ES2623704T3 - Derivados de ftalazina. - Google Patents
Derivados de ftalazina. Download PDFInfo
- Publication number
- ES2623704T3 ES2623704T3 ES14728832.8T ES14728832T ES2623704T3 ES 2623704 T3 ES2623704 T3 ES 2623704T3 ES 14728832 T ES14728832 T ES 14728832T ES 2623704 T3 ES2623704 T3 ES 2623704T3
- Authority
- ES
- Spain
- Prior art keywords
- phthalazin
- indicates
- acetamide
- phenyl
- atoms
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
-
- 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Compuestos de fórmula I**Fórmula** en la que R1 indica H, Hal, CH3, OCH3 o CH2OH, X indica Ar o Cyc, Ar indica fenilo, bifenilo o naftilo, estando cada uno de ellos sin sustituir o mono, di o trisustituido por HaI, NO2, CN, A, [C(R2)2]pOR2, S(O)mR2, [C(R2)2]pN(R2)2, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2, [C(R2)2]pSO2N(R2)2, NR2COR2, NR 2SO2R2 NR2CON(R2)2, NHCOOA, O[C(R2)2]nN(R2)2, CHO y/o COA, R2 indica H o A, A indica alquilo no ramificado o ramificado con 1-10 átomos de C, en el que dos átomos de carbono adyacentes pueden formar un doble enlace y/o pueden reemplazarse uno o dos grupos CH y/o CH2 no adyacentes por átomos de N, O y/o S y en el que pueden reemplazarse 1-7 átomos de H por F, Cl y/u OH, Cyc indica cicloalquilo con 3, 4, 5, 6 o 7 átomos de C, Hal indica F, Cl, Br o I, m indica 0, 1 o 2, n indica 1, 2 o 3, p indica 0, 1, 2, 3 o 4, y sales, tautómeros y estereoisómeros farmacéuticamente aceptables de los mismos, incluyendo mezclas de los mismos en cualquier proporción.
Description
- Compuesto n.º
- CI50 del ensayo enzimático de TNKS1 CI50 del ensayo enzimático de TNKS2 CI50 del ensayo celular
- "A16"
- A A C
- "A17"
- A B C
- "A18"
- B B C
- "A19"
- C C
- "A20"
- B B C
- "A21"
- C C
CI50: <0,3 mM= A 0,3 -3mM = B 3-50mM= C
Los compuestos mostrados en la tabla 1 son compuestos particularmente preferidos de acuerdo con la invención. Tabla 2. Inhibición de tanquirasas de algunos compuestos representativos de fórmula I
- Compuesto n.º
- CI50 de PARP CI50 de ELISA de TNKS1 CI50 de ELISA de TNKS2
- "A1"
- C A B
- "A2"
- C B B
- "A3"
- C A A
- "A4"
- C A A
- "A5"
- C B B
- “A6”
- B B B
- "A7"
- B B B
- “A8”
- C A A
- “A9”
- C A A
- "A10"
- C
- "A13"
- C A A
- "A14"
- A A
- "A15"
- C A A
- "A16"
- C A A
- "A17"
- A A
- "A18"
- B A A
- "A20"
- B A A
5
CI50: <0,3 mM= A 0,3 -3mM = B 3-50mM= C
Los compuestos mostrados en la tabla 2 son compuestos particularmente preferidos de acuerdo con la invención.
Los siguientes ejemplos se refieren a medicamentos:
Ejemplo A: Viales para inyección
10 Se ajusta a pH 6,5 una solución de 100 g de un principio activo de fórmula I y 5 g de hidrogenofosfato disódico en 3 l de agua bidestilada usando ácido clorhídrico 2 N, se esteriliza por filtración, se transfiere a viales para inyección, se liofiliza en condiciones estériles y se sella en condiciones estériles. Cada val para inyección contiene 5 mg de principio activo.
28
Claims (2)
-
imagen1 X indica Ar o Cyc,Ar indica fenilo, que no está sustituido o está mono-, di o trisustituido por HaI, NO2, CN, A y/o [C(R2)2]pOR2, R2 indica H o A, Cyc indica cicloalquilo con 3, 4, 5, 6 o 7 átomos de C, 5 A indica alquilo no ramificado o ramificado con 1-6 átomos de C, en el que pueden reemplazarse 1-5 átomos de H por F, Hal indica F, Cl, Br o I, p indica 0, 1, 2, 3 o 4, n indica 1, 2 o 3, 10 y sales, tautómeros y estereoisómeros farmacéuticamente aceptables de los mismos, incluyendo mezclas de los mismos en cualquier proporción. - 6. Compuestos de acuerdo con la reivindicación 1, seleccionados del grupo
- N.º
- Nombre
- "A1"
- 2-fenil-N-ftalazin-1’-il-acetamida
- "A2"
- 2-(3-metoxifenil)-N-ftalazin-1-il-acetamida
- "A3"
- 2-(4-metoxifenil)-N-ftalazin-1-il-acetamida
- "A4"
- 2-(4-etoxifenil)-N-ftalazin-1-il-acetamida
- "A5"
- N-ftalazin-1-il-2-(3-trifluorometoxifenil)-acetamida
- "A6"
- 2-(3-cianofenil)-N-ftalazin-1-il-acetamida
- "A7"
- 2-(3-nitrofenil)-N-ftalazin-1-il-acetamida
- "A8"
- N-ftalazin-1-il-2-(4-trifluorometoxifenil)-acetamida
- "A9"
- 2-(4-terc-butilfenil)-N-ftalazin-1-il-acetamida
- "A10"
- 2-(2,6-diclorofenil)-N-ftalazin-1-il-acetamida
- "A11"
- 2-(4-etoxi-fenil)-N-(5-fluoro-ftalazin-1-il)-acetamida
- "A12"
- N-(5-fluoro-ftalazin-1-il)-2-(4-metoxi-fenil)-acetamida
- "A13"
- 3-ciclohexil-N-ftalazin-1-il-propionamida
- "A14"
- 3-fenil-N-ftalazin-1-il-propionamida
- "A15"
- 3-ciclopentil-N-ftalazin-1-il-propionamida
- "A16"
- 3-(2-cloro-fenil)-N-ftalazin-1-il-propionamida
- "A17"
- 3-(2,3-dicloro-fenil)-N-ftalazin-1-il-propionamida
- "A18"
- N-(8-metil-ftalazin-1-il)-2-fenil-acetamida
- "A19"
- N-(5-metil-ftalazin-1-il)-2-fenil-acetamida
- "A20"
- 2-(4-metoxi-fenil)-N-(8-metil-ftalazin-1-il)-acetamida
- "A21"
- 2-(4-metoxi-fenil)-N-(5-metil-ftalazin-1-il)-acetamida
- "A22"
- 3-ciclohexil-N-(8-metil-ftalazin-1-il)-propionamida
- "A23"
- 3-fenil-N-(8-metil-ftalazin-1-il)-propionamida
31imagen2 imagen3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13003205 | 2013-06-24 | ||
| EP13003205 | 2013-06-24 | ||
| PCT/EP2014/001467 WO2014206524A1 (en) | 2013-06-24 | 2014-05-30 | Phthalazine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2623704T3 true ES2623704T3 (es) | 2017-07-12 |
Family
ID=48698872
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES14728832.8T Active ES2623704T3 (es) | 2013-06-24 | 2014-05-30 | Derivados de ftalazina. |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US9751842B2 (es) |
| EP (1) | EP3013804B1 (es) |
| JP (1) | JP6382964B2 (es) |
| KR (1) | KR20160023854A (es) |
| CN (1) | CN105339356B (es) |
| AR (1) | AR096652A1 (es) |
| AU (1) | AU2014301669B2 (es) |
| CA (1) | CA2916557C (es) |
| DK (1) | DK3013804T3 (es) |
| ES (1) | ES2623704T3 (es) |
| HK (1) | HK1221468A1 (es) |
| HR (1) | HRP20170291T1 (es) |
| IL (1) | IL243252A0 (es) |
| LT (1) | LT3013804T (es) |
| MX (1) | MX369393B (es) |
| PL (1) | PL3013804T3 (es) |
| PT (1) | PT3013804T (es) |
| RS (1) | RS55943B1 (es) |
| RU (1) | RU2663623C2 (es) |
| SG (1) | SG11201510584WA (es) |
| SI (1) | SI3013804T1 (es) |
| WO (1) | WO2014206524A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4466965A (en) | 1982-07-26 | 1984-08-21 | American Hospital Supply Corporation | Phthalazine compounds, compositions and use |
| IT1296984B1 (it) * | 1997-12-19 | 1999-08-03 | Zambon Spa | Derivati ftalazinici inibitori della fosfodiesterasi 4 |
| AU9578901A (en) * | 2000-10-30 | 2002-05-15 | Kudos Pharm Ltd | Phthalazinone derivatives |
| DE102004023507A1 (de) * | 2004-05-10 | 2005-12-01 | Grünenthal GmbH | Substituierte Cyclohexylessigsäure-Derivate |
| CA2569824C (en) | 2004-06-30 | 2013-03-19 | Janssen Pharmaceutica N.V. | Phthalazine derivatives as parp inhibitors |
| EP1833803A4 (en) * | 2005-01-03 | 2009-08-05 | Myriad Genetics Inc | PHARMACEUTICAL COMPOUNDS COMPRISING CASPASE ACTIVATORS AND INDUCERS OF APOPTOSIS AND THE USE THEREOF |
| JP2009286773A (ja) * | 2008-03-14 | 2009-12-10 | Bayer Cropscience Ag | 殺虫性縮環式アリール類 |
-
2014
- 2014-05-30 US US14/392,145 patent/US9751842B2/en active Active
- 2014-05-30 PL PL14728832T patent/PL3013804T3/pl unknown
- 2014-05-30 LT LTEP14728832.8T patent/LT3013804T/lt unknown
- 2014-05-30 SG SG11201510584WA patent/SG11201510584WA/en unknown
- 2014-05-30 MX MX2015016760A patent/MX369393B/es active IP Right Grant
- 2014-05-30 WO PCT/EP2014/001467 patent/WO2014206524A1/en active Application Filing
- 2014-05-30 CA CA2916557A patent/CA2916557C/en not_active Expired - Fee Related
- 2014-05-30 AU AU2014301669A patent/AU2014301669B2/en not_active Ceased
- 2014-05-30 EP EP14728832.8A patent/EP3013804B1/en active Active
- 2014-05-30 ES ES14728832.8T patent/ES2623704T3/es active Active
- 2014-05-30 JP JP2016522300A patent/JP6382964B2/ja not_active Expired - Fee Related
- 2014-05-30 KR KR1020167001936A patent/KR20160023854A/ko not_active Application Discontinuation
- 2014-05-30 PT PT147288328T patent/PT3013804T/pt unknown
- 2014-05-30 RS RS20170425A patent/RS55943B1/sr unknown
- 2014-05-30 SI SI201430206A patent/SI3013804T1/sl unknown
- 2014-05-30 CN CN201480036171.8A patent/CN105339356B/zh not_active Expired - Fee Related
- 2014-05-30 RU RU2016102057A patent/RU2663623C2/ru not_active IP Right Cessation
- 2014-05-30 DK DK14728832.8T patent/DK3013804T3/en active
- 2014-06-19 AR ARP140102314A patent/AR096652A1/es unknown
-
2015
- 2015-12-21 IL IL243252A patent/IL243252A0/en active IP Right Grant
-
2016
- 2016-08-12 HK HK16109622.9A patent/HK1221468A1/zh not_active IP Right Cessation
-
2017
- 2017-02-21 HR HRP20170291TT patent/HRP20170291T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SG11201510584WA (en) | 2016-01-28 |
| CA2916557C (en) | 2021-08-03 |
| PL3013804T3 (pl) | 2017-08-31 |
| US9751842B2 (en) | 2017-09-05 |
| HK1221468A1 (zh) | 2017-06-02 |
| CA2916557A1 (en) | 2014-12-31 |
| LT3013804T (lt) | 2017-04-10 |
| EP3013804A1 (en) | 2016-05-04 |
| EP3013804B1 (en) | 2017-02-01 |
| HRP20170291T1 (hr) | 2017-04-21 |
| JP2016523272A (ja) | 2016-08-08 |
| US20160318876A1 (en) | 2016-11-03 |
| RS55943B1 (sr) | 2017-09-29 |
| CN105339356A (zh) | 2016-02-17 |
| CN105339356B (zh) | 2018-10-19 |
| PT3013804T (pt) | 2017-05-08 |
| IL243252A0 (en) | 2016-02-29 |
| AU2014301669B2 (en) | 2018-03-01 |
| MX369393B (es) | 2019-11-07 |
| KR20160023854A (ko) | 2016-03-03 |
| RU2016102057A3 (es) | 2018-03-16 |
| AU2014301669A1 (en) | 2016-02-11 |
| AR096652A1 (es) | 2016-01-27 |
| DK3013804T3 (en) | 2017-04-10 |
| WO2014206524A1 (en) | 2014-12-31 |
| MX2015016760A (es) | 2016-04-13 |
| SI3013804T1 (sl) | 2017-05-31 |
| JP6382964B2 (ja) | 2018-08-29 |
| RU2016102057A (ru) | 2017-07-28 |
| RU2663623C2 (ru) | 2018-08-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CO2023008167A2 (es) | Inhibidores de prmt5 | |
| CY1122182T1 (el) | Ανοσοκατασταλτικες φαρμακοτεχνικες μορφες | |
| BR112015027951A8 (pt) | arilquinazolinas, seus usos, medicamento, composição farmacêutica, e kit | |
| UY37133A (es) | Derivados de pirazolo[1,5-a]pirazin-4-ilo | |
| BR112015029512A8 (pt) | derivados de pirazolopirrolidina, seus usos, e composição e combinação farmacêuticas | |
| AR079327A1 (es) | Derivados de 2-amino-5,5-difluor -5,6-dihidro-4h-(1,3) oxazin-4-il) fenil)-amida | |
| AR038863A1 (es) | Uso de un inhibidor de garft y/o de aicarft y de un agente antitoxico para preparar un medicamento para destruir selectivamente celulas mtap-deficientes de un mamifero | |
| UY30316A1 (es) | Derivados sustituidos de benzamidas, nicotinamidas, propanamidas, acetamidas y carboxamidas n-(2-(piperidin-1-ilmetil)ciclohexil)sustituidas, procesos de preparacion, composiciones conteniéndolos y aplicaciones | |
| UY32462A (es) | Derivados de bifenilo novedosos para el tratamiento de infección por virus de hepatitis c 644 | |
| GT200900283A (es) | "terapia de combinación con un compuesto actuando como un inhibidor del receptor adp plaquetario". | |
| BRPI0519287A2 (pt) | derivados de amida | |
| CU20110217A7 (es) | Derivados amino-propiónicos sustituidos como inhibidores de neprilisina | |
| AR078045A1 (es) | Derivados de pirimidina, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer | |
| ECSP088869A (es) | Derivados de 2-pirazinona para el tratamiento de enfermedades o condiciones en donde resulta beneficiosa la inhibición de la actividad de la elastasa neutrofílica | |
| BR112015027114A8 (pt) | compostos inibidores seletivos de histona desacetilase, sua composição farmacêutica e seu uso | |
| AR077478A2 (es) | Derivados de oxindol sustituido medicamentos que los comprenden y uso de los mismos | |
| BR112015029401A2 (pt) | derivados pirazolo-pirrolidin-4-ona e seu uso no tratamento de doenças | |
| ECSP099767A (es) | Derivados de n' - (fenil) -n- (morfolin-4-il-piridin-2-il) -pirimidina-2, 4-diamina como inhibidores de quinasas ephb4 para el tratamiento de afecciones proliferativas | |
| CY1120530T1 (el) | Απο του στοματος χορηγησιμη φαρμακευτικη συνθεση | |
| AR073769A1 (es) | Inhibidores de la integrasa del vih derivados de azepina y oxazepinas condensadas, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de infecciones por vih. | |
| AR085308A1 (es) | Formas solidas del inhibidor de girasa (r)-1-etil-3-[6-fluoro-5-[2-(1-hidroxi-1-metil-etil)pirimidin-5-il]-7-(tetrahidrofuran-2-il)-1h-benzimidazol-2-il]urea | |
| MX2020003993A (es) | Derivados de bencimidazol y sus usos. | |
| JP2016513687A5 (es) | ||
| BR112018003489A2 (pt) | n-[2-(2-amino-6,6-dissubstituído-4,4a,5,6-tetra-hidropirano[3,4-d][1,3]tiazin-8a(8h)-il)-1,3-tiazol-4-il]amidas | |
| ES2623704T3 (es) | Derivados de ftalazina. |