил-N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо-[а,с]циклогептен-5-ил]карбамат; и
4-(1-метилпиперазин-4-ил)-4-оксобутил-N-[(5S)-3,9,10,11-тетраметокси-6,7-дигидро-5Н-дибензо[а,с]циклогептен-5-ил]карбамат
и их фармацевтически приемлемые соли, сольваты и пролекарства.
14. Фармацевтическая композиция, содержащая соединение по любому из пп.1 - 13, или его фармацевтически приемлемые соль, сольват или пролекарство в сочетании с фармацевтически приемлемым носителем.
15. Применение соединения по любому из пп.1 - 13, или его фармацевтически приемлемых соли, сольвата или пролекарства в производстве лекарственного препарата для использования в создании повреждающего сосудообразование эффекта у теплокровного животного.
16. Применение соединения по любому из пп.1 - 13, или его фармацевтически приемлемых соли, сольвата или пролекарства в производстве лекарственного препарата для введения в разделенных дозах в создании повреждающего сосудообразование эффекта у теплокровного животного.
17. Способ получения соединения формулы (I) или соединения формулы (I), где, по меньшей мере, 1 функциональная группа является защищенной, а R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, А, В, D, а, b и с имеют определенные в п.1 значения, включающий
а) взаимодействие соединения формулы (Х)
с соединением формулы (ХI)
L1-А-[СН(Rа)]а-В-[СН(Rb)]b-D (ХI)
где L1 является удаляемой группой; или
b) превращения одного соединения формулы (I) в другое соединение формулы (I);
с) когда желательна фосфорилоксигруппа, взаимодействие соответствующего гидроксильного соединения с фосфорамидитом;
причем любые функциональные группы являются, необязательно, защищенными;
и затем, если необходимо
i) превращение соединения формулы (I) в другое соединение формулы (I);
ii) удаление защитных групп;
получения его фармацевтически приемлемой соли, сольвата или пролекарства.
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Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP1301498A1 (ru) |
| JP (1) | JP2004504391A (ru) |
| KR (1) | KR20030022264A (ru) |
| CN (1) | CN1255392C (ru) |
| AU (2) | AU6623201A (ru) |
| BR (1) | BR0112225A (ru) |
| CA (1) | CA2410562A1 (ru) |
| CZ (1) | CZ200331A3 (ru) |
| EE (1) | EE200300015A (ru) |
| HU (1) | HUP0301742A3 (ru) |
| IL (1) | IL153325A0 (ru) |
| IS (1) | IS6668A (ru) |
| MX (1) | MXPA02012903A (ru) |
| NO (1) | NO20030055D0 (ru) |
| NZ (1) | NZ522661A (ru) |
| PL (1) | PL359181A1 (ru) |
| RU (1) | RU2003103603A (ru) |
| SK (1) | SK52003A3 (ru) |
| WO (1) | WO2002008213A1 (ru) |
Families Citing this family (343)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
| SE9903544D0 (sv) | 1999-10-01 | 1999-10-01 | Astra Pharma Prod | Novel compounds |
| GB2359551A (en) | 2000-02-23 | 2001-08-29 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
| AR028948A1 (es) | 2000-06-20 | 2003-05-28 | Astrazeneca Ab | Compuestos novedosos |
| US6720323B2 (en) | 2000-07-07 | 2004-04-13 | Angiogene Pharmaceuticals Limited | Colchinol derivatives as angiogenesis inhibitors |
| SE0003828D0 (sv) | 2000-10-20 | 2000-10-20 | Astrazeneca Ab | Novel compounds |
| EP2292615A1 (en) | 2002-02-01 | 2011-03-09 | AstraZeneca AB | Quinazoline compounds |
| GB0217431D0 (en) | 2002-07-27 | 2002-09-04 | Astrazeneca Ab | Novel compounds |
| AU2003255819A1 (en) | 2002-08-24 | 2004-03-11 | Astrazeneca Ab | Pyrimidine derivatives as modulators of chemokine receptor activity |
| GB0221828D0 (en) | 2002-09-20 | 2002-10-30 | Astrazeneca Ab | Novel compound |
| UA83814C2 (ru) | 2002-12-24 | 2008-08-26 | Астразенека Аб | Производные фосфонооксихиназолина и их фармацевтическое применение |
| US8198302B2 (en) | 2003-02-28 | 2012-06-12 | Oxigene, Inc. | Compositions and methods with enhanced therapeutic activity |
| SE0301010D0 (sv) | 2003-04-07 | 2003-04-07 | Astrazeneca Ab | Novel compounds |
| SE0301569D0 (sv) | 2003-05-27 | 2003-05-27 | Astrazeneca Ab | Novel compounds |
| KR101190912B1 (ko) | 2003-11-19 | 2012-10-12 | 어레이 바이오파마 인크. | Ｍｅｋ의 헤테로시클릭 억제제 및 그의 사용 방법 |
| GB0328243D0 (en) | 2003-12-05 | 2004-01-07 | Astrazeneca Ab | Methods |
| JP2007517843A (ja) | 2004-01-05 | 2007-07-05 | アストラゼネカ アクチボラグ | Ｃｈｋ１阻害剤であるチオフェン誘導体 |
| SE0401657D0 (sv) | 2004-06-24 | 2004-06-24 | Astrazeneca Ab | Chemical compounds |
| GB0415320D0 (en) | 2004-07-08 | 2004-08-11 | Astrazeneca Ab | Novel compounds |
| EP2311827A1 (en) | 2004-08-28 | 2011-04-20 | AstraZeneca AB | Thiopyrimidine derivative, useful as an intermediate for chemokine receptor modulators. |
| ZA200705695B (en) | 2004-12-21 | 2009-02-25 | Astrazeneca Ab | Antibodies directed to angiopoietin-2 and uses thereof |
| DK2383268T3 (en) | 2005-02-04 | 2015-09-14 | Astrazeneca Ab | PYRAZOLYLAMINOPYRIDINDERIVATER useful as kinase inhibitors |
| TWI441637B (zh) | 2005-05-18 | 2014-06-21 | Array Biopharma Inc | Ｍｅｋ雜環抑制劑及其使用方法 |
| CA2615650A1 (en) | 2005-07-21 | 2007-01-25 | Astrazeneca Ab | Novel piperidine derivatives |
| TW200738634A (en) | 2005-08-02 | 2007-10-16 | Astrazeneca Ab | New salt |
| TW200738658A (en) | 2005-08-09 | 2007-10-16 | Astrazeneca Ab | Novel compounds |
| EP1939200A4 (en) | 2005-09-22 | 2010-06-16 | Dainippon Sumitomo Pharma Co | NEW ADENINE CONNECTION |
| WO2007034917A1 (ja) | 2005-09-22 | 2007-03-29 | Dainippon Sumitomo Pharma Co., Ltd. | 新規なアデニン化合物 |
| EP1939202A4 (en) | 2005-09-22 | 2010-06-16 | Dainippon Sumitomo Pharma Co | NEW ADENINE CONNECTION |
| JPWO2007034882A1 (ja) | 2005-09-22 | 2009-03-26 | 大日本住友製薬株式会社 | 新規アデニン化合物 |
| JPWO2007034881A1 (ja) | 2005-09-22 | 2009-03-26 | 大日本住友製薬株式会社 | 新規アデニン化合物 |
| EP1937632A1 (en) | 2005-10-06 | 2008-07-02 | Astra Zeneca AB | Novel compounds |
| BRPI0618011A2 (pt) | 2005-10-28 | 2011-08-16 | Astrazeneca Ab | composto ou um sal farmaceuticamente aceitável do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, métodos para produzir um efeito anti-proliferativo e um efeito pró-apoptósico em um animal de sangue quente, para tratar doença e para produzir um efeito inibidor de jak em um animal de sangue quente |
| DE602006021645D1 (de) | 2005-11-15 | 2011-06-09 | Array Biopharma Inc | Verfahren und Zwischenverbindungen zur Herstellung von N4-Phenyl-Quinazolin-4-Amin Derivaten |
| TW200730512A (en) | 2005-12-12 | 2007-08-16 | Astrazeneca Ab | Novel compounds |
| PL1979001T3 (pl) | 2005-12-13 | 2012-09-28 | Medimmune Ltd | Białka wiążące specyficzne dla insulinopodobnych czynników wzrostu i ich zastosowania |
| ES2380683T3 (es) | 2005-12-15 | 2012-05-17 | Astrazeneca Ab | Difenil-éteres, -amidas, -sulfuros y - metanos sustituidos para el tratamiento de la enfermedad respiratoria |
| TW200813091A (en) | 2006-04-10 | 2008-03-16 | Amgen Fremont Inc | Targeted binding agents directed to uPAR and uses thereof |
| US7741360B2 (en) | 2006-05-26 | 2010-06-22 | Astrazeneca Ab | Bi-aryl or aryl-heteroaryl substituted indoles |
| CL2007002225A1 (es) | 2006-08-03 | 2008-04-18 | Astrazeneca Ab | Agente de union especifico para un receptor del factor de crecimiento derivado de plaquetas (pdgfr-alfa); molecula de acido nucleico que lo codifica; vector y celula huesped que la comprenden; conjugado que comprende al agente; y uso del agente de un |
| DE102006037478A1 (de) | 2006-08-10 | 2008-02-14 | Merck Patent Gmbh | 2-(Heterocyclylbenzyl)-pyridazinonderivate |
| JP5227321B2 (ja) | 2006-08-23 | 2013-07-03 | クドス ファーマシューティカルズ リミテッド | Ｍｔｏｒ阻害剤としての２−メチルモルホリンピリド−、ピラゾ−及びピリミド−ピリミジン誘導体 |
| TW200825084A (en) | 2006-11-14 | 2008-06-16 | Astrazeneca Ab | New compounds 521 |
| TW200831528A (en) | 2006-11-30 | 2008-08-01 | Astrazeneca Ab | Compounds |
| KR20090094460A (ko) | 2006-12-19 | 2009-09-07 | 아스트라제네카 아베 | 무스카린 수용체 길항제로서 퀴누클리디놀 유도체 |
| CL2008000191A1 (es) | 2007-01-25 | 2008-08-22 | Astrazeneca Ab | Compuestos derivados de 4-amino-cinnotina-3-carboxamida; inhibidores de csf-1r quinasa; su proceso de preparacion; y su uso para tratar el cancer. |
| TW200902018A (en) | 2007-03-20 | 2009-01-16 | Dainippon Sumitomo Pharma Co | Novel adenine compound |
| EP2138497A4 (en) | 2007-03-20 | 2012-01-04 | Dainippon Sumitomo Pharma Co | NEW ADENINE CONNECTION |
| UA99459C2 (en) | 2007-05-04 | 2012-08-27 | Астразенека Аб | 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer |
| DE102007025717A1 (de) | 2007-06-01 | 2008-12-11 | Merck Patent Gmbh | Arylether-pyridazinonderivate |
| DE102007025718A1 (de) | 2007-06-01 | 2008-12-04 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102007026341A1 (de) | 2007-06-06 | 2008-12-11 | Merck Patent Gmbh | Benzoxazolonderivate |
| UA100983C2 (ru) | 2007-07-05 | 2013-02-25 | Астразенека Аб | Бифенилоксипропановая кислота как модулятор crth2 и интермедиаты |
| DE102007032507A1 (de) | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102007038957A1 (de) | 2007-08-17 | 2009-02-19 | Merck Patent Gmbh | 6-Thioxo-pyridazinderivate |
| DE102007041115A1 (de) | 2007-08-30 | 2009-03-05 | Merck Patent Gmbh | Thiadiazinonderivate |
| MX2010003698A (es) | 2007-10-04 | 2010-04-21 | Astrazeneca Ab | Compuestos de [3,2-c]pirazol esteroides con actividad glucocorticoide. |
| BRPI0818533B8 (pt) | 2007-10-11 | 2021-05-25 | Astrazeneca Ab | composto, composição farmacêutica, uso de um composto, e, processo para a preparação de um composto |
| MX2010006735A (es) | 2007-12-21 | 2010-09-30 | Medimmune Ltd | Miembros de union para receptor alfa de interleucina-4 (il-4ra) - 173. |
| US8092804B2 (en) | 2007-12-21 | 2012-01-10 | Medimmune Limited | Binding members for interleukin-4 receptor alpha (IL-4Rα)-173 |
| DE102007061963A1 (de) | 2007-12-21 | 2009-06-25 | Merck Patent Gmbh | Pyridazinonderivate |
| CN102083839B (zh) | 2008-02-06 | 2014-03-26 | 阿斯利康(瑞典)有限公司 | 化合物 |
| CA2712990C (en) | 2008-02-28 | 2016-09-27 | Bayard R. Huck | Benzonaphthyridinyl compounds as protein kinase inhibitors and use thereof |
| DE102008019907A1 (de) | 2008-04-21 | 2009-10-22 | Merck Patent Gmbh | Pyridazinonderivate |
| PT2297106E (pt) | 2008-05-27 | 2014-09-29 | Astrazeneca Ab | Derivados de fenoxipiridinilamida e seu uso no tratamento de estados de doença mediados por pde4 |
| DE102008025750A1 (de) | 2008-05-29 | 2009-12-03 | Merck Patent Gmbh | Dihydropyrazolderivate |
| DE102008028905A1 (de) | 2008-06-18 | 2009-12-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate |
| DE102008029734A1 (de) | 2008-06-23 | 2009-12-24 | Merck Patent Gmbh | Thiazolyl-piperidinderivate |
| UY31952A (es) | 2008-07-02 | 2010-01-29 | Astrazeneca Ab | 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim |
| DE102008037790A1 (de) | 2008-08-14 | 2010-02-18 | Merck Patent Gmbh | Bicyclische Triazolderivate |
| DE102008038221A1 (de) | 2008-08-18 | 2010-02-25 | Merck Patent Gmbh | 7-Azaindolderivate |
| CN102264763B (zh) | 2008-09-19 | 2016-04-27 | 米迪缪尼有限公司 | 定向于dll4的抗体及其用途 |
| DE102008052943A1 (de) | 2008-10-23 | 2010-04-29 | Merck Patent Gmbh | Azaindolderivate |
| WO2010067102A1 (en) | 2008-12-09 | 2010-06-17 | Astrazeneca Ab | Diazaspiro [5.5] undecane derivatives and related compounds as muscarinic-receptor antagonists and beta-adrenoreceptor agonists for the treatment of pulmonary disorders |
| US7863325B2 (en) | 2008-12-11 | 2011-01-04 | Axcentua Pharmaceuticals Ab | Crystalline genistein sodium salt dihydrate |
| KR20110106355A (ko) | 2008-12-11 | 2011-09-28 | 악센투아 파마슈투칼스 아베 | 제니스테인의 결정성 형태 |
| US20100152197A1 (en) | 2008-12-15 | 2010-06-17 | Astrazeneca Ab | (4-tert-butylpiperazin-2-yl)(piperazin-1-yl)methanone-n-carboxamide derivatives |
| ES2550101T3 (es) | 2008-12-17 | 2015-11-04 | Merck Patent Gmbh | Inhibidores de proteína quinasa de benzonaftiridinona tricíclica modificada con anillo C y su uso |
| US8853391B2 (en) | 2008-12-18 | 2014-10-07 | Merck Patent Gmbh | Tricyclic azaindoles |
| DE102008063667A1 (de) | 2008-12-18 | 2010-07-01 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-°[1,2,4]triazolo[4,3-b]pyrimidin-derivate |
| TW201028410A (en) | 2008-12-22 | 2010-08-01 | Astrazeneca Ab | Chemical compounds 610 |
| DE102008062826A1 (de) | 2008-12-23 | 2010-07-01 | Merck Patent Gmbh | Pyridazinonderivate |
| EP2379595A2 (en) | 2008-12-23 | 2011-10-26 | AstraZeneca AB | Targeted binding agents directed to 5 1 and uses thereof |
| DE102008062825A1 (de) | 2008-12-23 | 2010-06-24 | Merck Patent Gmbh | 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo [4,3-b]pyridazin-derivate |
| DE102009003975A1 (de) | 2009-01-07 | 2010-07-08 | Merck Patent Gmbh | Benzothiazolonderivate |
| DE102009003954A1 (de) | 2009-01-07 | 2010-07-08 | Merck Patent Gmbh | Pyridazinonderivate |
| DE102009004061A1 (de) | 2009-01-08 | 2010-07-15 | Merck Patent Gmbh | Pyridazinonderivate |
| WO2010089580A1 (en) | 2009-02-06 | 2010-08-12 | Astrazeneca Ab | Use of a mct1 inhibitor in the treatment of cancers expressing mct1 over mct4 |
| WO2010092371A1 (en) | 2009-02-10 | 2010-08-19 | Astrazeneca Ab | Triazolo [4,3-b] pyridazine derivatives and their uses for prostate cancer |
| GB0905127D0 (en) | 2009-03-25 | 2009-05-06 | Pharminox Ltd | Novel prodrugs |
| UY32520A (es) | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticoesteroides |
| US8389580B2 (en) | 2009-06-02 | 2013-03-05 | Duke University | Arylcyclopropylamines and methods of use |
| US20100317593A1 (en) | 2009-06-12 | 2010-12-16 | Astrazeneca Ab | 2,3-dihydro-1h-indene compounds |
| GB0913342D0 (en) | 2009-07-31 | 2009-09-16 | Astrazeneca Ab | Compounds - 801 |
| DE102009043260A1 (de) | 2009-09-28 | 2011-04-28 | Merck Patent Gmbh | Pyridinyl-imidazolonderivate |
| AU2010302420B2 (en) | 2009-10-02 | 2013-07-04 | Astrazeneca Ab | 2-pyridone compounds used as inhibitors of neutrophil elastase |
| DE102009049679A1 (de) | 2009-10-19 | 2011-04-21 | Merck Patent Gmbh | Pyrazolopyrimidinderivate |
| WO2011048409A1 (en) | 2009-10-20 | 2011-04-28 | Astrazeneca Ab | Cyclic amine derivatives having beta2 adrenergic receptor agonist and muscarinic receptor antagonist activity |
| US8399460B2 (en) | 2009-10-27 | 2013-03-19 | Astrazeneca Ab | Chromenone derivatives |
| ES2442797T3 (es) | 2009-11-18 | 2014-02-13 | Neomed Institute | Compuestos de benzoimidazol y sus utilizaciones |
| EP3279215B1 (en) | 2009-11-24 | 2020-02-12 | MedImmune Limited | Targeted binding agents against b7-h1 |
| JP2013512859A (ja) | 2009-12-03 | 2013-04-18 | 大日本住友製薬株式会社 | トール様受容体（ｔｌｒ）を介して作用するイミダゾキノリン |
| DE102009058280A1 (de) | 2009-12-14 | 2011-06-16 | Merck Patent Gmbh | Thiazolderivate |
| AU2010333338A1 (en) | 2009-12-14 | 2012-08-02 | Merck Patent Gmbh | Sphingosine kinase inhibitors |
| BR112012014884A2 (pt) | 2009-12-17 | 2016-03-22 | Merck Patent Gmbh | inibidores de esfingosina quinase |
| ES2654584T3 (es) | 2010-01-15 | 2018-02-14 | Suzhou Neupharma Co., Ltd | Ciertas entidades químicas, composiciones y métodos |
| US8198285B2 (en) | 2010-01-19 | 2012-06-12 | Astrazeneca Ab | Pyrazine derivatives |
| WO2011095807A1 (en) | 2010-02-07 | 2011-08-11 | Astrazeneca Ab | Combinations of mek and hh inhibitors |
| WO2011114148A1 (en) | 2010-03-17 | 2011-09-22 | Astrazeneca Ab | 4h- [1, 2, 4] triazolo [5, 1 -b] pyrimidin-7 -one derivatives as ccr2b receptor antagonists |
| US20130059916A1 (en) | 2010-05-26 | 2013-03-07 | Stephane Rocchi | Biguanide compounds and its use for treating cancer |
| WO2011154677A1 (en) | 2010-06-09 | 2011-12-15 | Astrazeneca Ab | Substituted n-[1-cyano-2-(phenyl)ethyl] 1-aminocycloalk-1-ylcarboxamide compounds - 760 |
| GB201009801D0 (en) | 2010-06-11 | 2010-07-21 | Astrazeneca Ab | Compounds 950 |
| SA111320519B1 (ar) | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
| UY33539A (es) | 2010-08-02 | 2012-02-29 | Astrazeneca Ab | Compuestos químicos alk |
| TWI535712B (zh) | 2010-08-06 | 2016-06-01 | 阿斯特捷利康公司 | 化合物 |
| DE102010034699A1 (de) | 2010-08-18 | 2012-02-23 | Merck Patent Gmbh | Pyrimidinderivate |
| US9018197B2 (en) | 2010-08-28 | 2015-04-28 | Suzhou Neupharma Co. Ltd. | Tetradecahydro-1H-cyclopenta[a]phenanthrene compounds, compositions, and related methods of use |
| GB201016442D0 (en) | 2010-09-30 | 2010-11-17 | Pharminox Ltd | Novel acridine derivatives |
| DE102010048800A1 (de) | 2010-10-20 | 2012-05-10 | Merck Patent Gmbh | Chinoxalinderivate |
| DE102010049595A1 (de) | 2010-10-26 | 2012-04-26 | Merck Patent Gmbh | Chinazolinderivate |
| WO2012067268A1 (en) | 2010-11-19 | 2012-05-24 | Dainippon Sumitomo Pharma Co., Ltd. | Cyclic amide compounds and their use in the treatment of disease |
| WO2012066336A1 (en) | 2010-11-19 | 2012-05-24 | Astrazeneca Ab | Benzylamine compounds as toll -like receptor 7 agonists |
| WO2012066335A1 (en) | 2010-11-19 | 2012-05-24 | Astrazeneca Ab | Phenol compounds als toll -like receptor 7 agonists |
| WO2012067269A1 (en) | 2010-11-19 | 2012-05-24 | Dainippon Sumitomo Pharma Co., Ltd. | Aminoalkoxyphenyl compounds and their use in the treatment of disease |
| CN103370317B (zh) | 2010-12-16 | 2015-10-07 | 阿斯利康(瑞典)有限公司 | 可用于治疗的咪唑并[4,5-c]喹啉-1-基衍生物 |
| WO2012080730A1 (en) | 2010-12-17 | 2012-06-21 | Astrazeneca Ab | Purine derivatives |
| BR112013015508B1 (pt) | 2010-12-20 | 2022-04-05 | Medimmune Limited | Molécula de anticorpo para il-18 humana, domínio vh isolado e domínio vl isolado, composição, uso de uma molécula de anticorpo ou do domínio vh isolado e do domínio vl isolado, molécula de ácido nucleico isolada, célula hospedeira procariótica recombinante, método para produzir um anticorpo, e método in vitro para medir il-18 em uma amostra de um indivíduo |
| EP3453714B1 (en) | 2011-02-02 | 2020-11-04 | Suzhou Neupharma Co., Ltd | Cardenolide and bufadienolide 3-carbonate and 3-carbamate derivatives for the treatment of cancer and compositions thereof |
| WO2012110773A1 (en) | 2011-02-17 | 2012-08-23 | Cancer Therapeutics Crc Pty Limited | Fak inhibitors |
| DK2675794T3 (da) | 2011-02-17 | 2019-05-06 | Cancer Therapeutics Crc Pty Ltd | Selektive fak-inhibitorer |
| GB201104267D0 (en) | 2011-03-14 | 2011-04-27 | Cancer Rec Tech Ltd | Pyrrolopyridineamino derivatives |
| US8530470B2 (en) | 2011-04-13 | 2013-09-10 | Astrazeneca Ab | Chromenone derivatives |
| WO2012175991A1 (en) | 2011-06-24 | 2012-12-27 | Pharminox Limited | Fused pentacyclic anti - proliferative compounds |
| US20140227293A1 (en) | 2011-06-30 | 2014-08-14 | Trustees Of Boston University | Method for controlling tumor growth, angiogenesis and metastasis using immunoglobulin containing and proline rich receptor-1 (igpr-1) |
| KR101946664B1 (ko) | 2011-07-12 | 2019-02-11 | 아스트라제네카 아베 | 케모카인 수용체 조절제로서의 n-(6-((2r,3s)-3,4-디히드록시부탄-2-일옥시)-2-(4-플루오로벤질티오)피리미딘-4-일)-3-메틸아제티딘-1-술폰아미드 |
| DK3686193T3 (da) | 2011-07-27 | 2022-05-30 | Astrazeneca Ab | 2-(2,4,5-substitueret anilino)pyrimidinforbindelser |
| DE102011111400A1 (de) | 2011-08-23 | 2013-02-28 | Merck Patent Gmbh | Bicyclische heteroaromatische Verbindungen |
| WO2013032951A1 (en) | 2011-08-26 | 2013-03-07 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| WO2013033250A1 (en) | 2011-09-01 | 2013-03-07 | Xiangping Qian | Certain chemical entities, compositions, and methods |
| AU2012308238B2 (en) | 2011-09-14 | 2017-05-25 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| US9249110B2 (en) | 2011-09-21 | 2016-02-02 | Neupharma, Inc. | Substituted quinoxalines as B-raf kinase inhibitors |
| US20140235573A1 (en) | 2011-09-29 | 2014-08-21 | The University Of Liverpool | Prevention and/or treatment of cancer and/or cancer metastasis |
| WO2013049701A1 (en) | 2011-09-30 | 2013-04-04 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| US20130178520A1 (en) | 2011-12-23 | 2013-07-11 | Duke University | Methods of treatment using arylcyclopropylamine compounds |
| EP2806874B1 (en) | 2012-01-25 | 2017-11-15 | Neupharma, Inc. | Quinoxaline-oxy-phenyl derivatives as kinase inhibitors |
| US9409914B2 (en) | 2012-01-28 | 2016-08-09 | Merck Patent Gmbh | Triazolo[4,5-d]pyrimidine derivatives |
| CN104093722B (zh) | 2012-02-09 | 2016-07-27 | 默克专利股份公司 | 作为TBK1和IKK抑制剂的呋喃并[3,2-b]-和噻吩并[3,2-b]吡啶衍生物 |
| US9339503B2 (en) | 2012-02-09 | 2016-05-17 | Merck Patent Gmbh | Tetrahydro-quinazolinone derivatives as TANK and PARP inhibitors |
| ES2606638T3 (es) | 2012-02-21 | 2017-03-24 | Merck Patent Gmbh | Derivados de furopiridina |
| JP6479476B2 (ja) | 2012-02-21 | 2019-03-06 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
| US9073944B2 (en) | 2012-02-21 | 2015-07-07 | Merck Patent Gmbh | Cyclic diaminopyrimidine derivatives |
| EP2822948B1 (en) | 2012-03-07 | 2016-04-06 | Merck Patent GmbH | Triazolopyrazine derivatives |
| HRP20160908T1 (hr) | 2012-03-28 | 2016-09-23 | Merck Patent Gmbh | Biciklički derivati pirazinona |
| WO2013144532A1 (en) | 2012-03-30 | 2013-10-03 | Astrazeneca Ab | 3 -cyano- 5 -arylamino-7 -cycloalkylaminopyrrolo [1, 5 -a] pyrimidine derivatives and their use as antitumor agents |
| KR101674784B1 (ko) | 2012-04-05 | 2016-11-09 | 에프. 호프만-라 로슈 아게 | 인간 tweak 및 인간 il17에 대한 이중특이적 항체 및 이의 용도 |
| EP3453713B1 (en) | 2012-04-29 | 2021-09-08 | Neupharma, Inc. | Bufadienolide compounds substituted in position 3 by an amine group for use in the treatment of cancer |
| SG11201406997WA (en) | 2012-05-04 | 2014-11-27 | Merck Patent Gmbh | Pyrrolotriazinone derivatives |
| GB201211021D0 (en) | 2012-06-21 | 2012-08-01 | Cancer Rec Tech Ltd | Pharmaceutically active compounds |
| US9624264B2 (en) | 2012-07-24 | 2017-04-18 | Merck Patent Gmbh | Hydroxystatin derivatives for the treatment of arthrosis |
| CA2881279C (en) | 2012-08-07 | 2020-07-07 | Merck Patent Gmbh | Pyridopyrimidine derivatives as protein kinase inhibitors |
| CN104507912B (zh) | 2012-08-08 | 2016-09-28 | 默克专利股份公司 | (氮杂-)异喹啉酮衍生物 |
| HK1209105A1 (en) | 2012-08-17 | 2016-03-24 | Cancer Therapeutics Crc Pty Limited | Vegfr3 inhibitors |
| WO2014041349A1 (en) | 2012-09-12 | 2014-03-20 | Cancer Therapeutics Crc Pty Ltd | Tetrahydropyran-4-ylethylamino- or tetrahydropyranyl-4-ethyloxy-pyrimidines or -pyridazines as isoprenylcysteincarboxymethyl transferase inhibitors |
| CN104812389B (zh) | 2012-09-24 | 2020-07-17 | 润新生物公司 | 某些化学实体、组合物及方法 |
| MX362855B (es) | 2012-09-26 | 2019-02-20 | Merck Patent Gmbh | Derivados de quinazolinona como inhidores poli (adp-ribosa) polimerasa (parp). |
| WO2014063205A1 (en) | 2012-10-26 | 2014-05-01 | The University Of Queensland | Use of endocytosis inhibitors and antibodies for cancer therapy |
| WO2014066955A1 (en) | 2012-11-05 | 2014-05-08 | Lindley Robyn Alice | Methods for determining the cause of somatic mutagenesis |
| US9725421B2 (en) | 2012-11-12 | 2017-08-08 | Neupharma, Inc. | Substituted quinoxalines as B-raf kinase inhibitors |
| US9732032B2 (en) | 2012-11-16 | 2017-08-15 | Merck Patent Gmbh | 3-aminocyclopentane carboxamide derivatives |
| US9353150B2 (en) | 2012-12-04 | 2016-05-31 | Massachusetts Institute Of Technology | Substituted pyrazino[1′,2′:1 ,5]pyrrolo[2,3-b]-indole-1,4-diones for cancer treatment |
| KR102120513B1 (ko) | 2013-01-31 | 2020-06-08 | 네오메드 인스티튜트 | 이미다조피리딘 화합물 및 이의 용도 |
| WO2014127881A1 (de) | 2013-02-25 | 2014-08-28 | Merck Patent Gmbh | 2-amino-3,4-dihydrc-chinazolin derivate und ihre verwendung als cathepsin d inhibitoren |
| EP2964648B1 (en) | 2013-03-05 | 2016-11-16 | Merck Patent GmbH | 9-(aryl or heteroaryl)-2-(pyrazolyl, pyrrolidinyl or cyclopentyl)aminopurine derivatives as anticancer agents |
| AR095443A1 (es) | 2013-03-15 | 2015-10-14 | Fundación Centro Nac De Investig Oncológicas Carlos Iii | Heterociclos condensados con acción sobre atr |
| WO2014144715A1 (en) | 2013-03-15 | 2014-09-18 | Memorial Sloan-Kettering Cancer Center | Hsp90-targeted cardiac imaging and therapy |
| US9937137B2 (en) | 2013-03-15 | 2018-04-10 | Neurocentria, Inc. | Magnesium compositions and uses thereof for cancers |
| WO2014161570A1 (en) | 2013-04-03 | 2014-10-09 | Roche Glycart Ag | Antibodies against human il17 and uses thereof |
| EP3004073A1 (en) | 2013-06-07 | 2016-04-13 | Université catholique de Louvain | 3-carboxy substituted coumarin derivatives with a potential utility for the treatment of cancer diseases |
| SG11201510369WA (en) | 2013-06-25 | 2016-01-28 | Univ Canberra | Methods and compositions for modulating cancer stem cells |
| ES3069593T3 (en) | 2013-08-23 | 2026-06-09 | Neupharma Inc | Quinazolin-8-yl derivatives for use in methods of treating melanoma, non-small cell lung cancer, thyroid cancer, ovarian cancer, or colon cancer |
| CA2923765C (en) | 2013-09-18 | 2021-06-29 | University Of Canberra | Stem cell modulation ii |
| WO2015048852A1 (en) | 2013-10-01 | 2015-04-09 | The University Of Queensland | Kits and methods for diagnosis, screening, treatment and disease monitoring |
| US8986691B1 (en) | 2014-07-15 | 2015-03-24 | Kymab Limited | Method of treating atopic dermatitis or asthma using antibody to IL4RA |
| US8980273B1 (en) | 2014-07-15 | 2015-03-17 | Kymab Limited | Method of treating atopic dermatitis or asthma using antibody to IL4RA |
| GB201403536D0 (en) | 2014-02-28 | 2014-04-16 | Cancer Rec Tech Ltd | Inhibitor compounds |
| AU2015309686B2 (en) | 2014-08-25 | 2020-05-14 | Epiaxis Therapeutics Pty Ltd | Compositions for modulating cancer stem cells and uses therefor |
| CN107430126B (zh) | 2014-11-17 | 2019-12-06 | 昆士兰大学 | 食管腺癌和巴雷特食管的糖蛋白生物标志物及其用途 |
| MA41179A (fr) | 2014-12-19 | 2017-10-24 | Cancer Research Tech Ltd | Composés inhibiteurs de parg |
| GB201501870D0 (en) | 2015-02-04 | 2015-03-18 | Cancer Rec Tech Ltd | Autotaxin inhibitors |
| GB201502020D0 (en) | 2015-02-06 | 2015-03-25 | Cancer Rec Tech Ltd | Autotaxin inhibitory compounds |
| EP3270694A4 (en) | 2015-02-17 | 2018-09-05 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| GB201510019D0 (en) | 2015-06-09 | 2015-07-22 | Cancer Therapeutics Crc Pty Ltd | Compounds |
| CN113336746A (zh) | 2015-08-04 | 2021-09-03 | 常州千红生化制药股份有限公司 | N-(吡啶-2-基)-4-(噻唑-5-基)嘧啶-2-胺类化合物作为治疗性化合物 |
| EP3341496B1 (en) | 2015-08-26 | 2021-02-24 | GMDx Co Pty Ltd | Methods of detecting cancer recurrence |
| AU2016377398B2 (en) | 2015-12-23 | 2022-10-13 | Repluca Pty Ltd | Nucleic acid oligomers and uses therefor |
| JP7341451B2 (ja) | 2016-02-01 | 2023-09-11 | エピアクシス セラピューティクス プロプライアタリー リミティド | タンパク質性化合物とその利用 |
| WO2017142871A1 (en) | 2016-02-15 | 2017-08-24 | Astrazeneca Ab | Methods comprising fixed intermittent dosing of cediranib |
| HRP20221051T8 (hr) | 2016-04-15 | 2023-07-21 | Cancer Research Technology Limited | Heterociklički spojevi kao inhibitori ret kinaze |
| GB2554333A (en) | 2016-04-26 | 2018-04-04 | Big Dna Ltd | Combination therapy |
| US10918627B2 (en) | 2016-05-11 | 2021-02-16 | Massachusetts Institute Of Technology | Convergent and enantioselective total synthesis of Communesin analogs |
| ES2925564T3 (es) | 2016-07-29 | 2022-10-18 | Rapt Therapeutics Inc | Derivados de azetidina tal como moduladores de receptores de quimiocinas y usos de los mismos |
| CN109843858B (zh) | 2016-08-15 | 2023-05-05 | 润新生物公司 | 某些化学实体、组合物及方法 |
| AU2017332839B2 (en) | 2016-09-22 | 2021-11-11 | Cancer Research Technology Limited | Preparation and uses of pyrimidinone derivatives |
| GB201617103D0 (en) | 2016-10-07 | 2016-11-23 | Cancer Research Technology Limited | Compound |
| WO2018106606A1 (en) | 2016-12-05 | 2018-06-14 | Apros Therapeutics, Inc. | Pyrimidine compounds containing acidic groups |
| US10786502B2 (en) | 2016-12-05 | 2020-09-29 | Apros Therapeutics, Inc. | Substituted pyrimidines containing acidic groups as TLR7 modulators |
| US11111245B2 (en) | 2017-02-01 | 2021-09-07 | Aucentra Therapeutics Pty Ltd | Derivatives of N-cycloalkyl/heterocycloalkyl-4-(imidazo[1,2-a]pyridine)pyrimidin-2-amine as therapeutic agents |
| US10703723B2 (en) | 2017-03-09 | 2020-07-07 | Truly Translational Sweden Ab | Prodrugs of sulfasalazine, pharmaceutical compositions thereof and their use in the treatment of autoimmune disease |
| GB201704325D0 (en) | 2017-03-17 | 2017-05-03 | Argonaut Therapeutics Ltd | Compounds |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| US11932650B2 (en) | 2017-05-11 | 2024-03-19 | Massachusetts Institute Of Technology | Potent agelastatin derivatives as modulators for cancer invasion and metastasis |
| CN108864079B (zh) | 2017-05-15 | 2021-04-09 | 深圳福沃药业有限公司 | 一种三嗪化合物及其药学上可接受的盐 |
| EP3630291B9 (en) | 2017-05-26 | 2024-05-29 | Cancer Research Technology Limited | Benzimidazolone derived inhibitors of bcl6 |
| EP3630749B9 (en) | 2017-05-26 | 2024-05-29 | Cancer Research Technology Limited | 2-quinolone derived inhibitors of bcl6 |
| ES2897200T3 (es) | 2017-05-31 | 2022-02-28 | Amplio Pharma Ab | Una composición farmacéutica que comprende una combinación de metotrexato y novobiocina, y el uso de la composición en terapia |
| EP3648797A1 (en) | 2017-07-05 | 2020-05-13 | EPOS-Iasis Research and Development, Ltd | Multifunctional conjugates |
| WO2019025099A1 (en) | 2017-08-01 | 2019-02-07 | Merck Patent Gmbh | THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS |
| CN111278840B (zh) | 2017-08-18 | 2023-11-17 | 癌症研究科技有限公司 | 吡咯并[2，3-b]吡啶化合物及其治疗癌症的用途 |
| KR20200043433A (ko) | 2017-08-21 | 2020-04-27 | 메르크 파텐트 게엠베하 | 아데노신 수용체 길항제로서의 벤즈이미다졸 유도체 |
| KR20200043434A (ko) | 2017-08-21 | 2020-04-27 | 메르크 파텐트 게엠베하 | 아데노신 수용체 길항제로서의 퀴녹살린 유도체 |
| TWI702205B (zh) | 2017-10-06 | 2020-08-21 | 俄羅斯聯邦商拜奧卡德聯合股份公司 | 表皮生長因子受體抑制劑 |
| US10640508B2 (en) | 2017-10-13 | 2020-05-05 | Massachusetts Institute Of Technology | Diazene directed modular synthesis of compounds with quaternary carbon centers |
| NL2019801B1 (en) | 2017-10-25 | 2019-05-02 | Univ Leiden | Delivery vectors |
| AU2018360766B2 (en) | 2017-11-06 | 2024-09-19 | Rapt Therapeutics, Inc. | Anticancer agents |
| ES2965337T3 (es) | 2017-11-23 | 2024-04-12 | Medac Ges Fuer Klinische Spezialpraeparate Mbh | Composición farmacéutica para administración oral que contiene sulfasalazina y/o una sal orgánica de sulfasalazina, proceso de producción y uso |
| EP3489222A1 (en) | 2017-11-23 | 2019-05-29 | medac Gesellschaft für klinische Spezialpräparate mbH | Sulfasalazine salts, production processes and uses |
| US11325900B2 (en) | 2018-01-15 | 2022-05-10 | Aucentra Holdings Pty Ltd | 5-(pyrimidin-4-yl)thiazol-2-yl urea derivatives as therapeutic agents |
| GB201801128D0 (en) | 2018-01-24 | 2018-03-07 | Univ Oxford Innovation Ltd | Compounds |
| US10683280B2 (en) | 2018-01-26 | 2020-06-16 | Rapt Therapeutics, Inc. | Chemokine receptor modulators and uses thereof |
| PL3749310T3 (pl) | 2018-02-08 | 2026-05-25 | Neupharma, Inc. | Określone jednostki chemiczne, kompozycje i sposoby |
| WO2019175093A1 (en) | 2018-03-12 | 2019-09-19 | Astrazeneca Ab | Method for treating lung cancer |
| IL296734B2 (en) | 2018-04-13 | 2025-06-01 | The Institute Of Cancer Res Royal Cancer Hospital | Bcl6 inhibitors |
| MX2020011344A (es) | 2018-04-27 | 2021-02-09 | Spruce Biosciences Inc | Métodos para tratar tumores en reposo suprarrenales testiculares y de ovarios. |
| GB201809102D0 (en) | 2018-06-04 | 2018-07-18 | Univ Oxford Innovation Ltd | Compounds |
| JP7351859B2 (ja) | 2018-06-04 | 2023-09-27 | アプロス セラピューティクス， インコーポレイテッド | Ｔｌｒ７の調節に関係する疾患を処置するのに有用な酸性基を含むピリミジン化合物 |
| EP3802544A1 (en) | 2018-06-05 | 2021-04-14 | RAPT Therapeutics, Inc. | Pyrazolo-pyrimidin-amino-cycloalkyl compounds and their therapeutic uses |
| GB201810092D0 (en) | 2018-06-20 | 2018-08-08 | Ctxt Pty Ltd | Compounds |
| GB201810581D0 (en) | 2018-06-28 | 2018-08-15 | Ctxt Pty Ltd | Compounds |
| HRP20240293T1 (hr) | 2018-09-18 | 2024-05-24 | F. Hoffmann - La Roche Ag | Derivati kinazolina kao protutumorska sredstva |
| US11084829B2 (en) | 2018-09-24 | 2021-08-10 | Rapt Therapeutics, Inc. | Ubiquitin-specific-processing protease 7 (USP7) modulators and uses thereof |
| EP3870294A1 (en) | 2018-10-25 | 2021-09-01 | Merck Patent GmbH | 5-azaindazole derivatives as adenosine receptor antagonists |
| KR20210083287A (ko) | 2018-10-25 | 2021-07-06 | 메르크 파텐트 게엠베하 | 아데노신 수용체 안타고니스트로서의 5-아자인다졸 유도체 |
| DK3880678T3 (da) | 2018-11-13 | 2025-06-10 | Glaxosmithkline Intellectual Property No 3 Ltd | Krystallinske former af p2x3-modulator methyl(s)-2-((2-(2,6-difluoro-4-(methylcarbamoyl )phenyl)-7-methylimidazo[1,2-a]pyridin-3-yl)methyl)morpholin-4-carboxylat |
| GB201819126D0 (en) | 2018-11-23 | 2019-01-09 | Cancer Research Tech Ltd | Inhibitor compounds |
| CA3124730A1 (en) | 2018-12-25 | 2020-07-02 | Institute Of Basic Medical Sciences Chinese Academy Of Medical Sciences | Small rna medicament for prevention and treatment of inflammation-related diseases and combinations thereof |
| AR117844A1 (es) | 2019-01-22 | 2021-09-01 | Merck Patent Gmbh | Derivados de tiazolopiridina como antagonistas del receptor de adenosina |
| CA3131312A1 (en) | 2019-02-25 | 2020-09-03 | Bellus Health Cough Inc. | Treatment with p2x3 modulators |
| US11033547B2 (en) | 2019-03-07 | 2021-06-15 | Merck Patent Gmbh | Carboxamide-pyrimidine derivatives as SHP2 antagonists |
| AU2020245902B2 (en) | 2019-03-28 | 2025-01-02 | Amplia Therapeutics Limited | A salt and crystal form of a FAK inhibitor |
| JP2022526159A (ja) | 2019-03-29 | 2022-05-23 | アストラゼネカ・アクチエボラーグ | 非小細胞肺がんの治療に使用するためのオシメルチニブ |
| CN111747950B (zh) | 2019-03-29 | 2024-01-23 | 深圳福沃药业有限公司 | 用于治疗癌症的嘧啶衍生物 |
| WO2020201773A1 (en) | 2019-04-05 | 2020-10-08 | Storm Therapeutics Ltd | Mettl3 inhibitory compounds |
| CN113646049B (zh) | 2019-04-08 | 2024-08-13 | 默克专利有限公司 | 作为shp2拮抗剂的嘧啶酮衍生物 |
| GB201905328D0 (en) | 2019-04-15 | 2019-05-29 | Azeria Therapeutics Ltd | Inhibitor compounds |
| WO2020247054A1 (en) | 2019-06-05 | 2020-12-10 | Massachusetts Institute Of Technology | Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof |
| GB201908885D0 (en) | 2019-06-20 | 2019-08-07 | Storm Therapeutics Ltd | Therapeutic compounds |
| JP2022545930A (ja) | 2019-08-31 | 2022-11-01 | 上海奕拓醫藥科技有限責任公司 | Ｆｇｆｒ阻害剤とするピラゾール類誘導体及びその調製方法 |
| IL291436B1 (en) | 2019-09-20 | 2026-07-01 | Ideaya Biosciences Inc | History of indole and indazole sulfonamido 4-mutates as PARG inhibitors |
| GB201913988D0 (en) | 2019-09-27 | 2019-11-13 | Celleron Therapeutics Ltd | Novel treatment |
| GB201914860D0 (en) | 2019-10-14 | 2019-11-27 | Cancer Research Tech Ltd | Inhibitor compounds |
| GB201915828D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| GB201915829D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| GB201915831D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| US12195458B2 (en) | 2019-12-02 | 2025-01-14 | Storm Therapeutics Limited | Polyheterocyclic compounds as METTL3 inhibitors |
| GB202004960D0 (en) | 2020-04-03 | 2020-05-20 | Kinsenus Ltd | Inhibitor compounds |
| CN115666561A (zh) | 2020-05-06 | 2023-01-31 | 澳升医药公司 | Cns的增殖性疾病的治疗 |
| GB202008201D0 (en) | 2020-06-01 | 2020-07-15 | Neophore Ltd | Inhibitor compounds |
| GB202012482D0 (en) | 2020-08-11 | 2020-09-23 | Univ Of Huddersfield | Novel compounds and therapeutic uses thereof |
| GB202012969D0 (en) | 2020-08-19 | 2020-09-30 | Univ Of Oxford | Inhibitor compounds |
| WO2022074379A1 (en) | 2020-10-06 | 2022-04-14 | Storm Therapeutics Limited | Mettl3 inhibitory compounds |
| US20240101589A1 (en) | 2020-10-08 | 2024-03-28 | Strom Therapeutics Limited | Inhibitors of mettl3 |
| WO2022182415A1 (en) | 2021-02-24 | 2022-09-01 | Massachusetts Institute Of Technology | Himastatin derivatives, and processes of preparation thereof, and uses thereof |
| GB202102895D0 (en) | 2021-03-01 | 2021-04-14 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| US11918582B2 (en) | 2021-03-15 | 2024-03-05 | Rapt Therapeutics, Inc. | Pyrazole pyrimidine compounds and uses thereof |
| US20250281633A1 (en) | 2021-05-03 | 2025-09-11 | Merck Patent Gmbh | Her2 targeting fc antigen binding fragment-drug conjugates |
| MX2023013690A (es) | 2021-05-17 | 2024-01-30 | Hk Inno N Corp | Derivado de benzamida, metodo para preparar el mismo, y composicion farmaceutica para la prevencion o tratamiento del cancer que contiene el mismo como ingrediente activo. |
| US20240226319A1 (en) | 2021-05-25 | 2024-07-11 | Merck Patent Gmbh | Egfr targeting fc antigen binding fragment-drug conjugates |
| GB202107907D0 (en) | 2021-06-02 | 2021-07-14 | Storm Therapeutics Ltd | Combination therapies |
| GB202108383D0 (en) | 2021-06-11 | 2021-07-28 | Argonaut Therapeutics Ltd | Compounds useful in the treatment or prevention of a prmt5-mediated disorder |
| GB202110373D0 (en) | 2021-07-19 | 2021-09-01 | Neophore Ltd | Inhibitor compounds |
| CA3225500A1 (en) | 2021-10-04 | 2023-04-13 | Ulrich Luecking | Parg inhibitory compounds |
| US20250002491A1 (en) | 2021-10-04 | 2025-01-02 | Forx Therapeutics Ag | N,n-dimethyl-4-(7-(n-(1-methylcyclopropyl)sulfamoyl)-imidazo[1,5-a]pyridin-5-yl)piperazine-1-carboxamide derivatives and the corresponding pyrazolo[1,5-a]pyridine derivatives as parg inhibitors for the treatment of cancer |
| GB202117225D0 (en) | 2021-11-29 | 2022-01-12 | Neophore Ltd | Protac compounds |
| GB202117224D0 (en) | 2021-11-29 | 2022-01-12 | Neophore Ltd | Inhibitor compounds |
| AU2023205435A1 (en) | 2022-01-10 | 2024-08-22 | Cancer Research Horizons | Substituted heterocycles as hset inhibitors |
| GB202202006D0 (en) | 2022-02-15 | 2022-03-30 | Chancellor Masters And Scholars Of The Univ Of Oxford | Anti-cancer treatment |
| GB202202199D0 (en) | 2022-02-18 | 2022-04-06 | Cancer Research Tech Ltd | Compounds |
| WO2023175184A1 (en) | 2022-03-17 | 2023-09-21 | Forx Therapeutics Ag | 2,4-dioxo-1,4-dihydroquinazoline derivatives as parg inhibitors for the treatment of cancer |
| WO2023175185A1 (en) | 2022-03-17 | 2023-09-21 | Forx Therapeutics Ag | 2,4-dioxo-1,4-dihydroquinazoline derivatives as parg inhibitors for the treatment of cancer |
| GB202204935D0 (en) | 2022-04-04 | 2022-05-18 | Cambridge Entpr Ltd | Nanoparticles |
| CA3255429A1 (en) | 2022-04-06 | 2023-10-12 | Rapt Therapeutics, Inc. | Chemokine Receptor Modulators and Their Uses |
| IL316261A (en) | 2022-04-28 | 2024-12-01 | Danatlas Pharmaceuticals Co Ltd | Tricyclic and heterocyclic derivatives, preparations and uses thereof |
| KR20250011134A (ko) | 2022-05-11 | 2025-01-21 | 캔써 리서치 테크놀로지 리미티드 | Ikk 억제제 |
| GB202209404D0 (en) | 2022-06-27 | 2022-08-10 | Univ Of Sussex | Compounds |
| EP4565592A1 (en) | 2022-08-01 | 2025-06-11 | Neupharma, Inc. | Crystalline salts of crystalline salts of (3s,5r,8r,9s,10s,13r,14s,17r)-14-hydroxy-10,13-dimethyl-17-(2- oxo-2h-pyran-5-yl)hexadecahydro-1h-cyclopenta[a]phenanthren-3-yl piperazine-1-carboxylate |
| GB202213166D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| GB202213164D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| GB202213167D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| GB202213162D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Prodrugs |
| GB202213163D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| IL320031A (en) | 2022-10-03 | 2025-06-01 | Forx Therapeutics Ag | Parg inhibitory compound |
| WO2024094962A1 (en) | 2022-11-02 | 2024-05-10 | Cancer Research Technology Limited | Pyrido[2,3-d]pyrimidin-2-amine derivatives as egfr inhibitors for the treatment of cancer |
| EP4612148A1 (en) | 2022-11-02 | 2025-09-10 | Cancer Research Technology Limited | 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one and 7-amino-1-pyrimido[4,5-d]pyrimidin-2(1 h)-one derivatives as egfr inhibitors for the treatment of cancer |
| CN120265629A (zh) | 2022-11-07 | 2025-07-04 | 默克专利股份公司 | 被取代的双环和三环hset抑制剂 |
| GB202218672D0 (en) | 2022-12-12 | 2023-01-25 | Storm Therapeutics Ltd | Inhibitory compounds |
| GB202300881D0 (en) | 2023-01-20 | 2023-03-08 | Neophore Ltd | Inhibitor compounds |
| WO2024173524A1 (en) | 2023-02-14 | 2024-08-22 | Ideaya Biosciences, Inc. | Heteroaryl-substituted benzimidazole compounds |
| WO2024173530A1 (en) | 2023-02-14 | 2024-08-22 | Ideaya Biosciences, Inc. | Heteroaryl-substituted pyrazolo/imidazo pyridine compounds |
| WO2024173514A1 (en) | 2023-02-14 | 2024-08-22 | Ideaya Biosciences, Inc. | Amide and ester-substituted imidazopyridine compounds |
| WO2024173453A1 (en) | 2023-02-14 | 2024-08-22 | Ideaya Biosciences, Inc. | Heteroaryl-substituted imidazopyridine compounds |
| KR20250153866A (ko) | 2023-03-10 | 2025-10-27 | 브레이크포인트 테라퓨틱스 게엠베하 | Dna 중합효소 세타 억제제 |
| WO2024209035A1 (en) | 2023-04-05 | 2024-10-10 | Forx Therapeutics Ag | Parg inhibitory compounds |
| GB202306601D0 (en) | 2023-05-04 | 2023-06-21 | Cancer Research Tech Ltd | Inhibitor compounds |
| GB202307924D0 (en) | 2023-05-26 | 2023-07-12 | Neophore Ltd | Inhibitor compounds |
| GB2631509A (en) | 2023-07-04 | 2025-01-08 | Univ Liverpool | Compositions |
| GB2631507A (en) | 2023-07-04 | 2025-01-08 | Univ Liverpool | Compositions |
| WO2025046148A1 (en) | 2023-09-01 | 2025-03-06 | Forx Therapeutics Ag | Novel parg inhibitors |
| WO2025056923A1 (en) | 2023-09-15 | 2025-03-20 | Cambridge Enterprise Limited | Combination therapy |
| WO2025073792A1 (en) | 2023-10-02 | 2025-04-10 | Forx Therapeutics Ag | Wrn inhibitory compounds |
| GB202315149D0 (en) | 2023-10-03 | 2023-11-15 | Celleron Therapeutics Ltd | Combination therapy |
| KR20260084620A (ko) | 2023-10-03 | 2026-06-05 | 포알엑스 테라퓨틱스 아게 | Parg 억제 화합물 |
| GB202316595D0 (en) | 2023-10-30 | 2023-12-13 | Storm Therapeutics Ltd | Inhibitory compounds |
| GB202316683D0 (en) | 2023-10-31 | 2023-12-13 | Storm Therapeutics Ltd | Inhibitory compounds |
| WO2025093755A1 (en) | 2023-11-01 | 2025-05-08 | Forx Therapeutics Ag | Novel parc inhibitors |
| GB202317368D0 (en) | 2023-11-13 | 2023-12-27 | Breakpoint Therapeutics Gmbh | Novel compounds, compositions and therapeutic uses thereof |
| WO2025104443A1 (en) | 2023-11-14 | 2025-05-22 | Storm Therapeutics Ltd | Inhibitory compounds |
| WO2025114480A1 (en) | 2023-11-28 | 2025-06-05 | Forx Therapeutics Ag | Wrn inhibitory compounds |
| IL328906A (en) | 2023-12-18 | 2026-08-01 | Ideaya Biosciences Inc | Chemical compounds and their uses |
| GB202319863D0 (en) | 2023-12-21 | 2024-02-07 | Breakpoint Therapeutics Gmbh | Movel compounds, compositions and therapeutics uses thereof |
| GB202319864D0 (en) | 2023-12-21 | 2024-02-07 | Breakpoint Therapeutics Gmbh | Novel compounds, compositions and therapeutic uses thereof |
| WO2025133396A1 (en) | 2023-12-22 | 2025-06-26 | Forx Therapeutics Ag | Novel bicyclo heteroaryl parg inhibitors |
| WO2025133395A1 (en) | 2023-12-22 | 2025-06-26 | Forx Therapeutics Ag | Bicyclic (hetero)arylene wrn inhibitory compounds |
| WO2025191176A1 (en) | 2024-03-14 | 2025-09-18 | Forx Therapeutics Ag | Wrn inhibitory compounds |
| NL2037411B1 (en) | 2024-04-08 | 2025-10-31 | Univ Leiden | Protac compounds |
| GB202407738D0 (en) | 2024-05-31 | 2024-07-17 | Storm Therapeutics Ltd | Inhibitory compounds |
| WO2025262192A1 (en) | 2024-06-21 | 2025-12-26 | Breakpoint Therapeutics Gmbh | Quinazoline derivatives suitable for use as werner syndrome helicase protein inhibitors |
| WO2026003380A1 (en) | 2024-06-28 | 2026-01-02 | Forx Therapeutics Ag | Wrn inhibitory compounds |
| WO2026022150A1 (en) | 2024-07-22 | 2026-01-29 | Forx Therapeutics Ag | Parg inhibitory compounds |
| WO2026062066A1 (en) | 2024-09-17 | 2026-03-26 | Forx Therapeutics Ag | Compounds inducing parg degradation |
| GB202416489D0 (en) | 2024-11-08 | 2024-12-25 | Institute Of Cancer Res Royal Cancer Hospital The | Therapeutic bifunctional agents |
| GB202417501D0 (en) | 2024-11-28 | 2025-01-15 | Neophore Ltd | Inhibitor compounds |
| WO2026125304A1 (en) | 2024-12-11 | 2026-06-18 | Merck Patent Gmbh | Carboxylic acids as dhx8/16 inhibitors |
| WO2026132784A2 (en) | 2024-12-19 | 2026-06-25 | Storm Therapeutics Ltd | Inhibitory compounds |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9714249D0 (en) * | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
-
2001
- 2001-07-04 EE EEP200300015A patent/EE200300015A/xx unknown
- 2001-07-04 NZ NZ522661A patent/NZ522661A/en unknown
- 2001-07-04 JP JP2002514119A patent/JP2004504391A/ja not_active Ceased
- 2001-07-04 CA CA002410562A patent/CA2410562A1/en not_active Abandoned
- 2001-07-04 HU HU0301742A patent/HUP0301742A3/hu unknown
- 2001-07-04 AU AU6623201A patent/AU6623201A/xx active Pending
- 2001-07-04 MX MXPA02012903A patent/MXPA02012903A/es unknown
- 2001-07-04 CZ CZ200331A patent/CZ200331A3/cs unknown
- 2001-07-04 EP EP01943701A patent/EP1301498A1/en not_active Withdrawn
- 2001-07-04 WO PCT/GB2001/002964 patent/WO2002008213A1/en not_active Ceased
- 2001-07-04 SK SK5-2003A patent/SK52003A3/sk not_active Application Discontinuation
- 2001-07-04 KR KR10-2003-7000098A patent/KR20030022264A/ko not_active Ceased
- 2001-07-04 RU RU2003103603/04A patent/RU2003103603A/ru not_active Application Discontinuation
- 2001-07-04 BR BR0112225-8A patent/BR0112225A/pt not_active IP Right Cessation
- 2001-07-04 PL PL01359181A patent/PL359181A1/xx not_active Application Discontinuation
- 2001-07-04 AU AU2001266232A patent/AU2001266232B2/en not_active Ceased
- 2001-07-04 IL IL15332501A patent/IL153325A0/xx unknown
- 2001-07-04 CN CNB01812402XA patent/CN1255392C/zh not_active Expired - Fee Related
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2003
- 2003-01-03 IS IS6668A patent/IS6668A/is unknown
- 2003-01-06 NO NO20030055A patent/NO20030055D0/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SK52003A3 (en) | 2003-07-01 |
| JP2004504391A (ja) | 2004-02-12 |
| NO20030055L (no) | 2003-01-06 |
| HUP0301742A2 (hu) | 2003-09-29 |
| CA2410562A1 (en) | 2002-01-31 |
| AU2001266232B2 (en) | 2005-09-15 |
| CN1255392C (zh) | 2006-05-10 |
| AU6623201A (en) | 2002-02-05 |
| WO2002008213A1 (en) | 2002-01-31 |
| MXPA02012903A (es) | 2004-07-30 |
| EP1301498A1 (en) | 2003-04-16 |
| CZ200331A3 (cs) | 2003-04-16 |
| EE200300015A (et) | 2004-10-15 |
| HUP0301742A3 (en) | 2005-08-29 |
| IS6668A (is) | 2003-01-03 |
| NZ522661A (en) | 2004-07-30 |
| KR20030022264A (ko) | 2003-03-15 |
| IL153325A0 (en) | 2003-07-06 |
| BR0112225A (pt) | 2003-05-06 |
| NO20030055D0 (no) | 2003-01-06 |
| PL359181A1 (en) | 2004-08-23 |
| CN1440396A (zh) | 2003-09-03 |
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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