AR084970A1 - Derivados de tetrahidro-pirido-pirimidina, una composicion farmaceutica en base al compuesto y un proceso para su preparacion - Google Patents
Derivados de tetrahidro-pirido-pirimidina, una composicion farmaceutica en base al compuesto y un proceso para su preparacionInfo
- Publication number
- AR084970A1 AR084970A1 ARP110102390A ARP110102390A AR084970A1 AR 084970 A1 AR084970 A1 AR 084970A1 AR P110102390 A ARP110102390 A AR P110102390A AR P110102390 A ARP110102390 A AR P110102390A AR 084970 A1 AR084970 A1 AR 084970A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- amino
- alkylcarbonyl
- halo
- Prior art date
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Classifications
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- 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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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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]
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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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- 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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Otolaryngology (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Estos compuestos son adecuados para el tratamiento de un trastorno o de una enfermedad que sea mediada por la actividad de las enzimas de PI3K, como los trastornos autoinmunes, enfermedades inflamatorias y alérgicas.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 C1-8-amino, 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, acetitinilo, 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, hidroxialquilo 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, hidroxialquilo C1-8-carbonilo o alcoxilo C1-8-alquilo C1-8-carbonilo; 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, haloalquilo 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 halo-alquilo C1-4; y m se selecciona a partir de 0 ó 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36158910P | 2010-07-06 | 2010-07-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR084970A1 true AR084970A1 (es) | 2013-07-24 |
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 After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (39)
| Country | Link |
|---|---|
| US (9) | 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) |
| HK (1) | HK1179966A1 (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) |
| 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)
| 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 |
| SG195067A1 (en) | 2011-06-27 | 2013-12-30 | Novartis Ag | Solid forms and salts of tetrahydro-pyrido-pyrimidine derivatives |
| EP2790705B1 (en) * | 2011-12-15 | 2017-12-06 | Novartis AG | Use of inhibitors of the activity or function of pi3k |
| IN2014CN04174A (es) | 2011-12-22 | 2015-09-04 | Novartis Ag | |
| EA035391B1 (ru) | 2012-11-08 | 2020-06-05 | Ризен Фармасьютикалз Са | Фармацевтические композиции, содержащие ингибитор pde4 и ингибитор pi3-дельта или двойной ингибитор pi3-дельта-гамма киназы |
| EP2920171B1 (en) | 2012-11-16 | 2018-08-29 | Merck Sharp & Dohme Corp. | Purine inhibitors of human phosphatidylinositol 3-kinase delta |
| MX2015006192A (es) | 2012-11-16 | 2015-08-10 | Merck Sharp & Dohme | Inhibidores de purina de fosfatidilinositol 3-quinasa delta humana. |
| 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 |
| JP6462155B2 (ja) * | 2015-05-04 | 2019-01-30 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｂ型肝炎ウイルス感染症の治療用のＨＢｓＡｇ（ＨＢＶ表面抗原）及びＨＢＶ ＤＮＡ産生の阻害剤としてのテトラヒドロピリドピリミジン類及びテトラヒドロピリドピリジン類 |
| SG10202109655VA (en) | 2015-12-04 | 2021-10-28 | Novartis Ag | Compositions and methods for immunooncology |
| RU2749731C2 (ru) * | 2016-02-10 | 2021-06-16 | Новартис Аг | Применение ингибиторов активности или функции pi3k для лечения первичного синдрома шегрена |
| MX2019011272A (es) | 2017-03-22 | 2019-10-24 | Novartis Ag | Composiciones y metodos para inmunooncologia. |
| 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 |
| CN111867590B (zh) | 2017-07-13 | 2023-11-17 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| JP7290627B2 (ja) | 2017-08-17 | 2023-06-13 | ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム | Ａｔｒキナーゼの複素環式阻害剤 |
| 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)
| 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 |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | 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 |
| EP3103799B1 (en) | 1995-03-30 | 2018-06-06 | OSI Pharmaceuticals, LLC | 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 |
| CA2224435C (en) | 1995-07-06 | 2008-08-05 | Novartis Ag | Pyrrolopyrimidines and processes for the preparation thereof |
| 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 |
| IL126351A0 (en) | 1996-04-12 | 1999-05-09 | Warner Lambert Co | Irreversible inhibitors of tyrosine kinases |
| JP2000512990A (ja) | 1996-06-24 | 2000-10-03 | ファイザー・インク | 過増殖性疾患を処置するためのフェニルアミノ置換三環式誘導体 |
| NZ334821A (en) | 1996-08-30 | 2000-12-22 | Novartis Ag | Method for producing epothilones |
| 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 |
| DK1367057T3 (da) | 1996-11-18 | 2009-01-19 | Biotechnolog Forschung Gmbh | Epothiloner E og F |
| 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 |
| CA2322157C (en) | 1998-02-25 | 2012-05-29 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| EP1135470A2 (en) | 1998-11-20 | 2001-09-26 | 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) |
| NZ535616A (en) | 2000-11-07 | 2006-03-31 | Novartis Ag | Indolymaleimide derivatives as protein kinase c inhibitors |
| 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 |
| TWI324064B (en) | 2002-04-03 | 2010-05-01 | Novartis Ag | Indolylmaleimide derivatives |
| PL376844A1 (pl) | 2002-12-09 | 2006-01-09 | The Board Of Regents Of The University Of Texas System | Sposoby selektywnego hamowania kinazy tyrozynowej 3 z grupy Janus (JAK3) |
| JP4733986B2 (ja) | 2002-12-27 | 2011-07-27 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー | ＨＩＶインテグラーゼ阻害薬として有用なテトラヒドロ−４Ｈ−ピリド［１，２−ａ］ピリミジン類および関連する化合物 |
| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
| CN100465173C (zh) | 2004-01-12 | 2009-03-04 | 西托匹亚研究有限公司 | 选择性激酶抑制剂 |
| US20050165032A1 (en) * | 2004-01-23 | 2005-07-28 | Norman Mark H. | Vanilloid receptor ligands and their use in treatments |
| CN101912400B (zh) | 2004-06-11 | 2013-06-26 | 日本烟草产业株式会社 | 用于治疗癌症的5-氨基-2,4,7-三氧代-3,4,7,8-四氢-2H-吡啶并[2,3-d]嘧啶衍生物和相关化合物 |
| US20060128710A1 (en) | 2004-12-09 | 2006-06-15 | Chih-Hung Lee | Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof |
| CA2606760C (en) * | 2005-05-04 | 2014-12-23 | Renovis, Inc. | Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds and compositions thereof useful in the treatment of conditions associated with neurological and inflammatory disorders and disfunctions |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| EP2136639B1 (en) * | 2007-04-02 | 2016-03-09 | Evotec AG | Pyrid-2-yl fused heterocyclic compounds, and compositions and uses thereof |
| PL2139334T3 (pl) | 2007-04-17 | 2013-11-29 | Evotec Ag | Skondensowane związki heterocykliczne 2-cyjanofenylu i ich kompozycje i zastosowania |
| US20100298289A1 (en) | 2007-10-09 | 2010-11-25 | Ucb Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| ES2553340T3 (es) | 2007-12-12 | 2015-12-07 | Rigel Pharmaceuticals, Inc. | Compuestos de carboxamida, sulfonamida y amina para trastornos metabólicos |
| 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 |
| TW201102391A (en) | 2009-03-31 | 2011-01-16 | Biogen Idec 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 |
| US20100280067A1 (en) | 2009-04-30 | 2010-11-04 | Pakala Kumara Savithru Sarma | Inhibitors of acetyl-coa carboxylase |
| ES2659725T3 (es) | 2009-05-05 | 2018-03-19 | Dana-Farber Cancer Institute, Inc. | Inhibidores de EGFR y procedimiento de tratamiento de trastornos |
| 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 |
| JP2013516479A (ja) | 2010-01-06 | 2013-05-13 | ジョゼフ・ピー・エリコ | 標的薬物を開発する方法および組成物 |
| 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 |
| AU2011255218B2 (en) | 2010-05-21 | 2015-03-12 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| UA112517C2 (uk) | 2010-07-06 | 2016-09-26 | Новартіс Аг | Тетрагідропіридопіримідинові похідні |
| EP2790705B1 (en) | 2011-12-15 | 2017-12-06 | Novartis AG | Use of inhibitors of the activity or function of pi3k |
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