AR099991A1 - TGF-b INHIBITORS AND METHODS OF USE - Google Patents
TGF-b INHIBITORS AND METHODS OF USEInfo
- Publication number
- AR099991A1 AR099991A1 ARP150101066A ARP150101066A AR099991A1 AR 099991 A1 AR099991 A1 AR 099991A1 AR P150101066 A ARP150101066 A AR P150101066A AR P150101066 A ARP150101066 A AR P150101066A AR 099991 A1 AR099991 A1 AR 099991A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- halo
- pyridinyl
- phenyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 10
- -1 (trimethylsilyl) ethynyl Chemical group 0.000 abstract 9
- 125000001475 halogen functional group Chemical group 0.000 abstract 9
- 150000001875 compounds Chemical class 0.000 abstract 6
- 206010028980 Neoplasm Diseases 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 201000011510 cancer Diseases 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 102000009618 Transforming Growth Factors Human genes 0.000 abstract 2
- 108010009583 Transforming Growth Factors Proteins 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- FSKYZRCACCHDGR-UHFFFAOYSA-N 1h-pyrido[3,2-d]pyrimidin-4-one Chemical compound C1=CN=C2C(=O)N=CNC2=C1 FSKYZRCACCHDGR-UHFFFAOYSA-N 0.000 abstract 1
- 102000005606 Activins Human genes 0.000 abstract 1
- 108010059616 Activins Proteins 0.000 abstract 1
- 239000000488 activin Substances 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 125000005873 benzo[d]thiazolyl group Chemical group 0.000 abstract 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 abstract 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Landscapes
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Compuestos y un método de tratamiento de cáncer que comprende la administración a un sujeto que tiene cáncer de uno de los compuestos junto con otro tratamiento terapéutico del cáncer. Los compuestos inhiben la señalización por un miembro de la superfamilia de TGF-b (TGF: factor de crecimiento transformante) tales como Nodal o Activina. Reivindicación 1: Un compuesto, caracterizado porque tiene la fórmula (1), o una de sus sales farmacéuticamente aceptables, en donde Cy¹ es fenilo opcionalmente sustituido con 1, 2, 3 ó 4 restos seleccionados, de modo independiente, de halo; alquilo C₁₋₃ opcionalmente sustituido con 1, 2 ó 3 halo, etinilo o (trimetilsilil)etinilo; -O-alquilo C₁₋₃ opcionalmente sustituido con 1 - 3 halo; benzofuranilo; 2,3-dihidrobenzofuranilo; y feniletenilo; o, cuando hay un sustituyente simple en Cy¹, el sustituyente es uno de los anteriores sustituyentes del fenilo, -O-(alquil C₀₋₃)RIIIᵉ o - C(O)N(Rˣ)₂, en donde RIIIᵉ es fenilo, heteroarilo o heterocicloalquilo y cada Rˣ es, de modo independiente, H o alquilo C₁₋₃; Cy² es pirazolo[1,5-a]pirimidinilo; benzo[d]tiazolilo; imidazo[1,2-a]piridinilo opcionalmente sustituido con fenil-S(O)₂-; [1,2,4]triazolo[1,5-a]piridinilo; piridinilo; quinazolinilo; 1H-pirrolo[2,3-b]piridinilo; pirido[3,2-d]pirimidinilo opcionalmente sustituido con amino, metilamino o metoxi; o pirido[3,2-d]pirimidin-4(3H)-ona, en donde el quinazolinilo está opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados, de modo independiente, de -N(RIIIᵃ)₂; RIIIᵈ; alquilo C₁₋₃ opcionalmente sustituido con 1 - 3 halo; halo; metoxi; y -N(H)(alquil C₁₋₃)RIV; cada RIIIᵃ es, de modo independiente, H; alquilo C₁₋₆ opcionalmente sustituido con -C(O)OH, -C(O)O(alquilo C₁₋₃) o -CONH₂; o heteroarilo opcionalmente sustituido con alquilo C₁₋₃; RIIIᵈ es H o alquilo C₁₋₃ opcionalmente sustituido con 1 - 3 halo; RIV es H, alquilo C₁₋₃, -pirrolidonilo, 4-metilpiperzinilo, -N(alquil C₁₋₂)(alquilo C₁₋₂) o morfolinilo; y RIIIᶜ es H, halo, -OH, alquilo C₁₋₃ opcionalmente sustituido con 1 - 3 halo u -O-alquilo C₁₋₃ opcionalmente sustituido con 1 - 3 halo; siempre que el compuesto no sea uno de compuestos 1 - 974.Compounds and a method of cancer treatment comprising administration to a subject having cancer of one of the compounds together with another therapeutic treatment of cancer. The compounds inhibit signaling by a member of the TGF-b superfamily (TGF: transforming growth factor) such as Nodal or Activin. Claim 1: A compound, characterized in that it has the formula (1), or a pharmaceutically acceptable salt thereof, wherein Cy¹ is phenyl optionally substituted with 1, 2, 3 or 4 moieties selected, independently, from halo; C₁₋₃ alkyl optionally substituted with 1, 2 or 3 halo, ethynyl or (trimethylsilyl) ethynyl; -O-C₁₋₃ alkyl optionally substituted with 1-3 halo; benzofuranyl; 2,3-dihydrobenzofuranyl; and phenyletenyl; or, when there is a simple substituent on Cy¹, the substituent is one of the above phenyl substituents, -O- (C₀₋₃ alkyl) RIIIᵉ or -C (O) N (Rˣ) ₂, wherein RIIIᵉ is phenyl, heteroaryl or heterocycloalkyl and each Rˣ is, independently, H or C₁₋₃ alkyl; Cy² is pyrazolo [1,5-a] pyrimidinyl; benzo [d] thiazolyl; imidazo [1,2-a] pyridinyl optionally substituted with phenyl-S (O) ₂-; [1,2,4] triazolo [1,5-a] pyridinyl; pyridinyl; quinazolinyl; 1H-pyrrolo [2,3-b] pyridinyl; pyrido [3,2-d] pyrimidinyl optionally substituted with amino, methylamino or methoxy; or pyrido [3,2-d] pyrimidin-4 (3H) -one, wherein the quinazolinyl is optionally substituted with 1 or 2 substituents independently selected from -N (RIIIᵃ) ₂; RIIIᵈ; C₁₋₃ alkyl optionally substituted with 1-3 halo; halo; methoxy; and -N (H) (C₁₋₃ alkyl) RIV; each RIIIᵃ is, independently, H; C₁₋₆ alkyl optionally substituted with -C (O) OH, -C (O) O (C₁₋₃ alkyl) or -CONH₂; or heteroaryl optionally substituted with C₁₋₃ alkyl; RIIIᵈ is H or C₁₋₃ alkyl optionally substituted with 1-3 halo; RIV is H, C₁₋₃ alkyl, -pyrrolidonyl, 4-methylpiperzinyl, -N (C₁₋₂ alkyl) (C₁₋₂ alkyl) or morpholinyl; and RIIIᶜ is H, halo, -OH, C₁₋₃ alkyl optionally substituted with 1-3 halo or -O-C₁₋₃ alkyl optionally substituted with 1-3 halo; provided that the compound is not one of compounds 1-974.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461976880P | 2014-04-08 | 2014-04-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR099991A1 true AR099991A1 (en) | 2016-08-31 |
Family
ID=58700003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150101066A AR099991A1 (en) | 2014-04-08 | 2015-04-08 | TGF-b INHIBITORS AND METHODS OF USE |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR099991A1 (en) |
-
2015
- 2015-04-08 AR ARP150101066A patent/AR099991A1/en unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PH12016501164A1 (en) | Heteroaryl substituted nicotinamide compounds | |
| PH12019500676A1 (en) | Substituted 1h-imidazo[4,5-b]pyridin-2(3h)-ones and their use as glun2b receptor modulators | |
| CL2016002836A1 (en) | Compounds derived from pyrimidin pyrido with modulating activity of smn2 genetic splicing; Pharmaceutical composition and use in the treatment of spinal muscular atrophy (ame). | |
| SG10201807952PA (en) | Jak1 inhibitors for the treatment of myelodysplastic syndromes | |
| IL260020B (en) | 4-amino-2-(1h-pyrazolo[3,4-b]pyridin-3-yl)-6-oxo-6,7-dihydro-5h-pyrrolo[2,3-d]pyrimidine derivatives and the respective (1h-indazol-3-yl) derivatives as cgmp modulators for treating cardiovascular diseases | |
| PE20171307A1 (en) | TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF | |
| EP2931722A4 (en) | 1H-PYRROLO [2,3-B] PYRIDINE AND 1H-PYRAZOLO [3,4-B] PYRIDINE SUBSTITUTED DERIVATIVES AS SALT-INDUCIBLE KINASE 2 INHIBITORS (SIK2) | |
| PE20170693A1 (en) | FUSED PENTACICLIC IMIDAZOLE DERIVATIVES | |
| SI3555097T1 (en) | Imidazo(4,5-d)pyrrolo(2,3-b)pyridine compounds as inhibitors of janus kinases | |
| PE20170403A1 (en) | IMIDAZO [4,5-c] QUINOLIN-2-ONA COMPOUNDS AND THEIR USE TO TREAT CANCER | |
| SI3674302T1 (en) | 1h-pyrrolo(2,3-c)pyridin-7(6h)-ones and pyrazolo(3,4-c)pyridin-7(6h)-ones as inhibitors of bet proteins | |
| SG11201907095UA (en) | DERIVATIVES OF N-CYCLOALKYL/HETEROCYCLOALKYL-4-(IMIDAZO [1,2-a]PYRIDINE)PYRIMIDIN-2-AMINE AS THERAPEUTIC AGENTS | |
| PE20190736A1 (en) | TRICICLIC COMPOUNDS REPLACED AS INHIBITORS OF THE RECEIVER OF THE FIBROBLAST GROWTH FACTOR (FGFR) | |
| PE20151755A1 (en) | FUSED PYRIMIDINES REPLACED WITH TRIFLUOROMETHYL AND ITS USES | |
| TR201907590T4 (en) | Imidazo [4,5-c] pyridine and pyrrolo [2,3-c] pyridine derivatives as Ssao inhibitors. | |
| ECSP19043790A (en) | Pyrazolo [3,4-b] pyridines and imidazo [1,5-b] pyridazines as PDE1 inhibitors | |
| MX2016015762A (en) | Alkyl and aryl derivatives of 1-oxa-4,9-diazaspiro undecane compounds having multimodal activity against pain. | |
| MX2016016363A (en) | Compounds comprising 1,1',2,5'-tetrahydrospiro[indole-3,2'-pyrrol e]-2,5'-dione system as inhibitors p53-mdm2 protein-protein interaction. | |
| ZA201701207B (en) | [1,2,4]triazolo[4,3-b]pyridazines for use in the treatment of proliferative diseases | |
| SI3723808T1 (en) | Combination treatments comprising administration of 1h-pyrazolo(4,3-b)pyridines | |
| SI3723807T1 (en) | Combination treatments comprising administration of 1h-pyrazolo(4,3-b)pyridines | |
| AR099991A1 (en) | TGF-b INHIBITORS AND METHODS OF USE | |
| MX2023004924A (en) | New treatment of sma. | |
| PL408803A1 (en) | New 5-aryl and 5-methyl derivatives of the 1H-pyrazolo[4,3-e][1,2,4]triazolo[3,4-b][1,2,4]triazine system |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |