AR080327A1 - Tienopirimidinas que contienen heterocicloalquilo 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 heterocicloalquilo 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.Info
- Publication number
- AR080327A1 AR080327A1 ARP110100601A ARP110100601A AR080327A1 AR 080327 A1 AR080327 A1 AR 080327A1 AR P110100601 A ARP110100601 A AR P110100601A AR P110100601 A ARP110100601 A AR P110100601A AR 080327 A1 AR080327 A1 AR 080327A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- group
- substituted
- phenyl
- 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 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000004069 aziridinyl group Chemical group 0.000 abstract 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 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
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
- 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
- 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
- A61P7/06—Antianaemics
-
- 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
-
- 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)
- 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)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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 H, halogeno, CN, CH3 o CF3, R2 es un grupo seleccionado de (2) donde el grupo puede estar sustituido en el átomo de nitrogeno con (3) -SO2-(alquilo C1-3), -CO-(alquilo C1-3), -CO-(CH2)n-O-(alquilo C1-3), -CO-(CH2)n-N(alquilo C1-3)2, alquilo C1-4, -(CH2)n-CF3, -(CH2)n-CHF2, -(CH2)n-OH, -(CH2)n-O-(alquilo C1-3), -(CH2)n-CN, (4) y donde puede estar sustituido en un átomo de carbono con un grupo -CH2OH, donde n es 1 o 2, y donde el grupo puede estar sustituido en el átomo de nitrogeno con alquilo (3) C1-4 lineal o ramificado, -(CH2)n-CF3, -(CH2)n-CHF2, -(CH2)n-OH, -(CH2)n-O-(aIquilo C1-3), -(CH2)n-CN, -(CH2)n-CO-N(alquilo C1-3)2, -SO2-(aIquilo C1-3), -CO-(alquilo C1-3), -CO2(alquilo C1-4), -CO2-(CH2)n-CF3, -CO2-(CH2)n-O-(alquilo C1-3), -CO2-(CH2)n-CO-N(alquilo C1-3)2, (4) donde n es 1 o 2, R3 un grupo alquilo C1-2, y R4 es -COOH, -CO2(alquilo C1-3), -CO2-(CH2)n-N(alquilo C1-3)2, -CONH2, -CO-NHR5, -CO-NH-(CH2)p-R6, -CO-NH-(CH2)m-R7, -CO-N(CH3)-(CH2)m-R7, CO-N(CH3)-(CH2)-ciclohexilo, (5), R5 es -CN, -OH, alquilo C1-6 lineal o ramificado, -O(alquilo C1-3), cicloalquilo C3-6, -SO2-(alquilo C1-3); pirazolilo opcionalmente sustituido con metilo; o piperidinilo opcionalmente sustituido con metilo, donde el grupo cicloalquilo C3-6 puede estar sustituido con -NH2, -OH u -OCH3; R6 es -C(CH3)2Cl; -C(CH3)2OH; -CHC3-6 cicloalquilo, que está opcionalmente sustituido con OH; imidazolilo, que está opcionalmente sustituido con metilo; pirrolidinilo, que está opcionalmente sustituido con alquilo C1-3 o con un grupo oxo; tetrahidrofuranilo; tetrahidropiranilo; fenilo, que está opcionalmente sustituido con uno o dos -F, -CI, -CN, -OH, alquilo C1-3 u -O(alquilo C1-3); naftilo; piridinilo; furanilo; tiofenilo; oxazolilo; tiazolilo; pirazolilo; morfolinilo, que está opcionalmente sustituido con metilo; benzotiofenilo; -CO-fenilo; o -SO2-N(alquilo C1-3)2, y R7 es F, -OH, -OCF3, -O-(alquilo C1-3), -O-fenilo, -O(CH2)m-OH, -N(alquilo C1-3)2, -NH-fenilo, piperidinilo, pirrolidinilo, azetedinilo o aziridinilo, y donde el átomo de hidrogeno en los grupos NH puede reemplazarse con alquilo C1-3, donde p es 1, 2 o 3, y m es 2 o 3, o un tautomero, enantiomero, díastereomero o la sal del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10154925 | 2010-02-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080327A1 true AR080327A1 (es) | 2012-03-28 |
Family
ID=43902874
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100601A AR080327A1 (es) | 2010-02-26 | 2011-02-25 | Tienopirimidinas que contienen heterocicloalquilo 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 (16)
| Country | Link |
|---|---|
| US (1) | US8648068B2 (es) |
| EP (1) | EP2539346B1 (es) |
| JP (1) | JP5639197B2 (es) |
| KR (1) | KR20120130052A (es) |
| CN (1) | CN102869669A (es) |
| AR (1) | AR080327A1 (es) |
| AU (1) | AU2011219761A1 (es) |
| BR (1) | BR112012021264A2 (es) |
| CA (1) | CA2791105A1 (es) |
| CL (1) | CL2012002318A1 (es) |
| EA (1) | EA201201193A1 (es) |
| MX (1) | MX2012009409A (es) |
| PH (1) | PH12012501691A1 (es) |
| TW (1) | TW201141482A (es) |
| UY (1) | UY33241A (es) |
| WO (1) | WO2011104337A1 (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006261082B2 (en) * | 2005-06-22 | 2012-04-19 | Boehringer Ingelheim International Gmbh | Thienopyrimidines for pharmaceutical compositions |
| CA2651898A1 (en) * | 2006-04-07 | 2007-10-18 | Develogen Aktiengesellschaft | Thienopyrimidines having mnk1/mnk2 inhibiting activity for pharmaceutical compositions |
| EP1889847A1 (en) * | 2006-07-10 | 2008-02-20 | DeveloGen Aktiengesellschaft | Pyrrolopyrimidines for pharmaceutical compositions |
| BRPI0918971A2 (pt) | 2008-08-26 | 2015-12-01 | Boehringer Ingelheim Int | tienopirimidinas para composições farmacêuticas |
| MX2012009735A (es) * | 2010-02-26 | 2012-09-12 | Boehringer Ingelheim Int | 4-[cicloalquiloxi (hetero) arilamino] tieno [2,3-d] pirimidinas que tienen actividad inhibitoria de mnk1/mnk2 para composiciones farmaceuticas. |
| CN102858771A (zh) | 2010-02-26 | 2013-01-02 | 日本烟草产业株式会社 | 1,3,4,8-四氢-2H-吡啶并[1,2-a]吡嗪衍生物及其作为HIV整合酶抑制剂的用途 |
| UY33241A (es) | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| ES2562959T3 (es) * | 2010-02-26 | 2016-03-09 | Evotec International Gmbh | Tienopirimidinas que contienen un grupo alquilo sustituido para composiciones farmacéuticas |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| US10280168B2 (en) | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| CN104507950B (zh) | 2012-05-21 | 2017-03-22 | 拜耳医药股份有限公司 | 噻吩并嘧啶 |
| CN104470931B (zh) | 2012-05-21 | 2016-10-26 | 拜耳医药股份有限公司 | 取代的苯并噻吩并嘧啶 |
| US20150182490A1 (en) | 2012-06-26 | 2015-07-02 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof |
| 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 |
| CN105189518A (zh) | 2013-02-01 | 2015-12-23 | 拜耳制药股份公司 | 取代的噻吩并吡啶和其药物用途 |
| US9556181B2 (en) | 2013-02-01 | 2017-01-31 | Bayer Pharma Aktiengesellschaft | Substituted pyrazolopyrimidinylamino-indazoles |
| HK1220972A1 (zh) | 2013-03-06 | 2017-05-19 | Bayer Pharma Aktiengesellschaft | 取代的噻唑并嘧啶 |
| CN105492011A (zh) | 2013-04-08 | 2016-04-13 | 丹尼斯·M·布朗 | 不理想给药化学化合物的治疗增效 |
| CN103356626B (zh) * | 2013-08-02 | 2015-01-07 | 上海市第十人民医院 | 吡唑并嘧啶类化合物在制备抗红色毛癣菌感染疾病药物中的应用 |
| CN103417545B (zh) * | 2013-08-02 | 2014-12-31 | 上海市第十人民医院 | 一种吡唑并嘧啶类化合物在制备抗烟曲霉菌感染性疾病药物中的应用 |
| CN103356627B (zh) * | 2013-08-02 | 2014-10-29 | 上海市第十人民医院 | 一种药物在光滑假丝酵母菌感染性疾病应用 |
| CN103356625B (zh) * | 2013-08-02 | 2014-10-29 | 上海市第十人民医院 | 嗓唑并嘧啶类在近平滑假丝酵母菌感染性疾病应用 |
| CN103356628B (zh) * | 2013-08-02 | 2014-10-29 | 上海市第十人民医院 | 嗓唑并嘧啶类化合物在制药中的应用 |
| CN103356624B (zh) * | 2013-08-02 | 2014-12-31 | 上海市第十人民医院 | 一种嘧啶类化合物在制备抗真菌药物中的应用 |
| US9512084B2 (en) * | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
| US10093660B2 (en) * | 2013-12-04 | 2018-10-09 | Evotec Internatonal 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 |
| JP6479854B2 (ja) * | 2014-05-07 | 2019-03-06 | エヴォテック・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Ｅｖｏｔｅｃ Ｉｎｔｅｒｎａｔｉｏｎａｌ ＧｍｂＨ | 医薬組成物のためのスルホキシイミン置換キナゾリン |
| GB201520500D0 (en) * | 2015-11-20 | 2016-01-06 | Medical Res Council Technology | Compounds |
| JP2019510061A (ja) * | 2016-03-31 | 2019-04-11 | サウス オーストラリアン ヘルス アンド メディカル リサーチ インスティテュート リミテッドＳｏｕｔｈ Ａｕｓｔｒａｌｉａｎ Ｈｅａｌｔｈ Ａｎｄ Ｍｅｄｉｃａｌ Ｒｅｓｅａｒｃｈ Ｉｎｓｔｉｔｕｔｅ Ｌｉｍｉｔｅｄ | 高脂肪食関連疾患を阻害する方法 |
| WO2019023651A2 (en) * | 2017-07-28 | 2019-01-31 | Massachusetts Institute Of Technology | MODULATORS OF THE SMALL MOLECULE ANDROGEN RECEPTOR |
| WO2025222091A1 (en) * | 2024-04-19 | 2025-10-23 | The Penn State Research Foundation | Poly inflammatory kinase inhibitors and pharmaceutical compositions |
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 |
| AU651337B2 (en) | 1990-03-30 | 1994-07-21 | Dowelanco | Thienopyrimidine derivatives |
| TW370529B (en) | 1992-12-17 | 1999-09-21 | 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 |
| ES2109796T3 (es) | 1994-05-03 | 1998-01-16 | Ciba Geigy Ag | Derivados de pirrolopirimidilo con efecto antiproliferante. |
| 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 |
| SK6652000A3 (en) | 1997-11-11 | 2002-05-09 | Pfizer Prod 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 |
| AU2002363175A1 (en) | 2001-10-29 | 2003-05-12 | Develogen Aktiengesellschaft Fur Entwicklungsbiologische Forschung | 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 |
| DE602004012559T2 (de) | 2003-05-28 | 2009-04-30 | Universita Degli Studi Di Siena | 4-SUBSTITUIERTE DERIVATE VON PYRAZOLOi3,4-D PYRIMIDIN UND DEREN VERWENDUNGEN |
| AU2004249495A1 (en) | 2003-06-20 | 2004-12-29 | Ucb Pharma S.A. | Thienopyridone derivatives as kinase inhibitors |
| JP4712702B2 (ja) | 2003-07-24 | 2011-06-29 | バイエル・シエリング・フアーマ・アクチエンゲゼルシヤフト | 高増殖性疾患を処置するために有用な置換されたテトラヒドロベンゾチエノピリミジンアミン化合物 |
| 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 |
| SI1703902T1 (sl) | 2004-01-05 | 2011-02-28 | Merz Pharma Gmbh & Co Kgaa | Memantin za zdravljenje blage do zmerne Alzheimerjeve bolezni |
| TW200538120A (en) | 2004-02-20 | 2005-12-01 | Kirin Brewery | Compound having TGF-beta inhibitory activity and pharmaceutical composition containing same |
| JPWO2005095419A1 (ja) * | 2004-04-01 | 2008-02-21 | 武田薬品工業株式会社 | チアゾロピリミジン誘導体 |
| GB0412467D0 (en) | 2004-06-04 | 2004-07-07 | Astrazeneca Ab | Chemical compounds |
| CA2572331A1 (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 |
| WO2006094791A1 (en) | 2005-03-08 | 2006-09-14 | Develogen Aktiengesellschaft | Crystallographic structure of mnk-1 and mnk-2 proteins |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| WO2008041053A2 (en) | 2005-05-20 | 2008-04-10 | Methylgene, Inc. | Inhibitors of vegf receptor and hgf receptor signaling |
| AU2006261082B2 (en) | 2005-06-22 | 2012-04-19 | Boehringer Ingelheim International Gmbh | Thienopyrimidines for pharmaceutical compositions |
| US20070213305A1 (en) | 2005-11-02 | 2007-09-13 | Cytovia, Inc. | N-alkyl-N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof |
| 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 |
| WO2007059905A2 (en) * | 2005-11-25 | 2007-05-31 | Develogen Aktiengesellschaft | Thienopyrimidines treating inflammatory diseases |
| WO2007081517A2 (en) | 2005-12-21 | 2007-07-19 | Abbott Laboratories | Anti-viral compounds |
| US20080108611A1 (en) | 2006-01-19 | 2008-05-08 | Battista Kathleen A | Substituted thienopyrimidine kinase inhibitors |
| CA2651898A1 (en) | 2006-04-07 | 2007-10-18 | Develogen Aktiengesellschaft | Thienopyrimidines having mnk1/mnk2 inhibiting activity for pharmaceutical compositions |
| DE602007004618D1 (de) | 2006-06-22 | 2010-03-18 | Biovitrum Ab Publ | Pyridin- und pyrazinderivate als mnk-kinaseinhibitoren |
| EP1889847A1 (en) * | 2006-07-10 | 2008-02-20 | DeveloGen Aktiengesellschaft | Pyrrolopyrimidines for pharmaceutical compositions |
| CA2706203A1 (en) * | 2007-11-22 | 2009-05-28 | Boehringer Ingelheim International Gmbh | Use of mnk inhibitors for the treatment of alzheimer's disease |
| BRPI0819453A2 (pt) * | 2007-11-28 | 2014-10-07 | Dana Farber Cancer Inst Inc | Composto, métodos para tratar um distúrbio relacionado com atividade de cinase, para tratar câncer em um paciente, para inibir a atividade de cinase e para identificar um composto que modula a atividade de cinase de bcr-abl, composição farmacêutica, e, kit |
| CN101981959B (zh) | 2008-01-25 | 2014-08-20 | 华为技术有限公司 | 移动站设备及其数据传输方法 |
| US20100015708A1 (en) | 2008-06-18 | 2010-01-21 | Mdrna, Inc. | Ribonucleic acids with non-standard bases and uses thereof |
| BRPI0918971A2 (pt) | 2008-08-26 | 2015-12-01 | Boehringer Ingelheim Int | tienopirimidinas para composições farmacêuticas |
| UY33241A (es) | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| EP2539344B1 (en) * | 2010-02-26 | 2014-10-15 | Boehringer Ingelheim International GmbH | Halogen or cyano substituted thieno[2,3-d]pyrimidines having mnk1/ mnk2 inhibiting activity for pharmaceutical compositions |
| ES2562959T3 (es) * | 2010-02-26 | 2016-03-09 | Evotec International Gmbh | Tienopirimidinas que contienen un grupo alquilo sustituido para composiciones farmacéuticas |
| MX2012009735A (es) | 2010-02-26 | 2012-09-12 | Boehringer Ingelheim Int | 4-[cicloalquiloxi (hetero) arilamino] tieno [2,3-d] pirimidinas que tienen actividad inhibitoria de mnk1/mnk2 para composiciones farmaceuticas. |
| EP2567807B1 (de) | 2011-09-07 | 2016-05-11 | Nordex Energy GmbH | Verfahren zur Herstellung eines Windenergieanlagenrotorblattbauteils mit einem vorgefertigten Hauptgurt |
-
2011
- 2011-02-24 UY UY0001033241A patent/UY33241A/es not_active Application Discontinuation
- 2011-02-25 EP EP11707387.4A patent/EP2539346B1/en not_active Ceased
- 2011-02-25 MX MX2012009409A patent/MX2012009409A/es not_active Application Discontinuation
- 2011-02-25 TW TW100106540A patent/TW201141482A/zh unknown
- 2011-02-25 US US13/034,913 patent/US8648068B2/en not_active Expired - Fee Related
- 2011-02-25 AR ARP110100601A patent/AR080327A1/es unknown
- 2011-02-25 CN CN2011800209929A patent/CN102869669A/zh active Pending
- 2011-02-25 BR BR112012021264A patent/BR112012021264A2/pt not_active Application Discontinuation
- 2011-02-25 PH PH1/2012/501691A patent/PH12012501691A1/en unknown
- 2011-02-25 AU AU2011219761A patent/AU2011219761A1/en not_active Abandoned
- 2011-02-25 WO PCT/EP2011/052810 patent/WO2011104337A1/en not_active Ceased
- 2011-02-25 CA CA2791105A patent/CA2791105A1/en not_active Abandoned
- 2011-02-25 JP JP2012554347A patent/JP5639197B2/ja not_active Expired - Fee Related
- 2011-02-25 EA EA201201193A patent/EA201201193A1/ru unknown
- 2011-02-25 KR KR1020127022310A patent/KR20120130052A/ko not_active Withdrawn
-
2012
- 2012-08-21 CL CL2012002318A patent/CL2012002318A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PH12012501691A1 (en) | 2012-11-05 |
| UY33241A (es) | 2011-09-30 |
| CN102869669A (zh) | 2013-01-09 |
| JP2013520472A (ja) | 2013-06-06 |
| EP2539346A1 (en) | 2013-01-02 |
| EA201201193A1 (ru) | 2013-04-30 |
| BR112012021264A2 (pt) | 2016-05-17 |
| AU2011219761A1 (en) | 2012-08-16 |
| CL2012002318A1 (es) | 2012-11-23 |
| MX2012009409A (es) | 2012-09-07 |
| WO2011104337A1 (en) | 2011-09-01 |
| US8648068B2 (en) | 2014-02-11 |
| JP5639197B2 (ja) | 2014-12-10 |
| TW201141482A (en) | 2011-12-01 |
| US20110212102A1 (en) | 2011-09-01 |
| CA2791105A1 (en) | 2011-09-01 |
| KR20120130052A (ko) | 2012-11-28 |
| EP2539346B1 (en) | 2014-04-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR111466A1 (es) | Inhibidores de hdac6 selectivos | |
| HRP20191579T1 (hr) | Spojevi kao modulatori za ror gama | |
| AR092869A1 (es) | Alcoxipirazoles como activadores de guanilato ciclasa soluble | |
| MX2022008434A (es) | Herbicidas de piridazinona. | |
| AR075951A1 (es) | Dihidropiridin sulfonamidas y dihidropiridin sulfamidas como inhibidores de mek | |
| MX389921B (es) | Herbicidas de piperidinona. | |
| AR099785A1 (es) | Compuestos heteroarilos y su uso como medicamentos | |
| EA201591429A1 (ru) | 2,3-дизамещенные производные 1-ацил-4-амино-1,2,3,4-тетрагидрохинолинов и их применение в качестве ингибиторов бромодомена | |
| PE20091458A1 (es) | Compuestos heterociclicos antiviricos | |
| AR084011A1 (es) | Compuestos nitrogenados heterociclicos utiles para el tratamiento de infecciones por el virus sincitial respiratorio (rsv), proceso para prepararlos y composiciones farmaceuticas que los contienen | |
| AR073136A1 (es) | Compuestos de pirrol | |
| AR095208A1 (es) | Pirrolotriazinas como inhibidores del canal del ión potasio | |
| AR082519A1 (es) | Fenilamidinas que tienen alta actividad fungicida, y su utilizacion | |
| AR092253A1 (es) | Inhibidores de serina/treonina cinasa | |
| MX382891B (es) | Composiciones y métodos para tratar trastornos de proliferación. | |
| CO6571878A2 (es) | Composición de control de fitoenfermedades y su uso | |
| MX343611B (es) | Composicion de control de fitoenfermedades y su uso. | |
| MX2015014406A (es) | Carboxamidas fungicidas. | |
| CO6351734A2 (es) | Compuestos de amida utiles en terapia | |
| AR059621A1 (es) | Acidos 4- fenil- tiazol-5- carboxilicos y amidas de acidos 4- fenil- tiazol5 carboxilicos como inhibidores de la plk1 | |
| HRP20192279T1 (hr) | Novi spojevi imidazopiridazina i njihova uporaba | |
| AR095267A1 (es) | Compuestos inhibidores de la fosfodiesterasa del tipo 10a | |
| AR109774A1 (es) | Compuestos heterocíclicos y su uso en la prevención o el tratamiento de infecciones bacterianas | |
| AR088596A1 (es) | Compuestos de bencilamina sustituidos | |
| PE20191488A1 (es) | Activador de nrf2 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |