AR073574A1 - Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad - Google Patents

Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad

Info

Publication number
AR073574A1
AR073574A1 ARP090103487A ARP090103487A AR073574A1 AR 073574 A1 AR073574 A1 AR 073574A1 AR P090103487 A ARP090103487 A AR P090103487A AR P090103487 A ARP090103487 A AR P090103487A AR 073574 A1 AR073574 A1 AR 073574A1
Authority
AR
Argentina
Prior art keywords
group
heterocycloalkyl
aminoalkyl
heteroaryl
cycloalkyl
Prior art date
Application number
ARP090103487A
Other languages
English (en)
Inventor
Allen J Borchardt
Robert L Davis
Travis Cook
Original Assignee
Alcon Res Ltd
Kalypsys 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42005738&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR073574(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Alcon Res Ltd, Kalypsys Inc filed Critical Alcon Res Ltd
Publication of AR073574A1 publication Critical patent/AR073574A1/es

Links

Classifications

    • 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
    • C07D487/04—Ortho-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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Neurosurgery (AREA)
  • Otolaryngology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos y métodos que pueden ser utiles como inhibidores de H1R y/o H4R para el tratamiento o la prevencion de enfermedades inflamatorias, autoinmunes, alérgicas y oculares. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula estructural (1) o una sal, en la cual: el anillo que comprende X1 - X5 es aromático; X1 y X5 se seleccionan, en forma independiente del grupo que consiste en C, CH y N; X2 se selecciona del grupo que consiste en [C(R6)(R7)]n, NR8, O y S; X3 se selecciona del grupo que consiste en [C(R9)(R10)]m, NR11, O y S; X4 se selecciona del grupo que consiste en [C(R12)(R13)], NR14, O y S; n y m son cada uno un numero entero desde 1 hasta 2; Y1 se selecciona del grupo que consiste en un enlace, alquilo inferior, alcoxi inferior, OR15, NR16R17, y aminoalquilo inferior; R1 se selecciona del grupo que consiste en: nulo, cuando Y1 se selecciona del grupo que consiste en OR15, y NR16R17; y arilo, heterocicloalquilo, cicloalquilo, y heteroarilo, cualquiera de los cuales puede estar sustituido en forma opcional, cuando Y1 es un enlace; R2, R3, R4 y R5 se seleccionan en forma independiente del grupo que consiste en hidrogeno, alquilo, alquenilo, heteroalquilo, alcoxi, halogeno, haloalquilo, perhaloalquilo, perhaloalcoxi, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, cualquiera de los cuales puede estar sustituido en forma opcional; R6, R7, R9, R10, R12 y R13 se seleccionan en forma independiente del grupo que cosiste en nulo, hidrogeno, alquilo, heteroalquilo, alcoxi, halogeno, haloalquilo, perhaloalquilo, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo y heteroarilalquilo, cualquiera de los cuales puede estar sustituido en forma opcional; R8, R11 y R14 se seleccionan en forma independiente del grupo que consiste en nulo, hidrogeno, alquilo, heteroalquilo, alcoxi, haloalquilo, perhalolalquilo, aminoalquilo, C-amido, carboxilo, acilo, hidroxi, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, cualquiera de los cuales puede estar sustituido en forma opcional; R15 y R16 se seleccionan en forma independiente del grupo que consiste en aminoalquilo, alquil aminoalquilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, éter, heterocicloalquilo, alquilamino heterocicloalquilo inferior, heterocicloalquilalquilo, heteroarilo, y heteroarilalquilo, cualquiera de los cuales puede estar sustituido en forma opcional; y R17 se selecciona en forma independiente del grupo que consiste en hidrogeno, aminoalquilo, alquil aminoalquilo arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, éter, heterocicloalquilo, alquilamino heterocicloalquilo inferior, heterocicloalquilalquilo, heteroarilo, y hetereroarilalquilo, cualquiera de los cuales puede estar sustituido en forma opcional.
ARP090103487A 2008-09-10 2009-09-10 Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad AR073574A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9582608P 2008-09-10 2008-09-10
US23174909P 2009-08-06 2009-08-06

Publications (1)

Publication Number Publication Date
AR073574A1 true AR073574A1 (es) 2010-11-17

Family

ID=42005738

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090103487A AR073574A1 (es) 2008-09-10 2009-09-10 Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad

Country Status (14)

Country Link
US (2) US20100120741A1 (es)
EP (1) EP2324029A4 (es)
JP (1) JP2012502067A (es)
KR (1) KR20110095857A (es)
CN (1) CN102388044A (es)
AR (1) AR073574A1 (es)
AU (1) AU2009291719A1 (es)
CA (1) CA2735369A1 (es)
CL (1) CL2011000431A1 (es)
MX (1) MX2011002264A (es)
RU (1) RU2011113419A (es)
TW (1) TW201024297A (es)
UY (1) UY32111A (es)
WO (1) WO2010030785A2 (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102004031656A1 (de) * 2004-06-30 2006-01-19 Merck Patent Gmbh Tetrahydrochinoline
WO2009111337A1 (en) 2008-03-03 2009-09-11 Irm Llc Compounds and compositions as tlr activity modulators
TWI547522B (zh) 2009-07-07 2016-09-01 愛爾康研究有限公司 環氧乙烷環氧丁烷嵌段共聚物組成物
IN2012DN02596A (es) * 2009-08-26 2015-08-28 Cylene Pharmaceuticals Inc
JP2013053070A (ja) * 2009-11-06 2013-03-21 Takeda Chem Ind Ltd ジヒドロピロロキノリン誘導体
TW201200518A (en) * 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
DE102010025786A1 (de) * 2010-07-01 2012-01-05 Merck Patent Gmbh Pyrazolochinoline
TW201206936A (en) 2010-07-19 2012-02-16 Alcon Res Ltd Methods and compositions for the treatment of allergy
US9540379B2 (en) 2011-01-31 2017-01-10 Boehringer Ingelheim International Gmbh (1,2,4)triazolo[4,3-A]quinoxaline derivatives as inhibitors of phosphodiesterases
WO2012143143A1 (en) * 2011-04-21 2012-10-26 Origenis Gmbh Heterocyclic compounds as kinase inhibitors
US8859550B2 (en) 2011-09-12 2014-10-14 Kalypsys, Inc. Heterocyclic inhibitors of histamine receptors for the treatment of disease
BR112014007645A2 (pt) * 2011-09-30 2017-04-18 C&C Res Lab composto heterocíclico, métodos para a preparação de um composto heterocíclico, e, composição farmacêutica
CA2850932A1 (en) 2011-10-04 2013-04-11 Janus Biotherapeutics, Inc. Novel imidazole quinoline-based immune system modulators
US20140045856A1 (en) 2012-07-31 2014-02-13 Boehringer Ingelheim International Gmbh 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes
US10000482B2 (en) 2012-10-19 2018-06-19 Origenis Gmbh Kinase inhibitors
WO2014087208A2 (en) * 2012-12-06 2014-06-12 Enaltec Labs Pvt. Ltd. A process of preparing alcaftadine
MX369611B (es) 2013-02-01 2019-11-14 Wellstat Therapeutics Corp Compuestos de amina que tienen actividad anti-inflamatoria, antifungica, antiparasitaria y anticancer.
CA2904364A1 (en) * 2013-03-15 2014-09-25 Epigenetix, Inc. Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors
SI3027613T1 (sl) * 2013-07-25 2018-10-30 Uniwersytet Jagiellonski Derivati pirolokvinolina kot 5-HT6 antagonisti, postopek priprave in uporabe le-teh
EP3307067B1 (en) 2015-06-11 2022-11-02 Merck Sharp & Dohme LLC Aminopyrazine compounds with a2a antagonist properties
KR102070265B1 (ko) * 2017-01-26 2020-01-28 한국화학연구원 신규한 [1,2,4]트리아졸로[4,3-a]퀴녹살린 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 BET 단백질 관련 질환의 예방 또는 치료용 약학적 조성물
WO2019177971A1 (en) * 2018-03-12 2019-09-19 Mavupharma, Inc. Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitors and uses thereof
WO2019200500A1 (zh) * 2018-04-15 2019-10-24 苏州大学张家港工业技术研究院 1,2,4-三氮唑及其制备方法
TW202021969A (zh) * 2018-05-31 2020-06-16 南韓商Ｃ＆Ｃ新藥研究所 雜環衍生物及其用途
CN109705141B (zh) * 2019-02-20 2020-05-29 苏州大学 一种恶唑并喹啉类化合物及其制备方法与应用
WO2021098734A1 (zh) * 2019-11-19 2021-05-27 南京明德新药研发有限公司 作为atm抑制剂的有取代的喹啉吡咯酮类合物及其应用
US11530218B2 (en) 2020-01-20 2022-12-20 Incyte Corporation Spiro compounds as inhibitors of KRAS
WO2021231526A1 (en) 2020-05-13 2021-11-18 Incyte Corporation Fused pyrimidine compounds as kras inhibitors
WO2022047093A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
WO2022072783A1 (en) 2020-10-02 2022-04-07 Incyte Corporation Bicyclic dione compounds as inhibitors of kras
EP4067357A1 (en) * 2021-03-30 2022-10-05 JW Pharmaceutical Corporation Novel crystalline form of 1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-n-methylazetidin-3-amine hydrogen sulfate monohydrate
IL312114A (en) 2021-10-14 2024-06-01 Incyte Corp Quinoline compounds as Kras inhibitors
WO2024027370A1 (zh) * 2022-08-03 2024-02-08 上海和誉生物医药科技有限公司 一种含氮三稠环prmt5抑制剂，其制备方法和药学上的用途
WO2024067433A1 (zh) * 2022-09-26 2024-04-04 上海湃隆生物科技有限公司 新型prmt5抑制剂及其应用
WO2024069235A2 (en) 2022-09-30 2024-04-04 Sixfold Bioscience Ltd. Compositions containing oligonucleotides with theranostic applications

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4053600A (en) * 1973-03-08 1977-10-11 Sandoz, Inc. Tricyclic 1,2,4-triazolo-quinazolines
US4495187A (en) * 1982-10-18 1985-01-22 Pfizer Inc. Method of using [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives as antidepressant and antifatigue agents
IN160956B (es) * 1982-10-18 1987-08-22 Pfizer
US6451796B1 (en) * 1997-11-11 2002-09-17 Ono Pharmaceutical Co., Ltd. Fused pyrazine compounds
US20050107611A1 (en) * 2001-12-21 2005-05-19 Barbara Matuszczak Pyrazolyl-substituted triazoloquinoxalines
EP2066645A2 (en) * 2006-09-12 2009-06-10 UCB Pharma S.A. 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions
EP1972629A1 (en) * 2007-03-23 2008-09-24 Mutabilis SA New imidazolo-heteroaryl derivatives with antibacterial properties
FR2921927B1 (fr) * 2007-10-03 2012-10-12 Univ De Montpellier 1 Imidazo°1,2-a!quinoxalines et derives pour le traitement des cancers

Also Published As

Publication number Publication date
WO2010030785A2 (en) 2010-03-18
CL2011000431A1 (es) 2012-01-20
RU2011113419A (ru) 2012-10-20
AU2009291719A1 (en) 2010-03-18
EP2324029A2 (en) 2011-05-25
EP2324029A4 (en) 2011-09-14
CA2735369A1 (en) 2010-03-18
UY32111A (es) 2010-04-30
JP2012502067A (ja) 2012-01-26
WO2010030785A3 (en) 2010-07-01
KR20110095857A (ko) 2011-08-25
US20120065187A1 (en) 2012-03-15
CN102388044A (zh) 2012-03-21
MX2011002264A (es) 2011-05-23
US20100120741A1 (en) 2010-05-13
TW201024297A (en) 2010-07-01

Similar Documents

Publication Publication Date Title
AR073574A1 (es) Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad
AR080496A1 (es) Inhibidores heterociclicos de los receptores de histamina para el tratamiento de una enfermedad
AR121661A2 (es) Esteroides neuroactivos, composiciones y usos de los mismos
AR082168A1 (es) Metodos y composiciones para el tratamiento de la alergia
AR072906A1 (es) Nucleosidos modificados utiles como antivirales
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20190656A1 (es) Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
PE20142456A1 (es) COMPUESTOS DE OXAZOLIDIN-2-ONA Y USOS DE LOS MISMOS COMO INHIBIDORES DE LA PI3Ks
AR086357A1 (es) Derivados de indazol sustituidos activos como inhibidores de quinasas
EA201270339A1 (ru) Замещенные производные ксантина
AR077975A1 (es) Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
AR082029A1 (es) Derivados de heterociclos nitrogenados, composiciones y metodos para modular la via de señalizacion de wnt
AR077977A1 (es) Compuestos y composiciones como inhibidores de cinasa de proteina
PE20090189A1 (es) Derivados de aza-piridopirimidinona como agonistas de hm74a
ECSP14013245A (es) Nuevos derivados dihidroquinolina-2-ona
AR074089A1 (es) Antagonistas de cicloalcano (b) azaindol de los receptores de la postaglandina d2
UY28936A1 (es) Grupo de compuestos benzoil-amino-heterociclilo y composiciones farmaceuticas que los comprenden, utiles para tratamiento de enfermedades mediadas por glucoquinasa (gq)
PE20141598A1 (es) Derivados de dihidro-benzo-oxazina y dihidro-pirido-oxazina
AR078609A1 (es) 8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de trastornos del sistema nervioso central,tales como depresion y canceres de ovario y renales, entre otros.
AR054024A1 (es) Derivados de piridina -3- carboxamida como agonistas inversos de cb1
AR080785A1 (es) Derivados de imidazo[1,2-a]pirimidina ,proceso para prepararlos e intermediarios de dicha sintesis, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de patologias del sistema nervioso central,tales como esquizofrenia y parkinson, entre otros.
EA201001178A1 (ru) 2-АЛКИЛАМИНО-3-АРИЛСУЛЬФОНИЛ-ЦИКЛОАЛКАНО[e ИЛИ d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТРЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ
ES2603931T3 (es) Compuestos de triazolo
CL2012000042A1 (es) Compuestos derivados de imidazo[1,2-a]pirazin-7-il; composición farmacéutica que comprende a uno de los compuestos; y uso de uno de los compuestos en la preparación de un medicamento útil para tratar una enfermedad relacionada con el género plasmodium en un sujeto.
AR085398A1 (es) Ureas asimetricas y usos medicos de las mismas

Legal Events

Date Code Title Description
FA Abandonment or withdrawal