AR057911A1 - Compuestos de pirimidinil benzotiofeno formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento - Google Patents
Compuestos de pirimidinil benzotiofeno formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamentoInfo
- Publication number
- AR057911A1 AR057911A1 ARP060105065A ARP060105065A AR057911A1 AR 057911 A1 AR057911 A1 AR 057911A1 AR P060105065 A ARP060105065 A AR P060105065A AR P060105065 A ARP060105065 A AR P060105065A AR 057911 A1 AR057911 A1 AR 057911A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- cycloalkyl
- halo
- hydroxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P33/00—Antiparasitic agents
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuesto de pirimidinil benzotiofeno de formula (1) en donde R1 es H, hidroxi, halo, metiltio, aminosulfonilo, pirid-2-ilamino, 3-,metilaminocarbonilfenilo, -C(O)NR8R9, -(CH2)0-1NHSO2R12, -CH2NHCONHR13, -NHC(O)R14, o pirrolidinonilo opcionalmente sustituido con etiloxicarbonilo; R2 es H, hidroxi, halo, ciano, alquilo C1-4 o alcoxi C1-4; R3 es H, halo o metilo; R4 es (a) -NR6R7 o (b) aminometilociclohexilo, piperidinilo, 2,2,6-6-tetrametilpiperidin-4-ilo; 2,2,6,6-tetrametilpiperidin-4- iletenilo, 4-alquilpiperidin(C1-4)-4-ilo, o pirrolidinilo; en donde (b) puede ser opcionalmente sustituido con un sustituyente seleccionado del grupo que consiste de alquenilo C2-4, cicloalquilo C3-6, C(O)R10, y alquilo C1-4 opcionalmente sustituido con halo, alcoxi C1-4 o cicloalquilo C3-6; R5 es H cuando n es 1-7 o hidroxi cuando n es 2-7; R6 es H o alquilo C1-4; R7 es seleccionado del grupo que consiste de H, alquilo C1-4, piperidin-4-ilo opcionalmente sustituido con alquilo C1-4, piperidinilcarbonilo opcionalmente sustituido con alquilo C1-4, pirrolidin-3-ilo opcionalmente sustituido con alquilo C1-4, y pirrolidinilocarbonilo opcionalmente sustituido con alquilo C1-4, alternativamente R6 y R7 junto con el N al cual están unidos, forman un anillo seleccionado del grupo que consiste de piperazinilo, homopiperazinilo, 4-dimetiloaminopiperidin-1-ilo, 3-dimetiloaminopirrolidin-1-ilo, o hexahidro-pirrol[3,4-c]pirrolilo; en donde el anillo puede ser opcionalmente sustituido del grupo que consiste de alquenilo C2-4, cicloalquilo C3-6, C(O)R10, y uno a tres sustituyentes alquilo C1-4 opcionalmente sustituidos con hidroxi; R8 es H o alquilo C1-4; R9 es H, alquilo C1-4, alcoxi C1-4, cicloalquilo C3-6, tiazolilo, imidazolilo, piridilo, fenilo opcionalmente sustituido con halo, 2-hidroxi-2-fenilo-etilo, imidazoliletilo, 6-cloropirid-3-ilmetilo, o furan-2-ilo-(alquilo C1-4); alternativamente R8 y R9 junto con el N al cual están unidos, forman un heterociclo seleccionado del grupo que consiste de morfolinilo y tiazinilo; R10 es H, alquilo C1-4, o NHR11; R11 es H o alquilo C1-4; R12 es alquilo C1-4, trifluoroalquilo C1-4, bencilo, o cicloalquilo C3-6; R13 es alquilo C1-4, cicloalquilo C3-6, o bencilo opcionalmente sustituido co alquilo C1-4, halo, o alcoxi C1-4; R14 es cicloalquilo C3-6, piperidinilo, indolilo metilo, o bencilo opcionalmente sustituido con 3-dimetilamino-2-hidroxipropoxi; siempre que cuando R4 es piperidinilo, R1 es -C(O)NR8R9; y n es 1-7 o una sal del mismo farmacéuticamente aceptable. Formulacion farmacéutica que lo comprende. Uso de dicho compuesto para la manufactura de un medicamento para el tratamiento de un cáncer seleccionado de mieloma multiple, cáncer de colon, cáncer de pulmon de célula grande, glioblastoma y cáncer de ovario, o para el tratamiento de enfermedades inflamatorias seleccionadas de artritis reumatoide y enfermedad pulmonar obstructiva cronica.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US73809705P | 2005-11-18 | 2005-11-18 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR057911A1 true AR057911A1 (es) | 2007-12-26 |
Family
ID=38345605
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP060105065A AR057911A1 (es) | 2005-11-18 | 2006-11-17 | Compuestos de pirimidinil benzotiofeno formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento |
Country Status (27)
Country | Link |
---|---|
US (1) | US7547691B2 (es) |
EP (1) | EP1989200B1 (es) |
JP (1) | JP2009516697A (es) |
KR (1) | KR100990771B1 (es) |
CN (1) | CN101309918B (es) |
AR (1) | AR057911A1 (es) |
AT (1) | ATE437873T1 (es) |
AU (1) | AU2006337626B2 (es) |
BR (1) | BRPI0618245A2 (es) |
CA (1) | CA2629336A1 (es) |
CR (1) | CR9947A (es) |
DE (1) | DE602006008187D1 (es) |
DK (1) | DK1989200T3 (es) |
EA (1) | EA014426B1 (es) |
EC (1) | ECSP088456A (es) |
ES (1) | ES2329085T3 (es) |
IL (1) | IL190489A0 (es) |
MA (1) | MA30053B1 (es) |
NO (1) | NO20082594L (es) |
PE (1) | PE20070833A1 (es) |
PL (1) | PL1989200T3 (es) |
PT (1) | PT1989200E (es) |
SI (1) | SI1989200T1 (es) |
TN (1) | TNSN08227A1 (es) |
TW (1) | TW200800201A (es) |
WO (1) | WO2007092095A2 (es) |
ZA (1) | ZA200803940B (es) |
Families Citing this family (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101460483B (zh) | 2006-03-31 | 2013-05-08 | 詹森药业有限公司 | 作为组胺h4受体调节剂的苯并咪唑-2-基嘧啶和吡嗪 |
AU2007275221A1 (en) * | 2006-07-20 | 2008-01-24 | Allen J. Borchardt | Benzothiophene inhibitors of RHO kinase |
PT2125794E (pt) | 2006-12-21 | 2011-01-10 | Lilly Co Eli | Compostos imidazolidinonilo aminopirimidina para o tratamento do cancro |
WO2008076704A1 (en) * | 2006-12-21 | 2008-06-26 | Eli Lilly And Company | Imidazolidinonyl aminopyrimidine compounds for the treatment' of cancer |
CA2691997A1 (en) | 2007-05-16 | 2008-11-27 | Eli Lilly And Company | Triazolyl aminopyrimidine compounds |
MX2009012233A (es) | 2007-05-16 | 2009-12-01 | Lilly Co Eli | Compuestos de triazolil aminopirimidina. |
WO2010002774A1 (en) | 2008-06-30 | 2010-01-07 | Janssen Pharmaceutica Nv | Process for the preparation of substituted pyrimidine derivatives |
US9371311B2 (en) | 2008-06-30 | 2016-06-21 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine derivatives |
KR101123178B1 (ko) * | 2009-04-09 | 2012-06-13 | (주)에스메디 | 2-아릴벤조싸이오펜 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 퇴행성 뇌질환의 진단 또는 치료용 약학적 조성물 |
CA2770454A1 (en) | 2009-08-19 | 2011-02-24 | Ambit Biosciences Corporation | Biaryl compounds and methods of use thereof |
RU2552999C2 (ru) | 2010-04-27 | 2015-06-10 | Хатчисон Медифарма Лимитед | Соединения пиримидинилиндола |
JP2014512364A (ja) | 2011-04-07 | 2014-05-22 | コーネル ユニバーシティー | 水溶液中で二量体化できる単量体、およびその使用法 |
US9245773B2 (en) | 2011-09-02 | 2016-01-26 | Taiwan Semiconductor Manufacturing Company, Ltd. | Semiconductor device packaging methods and structures thereof |
CN103159742B (zh) * | 2011-12-16 | 2015-08-12 | 北京韩美药品有限公司 | 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用 |
AU2013216935C1 (en) | 2012-02-08 | 2017-12-14 | John Emmerson Campbell | Heteroaryl compounds and methods of use thereof |
TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
CN105085434B (zh) * | 2014-05-09 | 2018-02-09 | 上海特化医药科技有限公司 | 硫乙拉嗪或其中间体的制备方法 |
WO2017076888A1 (en) * | 2015-11-03 | 2017-05-11 | Janssen Pharmaceutica Nv | 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same |
EP3490607A4 (en) | 2016-07-29 | 2020-04-08 | Sunovion Pharmaceuticals Inc. | COMPOUNDS AND COMPOSITIONS, AND USES THEREOF |
WO2018023072A2 (en) | 2016-07-29 | 2018-02-01 | Sunovion Pharmaceuticals, Inc. | Compounds and compositions and uses thereof |
EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
US11358959B2 (en) * | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
CN110869358A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
JP7191085B2 (ja) | 2017-08-02 | 2022-12-16 | サノビオン ファーマシューティカルズ インク | イソクロマン化合物およびその使用 |
MX2021010880A (es) | 2019-03-14 | 2022-01-18 | Sunovion Pharmaceuticals Inc | Sales de un compuesto de isocromanilo y formas cristalinas, procesos de preparacion, usos terapeuticos y composiciones farmaceuticas de las mismas. |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1989011279A1 (en) * | 1988-05-16 | 1989-11-30 | Georgia State University Foundation, Inc. | Nucleic acid interacting unfused heteropolycyclic compounds |
GB0308466D0 (en) * | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
AU2005316312B2 (en) * | 2004-12-17 | 2009-10-22 | Amgen, Inc. | Aminopyrimidine compounds and methods of use |
-
2006
- 2006-10-23 TW TW095139053A patent/TW200800201A/zh unknown
- 2006-11-15 EP EP06850430A patent/EP1989200B1/en active Active
- 2006-11-15 PT PT06850430T patent/PT1989200E/pt unknown
- 2006-11-15 KR KR1020087011830A patent/KR100990771B1/ko not_active IP Right Cessation
- 2006-11-15 US US12/093,024 patent/US7547691B2/en not_active Expired - Fee Related
- 2006-11-15 DE DE602006008187T patent/DE602006008187D1/de active Active
- 2006-11-15 SI SI200630446T patent/SI1989200T1/sl unknown
- 2006-11-15 AT AT06850430T patent/ATE437873T1/de active
- 2006-11-15 AU AU2006337626A patent/AU2006337626B2/en not_active Ceased
- 2006-11-15 CA CA002629336A patent/CA2629336A1/en not_active Abandoned
- 2006-11-15 PL PL06850430T patent/PL1989200T3/pl unknown
- 2006-11-15 BR BRPI0618245-3A patent/BRPI0618245A2/pt not_active IP Right Cessation
- 2006-11-15 CN CN2006800428126A patent/CN101309918B/zh not_active Expired - Fee Related
- 2006-11-15 EA EA200801362A patent/EA014426B1/ru not_active IP Right Cessation
- 2006-11-15 JP JP2008541463A patent/JP2009516697A/ja not_active Ceased
- 2006-11-15 WO PCT/US2006/060911 patent/WO2007092095A2/en active Application Filing
- 2006-11-15 PE PE2006001456A patent/PE20070833A1/es not_active Application Discontinuation
- 2006-11-15 DK DK06850430T patent/DK1989200T3/da active
- 2006-11-15 ES ES06850430T patent/ES2329085T3/es active Active
- 2006-11-17 AR ARP060105065A patent/AR057911A1/es unknown
-
2008
- 2008-03-27 IL IL190489A patent/IL190489A0/en unknown
- 2008-04-29 CR CR9947A patent/CR9947A/es not_active Application Discontinuation
- 2008-05-08 ZA ZA200803940A patent/ZA200803940B/xx unknown
- 2008-05-16 TN TNP2008000227A patent/TNSN08227A1/en unknown
- 2008-05-16 EC EC2008008456A patent/ECSP088456A/es unknown
- 2008-06-10 NO NO20082594A patent/NO20082594L/no not_active Application Discontinuation
- 2008-06-13 MA MA31035A patent/MA30053B1/fr unknown
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