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AR071072A1 - Inhibidores de desacetilasas b a base de hidroxamato - Google Patents

Inhibidores de desacetilasas b a base de hidroxamato

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Publication number
AR071072A1
AR071072A1 ARP090101062A ARP090101062A AR071072A1 AR 071072 A1 AR071072 A1 AR 071072A1 AR P090101062 A ARP090101062 A AR P090101062A AR P090101062 A ARP090101062 A AR P090101062A AR 071072 A1 AR071072 A1 AR 071072A1
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AR
Argentina
Prior art keywords
alkyl
group
alkynyl
divalent
alkenyl
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ARP090101062A
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English (en)
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Novartis Ag
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40591831&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR071072(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR071072A1 publication Critical patent/AR071072A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
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    • 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
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

También proporcionan métodos para preparar los compuestos de la formula 1 y métodos para utilizar compuestos de la formula 1 para el tratamiento, inhibicion, o prevencion de condiciones o trastornos patologicos transmitidos en su totalidad o en parte por desacetilasas. Reivindicacion 1: Un compuesto de la formula 1 o una sal farmacéuticamente aceptable, hidrato éster del mismo, donde: ---- es a) un enlace simple o b) un enlace doble; Y y Z son independientemente a) -L-, b) -L-O-L-, c) -L-S(O)m-L, o d) L-NR4-L; L, en cada surgimiento, es a) un grupo alquilo C1-10 divalente, b) alquenilo C1-10 divalente, c) alquinilo C2-10 divalente, o d) un enlace covalente, en donde cada uno de a)-c) es opcionalmente sustituido con 1 a 4 L'-R5; R1 es a) H, b) alquilo C1-10, c) alquinilo C2-10, e) cicloalquilo C3-14, f) arilo C61-4, g) un grupo cicloheteroalquilo de 3 a 14 miembros, o h) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno de b) a h) es sustituido opcionalmente con 1 a 4 grupos -L'-R5; R2 y R3 son independientemente a) H, b) halogeno, c) - NO2, d) -CN, e) un grupo alquilo C1-10, f) alquenilo C2-10, g) alquinilo C2-10, h) cicloalquilo C3-14, i) arilo C61-6, j) un grupo cicloheteroalquilo de 3 a 14 miembros, k) un grupo heteroarilo de 5 a 14 miembros, l) alcoxi C1-10, m) un grupo -N-alquilo C1-10, n) C(O)alquilo C1-10, y o) C(O)Oalquilo C1-10, en donde cada uno de e) a o) es sustituido opcionalmente con 1 a 4 grupos -L'-R7;R4 es a) H, b) -C(O)OR6, o c) alquilo C1-10; R5 en cada surgimiento, es a) halogeno, b) -CN, c) -NO2, d) oxo, e) -N-L'-R6, f) -O-L'-R6, g) -S(O)mR7, h) un grupo alquilo C1-10, i) alquenilo C2-10, j) alquinilo C2-10, k) cicloalquilo C3-14, l) arilo C61-4, m) un grupo cicloheteroalquilo de 3 a 14 miembros, o n) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno de h) a n) es opcionalmente sustituido con 1 a 4 grupos -L'-R10; R6, en cada surgimiento, es a) H, b) -OR8, c) S(O)mR8, o d) un grupo alquilo C1-10 opcionalmente sustituido con 1 a 4 grupos -L'-R10; R7 es a) H, b), -OR8, c) -NR8R9, d) alquilo C1-10, e) alquenilo C2-10, f) alquinilo C2-10, g) cicloalquilo C3-14, h) arilo C6-14, i) un grupo cicloheteroalquilo de 3 a 14 miembros, o j) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno de d) a j) es sustituido opcionalmente con de 1 a 4 grupos -L'-R10; R8 y R9, en cada surgimiento, son independientemente a) H, b) alquilo C1-10, c) alquenilo C2-10, d) alquinilo C2-10, e) cicloalquilo C3-14, f) arilo C6-14, g) un grupo cicloheteroalquilo de 3 a 14 miembros, o h) un grupo heteroarilo de 5 a 14 miembros, en donde cada uno de b) a h) es sustituido opcionalmente con de 1 a 4 grupos -L'-R10; R10 en cada surgimiento, a) halogeno, b) -CN, c) -NO2, d) oxo, e) -OH, f) -NH2, g) -NHalquil C1-10, h) -N(alquil C1-10)2, i) -CHO, j) -C(O)-alquilo C1-10, k) -C(O)OH, l) -C(O)-Oalquil C1-10, m), -C(O)SH, n) -C(O)Salquilo C1-10, o) -C(O)NH2, p) - C(O)Nhalquil C1-10, q) -C(O)Nalquil C1-10, r) -C(S)H, s) -C(S)-alquilo C1-10, t) -C(S)NH2, u) -C(S)NHalquil C1-10, v) - C(S)N alquil C1-10, w) -C(NH)H, x) -C(NH)alquilo C1-10, y) -C(NH)NH2, z) -C(NH)NHalquil C1-10, aa) -C(NH)N(alquil C1-10)2, ab) -C(Nalquil C1-10)H, ac) -C(Nalquil C1-10)-alquilo C1-10, ad) -C(Nalquil C1-10)NHalquil C1-10, ae) -C(Nalquil C1-10)N(alquil C1-10), af) -S(O)mH, ag) S(O)m-alquil C1-10, ah) -S(O)2OH, ai) S(O)m-Oalquilo C1-10, aj) -S(O)mNH2, ak) -S(O)mNH(alquil C1-10), al) S(O)mN(alquil C1-10)2, am) -Si(alquil C1-10), an) un grupo alquilo C1-10, ao) alquenilo C2-10, ap) alquinilo C2-10, aq) alcoxi C1-10, ar) haloalquilo C1-10, as) cicloalquilo C3-14, at) arilo C61-4, au) un grupo cicloheteroalquilo de 3 a 14 miembros, o ay) un grupo heteroarilo de 5 a 14 miembros; L', en cada surgimiento, es a) un grupo alquilo C1-10 divalente, b) alquenilo C2-10 divalente, c) alquinilo C2-10 divalente, d) haloalquilo C1-10 divalente, d) alcoxi C1-10divalente, o f) un enlace covalente; y m, en cada surgimiento, es 0, 1 o 2.
ARP090101062A 2008-03-26 2009-03-25 Inhibidores de desacetilasas b a base de hidroxamato AR071072A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3967408P 2008-03-26 2008-03-26

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AR071072A1 true AR071072A1 (es) 2010-05-26

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US (2) US7943652B2 (es)
EP (2) EP2628726A1 (es)
JP (1) JP5330498B2 (es)
KR (1) KR101252349B1 (es)
CN (1) CN102036955B (es)
AR (1) AR071072A1 (es)
AU (1) AU2009228778B2 (es)
BR (1) BRPI0909159A2 (es)
CA (1) CA2719477C (es)
CL (1) CL2009000727A1 (es)
CO (1) CO6531501A2 (es)
CR (1) CR11680A (es)
DO (1) DOP2010000283A (es)
EA (1) EA019033B1 (es)
EC (1) ECSP10010497A (es)
ES (1) ES2519474T3 (es)
GE (1) GEP20125708B (es)
IL (1) IL208212A0 (es)
MA (1) MA32240B1 (es)
MX (1) MX2010010502A (es)
MY (1) MY150437A (es)
NI (1) NI201000157A (es)
NZ (1) NZ588069A (es)
PA (1) PA8821301A1 (es)
PE (1) PE20091736A1 (es)
PL (1) PL2260020T3 (es)
PT (1) PT2260020E (es)
SM (1) SMP201000116B (es)
SV (1) SV2010003677A (es)
TW (1) TWI510467B (es)
UY (1) UY31738A (es)
WO (1) WO2009118305A1 (es)
ZA (1) ZA201006474B (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2451790A4 (en) * 2009-07-07 2012-12-26 Anthem Biosciences Private Ltd INHIBITORS OF HISTONE DEACETYLASE
US8877795B2 (en) 2010-05-07 2014-11-04 The Board Of Trustees Of The Leland Stanford Junior University Identification of stabilizers of multimeric proteins
CA2862259A1 (en) * 2011-12-29 2013-07-04 Pharmacyclics, Inc. Cinnamic acid hydroxyamides as inhibitors of histone deacetylase 8
FR2992317B1 (fr) 2012-06-22 2016-05-13 Diverchim Procede de preparation de peptides chiraux
JP6543342B2 (ja) 2014-08-14 2019-07-10 アルハマドシャー，マモウン，エム． 血清半減期を延長するための、調節可能リンカーを介した薬学的活性剤とトランスサイレチンリガンドのコンジュゲーション
CN104910074B (zh) * 2015-03-11 2017-07-14 常州大学 一类含有羟肟酸基团的吡唑类衍生物及其制备方法及用途
EA201792028A1 (ru) 2015-03-13 2018-04-30 Форма Терапьютикс, Инк. Альфа-цинамидные соединения и композиции как ингибиторы hdac8
CN106854189A (zh) * 2015-12-08 2017-06-16 湖南华腾制药有限公司 一种哌嗪化合物的合成方法
US20170273307A1 (en) * 2016-03-28 2017-09-28 Trent University Silane-based antimicrobial coatings and methods of making and using the same
IL298196A (en) 2017-02-17 2023-01-01 Eidos Therapeutics Inc Processes for preparing ag-10, its intermediates, and salts thereof
KR20200135996A (ko) 2018-03-23 2020-12-04 에이도스 테라퓨틱스, 인코포레이티드 Ag10을 사용하여 ttr 아밀로이드증을 치료하는 방법
MA53238A (fr) 2018-08-17 2022-04-13 Eidos Therapeutics Inc Formules d'ag10
CN113956182B (zh) * 2021-10-11 2023-11-17 杭州师范大学 Hdac/mao-b双重抑制剂及其制备和应用
US20250059184A1 (en) * 2021-12-15 2025-02-20 Delix Therapeutics, Inc. Imidazopyridine psychoplastogens and uses thereof

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
LU88769I2 (fr) 1982-07-23 1996-11-05 Zeneca Ltd Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R))
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
US5395855A (en) 1990-05-07 1995-03-07 Ciba-Geigy Corporation Hydrazones
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
ATE348110T1 (de) 1992-10-28 2007-01-15 Genentech Inc Hvegf rezeptor als vegf antagonist
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
ATE205483T1 (de) 1995-03-30 2001-09-15 Pfizer Chinazolinderivate
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
JP4146514B2 (ja) 1995-07-06 2008-09-10 ノバルティス アクチエンゲゼルシャフト ピロロピリミジン類およびその製造方法
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
ES2174250T5 (es) 1996-04-12 2010-04-21 Warner-Lambert Company Llc Inhibidores irreversibles de tirosina quinasas.
AU2912997A (en) 1996-06-24 1998-01-14 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
WO1998008849A1 (de) 1996-08-30 1998-03-05 Novartis Aktiengesellschaft Verfahren zur herstellung von epothilonen und zwischenprodukte innerhalb des verfahrens
CA2264908C (en) 1996-09-06 2006-04-25 Obducat Ab Method for anisotropic etching of structures in conducting materials
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
WO1998010767A2 (en) 1996-09-13 1998-03-19 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
PL193229B1 (pl) 1996-11-18 2007-01-31 F Biotechnologische Forschung Epotylon C, epotylon D, epotylon E i epotylon F, sposób biotransformacji epotylonu A, sposób biotransformacji epotylonu B oraz środek leczniczy
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
MXPA00008365A (es) 1998-02-25 2002-11-07 Sloan Kettering Inst Cancer Sintesis de epotilonas, intermediarios y analogos de las mismas.
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
EP1135470A2 (en) 1998-11-20 2001-09-26 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
DE69926536T3 (de) 1998-12-22 2013-09-12 Genentech, Inc. Antagonisten von vaskular-endothelialen zellwachstumsfaktoren und ihre anwendung
CA2366857C (en) 1999-03-30 2010-12-14 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
CA2369308A1 (en) * 1999-06-30 2001-01-04 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitor compounds
PE20020354A1 (es) * 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
AU2002306848A1 (en) * 2001-03-23 2002-10-08 Elan Pharmaceuticals, Inc. Methods of treating alzheimer's disease with piperidin derivates
AR035885A1 (es) 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
US20040091951A1 (en) * 2002-02-07 2004-05-13 Axys Pharmaceuticals, Inc. Assay for measuring acetylation or deacetylation activity of an enzyme
US7135493B2 (en) * 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
CN1764648A (zh) * 2003-01-13 2006-04-26 安斯泰来制药有限公司 作为组蛋白脱乙酰酶(hdac)抑制剂的异羟肟酸衍生物
JP2004345953A (ja) 2003-01-16 2004-12-09 Hiroki Koma 抗菌活性を有する新規な第四級アンモニウム塩化合物およびその製造方法
JP2007501775A (ja) 2003-08-07 2007-02-01 ノバルティス アクチエンゲゼルシャフト 免疫抑制剤としてのヒストンデアセチラーゼ阻害剤
EP1653973A1 (en) 2003-08-08 2006-05-10 Novartis AG Combinations comprising staurosporines
WO2007030454A2 (en) 2005-09-07 2007-03-15 Novartis Ag Mutations and polymorphisms of hdac9
WO2007030455A2 (en) 2005-09-07 2007-03-15 Novartis Ag Mutations and polymorphisms of hdac10
ATE554084T1 (de) * 2006-02-07 2012-05-15 Astellas Pharma Inc N-hydroxyacrylamidverbindungen
US7783564B2 (en) 2006-07-25 2010-08-24 Visa U.S.A. Inc. Compliance control in a card based program
WO2008070011A2 (en) 2006-12-04 2008-06-12 Novartis Ag Combination of an hdac inhibitor and an antimetabolite
US20100179208A1 (en) 2007-05-30 2010-07-15 Novartis Ag Use of HDAC Inhibitors for the Treatment of Bone Destruction

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CR11680A (es) 2010-11-23
US20090247547A1 (en) 2009-10-01
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