AR058065A1 - Compuestos de carboxiamina y uso de los mismos.composiciones farmaceuticas. - Google Patents

Compuestos de carboxiamina y uso de los mismos.composiciones farmaceuticas.

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Publication number
AR058065A1
AR058065A1 ARP060104167A ARP060104167A AR058065A1 AR 058065 A1 AR058065 A1 AR 058065A1 AR P060104167 A ARP060104167 A AR P060104167A AR P060104167 A ARP060104167 A AR P060104167A AR 058065 A1 AR058065 A1 AR 058065A1
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AR
Argentina
Prior art keywords
substituted
lower alkyl
hetero
aryl
alkyl
Prior art date
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ARP060104167A
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English (en)
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Novartis Ag
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Publication of AR058065A1 publication Critical patent/AR058065A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/20Spiro-condensed ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems

Abstract

Composiciones farmacéuticas y uso de las mismas para el tratamiento de enfermedades dependientes de histona desacetilasa (HDAC). Reivindicacion 1: Un compuesto de la formula (1) en donde: R1 se selecciona de H, NH2, NHR6, SR6, SOR6, O y OR6; R2 y R3 se seleccionan independientemente de H, un alquilo C1-6 de cadena recta o ramificada, un alquilo o alquenilo C1-6R7 de cadena recta o ramificada, cualquiera de los cuales puede estar opcionalmente heterosustituido, y en donde por lo menos uno de R2 y R3 es un H; X se selecciona de un cicloalquilo C3-6, cicloalquenilo C3-6, arilo, heterocicloalquilo C3-6, heteroarilo C3-6, y un poliheterociclo, cualquiera de los cuales además puede estar heterosustituido, en donde ejemplos específicos de poliheterociclos se pueden seleccionar de las estructuras del grupo de formulas (2); R4 está presente en n ocurrencias, n es un entero de 0 a 4, y R4 es igual o diferente y se selecciona independientemente de H, alquilo inferior, hetero-sustituido alquilo inferior, alquilarilo, hetero-sustituido alquilarilo, alcoxi inferior, cicloalquilo C3-6, arilo, heterocicloalquilo C3-6, heteroarilo C3-6, N-(R13)2, S-R13, O-R13, o un arilo mezclado y un anillo poliheterociclo que no es arilo (tal como, por ejemplo, benzhidrilo o 9H-fluorenilo), cualquiera de los cuales además puede estar sustituido por R8; R5 está presente en p ocurrencias, p es un entero de 0 a 4, y R5 es igual o diferente y se selecciona independientemente de H, O, halogeno, alcoxi inferior, y un alquilo inferior de cadena recta o ramificada o hetero-sustituido alquilo inferior; R6 se selecciona de H y un alquilo inferior de cadena recta o ramificada; R7 se selecciona de H, cicloalquilo C3-10, heterocicloalquilo C3-20, arilo C3-10, heteroarilo C3-10, oxiarilo, arilalcona, y cicloalquilarilo, cualquiera de los cuales además puede estar sustituido por R8; R8 se selecciona de uno o más de H, halogeno, alquilo inferior, alquilo inferior hetero-sustituido, alquenilo inferior, alcoxi inferior, cicloalquilo C3-10, heterocicloalquilo C3-10, arilo C3-10, heteroarilo C3-10, arilalquilo, heteroarilalquilo, alquil éster ácido, alcona, alcoxi; cualquiera de los cuales además puede estar sustituido por R9; y R9 se selecciona de uno o más H, halogeno, COOH, alquilo inferior, alquilo inferior hetero-sustituido, arilo, y alcoxi inferior; R10 y R11 se seleccionan de H, O, halogeno, alquilo inferior, alquilo inferior hetero-sustituido, y alcoxi inferior; y R12 está presente en q ocurrencias, en donde q es un entero de 0 a 4, y R12 es igual o diferente y se selecciona independientemente de H, O, halogeno, alquilo inferior, alquilo inferior hetero-sustituido, y alcoxi inferior; R13 se selecciona de uno o más de H, alquilo inferior, alquilo inferior hetero-sustituido, alcoxi inferior, cicloalquilo C3-10, heterocicloalquilo C3-10, arilo C3-10, heteroarilo C3-10, arilalquilo, heteroarilalquilo, cualquiera de los cuales además puede estar sustituido por R8, o una sal farmacéuticamente aceptable del mismo.
ARP060104167A 2005-09-27 2006-09-25 Compuestos de carboxiamina y uso de los mismos.composiciones farmaceuticas. AR058065A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US72090005P 2005-09-27 2005-09-27
US75496005P 2005-12-28 2005-12-28

Publications (1)

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AR058065A1 true AR058065A1 (es) 2008-01-23

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ARP060104167A AR058065A1 (es) 2005-09-27 2006-09-25 Compuestos de carboxiamina y uso de los mismos.composiciones farmaceuticas.

Country Status (13)

Country Link
US (1) US20080255149A1 (es)
EP (1) EP1996550A2 (es)
JP (1) JP2009510073A (es)
KR (1) KR20080054417A (es)
AR (1) AR058065A1 (es)
AU (1) AU2006294850A1 (es)
BR (1) BRPI0616755A2 (es)
CA (1) CA2623034A1 (es)
GT (1) GT200600430A (es)
PE (1) PE20070602A1 (es)
RU (1) RU2008116314A (es)
TW (1) TW200800894A (es)
WO (1) WO2007038459A2 (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA200701232B (en) 2004-07-15 2008-08-27 Amr Technology Inc Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine and serotonin
US7507842B2 (en) 2005-08-12 2009-03-24 Radiorx, Inc. Cyclic nitro compounds, pharmaceutical compositions thereof and uses thereof
US20070135380A1 (en) 2005-08-12 2007-06-14 Radiorx, Inc. O-nitro compounds, pharmaceutical compositions thereof and uses thereof
US20070207950A1 (en) * 2005-12-21 2007-09-06 Duke University Methods and compositions for regulating HDAC6 activity
EP2100879A1 (en) * 2008-03-13 2009-09-16 4Sc Ag Novel N-substituted tetrahydroisoquinoline/isoindoline hydroxamic acid compounds
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
WO2010059390A1 (en) 2008-10-30 2010-05-27 Janssen Pharmaceutica Nv Modulators of serotonin receptor
WO2010059393A1 (en) 2008-10-30 2010-05-27 Janssen Pharmaceutica Nv Serotonin receptor modulators
US8664182B2 (en) 2008-11-12 2014-03-04 Duke University Methods of inhibiting cancer cell growth with HDAC inhibitors and methods of screening for HDAC10 inhibitors
CN102638982B (zh) 2009-05-12 2015-07-08 百时美施贵宝公司 (S)-7-([1,2,4]***并[1,5-a]吡啶-6-基)-4-(3,4-二氯苯基)-1,2,3,4-四氢异喹啉的晶型及其用途
CA2760837C (en) 2009-05-12 2018-04-03 Albany Molecular Research, Inc. 7-([1,2,4]triazolo[1,5-.alpha.]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof
KR20120034644A (ko) 2009-05-12 2012-04-12 알바니 몰레큘라 리써치, 인크. 아릴, 헤테로아릴, 및 헤테로사이클 치환된 테트라하이드로이소퀴놀린 및 이의 용도
US8314250B2 (en) 2009-11-24 2012-11-20 Hoffmann-La Roche Inc. Sultam derivatives
US8552032B2 (en) * 2009-12-18 2013-10-08 Janssen Pharmaceutica Nv Bicyclic derivatives useful as inhibitors of DPP-1
US8471041B2 (en) * 2010-02-09 2013-06-25 Alliant Techsystems Inc. Methods of synthesizing and isolating N-(bromoacetyl)-3,3-dinitroazetidine and a composition including the same
US8664247B2 (en) 2011-08-26 2014-03-04 Radiorx, Inc. Acyclic organonitro compounds for use in treating cancer
ES2935573T3 (es) 2011-10-07 2023-03-08 Epicentrx Inc Compuestos de organonitro tioéter y usos médicos de estos
US20140308260A1 (en) 2011-10-07 2014-10-16 Radiorx, Inc. Methods and compositions comprising a nitrite-reductase promoter for treatment of medical disorders and preservation of blood products
AU2014260605B2 (en) 2013-04-29 2016-07-14 Chong Kun Dang Pharmaceutical Corp. Novel compounds for selective histone deacetylase inhibitors, and pharmaceutical composition comprising the same
US20180021331A1 (en) 2014-12-30 2018-01-25 University Of Utah Research Foundation Hdac1,2 inhibitors and methods of using the same
US10342778B1 (en) 2015-10-20 2019-07-09 Epicentrx, Inc. Treatment of brain metastases using organonitro compound combination therapy
US9987270B1 (en) 2015-10-29 2018-06-05 Epicentrix, Inc. Treatment of gliomas using organonitro compound combination therapy
JP6931004B2 (ja) 2016-01-11 2021-09-01 エピセントアールエックス,インコーポレイテッド 2−ブロモ−1−(3,3−ジニトロアゼチジン−1−イル)エタノンの静脈内投与のための組成物および方法
JP6643764B2 (ja) * 2016-02-05 2020-02-12 国立大学法人岐阜大学 抗がん剤
WO2018071741A1 (en) 2016-10-14 2018-04-19 Epicentrix, Inc. Sulfoxyalkyl organonitro and related compounds and pharmaceutical compositions for use in medicine
CA3048376A1 (en) 2016-12-27 2018-07-05 Riken Bmp-signal-inhibiting compound
MX2020000265A (es) 2017-07-07 2020-07-22 Epicentrx Inc Composiciones para la administración parenteral de agentes terapéuticos.
WO2019164593A2 (en) 2018-01-08 2019-08-29 Epicentrx, Inc. Methods and compositions utilizing rrx-001 combination therapy for radioprotection
ES2910071T3 (es) 2018-03-08 2022-05-11 Incyte Corp Compuestos de aminopirazina diol como inhibidores de PI3K-Y
DK3770162T3 (da) * 2018-03-20 2023-04-24 Sumitomo Pharma Co Ltd Dihydrochromenderivater
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
JP7287929B2 (ja) 2019-09-25 2023-06-06 住友ファーマ株式会社 ジヒドロクロメン誘導体を含有する医薬
WO2022178544A1 (en) * 2021-02-20 2022-08-25 Klotho Therapeutics, Inc. Novel heterocyclic compounds and related methods of manufacture and use in hdac inhibition

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB872448A (en) * 1958-12-23 1961-07-12 Lepetit Spa 1-acyl-3 substituted azetidines
DE2016970A1 (de) * 1970-04-09 1971-11-04 Farbwerke Hoechst AG, vorm Meister Lucius & Brumng, 6000 Frankfurt Neue Dipeptid amide
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
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
CA2145985C (en) 1992-10-28 2003-09-16 Napoleone Ferrara Vascular endothelial cell growth factor antagonists
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
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)
DE59712968D1 (de) 1996-11-18 2008-10-30 Biotechnolog Forschung Gmbh Epothilone E und F
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
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
JP2002504540A (ja) 1998-02-25 2002-02-12 スローン−ケッタリング インスティトゥート フォア キャンサー リサーチ エポチロンの合成、その中間体およびそのアナログ
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
KR100716272B1 (ko) 1998-11-20 2007-05-09 코산 바이오사이언시즈, 인코포레이티드 에포틸론 및 에포틸론 유도체의 생산을 위한 재조합 방법 및 물질
DK1140173T4 (da) 1998-12-22 2013-06-10 Genentech Inc Vaskulære endothelcellevækstfaktorantagonister og anvendelser deraf
DE60028740T2 (de) 1999-03-30 2007-05-24 Novartis Ag Phthalazinderivate zur behandlung von entzündlichen erkrankungen
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
ES2309313T3 (es) * 2002-04-03 2008-12-16 Topotarget Uk Limited Compuestos del acido carbamico que comprenden un acoplamiento de piperacina como hdac inhibidores.
ES2286345T3 (es) * 2003-03-20 2007-12-01 Santhera Pharmaceuticals (Schweiz) Ag Derivados de piperidina y piperazina substituidos como moduladores del receptor de melanocortina-4.
KR101223914B1 (ko) * 2003-11-21 2013-01-18 어레이 바이오파마 인크. Akt 단백질 키나제 억제제
ITFI20050041A1 (it) * 2005-03-15 2006-09-16 Menarini Internat Operations Luxembourg Sa Idrossammati come inibitori dell'istone deacelitasi, loro preparazione e formulazioni farmaceutiche che li contengono

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AU2006294850A1 (en) 2007-04-05
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