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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 medicamento

Info

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
Application number
ARP060105065A
Other languages
English (en)
Original Assignee
Lilly Co Eli
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR057911A1 publication Critical patent/AR057911A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pulmonology (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.
ARP060105065A 2005-11-18 2006-11-17 Compuestos de pirimidinil benzotiofeno formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento AR057911A1 (es)

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)

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UA95949C2 (ru) 2006-03-31 2011-09-26 Янссен Фармацевтика, Н.В. Бензоимидазол-2-илпиримидины и пиразины как модуляторы рецептора гистамина h4
US20080021217A1 (en) * 2006-07-20 2008-01-24 Allen Borchardt Heterocyclic inhibitors of rho kinase
US8063212B2 (en) 2006-12-21 2011-11-22 Eli Lilly And Company Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer
JP5166441B2 (ja) * 2006-12-21 2013-03-21 イーライ リリー アンド カンパニー 癌治療用イミダゾリジノニルアミノピリミジン化合物
PE20090216A1 (es) 2007-05-16 2009-02-28 Lilly Co Eli Compuestos triazolil aminopirimidina
KR101131254B1 (ko) 2007-05-16 2012-04-24 일라이 릴리 앤드 캄파니 트리아졸릴 아미노피리미딘 화합물
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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
EP2467137A1 (en) 2009-08-19 2012-06-27 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
EP2812324B1 (en) 2012-02-08 2021-09-01 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
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
CN116283877A (zh) 2016-07-29 2023-06-23 赛诺维信制药公司 化合物、组合物及其用途
AU2017301767A1 (en) 2016-07-29 2019-02-14 Pgi Drug Discovery Llc Compounds and compositions and uses thereof
WO2018140512A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
EP3573964A1 (en) * 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
EP3630745A2 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Covalent inhibitors of kras
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
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Also Published As

Publication number Publication date
PL1989200T3 (pl) 2009-12-31
BRPI0618245A2 (pt) 2011-08-23
EP1989200B1 (en) 2009-07-29
US20080306082A1 (en) 2008-12-11
MA30053B1 (fr) 2008-12-01
AU2006337626A1 (en) 2007-08-16
CA2629336A1 (en) 2007-08-16
KR100990771B1 (ko) 2010-10-29
DK1989200T3 (da) 2009-11-09
ZA200803940B (en) 2009-09-30
ATE437873T1 (de) 2009-08-15
KR20080059451A (ko) 2008-06-27
EA014426B1 (ru) 2010-12-30
ES2329085T3 (es) 2009-11-20
US7547691B2 (en) 2009-06-16
IL190489A0 (en) 2008-11-03
CR9947A (es) 2008-11-28
PE20070833A1 (es) 2007-08-27
PT1989200E (pt) 2009-10-12
TNSN08227A1 (en) 2009-10-30
SI1989200T1 (sl) 2009-12-31
EP1989200A2 (en) 2008-11-12
NO20082594L (no) 2008-06-10
AU2006337626A8 (en) 2008-06-19
JP2009516697A (ja) 2009-04-23
ECSP088456A (es) 2008-06-30
CN101309918B (zh) 2010-12-29
DE602006008187D1 (de) 2009-09-10
AU2006337626B2 (en) 2012-03-22
TW200800201A (en) 2008-01-01
EA200801362A1 (ru) 2009-02-27
CN101309918A (zh) 2008-11-19
WO2007092095A2 (en) 2007-08-16
WO2007092095A3 (en) 2007-11-08

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