AR080328A1 - Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros - Google Patents
Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otrosInfo
- Publication number
- AR080328A1 AR080328A1 ARP110100602A ARP110100602A AR080328A1 AR 080328 A1 AR080328 A1 AR 080328A1 AR P110100602 A ARP110100602 A AR P110100602A AR P110100602 A ARP110100602 A AR P110100602A AR 080328 A1 AR080328 A1 AR 080328A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- alkyl
- alkyl group
- group
- tienopirimidines
- Prior art date
Links
- 102100026299 MAP kinase-interacting serine/threonine-protein kinase 1 Human genes 0.000 title 1
- 101710139011 MAP kinase-interacting serine/threonine-protein kinase 1 Proteins 0.000 title 1
- 102100033610 MAP kinase-interacting serine/threonine-protein kinase 2 Human genes 0.000 title 1
- 101710138999 MAP kinase-interacting serine/threonine-protein kinase 2 Proteins 0.000 title 1
- 206010012601 diabetes mellitus Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 208000030159 metabolic disease Diseases 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- -1 more preferably Me Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicacion 1: Un compuesto caracterizado porque tiene la formula general (1), en la que X es CH o N, R1 es un átomo de hidrogeno o halogeno o CN o un grupo alquilo C1-3 o CONH2, R2 es un grupo alquilo C1-6 de cadena lineal o ramificada que está sustituido independientemente con uno o dos átomos de fluor, o uno o dos grupos trifluorometilo, tetrahidropiranilo, ciclopropilo, H2N-CO-, R5NHCO- o (R5)2N-CO-, en la que el grupo ciclopropilo anteriormente mencionado puede estar sustituido con uno o dos F o -CH2-CN, y en la que los dos grupos R5 junto con el átomo de N al que están unidos pueden formar un anillo de 4 a 8 miembros, en el que un átomo de carbono puede estar sustituido por un O, S, SO, SO2 y/o que puede estar sustituido con OH, NH2, N(alquil-C1-3)2, NH(alquil C1-3), CF3 o alquilo-C1-3, o un grupo alquilo C2-6 de cadena lineal o ramificada que está sustituido independientemente en la posicion 2 a 6 con uno o dos grupos hidroxi, alcoxi C1-3, amino, CN, R5NH-, (R5)2N-, R5OCONH-, R5CONH-, R5SO2NH-, R5NHCONH-, en el que R5 es un grupo alquilo C1-5, preferiblemente un grupo alquilo C1-4, más preferiblemente Me, i-Pr o t-Bu, cada uno opcionalmente sustituido con un grupo CF3, NH2, NH(alquil C1-3), N(alquil C1-3)2 o MeO-, y en el que los átomos de hidrogeno de cualquiera de los restos NH anteriormente mencionados pueden estar sustituidos por metilo, R3 es un grupo alquilo C1-2 y R4 es un grupo carboxi, alcoxi C1-3-carbonilo, -CONH2, -CONHR7, -CONH-OR7, -CONH-SO2R7 o -CO-NH-L-R6, en el que L es un -(CH2)-, -CH2-C:::C-CH2, o (2) R6 es OH, -NH2, -NHR7, -N(R7)2, -NH-CO2R7 o una amina cíclica de 3 a 6 miembros tal como pirrolidina o piperidina, n es 2 o 3 y R7 es alquilo C1-4 preferiblemente metilo, o una sal del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10154930 | 2010-02-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080328A1 true AR080328A1 (es) | 2012-03-28 |
Family
ID=43970925
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100602A AR080328A1 (es) | 2010-02-26 | 2011-02-25 | Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8853193B2 (es) |
| EP (1) | EP2539343B1 (es) |
| JP (1) | JP5575275B2 (es) |
| KR (1) | KR20120131171A (es) |
| CN (1) | CN102858783A (es) |
| AR (1) | AR080328A1 (es) |
| AU (1) | AU2011219764A1 (es) |
| BR (1) | BR112012021453A2 (es) |
| CA (1) | CA2791114A1 (es) |
| CL (1) | CL2012002319A1 (es) |
| EA (1) | EA201201192A1 (es) |
| ES (1) | ES2562959T3 (es) |
| IL (1) | IL221164A0 (es) |
| MX (1) | MX2012009851A (es) |
| PH (1) | PH12012501692A1 (es) |
| TW (1) | TW201141483A (es) |
| UY (1) | UY33245A (es) |
| WO (1) | WO2011104340A1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5302883B2 (ja) | 2006-04-07 | 2013-10-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 医薬組成物用のｍｎｋ１／ｍｎｋ２阻害活性を有するチエノピリミジン |
| EP1889847A1 (en) | 2006-07-10 | 2008-02-20 | DeveloGen Aktiengesellschaft | Pyrrolopyrimidines for pharmaceutical compositions |
| KR20110045019A (ko) | 2008-08-26 | 2011-05-03 | 베링거 인겔하임 인터내셔날 게엠베하 | 약제학적 조성물을 위한 티에노피리미딘 |
| MX2012009869A (es) | 2010-02-26 | 2012-09-12 | Japan Tobacco Inc | Derivado de 1, 3,4, 8-tetrahidro-2h-pirido[1, 2-a]pirazina y sus uso como inhibidor de la integrasa del vih. |
| EA201201191A1 (ru) | 2010-02-26 | 2013-04-30 | Бёрингер Ингельхайм Интернациональ Гмбх | 4-[циклоалкилокси(гетеро)ариламино]тиено[2,3-d]пиримидины, обладающие ингибирующей активностью по отношению к mnkl/mnk2, предназначенные для фармацевтических композиций |
| UY33241A (es) * | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| AR080328A1 (es) | 2010-02-26 | 2012-03-28 | Boehringer Ingelheim Int | Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros |
| EP2852596B1 (en) | 2012-05-21 | 2016-06-22 | Bayer Pharma Aktiengesellschaft | Thienopyrimidines |
| CA2873967A1 (en) | 2012-05-21 | 2013-11-28 | Bayer Pharma Aktiengesellschaft | Substituted benzothienopyrimidines |
| SG10201610869TA (en) | 2012-06-26 | 2017-02-27 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalacti |
| TW201412740A (zh) | 2012-09-20 | 2014-04-01 | Bayer Pharma AG | 經取代之吡咯并嘧啶胺基苯并噻唑酮 |
| EP2917185B1 (en) | 2012-11-09 | 2017-05-10 | Evotec International GmbH | Sulfoximine substituted quinazolines for pharmaceutical compositions |
| CA2899665A1 (en) | 2013-02-01 | 2014-08-07 | Bayer Pharma Aktiengesellschaft | Substituted thienopyrimidines and pharmaceutical use thereof |
| EP2951175B1 (en) | 2013-02-01 | 2017-10-04 | Bayer Pharma Aktiengesellschaft | Substituted pyrazolopyrimidinylamino-indazoles |
| WO2014135480A1 (en) | 2013-03-06 | 2014-09-12 | Bayer Pharma Aktiengesellschaft | Substituted thiazolopyrimidines |
| EP2983674A4 (en) | 2013-04-08 | 2017-05-10 | Dennis M. Brown | Therapeutic benefit of suboptimally administered chemical compounds |
| DK3013805T3 (en) | 2013-06-28 | 2018-04-23 | Evotec Int Gmbh | Sulfoximine-substituted quinazolines and their use as MNK1 and / or MNK2 kinase inhibitors |
| PE20160125A1 (es) * | 2013-07-08 | 2016-03-17 | Bayer Pharma AG | Pirazolpiridinas sustituidas |
| US9512084B2 (en) * | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
| AU2014359456B2 (en) | 2013-12-04 | 2019-01-24 | Evotec International Gmbh | Sulfoximine substituted quinazolines for pharmaceutical compositions |
| WO2015091156A1 (en) | 2013-12-17 | 2015-06-25 | Boehringer Ingelheim International Gmbh | Sulfoximine substituted pyrrolotriazines for pharmaceutical compositions |
| AU2015257917C1 (en) * | 2014-05-07 | 2019-03-14 | Evotec International Gmbh | Sulfoximine substituted quinazolines for pharmaceutical compositions |
| GB201520500D0 (en) * | 2015-11-20 | 2016-01-06 | Medical Res Council Technology | Compounds |
| GB201520499D0 (en) | 2015-11-20 | 2016-01-06 | Medical Res Council Technology | Compounds |
| AU2017239932A1 (en) * | 2016-03-31 | 2018-10-25 | Ocean University Of China | Method of inhibiting high fat diet-related conditions |
| WO2019023651A2 (en) * | 2017-07-28 | 2019-01-31 | Massachusetts Institute Of Technology | MODULATORS OF THE SMALL MOLECULE ANDROGEN RECEPTOR |
| WO2020139701A1 (en) * | 2018-12-28 | 2020-07-02 | Kronos Bio, Inc. | Compounds, compositions, and methods for modulating androgen receptor activity |
| WO2021241725A1 (ja) * | 2020-05-29 | 2021-12-02 | 富士フイルム富山化学株式会社 | 高純度のｎ－（５－メトキシ―２－フェノキシフェニル）メタンスルホンアミド及びその製造方法 |
| KR102766048B1 (ko) | 2021-11-17 | 2025-02-13 | 중앙대학교 산학협력단 | 티에노피리미딘 유도체를 유효성분으로 함유하는 lrrk2 억제용 조성물 |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH408945A (de) | 1956-02-10 | 1966-03-15 | Ciba Geigy | Verfahren zur Herstellung von heterocyclischen Verbindungen |
| DE3036390A1 (de) | 1980-09-26 | 1982-05-13 | Troponwerke GmbH & Co KG, 5000 Köln | Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen |
| DD248593A1 (de) | 1985-01-11 | 1987-08-12 | Univ Halle Wittenberg | Verfahren zur herstellung von 4-basischsubstituierten thieno/2,3-d/pyrimidin-6-ylcarbonsaeureestern |
| DE4008726A1 (de) | 1990-03-19 | 1991-09-26 | Basf Ag | Thieno(2,3-d)pyrimidinderivate |
| EP0452002A3 (en) | 1990-03-30 | 1992-02-26 | Dowelanco | Thienopyrimidine derivatives |
| TW444018B (en) | 1992-12-17 | 2001-07-01 | Pfizer | Pyrazolopyrimidines |
| IL112249A (en) | 1994-01-25 | 2001-11-25 | Warner Lambert Co | Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds |
| DE59500788D1 (de) | 1994-05-03 | 1997-11-20 | Ciba Geigy Ag | Pyrrolopyrimidinderivate mit antiproliferativer Wirkung |
| EP0729758A3 (en) | 1995-03-02 | 1997-10-29 | Pfizer | Pyrazolopyrimidines and pyrrolopyrimidines for the treatment of neuronal and other diseases |
| US6395733B1 (en) | 1995-06-07 | 2002-05-28 | Pfizer Inc | Heterocyclic ring-fused pyrimidine derivatives |
| AR004010A1 (es) | 1995-10-11 | 1998-09-30 | Glaxo Group Ltd | Compuestos heterociclicos |
| WO1999024440A1 (en) | 1997-11-11 | 1999-05-20 | Pfizer Products Inc. | Thienopyrimidine and thienopyridine derivatives useful as anticancer agents |
| US20030162795A1 (en) | 1998-10-22 | 2003-08-28 | Pfizer Inc. | Thienopyrimidine and thienopyridine derivatives useful as anticancer agents |
| GB9906566D0 (en) | 1999-03-23 | 1999-05-19 | Zeneca Ltd | Chemical compounds |
| HK1045306A1 (zh) | 1999-06-03 | 2002-11-22 | Abbott Laboratories | 抑制细胞黏附的抗炎化合物 |
| US6643277B2 (en) | 2000-06-29 | 2003-11-04 | Harris Broadband Wireless Access, Inc. | Frequency re-use for point to multipoint applications |
| JP2002020386A (ja) * | 2000-07-07 | 2002-01-23 | Ono Pharmaceut Co Ltd | ピラゾロピリジン誘導体 |
| CN101100472A (zh) | 2001-04-30 | 2008-01-09 | 美国拜尔公司 | 4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物及其应用 |
| SE0102147D0 (sv) | 2001-06-18 | 2001-06-18 | Pharmacia Ab | New methods |
| US20050080026A1 (en) | 2001-10-29 | 2005-04-14 | Arnd Steuernagel | Mnk kinase homologous proteins involved in the regulation of energy homeostasis and organelle metabolism |
| WO2004037159A2 (en) | 2002-10-23 | 2004-05-06 | Obetherapy Biotechnology | Compounds, compositions and methods for modulating fat metabolism |
| US20050012622A1 (en) | 2003-05-19 | 2005-01-20 | Sutton William R. | Monitoring and control of sleep cycles |
| CA2527496C (en) | 2003-05-28 | 2012-08-14 | Francesco Bondavalli | 4-substituted derivatives of pyrazolo [3,4-d] pyrimidine and pyrrolo [2,3-d] pyrimidine and uses thereof |
| EP1641804A1 (en) | 2003-06-20 | 2006-04-05 | Celltech R & D Limited | Thienopyridone derivatives as kinase inhibitors |
| CA2530281C (en) | 2003-07-24 | 2013-02-12 | Bayer Pharmaceuticals Corporation | Substituted tetrahydrobenzothienopyrimidinamine compounds useful for treating hyper-proliferative disorders |
| US7419978B2 (en) | 2003-10-22 | 2008-09-02 | Bristol-Myers Squibb Company | Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors |
| DE10351436A1 (de) * | 2003-11-04 | 2005-06-09 | Merck Patent Gmbh | Verwendung von Thienopyrimidinen |
| AU2005204358B2 (en) | 2004-01-05 | 2008-09-04 | Merz Pharma Gmbh & Co. Kgaa | Memantine for the treatment of mild and mild-to-moderate Alzheimer's disease |
| WO2005080377A1 (ja) | 2004-02-20 | 2005-09-01 | Kirin Beer Kabushiki Kaisha | TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物 |
| US20080269238A1 (en) * | 2004-04-01 | 2008-10-30 | Takeda Pharmaceutical Company Limited | Thiazolopyrimidine Derivative |
| GB0412467D0 (en) | 2004-06-04 | 2004-07-07 | Astrazeneca Ab | Chemical compounds |
| WO2006014325A2 (en) | 2004-07-02 | 2006-02-09 | Exelixis, Inc. | C-met modulators and method of use |
| EP1746099A1 (en) | 2004-12-23 | 2007-01-24 | DeveloGen Aktiengesellschaft | Mnk1 or Mnk2 inhibitors |
| US7943357B2 (en) | 2005-03-08 | 2011-05-17 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Crystallographic structure of Mnk-1 and Mnk-2 proteins |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| JP5148499B2 (ja) | 2005-05-20 | 2013-02-20 | メチルジーン インコーポレイテッド | Ｖｅｇｆ受容体およびｈｇｆ受容体シグナル伝達の阻害剤 |
| EP1899353A1 (en) | 2005-06-22 | 2008-03-19 | DeveloGen Aktiengesellschaft | Thienopyrimidines for pharmaceutical compositions |
| US20070099877A1 (en) | 2005-11-02 | 2007-05-03 | Cytovia, Inc. | N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof |
| WO2007056214A2 (en) | 2005-11-02 | 2007-05-18 | Cytovia, Inc | N-alkyl-n-aryl-thienopyrimidin-r-amines and uses thereof |
| WO2007059905A2 (en) | 2005-11-25 | 2007-05-31 | Develogen Aktiengesellschaft | Thienopyrimidines treating inflammatory diseases |
| US7915411B2 (en) | 2005-12-21 | 2011-03-29 | Abbott Laboratories | Anti-viral compounds |
| US20080108611A1 (en) * | 2006-01-19 | 2008-05-08 | Battista Kathleen A | Substituted thienopyrimidine kinase inhibitors |
| JP5302883B2 (ja) * | 2006-04-07 | 2013-10-02 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 医薬組成物用のｍｎｋ１／ｍｎｋ２阻害活性を有するチエノピリミジン |
| US20080039450A1 (en) | 2006-06-22 | 2008-02-14 | Jensen Annika J | Compounds |
| EP1889847A1 (en) * | 2006-07-10 | 2008-02-20 | DeveloGen Aktiengesellschaft | Pyrrolopyrimidines for pharmaceutical compositions |
| US20100247517A1 (en) | 2007-11-22 | 2010-09-30 | Boehringer Ingelheim Internationational GmbH | Use of mnk inhibitors for the treatment of alzheimer's disease |
| ES2734288T3 (es) * | 2007-11-28 | 2019-12-05 | Dana Farber Cancer Inst Inc | Inhibidores de miristato de moléculas pequeñas de Bcr-abl y métodos de uso |
| WO2009093662A1 (ja) | 2008-01-25 | 2009-07-30 | Sharp Kabushiki Kaisha | 移動局装置及びプログラム |
| US20100015708A1 (en) | 2008-06-18 | 2010-01-21 | Mdrna, Inc. | Ribonucleic acids with non-standard bases and uses thereof |
| KR20110045019A (ko) * | 2008-08-26 | 2011-05-03 | 베링거 인겔하임 인터내셔날 게엠베하 | 약제학적 조성물을 위한 티에노피리미딘 |
| EA201201191A1 (ru) | 2010-02-26 | 2013-04-30 | Бёрингер Ингельхайм Интернациональ Гмбх | 4-[циклоалкилокси(гетеро)ариламино]тиено[2,3-d]пиримидины, обладающие ингибирующей активностью по отношению к mnkl/mnk2, предназначенные для фармацевтических композиций |
| AR080328A1 (es) | 2010-02-26 | 2012-03-28 | Boehringer Ingelheim Int | Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros |
| US20130065914A1 (en) * | 2010-02-26 | 2013-03-14 | Boehringer Ingelheim International Gmbh | Halogen or cyano substituted thieno [2,3-d]pyrimidines having mnk1/mnk2 inhibiting activity for pharmaceutical compositions |
| UY33241A (es) * | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| DK2567807T3 (en) | 2011-09-07 | 2016-08-22 | Nordex Energy Gmbh | A process for producing a rotor blade-construction part for a wind power plant and of a previously prepared headband |
-
2011
- 2011-02-25 AR ARP110100602A patent/AR080328A1/es unknown
- 2011-02-25 KR KR1020127022314A patent/KR20120131171A/ko not_active Withdrawn
- 2011-02-25 UY UY0001033245A patent/UY33245A/es not_active Application Discontinuation
- 2011-02-25 CA CA2791114A patent/CA2791114A1/en not_active Abandoned
- 2011-02-25 WO PCT/EP2011/052813 patent/WO2011104340A1/en not_active Ceased
- 2011-02-25 EP EP11705567.3A patent/EP2539343B1/en active Active
- 2011-02-25 PH PH1/2012/501692A patent/PH12012501692A1/en unknown
- 2011-02-25 EA EA201201192A patent/EA201201192A1/ru unknown
- 2011-02-25 TW TW100106541A patent/TW201141483A/zh unknown
- 2011-02-25 BR BR112012021453A patent/BR112012021453A2/pt not_active IP Right Cessation
- 2011-02-25 JP JP2012554350A patent/JP5575275B2/ja not_active Expired - Fee Related
- 2011-02-25 US US13/035,023 patent/US8853193B2/en active Active
- 2011-02-25 ES ES11705567.3T patent/ES2562959T3/es active Active
- 2011-02-25 AU AU2011219764A patent/AU2011219764A1/en not_active Abandoned
- 2011-02-25 MX MX2012009851A patent/MX2012009851A/es not_active Application Discontinuation
- 2011-02-25 CN CN2011800209897A patent/CN102858783A/zh active Pending
-
2012
- 2012-07-29 IL IL221164A patent/IL221164A0/en unknown
- 2012-08-21 CL CL2012002319A patent/CL2012002319A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2562959T3 (es) | 2016-03-09 |
| JP5575275B2 (ja) | 2014-08-20 |
| BR112012021453A2 (pt) | 2017-02-21 |
| CL2012002319A1 (es) | 2012-10-12 |
| WO2011104340A1 (en) | 2011-09-01 |
| UY33245A (es) | 2011-09-30 |
| CN102858783A (zh) | 2013-01-02 |
| EA201201192A1 (ru) | 2013-04-30 |
| US20110212103A1 (en) | 2011-09-01 |
| PH12012501692A1 (en) | 2012-11-05 |
| AU2011219764A1 (en) | 2012-08-16 |
| IL221164A0 (en) | 2012-09-24 |
| JP2013520474A (ja) | 2013-06-06 |
| US8853193B2 (en) | 2014-10-07 |
| EP2539343A1 (en) | 2013-01-02 |
| TW201141483A (en) | 2011-12-01 |
| CA2791114A1 (en) | 2011-09-01 |
| EP2539343B1 (en) | 2015-12-30 |
| KR20120131171A (ko) | 2012-12-04 |
| MX2012009851A (es) | 2012-09-12 |
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