[go: up one dir, main page]

AR057579A1 - Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) - Google Patents

Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)

Info

Publication number
AR057579A1
AR057579A1 ARP060104989A ARP060104989A AR057579A1 AR 057579 A1 AR057579 A1 AR 057579A1 AR P060104989 A ARP060104989 A AR P060104989A AR P060104989 A ARP060104989 A AR P060104989A AR 057579 A1 AR057579 A1 AR 057579A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
substituted
independently selected
unsubstituted
Prior art date
Application number
ARP060104989A
Other languages
English (en)
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR057579A1 publication Critical patent/AR057579A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Se refiere a una clase de compuestos espirocíclicos sustituidos. Estos compuestos pueden inhibir la histona deacetilasa y son adecuadas para su uso en la induccion de forma selectiva de la diferenciacion terminal y de la detencion del crecimiento celular y/o apoptosis de células neoplásicas, inhibiendo de este modo la proliferacion de dichas células. De esta manera, los compuestos de la presente son utiles para tratar a un paciente que tiene un tumor caracterizado por la proliferacion de células neoplásicas. Los compuestos de la presente también pueden ser utiles en la prevencion y tratamiento de enfermedades mediadas por TRX, tales como enfermedades autoinmunes, alérgicas e inflamatorias, y en la prevencion y/o tratamiento de enfermedades del sistema nervioso central (SNC), tales como enfermedades neurodegenerativas. La presente también proporciona composiciones farmacéuticas que comprenden los compuestos de la presente y regímenes de dosificacion seguros de estas composiciones farmacéuticas, que son fáciles de seguir, y que dan como resultado una cantidad terapéuticamente eficaz de estos compuestos in vivo. Reivindicacion 1: Un compuesto, representado por la formula (1), en la que: A, B y D se seleccionan independientemente entre CR12; NR1a, C(O) y O; E se selecciona entre un enlace, CR12, NR1a, C(O) y O; donde al menos uno de A, B, D o E es CR12; y con la condicion de que cuando A es O, entonces E no es O; ôla línea de puntosö es un doble enlace opcional; ôel círculo Wö es un arilo o heteroarilo, opcionalmente sustituido con 1 a 3 sustituyentes seleccionados entre R7; ôel círculo Zö es un arilo o heteroarilo; R1 se selecciona independientemente entre hidrogeno, alquilo C1-6, (CR62)nR10, (CR62)nC(O)R4, (CR62)nC(O)OR4, (CR62)nC(O)R52, (CR62)nS(O)R4, (CR62)nOH y halo; R1a se selecciona independientemente entre hidrogeno, alquilo C1-6, (CR62)nR10, (CR62)nC(O)R4, (CR62)nC(O)OR4, (CR62)nC(O)NR52 o (CR62)nS(O)2R4; L1 se selecciona entre un enlace, -CR112-, -C(O)NR5-, -NR5C(O)- y -C(O)-; R3 se selecciona entre H, alquilo C1-6 sin sustituir o sustituido, arilo sin sustituir o sustituido, heteroarilo sin sustituir o sustituido, halo, CN, amida, carboxilo, alcoxi C1-7, haloalquilo C1- 7, haloalquiloxi C1-7, hidroxialquilo C1-7, alquenilo C1-7, alquinilo C1-7, alquilC1-7-C(=O)O-, alquilC1-7-C(=O)-, hidroxialcoxi, -NHSO2, -SO2NH, alquilC1-7-NHSO2-, alquilC1-7-SO2NH-, alquiloC1-7-sulfonilo, alquilC1-7-amino, dialquilC1-7-amino, y L2- R12; R4 se selecciona independientemente entre H, alquilo C1-6, arilo, y heterociclilo, donde alquilo, arilo o heterociclilo puede estar opcionalmente sustituido; R5 se selecciona independientemente entre hidrogeno, alquilo C1-6, y arilo, que pueden estar opcionalmente sustituidos con 1 a3 sustituyentes seleccionados entre alquilo C1-6, arilo, heteroarilo o halo; R6 se selecciona independientemente entre hidrogeno, alquilo C1-6, arilo, OR11, halo, y NR11; donde el alquilo o arilo puede estar opcionalmente sustituido con 1 a 3 sustituyentes seleccionados entre alquilo C1-6, arilo, heteroarilo o halo; R7 se selecciona independientemente entre hidrogeno, OH, NR112, nitro, CN, amida, carboxilo, alcoxi C1-7, alquilo C1-7, haloalquilo C1-7, haloalquiloxi C1-7, hidroxialquilo C1-7, alquenilo C1-7, alquilC1-7-C(=O)O-, alquilC1-7-C(=O)-, alquinilo C1-7, grupo halo, amida, hidroxialcoxi, -NR11SO2, -SO2NR11, alquilC1-7-NR11SO2-, alquilC1-7-SO2NR11-, alquilC1-7-sulfonilo, alquilC1-7-amino y dialquilC1-7-amino; R10 se selecciona independientemente entre arilo, y heterociclilo, que pueden estar opcionalmente sustituidos; R11 se selecciona independientemente entre hidrogeno, alquilo C1-6 sin sustituir o sustituido, y arilo sin sustituir o sustituido; L2 se selecciona entre un enlace, alquileno C1-4, alquinilo C1-4, alquenilo C1-4, -O-, -S-, -NH-, -C(=O)NH-, -NHC(=O)-, -NHC(=O)NH-, -SO2NH-, -NHSO2-, -SO2-, -C(=O)- y -C(=O)O-; R12 se selecciona entre: heteroarilo sustituido o sin sustituir, heterociclilo sustituido o sin sustituir, arilo sustituido o sin sustituir, y cicloalquilo C3-8 sustituido o sin sustituir; m es 0, 1 o 2; n se selecciona independientemente entre 0, 1, 2, 3 y 4; p es 0, 1 o 2, con la condicion de que la suma de las variables m y p no sea mayor de 2; q es 1, 2, 3, o 4; o un estereoisomeros o una sal farmacéuticamente aceptable del mismo.
ARP060104989A 2005-11-23 2006-11-14 Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) AR057579A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US73932405P 2005-11-23 2005-11-23

Publications (1)

Publication Number Publication Date
AR057579A1 true AR057579A1 (es) 2007-12-05

Family

ID=37811669

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060104989A AR057579A1 (es) 2005-11-23 2006-11-14 Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)

Country Status (17)

Country Link
US (4) US7544695B2 (es)
EP (1) EP1954698B1 (es)
JP (1) JP4921485B2 (es)
KR (1) KR20080069630A (es)
CN (1) CN101312976A (es)
AR (1) AR057579A1 (es)
AT (1) ATE434618T1 (es)
AU (1) AU2006318773B2 (es)
BR (1) BRPI0618904A2 (es)
CA (1) CA2629777C (es)
DE (1) DE602006007482D1 (es)
DO (1) DOP2006000260A (es)
NO (1) NO20082823L (es)
PE (1) PE20071084A1 (es)
RU (1) RU2008125068A (es)
TW (1) TW200804381A (es)
WO (2) WO2007061978A1 (es)

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
JP2008536924A (ja) 2005-04-20 2008-09-11 メルク エンド カムパニー インコーポレーテッド ベンゾチオフェンヒドロキサミン酸のカーバメート、ウレア、アミドおよびスルホンアミド置換誘導体
EP1874755A4 (en) 2005-04-20 2010-04-28 Merck Sharp & Dohme BENZOTHIOPHENE-hydroxamic acid derivatives
EP1896395B1 (en) 2005-06-24 2015-07-15 Merck Sharp & Dohme Corp. Modified malonate derivatives
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
US20070213311A1 (en) * 2006-03-02 2007-09-13 Yun-Long Li Modulators of 11-beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
US20070208001A1 (en) * 2006-03-03 2007-09-06 Jincong Zhuo Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same
CN101466670B (zh) * 2006-04-07 2013-04-17 梅特希尔基因公司 组蛋白脱乙酰酶抑制剂
US20080247964A1 (en) * 2006-05-08 2008-10-09 Yuelian Xu Substituted azaspiro derivatives
US8119652B2 (en) * 2006-05-18 2012-02-21 Merck Sharp & Dohme Corp. Aryl-fused spirocyclic compounds
US8030344B2 (en) 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
CL2008001839A1 (es) 2007-06-21 2009-01-16 Incyte Holdings Corp Compuestos derivados de 2,7-diazaespirociclos, inhibidores de 11-beta hidroxil esteroide deshidrogenasa tipo 1; composicion farmaceutica que comprende a dichos compuestos; utiles para tratar la obesidad, diabetes, intolerancia a la glucosa, diabetes tipo ii, entre otras enfermedades.
FR2920774B1 (fr) * 2007-09-06 2009-10-30 Galderma Res & Dev Nouveaux derives de n-phenul acatamide, inhibiteurs de l'enzyme soat-1, compositions pharmaceutiques et cosmetiques les contentant
US9745278B2 (en) 2007-09-10 2017-08-29 Boston Biomedical, Inc. Group of STAT3 pathway inhibitors and cancer stem cell pathway inhibitors
WO2009037542A2 (en) * 2007-09-20 2009-03-26 Glenmark Pharmaceuticals, S.A. Spirocyclic compounds as stearoyl coa desaturase inhibitors
WO2009039431A2 (en) * 2007-09-21 2009-03-26 Neurogen Corporation Substituted aryl-fused spirocyclic amines
US8614324B2 (en) * 2008-10-31 2013-12-24 Pain Therapeutics, Inc. Filamin A binding anti-inflammatory and analgesic
US8653068B2 (en) * 2009-10-30 2014-02-18 Pain Therapeutics, Inc. Filamin A binding anti-inflammatory and analgesic
US9340558B2 (en) 2007-11-02 2016-05-17 Pain Therapeutics Inc. Filamin a binding anti-inflammatory and analgesic
EP2708559B1 (en) 2008-04-11 2018-03-28 Chugai Seiyaku Kabushiki Kaisha Antigen-binding molecule capable of binding to two or more antigen molecules repeatedly
EP2110377A1 (en) * 2008-04-15 2009-10-21 DAC S.r.l. Spirocyclic derivatives as histone deacetylase inhibitors
EP2311840A1 (en) 2009-10-13 2011-04-20 DAC S.r.l. Spirocyclic derivatives as histone deacetylase inhibitors
NZ591896A (en) 2008-08-29 2013-03-28 Treventis Corp Compositions and methods of treating amyloid disease
WO2010028192A1 (en) 2008-09-03 2010-03-11 Repligen Corporation Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors
EP2488177B1 (en) * 2008-10-31 2016-10-12 Pain Therapeutics, Inc. Filamin a binding anti-inflammatory and analgesic
US8580808B2 (en) * 2009-10-30 2013-11-12 Pain Therapeutic, Inc. Filamin A-binding anti-inflammatory analgesic
CN101397295B (zh) * 2008-11-12 2012-04-25 深圳微芯生物科技有限责任公司 作为组蛋白去乙酰化酶抑制剂的2-吲哚满酮衍生物、其制法和用途
WO2010141817A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
WO2010143803A2 (en) * 2009-06-08 2010-12-16 Industry Foundation Of Chonnam National University New nicotinamide derivatives with anti-androgen effects, processes of preparing, and antiandrogens comprising the same
US8580809B2 (en) * 2009-10-30 2013-11-12 Pain Therapeutics, Inc. Filamin A-binding anti-inflammatory analgesic
WO2011140425A1 (en) 2010-05-06 2011-11-10 Vertex Pharmaceuticals Incorporated Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels
PT2670752E (pt) 2011-02-02 2016-06-14 Vertex Pharma Piperidinamidas pirrolopirazina-espirocíclicas como moduladores de canais iónicos
CA2827311A1 (en) 2011-02-18 2012-08-23 Vertex Pharmaceuticals Incorporated Chroman-spirocyclic piperidine amides as modulators of ion channels
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
JP6250403B2 (ja) 2011-02-28 2017-12-20 バイオマリン ファーマシューティカル インク ヒストン脱アセチル化酵素阻害剤
CA2829803A1 (en) 2011-03-14 2012-09-20 Vertex Pharmaceuticals Incorporated Morpholine-spirocyclic piperidine amides as modulators of ion channels
WO2012122969A1 (de) 2011-03-16 2012-09-20 Creative Therapeutics Gmbh Substituierte diphenylderivate
CN103492371B (zh) * 2011-03-18 2015-11-25 山东亨利医药科技有限责任公司 含有螺环的二氢吡唑类化合物
EP2557075A1 (de) 2011-08-09 2013-02-13 Trin Therapeutics GmbH Neue Triazenverbindungen zur Behandlung von Krebs
RU2014116229A (ru) 2011-09-23 2015-10-27 Даблхил Гмбх Новые соединения изоцианата и изотиоцианата для лечения злокачественных новообразований
WO2014012054A1 (en) 2012-07-13 2014-01-16 Pain Therapeutics, Inc. Alzheimer's disease assay in a living patent
DK2882428T3 (en) 2012-07-13 2019-04-15 Pain Therapeutics Inc PROCEDURE TO INHIBIT TAU PHOSPHORIZATION
US9346802B2 (en) 2013-03-15 2016-05-24 Epizyme, Inc. CARM1 inhibitors and uses thereof
EP2970219B1 (en) 2013-03-15 2019-02-27 Epizyme, Inc. Carm1 inhibitors and uses thereof
WO2014143666A1 (en) 2013-03-15 2014-09-18 Biomarin Pharmaceutical Inc. Hdac inhibitors
WO2014144455A1 (en) 2013-03-15 2014-09-18 Epizyme, Inc. 1 -phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
HK1220155A1 (zh) 2013-04-09 2017-04-28 Boston Biomedical, Inc. 治疗癌症的方法
UA119247C2 (uk) 2013-09-06 2019-05-27 РОЙВЕНТ САЙЕНСИЗ ҐмбГ Спіроциклічні сполуки як інгібітори триптофангідроксилази
US9433604B2 (en) 2013-10-08 2016-09-06 Pain Therapeutics Inc. Method for inhibiting growth of cancer cells
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
US9636298B2 (en) 2014-01-17 2017-05-02 Methylgene Inc. Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
JP6643545B2 (ja) * 2014-03-14 2020-02-12 ラクオリア創薬株式会社 Ｔｒｐｍ８拮抗剤としてのアザスピロ誘導体
TW201607923A (zh) 2014-07-15 2016-03-01 歌林達有限公司 被取代之氮螺環（４．５）癸烷衍生物
US10214520B2 (en) 2014-07-15 2019-02-26 Gruenenthal Gmbh Substituted azaspiro(4.5)decane derivatives
EP3194398A4 (en) * 2014-09-17 2018-02-21 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of a co-activator-associated arginine methyltransferase 1 (carm1) inhibitor
SG11201704759QA (en) 2014-12-12 2017-07-28 Regenacy Pharmaceuticals Llc Piperidine derivatives as hdac1/2 inhibitors
CA2963760A1 (en) 2014-12-19 2016-06-23 Yoshinao Ruike Anti-myostatin antibodies, polypeptides containing variant fc regions, and methods of use
CN114057765A (zh) 2015-02-02 2022-02-18 瓦洛健康股份有限公司 作为hdac抑制剂的3-芳基-4-酰氨基-二环[4,5,0]异羟肟酸
AR103598A1 (es) 2015-02-02 2017-05-24 Forma Therapeutics Inc Ácidos bicíclicos[4,6,0]hidroxámicos como inhibidores de hdac
EP3932914A1 (en) 2015-03-13 2022-01-05 Valo Health, Inc. Alpha-cinnamide compounds and compositions as hdac8 inhibitors
BR112017021194A2 (pt) * 2015-04-03 2019-01-08 Kalyra Pharmaceuticals Inc compostos espirocíclicos
BR112017028139A2 (pt) * 2015-07-02 2018-08-28 Biomarin Pharmaceutical Inc. inibidores de histona desacetilase
EP3317279B1 (en) * 2015-07-03 2021-01-27 H. Hoffnabb-La Roche Ag Triaza-spirodecanones as ddr1 inhibitors
JP6936796B2 (ja) 2015-07-06 2021-09-22 ロダン・セラピューティクス，インコーポレーテッド ヒストンデアセチラーゼのヘテロハロ阻害剤
WO2017007755A1 (en) 2015-07-06 2017-01-12 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
WO2017161028A1 (en) 2016-03-16 2017-09-21 Kura Oncology, Inc. Substituted inhibitors of menin-mll and methods of use
CN105601617B (zh) * 2016-03-24 2019-02-22 山东省科学院生物研究所 一种邻二氮杂环化合物及其制备方法与应用
US10555935B2 (en) 2016-06-17 2020-02-11 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as HDAC inhibitors
TWI831965B (zh) 2016-08-05 2024-02-11 日商中外製藥股份有限公司 Il-8相關疾病之治療用或預防用組成物
CN106397575A (zh) * 2016-10-20 2017-02-15 上海懿贝瑞生物医药科技有限公司 一种具有胞外组蛋白毒性抑制作用的多肽制备方法及用途
US11299469B2 (en) 2016-11-29 2022-04-12 Sumitomo Dainippon Pharma Oncology, Inc. Naphthofuran derivatives, preparation, and methods of use thereof
TW201829381A (zh) * 2016-12-22 2018-08-16 美商拜奧馬林製藥公司 組蛋白脫乙醯基酶抑制劑
AU2018207402B2 (en) 2017-01-11 2023-09-28 Alkermes, Inc. Bicyclic inhibitors of histone deacetylase
JP2020520923A (ja) 2017-05-17 2020-07-16 ボストン バイオメディカル， インコーポレイテッド がんを処置するための方法
WO2019032528A1 (en) 2017-08-07 2019-02-14 Rodin Therapeutics, Inc BICYCLIC HISTONE DEACETYLASE INHIBITORS
EP3684361A4 (en) * 2017-09-20 2021-09-08 Kura Oncology, Inc. SUBSTITUTED INHIBITORS OF MENIN-MLL AND METHOD OF USING
CN110156674A (zh) * 2018-02-13 2019-08-23 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的螺环化合物
CN112312904B (zh) * 2018-04-16 2025-01-07 C4医药公司 螺环化合物
TWI731420B (zh) * 2018-09-27 2021-06-21 大陸商深圳微芯生物科技股份有限公司 具有吲哚胺-2,3-雙加氧酶抑制活性的喹啉衍生物及其製備方法、藥物組合物、聯合用藥物與用途
US20210403479A1 (en) * 2018-11-08 2021-12-30 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase useful for the treatment or prevention of hiv infection
PE20240050A1 (es) 2021-01-29 2024-01-09 Cedilla Therapeutics Inc Inhibidores de cdk2 y metodos de uso de los mismos
EP4358954A4 (en) 2021-06-26 2025-09-03 Cedilla Therapeutics Inc CDK2 INHIBITORS AND METHODS OF USE THEREOF
EP4422621A4 (en) * 2021-10-27 2025-08-27 Merck Sharp & Dohme Llc SPIROTRICYCLIC RIPK1 INHIBITORS AND METHODS OF USE THEREOF
CN116375717B (zh) * 2021-12-30 2025-10-28 成都先导药物开发股份有限公司 螺环化合物及其双功能化合物和用途

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5369108A (en) * 1991-10-04 1994-11-29 Sloan-Kettering Institute For Cancer Research Potent inducers of terminal differentiation and methods of use thereof
US5700811A (en) * 1991-10-04 1997-12-23 Sloan-Kettering Institute For Cancer Research Potent inducers of terminal differentiation and method of use thereof
SK45898A3 (en) * 1995-10-17 1999-01-11 Astra Pharma Prod Pharmaceutically active quinazoline compounds
US5833102A (en) * 1996-11-13 1998-11-10 Jacobson; Jeffery Thomas Portable vehicle-mounted support
JPH11335375A (ja) 1998-05-20 1999-12-07 Mitsui Chem Inc ヒストン脱アセチル化酵素阻害作用を有するベンズアミド誘導体
EA007649B1 (ru) * 1999-09-08 2006-12-29 Слоан-Кеттеринг Инститьют Фор Кэнсер Рисёч Ингибиторы гистондеацетилазы, вызывающие дифференцировку клеток, и их применение
JP2003514777A (ja) 1999-10-27 2003-04-22 シーオーアール セラピューティクス インコーポレイテッド フィブリノゲン依存性血小板凝集の阻害剤としてのピリジル含有スピロ環化合物
PT1233958E (pt) 1999-11-23 2011-09-20 Methylgene Inc Inibidores de histona desacetilase
CZ20032531A3 (cs) 2001-03-19 2004-01-14 Ono Pharmaceutical Co., Ltd. Derivát triazaspiro[5.5]undekanu a farmaceutická kompozice obsahující tento derivát jako účinnou složku
US6784173B2 (en) * 2001-06-15 2004-08-31 Hoffmann-La Roche Inc. Aromatic dicarboxylic acid derivatives
WO2003024448A2 (en) 2001-09-14 2003-03-27 Methylgene, Inc. Inhibitors of histone deacetylase
US7868204B2 (en) * 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
CN100503599C (zh) * 2002-03-13 2009-06-24 詹森药业有限公司 作为组蛋白脱乙酰酶的新颖抑制剂的羰基氨基衍生物
KR20040090978A (ko) 2002-03-13 2004-10-27 얀센 파마슈티카 엔.브이. 히스톤 디아세틸라제의 신규한 저해제로서의 설포닐-유도체
AU2003218736B2 (en) 2002-03-13 2009-01-08 Janssen Pharmaceutica N.V. New inhibitors of histone deacetylase
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
PL376154A1 (en) 2002-09-18 2005-12-27 Ono Pharmaceutical Co, Ltd. Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient
EP1738752A1 (en) 2002-12-27 2007-01-03 Schering Aktiengesellschaft Pharmaceutical combinations comprising cis-retine acid
WO2005030704A1 (en) 2003-09-24 2005-04-07 Methylgene, Inc. Inhibitors of histone deacetylase
IN2003CH00929A (es) * 2003-11-13 2008-10-06
JP5319113B2 (ja) 2004-03-26 2013-10-16 メチルジーン インコーポレイテッド ヒストンデアセチラーゼの阻害剤
US7345043B2 (en) * 2004-04-01 2008-03-18 Miikana Therapeutics Inhibitors of histone deacetylase
AR057579A1 (es) * 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)

Also Published As

Publication number Publication date
WO2007061880A1 (en) 2007-05-31
WO2007061978A1 (en) 2007-05-31
US7834026B2 (en) 2010-11-16
DE602006007482D1 (de) 2009-08-06
TW200804381A (en) 2008-01-16
US20110098268A1 (en) 2011-04-28
US8349825B2 (en) 2013-01-08
ATE434618T1 (de) 2009-07-15
US20090209566A1 (en) 2009-08-20
US20070117824A1 (en) 2007-05-24
US8686020B2 (en) 2014-04-01
PE20071084A1 (es) 2008-01-10
US7544695B2 (en) 2009-06-09
JP2009516743A (ja) 2009-04-23
AU2006318773A1 (en) 2007-05-31
EP1954698A1 (en) 2008-08-13
AU2006318773B2 (en) 2012-03-22
JP4921485B2 (ja) 2012-04-25
US20130131041A1 (en) 2013-05-23
KR20080069630A (ko) 2008-07-28
RU2008125068A (ru) 2009-12-27
CA2629777C (en) 2011-08-16
CN101312976A (zh) 2008-11-26
DOP2006000260A (es) 2007-06-30
CA2629777A1 (en) 2007-05-31
NO20082823L (no) 2008-08-19
BRPI0618904A2 (pt) 2016-09-13
EP1954698B1 (en) 2009-06-24

Similar Documents

Publication Publication Date Title
AR057579A1 (es) Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
ECSP088762A (es) Tratamiento del dolor
AR126076A1 (es) Compuestos de benzotia(di)azepina y su uso como moduladores del ácido biliar
WO2007136605A3 (en) Aryl-fused spirocyclic compounds
WO2007087129A8 (en) Fluorinated arylamide derivatives
WO2007087130A3 (en) Hydroxyalkylarylamide derivatives
WO2007100657A3 (en) Inhibitors of histone deacetylase
AR076706A1 (es) Derivados aminobutiricos sustituidos como inhibidores de neprilisina
AR085004A1 (es) Inhibidores selectivos de glicosidasas y usos de los mismos
WO2007127137A3 (en) Disubstituted aniline compounds
AR038814A1 (es) Compuestos de 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-ona y uso en la fabricacion de medicamentos
ECSP045073A (es) Nuevos derivados de piperazina
AR049399A1 (es) Difenilimidazopirimidina e -imidazol aminas como inhibidores de b-secretasa y metodo de obtencion de los mismos
AR088919A2 (es) Derivados de pirazol, composiciones que contienen dichos compuestos y uso
AR074775A1 (es) Compuestos aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10
AR070828A1 (es) Derivados de azetidina y ciclobutano como inhibidores de jak
PE20090648A1 (es) Compuestos para el tratamiento de la hepatitis c
WO2008010985A3 (en) Phosphorus derivatives as histone deacetylase inhibitors
EA201100750A1 (ru) Замещенные диоксопиперидинилфталимидные производные
ECSP088457A (es) Compuestos de benzamida útiles como inhibidores de la histona deacetilasa
EA200900615A1 (ru) Фенилпропионамидные соединения и их применение
AR064253A1 (es) Compuestos de biciclocarboxiamida sustituidos composiciones farmaceuticas y una combinacion que los incluye y su uso en fabaricacion de un medicamento para el tratamiento de enfermedades mediadas por la actividad del receptor vr1
AR082619A1 (es) Inhibidores del virus de la hepatitis c
WO2005053610A3 (en) Diamine and iminodiacetic acid hydroxamic acid derivatives
AR068466A1 (es) Cianoisoquinolina

Legal Events

Date Code Title Description
FA Abandonment or withdrawal