[go: up one dir, main page]

AR118919A2 - Derivados de tetrahidro-pirido-pirimidina - Google Patents

Derivados de tetrahidro-pirido-pirimidina

Info

Publication number
AR118919A2
AR118919A2 ARP200101358A ARP200101358A AR118919A2 AR 118919 A2 AR118919 A2 AR 118919A2 AR P200101358 A ARP200101358 A AR P200101358A AR P200101358 A ARP200101358 A AR P200101358A AR 118919 A2 AR118919 A2 AR 118919A2
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
alkylcarbonyl
hydroxy
halo
Prior art date
Application number
ARP200101358A
Other languages
English (en)
Inventor
Gregory HOLLINGWORTH
Alexander Baxter Smith
Nicolas Soldermann
Frank Stowasser
Ross Strang
Nicola Tufilli
Matt Anette Von
Romain Wolf
Frdric Zecri
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR118919A2 publication Critical patent/AR118919A2/es

Links

Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/28Drugs 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
    • 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
    • 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

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

Abstract

Reivindicación 1: Un derivado de tetrahidro-pirido-pirimidina de la fórmula (1), y/o los tautómeros y/o los N-óxidos y/o las sales farmacéuticamente aceptables del mismo, en donde: Y se selecciona a partir de O ó NR³; R¹ se selecciona a partir de fenilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, 1,2,3-triazinilo, 1,2,4-triazinilo, 1,3,5-triazinilo, o -C(O)-R⁴ en donde: R⁴ se selecciona a partir de alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, alquilo C₁₋₈-sulfonil-alquilo C₁₋₈, heterociclilo, heterocicliloxilo, heterociclil-alquilo C₁₋₈, cicloalquilo C₃₋₁₂, cicloalquilo C₃₋₁₂-alquilo C₁₋₈, heteroarilo, heteroariloxilo, heteroaril-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, amino, N-alquilo C₁₋₈amino, o N,N-di-alquilo C₁₋₈-amino, en donde ‘alquilo C₁₋₈’ en N-alquilo C₁₋₈-amino y N,N-di-alquilo C₁₋₈-amino puede estar insustituido o sustituido por halógeno, hidroxilo, o alcoxilo C₁₋₄; en donde ‘cicloalquilo C₃₋₁₂’ en cicloalquilo C₃₋₁₂ y cicloalquilo C₃₋₁₂-alquilo C₁₋₈, puede estar insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de oxo, halógeno, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo, hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈-carbonilo; en donde ‘heterociclilo’ se selecciona a partir de oxiranilo, aziridinilo, oxetanilo, tietanilo, azetidinilo, pirrolidinilo, tetrahidro-furanilo, tetrahidro-tiofenilo, 2,3-dihidro-furanilo, 2,5-dihidro-furanilo, 2,3-dihidro-tiofenilo, 1-pirrolinilo, 2-pirrolinilo, 3-pirrolinilo, tetrahidro-piranilo, piperidinilo, tetrahidro-tiopiranilo, morfolinilo, tiomorfolinilo, piperazinilo, azepanilo, tiepanilo u oxepanilo; cada uno de los cuales está insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de oxo, halógeno, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo, hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈-carbonilo; en donde ‘heterociclilo’ se puede unir en un heteroátomo o en un átomo de carbono, y en donde los heteroátomos de N y/o S también se pueden oxidar opcionalmente hasta diferentes estados de oxidación; en donde ‘heteroarilo’ se selecciona a partir de furanilo, tiofenilo, pirrolilo, imidazolilo, pirazolilo, tiazolilo, isotiazolilo, oxazolilo, isoxazolilo, 1,2,5-oxadiazolilo, 1,2,4-oxadiazolilo, 1,2,3-oxadiazolilo, 1,3,4-oxadiazolilo, 1,2,5-tiadiazolilo, 1,2,4-tiadiazolilo, 1,2,3-tiadiazolilo, 1,3,4-tiadiazolilo, 1,2,3-triazolilo, 1,2,4-triazolilo, 1,2,5-triazolilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, 1,2,3-triazinilo, 1,2,4-triazinilo o 1,3,5-triazinilo; cada uno de los cuales está insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de halógeno, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo, hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈carbonilo; en donde ‘heteroarilo’ se puede unir en un heteroátomo o en un átomo de carbono, y en donde los heteroátomos de N y/o S también se pueden oxidar opcionalmente hasta diferentes estados de oxidación; R² se selecciona a partir de fenilo, naftilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, quinolinilo o isoquinolinilo, cada uno de los cuales está insustituido o sustituido por 1 a 5 sustituyentes seleccionados independientemente a partir de halógeno, ciano, nitro, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxi-alquilo C₁₋₈, hidroxilo, alcoxilo C₁₋₈, alcoxilo C₁₋₈-alquilo C₁₋₈, amino, N-alquilo C₁₋₈-amino, N,N-di-alquilo C₁₋₈-amino, alquilo C₁₋₈-carbonilo, halo-alquilo C₁₋₈-carbonilo, hidroxi-alquilo C₁₋₈-carbonilo o alcoxilo C₁₋₈-alquilo C₁₋₈-carbonilo; R³ se selecciona a partir de H, alquilo C₁₋₄, o haloalquilo C₁₋₄; y m se selecciona a partir de 0 ó 1.
ARP200101358A 2010-07-06 2020-05-12 Derivados de tetrahidro-pirido-pirimidina AR118919A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US36158910P 2010-07-06 2010-07-06

Publications (1)

Publication Number Publication Date
AR118919A2 true AR118919A2 (es) 2021-11-10

Family

ID=44532774

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP110102390A AR084970A1 (es) 2010-07-06 2011-07-04 Derivados de tetrahidro-pirido-pirimidina, una composicion farmaceutica en base al compuesto y un proceso para su preparacion
ARP190102244A AR115927A2 (es) 2010-07-06 2019-08-07 Derivados de tetrahidro-pirido-pirimidina
ARP200101358A AR118919A2 (es) 2010-07-06 2020-05-12 Derivados de tetrahidro-pirido-pirimidina

Family Applications Before (2)

Application Number Title Priority Date Filing Date
ARP110102390A AR084970A1 (es) 2010-07-06 2011-07-04 Derivados de tetrahidro-pirido-pirimidina, una composicion farmaceutica en base al compuesto y un proceso para su preparacion
ARP190102244A AR115927A2 (es) 2010-07-06 2019-08-07 Derivados de tetrahidro-pirido-pirimidina

Country Status (39)

Country Link
US (10) US8653092B2 (es)
EP (1) EP2590974B1 (es)
JP (1) JP5770842B2 (es)
KR (1) KR101560066B1 (es)
CN (1) CN102971317B (es)
AR (3) AR084970A1 (es)
AU (1) AU2011275777C1 (es)
BR (1) BR112013000275B1 (es)
CA (1) CA2802132C (es)
CL (1) CL2013000033A1 (es)
CO (1) CO6670566A2 (es)
CR (1) CR20130004A (es)
DK (1) DK2590974T3 (es)
DO (1) DOP2013000027A (es)
EA (1) EA024123B1 (es)
EC (1) ECSP13012420A (es)
ES (1) ES2494718T3 (es)
GT (1) GT201300009A (es)
HR (1) HRP20140778T1 (es)
IL (1) IL223795A (es)
JO (1) JO2939B1 (es)
MA (1) MA34361B1 (es)
MX (1) MX2012015088A (es)
MY (1) MY166026A (es)
NI (1) NI201300002A (es)
NZ (1) NZ604302A (es)
PE (1) PE20130650A1 (es)
PH (1) PH12013500031A1 (es)
PL (1) PL2590974T3 (es)
PT (1) PT2590974E (es)
RS (1) RS53490B1 (es)
SG (1) SG186187A1 (es)
SI (1) SI2590974T1 (es)
TN (1) TN2012000578A1 (es)
TW (1) TWI534145B (es)
UA (1) UA112517C2 (es)
UY (1) UY33486A (es)
WO (1) WO2012004299A1 (es)
ZA (1) ZA201209117B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8759362B2 (en) * 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
JO3733B1 (ar) 2011-04-05 2021-01-31 Bayer Ip Gmbh استخدام 3,2-دايهيدروايميدازو[1, 2 -c]كوينازولينات مستبدلة
CA2840315A1 (en) 2011-06-27 2013-01-03 Novartis Ag Solid forms and salts of tetrahydro-pyrido-pyrimidine derivatives
DK2790705T3 (en) * 2011-12-15 2018-03-12 Novartis Ag Use of inhibitors of the activity or function of PI3K
JO3398B1 (ar) 2011-12-22 2019-10-20 Novartis Ag مشتقات 2،3- ثانى هيدرو- بنزو[1,4] أوكسازين والمركبات المتعلقة بها كمثبطات كيناز فسفواينوسيتيد-3 (pi3k) لمعالجة على سبيل المثال التهاب المفاصل الروماتيدي
JP6434416B2 (ja) 2012-11-08 2018-12-05 ライゼン・ファーマシューティカルズ・エスアー PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物
AU2013347538B2 (en) 2012-11-16 2017-04-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
RU2661896C2 (ru) * 2012-11-16 2018-07-23 Мерк Шарп И Доум Корп. Пуриновые ингибиторы фосфатидилинозитол-3-киназы дельта человека
EP2742940B1 (en) 2012-12-13 2017-07-26 IP Gesellschaft für Management mbH Fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-l-aza-bicyclo-[2.2.2]octane for adminstration once daily, twice daily or thrice daily
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
WO2015162584A1 (en) 2014-04-24 2015-10-29 Novartis Ag Crystalline forms of the sulfate salt of n-[5-(3-imidazol-1-yl-4-methanesulfonyl-phenyl)-4-methyl-thiazol-2-yl]-acetamide
GB201506786D0 (en) * 2015-04-21 2015-06-03 Ucb Biopharma Sprl Therapeutic use
EP3292120B1 (en) * 2015-05-04 2019-06-19 H. Hoffnabb-La Roche Ag Tetrahydropyridopyrimidines and tetrahydropyridopyridines as inhibitors of hbsag (hbv surface antigen) and hbv dna production for the treatment of hepatitis b virus infections
AU2016362129A1 (en) 2015-12-04 2018-06-14 Intellia Therapeutics, Inc. Compositions and methods for immunooncology
ES2797091T3 (es) * 2016-02-10 2020-12-01 Novartis Ag Uso de inhibidores de la actividad o de la función de la PI3K para el tratamiento del síndrome de Sjögren primario
SG11201907434RA (en) 2017-03-22 2019-10-30 Novartis Ag Compositions and methods for immunooncology
EP3630116B1 (en) 2017-05-26 2024-05-01 The Board Of Regents Of The University Of Texas System Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase
IL271930B (en) 2017-07-13 2022-07-01 Univ Texas Heterocyclic inhibitors of atr kinase
US10800774B2 (en) 2017-08-17 2020-10-13 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of ATR kinase
CN112218631B (zh) 2018-03-16 2023-12-22 德州大学系统董事会 Atr激酶的杂环抑制剂
CN114315826B (zh) * 2021-11-30 2023-05-16 西安交通大学 一种吡啶并嘧啶类化合物及其应用
KR20230160977A (ko) 2022-05-17 2023-11-27 에이치앤오바이오시스(주) 항암 치료에 사용되는 5종 이상의 생약 추출물

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1197466B (de) 1962-03-22 1965-07-29 Thomae Gmbh Dr K Verfahren zur Herstellung von neuen 5, 6, 7, 8-Tetrahydropyrido-[4, 3-d]pyrimidinen
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
ATE28864T1 (de) 1982-07-23 1987-08-15 Ici Plc Amide-derivate.
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
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
TW225528B (es) 1992-04-03 1994-06-21 Ciba Geigy Ag
US5300645A (en) 1993-04-14 1994-04-05 Eli Lilly And Company Tetrahydro-pyrido-indole
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
EP2295415A1 (en) 1995-03-30 2011-03-16 OSI Pharmaceuticals, Inc. Quinazoline derivatives
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
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
CZ1598A3 (cs) 1995-07-06 1998-04-15 Novartis Ag Pyrrolopyrimidiny a způsoby jejich přípravy
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
GEP20012442B (en) 1996-04-12 2001-05-25 Warner Lambert Co Irreversible Inhibitors of Tyrosine Kinases
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
AU716610B2 (en) 1996-08-30 2000-03-02 Novartis Ag Method for producing epothilones, and intermediate products obtained during the production process
DE69724269T2 (de) 1996-09-06 2004-06-09 Obducat Ab Verfahren für das anisotrope ätzen von strukturen in leitende materialien
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon 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
CN1196698C (zh) 1996-11-18 2005-04-13 生物技术研究有限公司(Gbf) Epothilone D、E和F,其制备方法,以及作为细胞抑制剂和植物保护剂的应用
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
US5939421A (en) * 1997-07-01 1999-08-17 Signal Pharmaceuticals, Inc. Quinazoline analogs and related compounds and methods for treating inflammatory conditions
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
EP1058679B1 (en) 1998-02-25 2005-10-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues therof
WO2000031247A2 (en) 1998-11-20 2000-06-02 Kosan Biosciences, Inc. Recombinant methods and materials for producing epothilone and epothilone derivatives
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
BRPI0115193B1 (pt) 2000-11-07 2016-08-09 Novartis Ag derivados de indolilmaleimida, processo para preparação dos mesmos, bem como composição farmacêutica que os compreende
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
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
PE20040079A1 (es) 2002-04-03 2004-04-19 Novartis Ag Derivados de indolilmaleimida
EP1578411A4 (en) 2002-12-09 2007-05-02 Univ Texas PROCESS FOR THE SELECTIVE INHIBITION OF JANUS TYROSINE KINASE3 (JAK3)
HRP20050593A2 (en) 2002-12-27 2006-03-31 Instituto di Ricerche di Biologia Molecolare P. An Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors
US20080207613A1 (en) 2004-01-12 2008-08-28 Cytopia Research Pty Ltd Selective Kinase Inhibitors
CA2553969A1 (en) 2004-01-23 2005-08-04 Amgen Inc. Vanilloid receptor ligands and their use in treatments
PL2298768T3 (pl) 2004-06-11 2013-03-29 Japan Tobacco Inc Pochodne 5-amino-2,4,7-triokso-3,4,7,8-tetrahydro-2H-pirydo[2,3-d]pirymidyny i związki pokrewne do leczenia nowotworu
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
ES2552804T3 (es) * 2005-05-04 2015-12-02 Evotec Ag Compuestos heterocíclicos condensados, y sus composiciones y usos
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
ES2566387T3 (es) * 2007-04-02 2016-04-12 Evotec Ag Compuestos heterocíclicos condensados de pirid-2-ilo, y composiciones y usos de los mismos
DK2139334T3 (da) * 2007-04-17 2013-09-23 Evotec Ag Kondenserede heterocykliske 2-cyanophenylforbindelser og sammensætninger og anvendelser deraf
WO2009047255A1 (en) 2007-10-09 2009-04-16 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
WO2009076631A1 (en) 2007-12-12 2009-06-18 Rigel Pharmaceuticals, Inc. Carboxamide, sulfonamide and amine compounds for metabolic disorders
US8436005B2 (en) 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
US20120028940A1 (en) 2008-09-16 2012-02-02 Merck Sharp & Dohme Corp. Functionally selective azanitrile alpha-2c adrenoreceptor agonists
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US8759362B2 (en) 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
US8546388B2 (en) 2008-10-24 2013-10-01 Purdue Pharma L.P. Heterocyclic TRPV1 receptor ligands
JP2010105951A (ja) 2008-10-29 2010-05-13 Dainippon Sumitomo Pharma Co Ltd 6−アルキル置換テトラヒドロピリド[4,3−d]ピリミジン誘導体
WO2010117425A1 (en) 2009-03-31 2010-10-14 Biogen Idec Ma Inc. Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use
WO2010120991A1 (en) 2009-04-17 2010-10-21 Wyeth Llc 5, 6, 7, 8-tetrahydropyrido[4,3-d]pyrimidine compounds, their use as mtor, pi3, and hsmg-1 kinase inhibitors, and their syntheses
WO2010127212A1 (en) 2009-04-30 2010-11-04 Forest Laboratories Holdings Limited Inhibitors of acetyl-coa carboxylase
US9908884B2 (en) 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
WO2010138430A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Alkoxy tetrahydro-pyridopyrimidine pde10 inhibitors
JP2013032290A (ja) 2009-11-20 2013-02-14 Dainippon Sumitomo Pharma Co Ltd 新規縮合ピリミジン誘導体
SG182343A1 (en) 2010-01-06 2012-08-30 Joseph P Errico Methods and compositions of targeted drug development
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
WO2011103715A1 (en) 2010-02-25 2011-09-01 Merck Sharp & Dohme Corp. Task channel antagonists
WO2011143495A1 (en) 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
EP2571357B1 (en) 2010-05-21 2016-07-06 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
DK2790705T3 (en) 2011-12-15 2018-03-12 Novartis Ag Use of inhibitors of the activity or function of PI3K

Also Published As

Publication number Publication date
EA024123B1 (ru) 2016-08-31
PE20130650A1 (es) 2013-06-15
WO2012004299A1 (en) 2012-01-12
BR112013000275B1 (pt) 2020-12-01
US20190218217A1 (en) 2019-07-18
CN102971317A (zh) 2013-03-13
NI201300002A (es) 2013-04-15
TWI534145B (zh) 2016-05-21
EP2590974A1 (en) 2013-05-15
AU2011275777B2 (en) 2014-07-31
US20220267318A1 (en) 2022-08-25
MA34361B1 (fr) 2013-07-03
TW201206930A (en) 2012-02-16
US20190040061A1 (en) 2019-02-07
KR20130041068A (ko) 2013-04-24
DOP2013000027A (es) 2013-09-30
CL2013000033A1 (es) 2013-05-10
TN2012000578A1 (en) 2014-04-01
BR112013000275A2 (pt) 2016-06-14
MY166026A (en) 2018-05-21
UY33486A (es) 2012-02-29
US20170267678A1 (en) 2017-09-21
KR101560066B1 (ko) 2015-10-13
SG186187A1 (en) 2013-01-30
NZ604302A (en) 2014-11-28
US8653092B2 (en) 2014-02-18
CN102971317B (zh) 2016-01-20
US20200392132A1 (en) 2020-12-17
US9499536B2 (en) 2016-11-22
EA201291317A1 (ru) 2013-05-30
US20120065183A1 (en) 2012-03-15
RS53490B1 (sr) 2015-02-27
JP2013535411A (ja) 2013-09-12
AU2011275777A1 (en) 2012-12-20
SI2590974T1 (sl) 2014-08-29
JO2939B1 (en) 2016-03-15
US20250059181A1 (en) 2025-02-20
CA2802132A1 (en) 2012-01-12
DK2590974T3 (da) 2014-07-28
MX2012015088A (es) 2013-02-12
AR115927A2 (es) 2021-03-10
HRP20140778T1 (hr) 2014-09-12
CR20130004A (es) 2013-04-17
HK1179966A1 (en) 2013-10-11
JP5770842B2 (ja) 2015-08-26
US20180265509A1 (en) 2018-09-20
PL2590974T3 (pl) 2014-10-31
PT2590974E (pt) 2014-09-01
EP2590974B1 (en) 2014-05-21
CO6670566A2 (es) 2013-05-15
GT201300009A (es) 2015-06-02
ECSP13012420A (es) 2013-03-28
PH12013500031A1 (en) 2015-04-15
UA112517C2 (uk) 2016-09-26
IL223795A (en) 2015-11-30
CA2802132C (en) 2019-02-26
ZA201209117B (en) 2013-09-25
AU2011275777C1 (en) 2015-02-05
US20170022199A1 (en) 2017-01-26
US20140128370A1 (en) 2014-05-08
ES2494718T3 (es) 2014-09-16
AR084970A1 (es) 2013-07-24

Similar Documents

Publication Publication Date Title
AR118919A2 (es) Derivados de tetrahidro-pirido-pirimidina
BR112013010552A2 (pt) derivado de piridina e agente medicinal
ES2640049T3 (es) Derivados de 3,6-dihidropirimidina 2,4,5,6-sustituidos como inhibidores de la polimerasa del virus de la hepatitis B (VHB) para el tratamiento de, por ejemplo, la hepatitis crónica
AR100645A1 (es) Derivados de pirazolo-pirimidina
CO6241124A2 (es) Moduladores de gamma secretasa
AR108745A1 (es) Derivados de oxadiazol microbiocidas
BRPI0821653B8 (pt) composto de piridina substituída com anel heterocíclico e grupo fosfonoximetila ou um sal do mesmo, composição farmacêutica compreendendo-os e uso dos mesmos para tratar uma doença fungíca
ME02729B (me) Indolski i indazolski spojevi koji aktiviraju ampk
AR109805A1 (es) Derivados de oxadiazol microbiocidas
AR088692A1 (es) Derivados de 2-(1,2,3-triazol-2-il)benzamina y 3-(1,2,3-triazol-2-il)picolinamida
HRP20201171T1 (hr) Derivati izoindolin-1-ona kao modulatori aktivnosti pozitivnog alosternog modulatora kolinergijskog muskarinskog m1 receptora za liječenje alzheimerove bolesti
AR084913A1 (es) Derivados de aril-benzocicloalquil-amida
AR064824A1 (es) Derivados de espirocromanona sustituidos
NO20084832L (no) Pyrimidinderivater som P13K-inhibitorer
AR092684A1 (es) Compuestos de sulfonamida sustituidos
AR082887A1 (es) Derivados de piridin-3-il-metil, y composiciones para la inhibicion de nampt
AR086198A1 (es) Inhibidores sustituidos de acetil-coa carboxilasa y composiciones farmaceuticas que los contienen
EA201591675A1 (ru) Замещенные 7-азабициклы и их применение в качестве модуляторов рецепторов орексина
BRPI1007456A2 (pt) derivados de azaespiranil-alquilcarbamatos de compostos heterocíclicos com 5 membros, o respectivo preparo e a respectiva aplicação em terapêutica
AR073136A1 (es) Compuestos de pirrol
AR086590A1 (es) Compuestos de ciclohexanona y herbicidas que los comprenden
AR072229A1 (es) Derivados de n- oxido pirazina sustituidos
AR111682A1 (es) Derivados de imidazopirimidina con sustituyentes fenilo y piridilo que contienen azufre
EA201401083A1 (ru) Применение ингибиторов ccr3
RU2010108943A (ru) Новые пиперазинамидные производные