ECSP045115A - INDOL-2-CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa - Google Patents
INDOL-2-CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR XaInfo
- Publication number
- ECSP045115A ECSP045115A EC2004005115A ECSP045115A ECSP045115A EC SP045115 A ECSP045115 A EC SP045115A EC 2004005115 A EC2004005115 A EC 2004005115A EC SP045115 A ECSP045115 A EC SP045115A EC SP045115 A ECSP045115 A EC SP045115A
- Authority
- EC
- Ecuador
- Prior art keywords
- compounds
- factor
- formula
- factor viia
- relates
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 6
- 108010054265 Factor VIIa Proteins 0.000 abstract 4
- 108010074860 Factor Xa Proteins 0.000 abstract 4
- 229940012414 factor viia Drugs 0.000 abstract 4
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000002785 anti-thrombosis Effects 0.000 abstract 1
- 230000023555 blood coagulation Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229940127557 pharmaceutical product Drugs 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 230000002441 reversible effect Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/22—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an aralkyl radical attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Ceramic Engineering (AREA)
- Manufacturing & Machinery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Structural Engineering (AREA)
- Materials Engineering (AREA)
- Inorganic Chemistry (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la fórmula I en la que R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G Y M poseen los significados indicados en las reivindicaciones. Los compuestos de la fórmula I son compuestos valiosos, farmacológicamente activos. Estos compuestos ponen de manifiesto un fuerte efecto antitrombótico y son adecuados, por ejemplo, para el tratamiento terapéutico y la profilaxis de trastornos cardiovasculares tales como enfermedades tromboembólicas ó restenosis. Los compuestos son inhibidores reversibles de las enzimas de la coagulación sanguínea factor Xa (FXa) y/o factor VIIa (FVIIa) y, en general, pueden ser aplicados en condiciones en las que se encuentra presente una actividad indeseada de factor Xa y/o de factor VIIa ó para la curación ó prevención de la cual se pretende una inhibición del factor Xa y/o del factor VIIa. La invención se refiere, además, a procedimientos de preparación de compuestos de la fórmula I, a su uso, en particular como ingredientes activos en productos farmacéuticos, y a preparaciones farmacéuticas que los contienen.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01127809A EP1314733A1 (en) | 2001-11-22 | 2001-11-22 | Indole-2-carboxamides as factor Xa inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP045115A true ECSP045115A (es) | 2004-07-23 |
Family
ID=8179313
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2004005115A ECSP045115A (es) | 2001-11-22 | 2004-05-20 | INDOL-2-CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US6906084B2 (es) |
| EP (2) | EP1314733A1 (es) |
| JP (1) | JP4664592B2 (es) |
| KR (2) | KR100954508B1 (es) |
| CN (1) | CN1283638C (es) |
| AR (1) | AR037656A1 (es) |
| AU (1) | AU2002351918B2 (es) |
| BR (1) | BR0214396A (es) |
| CA (1) | CA2467374C (es) |
| CO (1) | CO5580764A2 (es) |
| EC (1) | ECSP045115A (es) |
| HR (1) | HRP20040453A2 (es) |
| HU (1) | HUP0402063A3 (es) |
| IL (2) | IL162105A0 (es) |
| MA (1) | MA27350A1 (es) |
| ME (1) | MEP43008A (es) |
| MX (1) | MXPA04004797A (es) |
| MY (1) | MY131516A (es) |
| NO (1) | NO327466B1 (es) |
| NZ (1) | NZ533044A (es) |
| OA (1) | OA12727A (es) |
| PE (1) | PE20030593A1 (es) |
| PL (1) | PL210986B1 (es) |
| RS (1) | RS40404A (es) |
| RU (1) | RU2299881C2 (es) |
| TN (1) | TNSN04091A1 (es) |
| TW (1) | TWI291950B (es) |
| UA (1) | UA78731C2 (es) |
| WO (1) | WO2003044014A1 (es) |
| ZA (1) | ZA200402945B (es) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101684091A (zh) * | 2001-11-14 | 2010-03-31 | 先灵公司 | 类大麻苷受体配体 |
| US7358268B2 (en) * | 2002-12-04 | 2008-04-15 | Sanofi-Aventis Deutschland Gmbh | Imidazole derivatives as factor Xa inhibitors |
| US7429581B2 (en) * | 2002-12-23 | 2008-09-30 | Sanofi-Aventis Deutschland Gmbh | Pyrazole-derivatives as factor Xa inhibitors |
| ES2337254T3 (es) | 2003-02-14 | 2010-04-22 | Glaxo Group Limited | Derivados de carboxamida. |
| US7539725B2 (en) * | 2003-04-03 | 2009-05-26 | Zix Corporation | Auditor system |
| EP1479675A1 (en) * | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Indazole-derivatives as factor Xa inhibitors |
| EP1479677A1 (en) * | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | New indole derivatives as factor xa inhibitors |
| EP1479680A1 (en) * | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Azaindole derivatives as Factor Xa inhibitors |
| US7741341B2 (en) | 2003-05-19 | 2010-06-22 | Sanofi-Aventis Deutschland Gmbh | Benzimidazole-derivatives as factor Xa inhibitors |
| US7223780B2 (en) * | 2003-05-19 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Triazole-derivatives as blood clotting enzyme factor Xa inhibitors |
| US7317027B2 (en) * | 2003-05-19 | 2008-01-08 | Sanofi-Aventis Deutschland Gmbh | Azaindole-derivatives as factor Xa inhibitors |
| WO2004108671A1 (en) * | 2003-06-06 | 2004-12-16 | Suven Life Sciences Limited | Substituted indoles with serotonin receptor affinity, process for their preparation and pharmaceutical compositions containing them |
| TWI372050B (en) | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| EP1568698A1 (en) | 2004-02-27 | 2005-08-31 | Aventis Pharma Deutschland GmbH | Pyrrole-derivatives as factor Xa inhibitors |
| EP1571154A1 (en) * | 2004-03-03 | 2005-09-07 | Aventis Pharma Deutschland GmbH | Beta-aminoacid-derivatives as factor Xa inhibitors |
| CA2570363A1 (en) | 2004-06-18 | 2005-12-29 | Biolipox Ab | Indoles useful in the treatment of inflammation |
| US7868037B2 (en) | 2004-07-14 | 2011-01-11 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| JP2008506702A (ja) | 2004-07-14 | 2008-03-06 | ピーティーシー セラピューティクス，インコーポレーテッド | Ｃ型肝炎を治療するための方法 |
| US7781478B2 (en) | 2004-07-14 | 2010-08-24 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| US7772271B2 (en) | 2004-07-14 | 2010-08-10 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| NZ553329A (en) | 2004-07-22 | 2010-09-30 | Ptc Therapeutics Inc | Thienopyridines for treating hepatitis C |
| FR2874015B1 (fr) * | 2004-08-05 | 2006-09-15 | Sanofi Synthelabo | Derives de n-(1h-indolyl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique |
| EP1807082A4 (en) | 2004-10-26 | 2010-12-01 | Janssen Pharmaceutica Nv | INHIBITOR COMPOUNDS OF XA FACTORS |
| EP1828152B1 (en) * | 2004-12-08 | 2008-08-20 | Bristol-Myers Squibb Company | Heterocyclic compounds as inhibitors of factor viia |
| EP2395000A1 (en) | 2004-12-30 | 2011-12-14 | Astex Therapeutics Limited | Benzimidazole compounds that modulate the activity of CDK, GSK and aurora kinases |
| FR2880625B1 (fr) * | 2005-01-07 | 2007-03-09 | Sanofi Aventis Sa | Derives de n-(heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique |
| AU2005325497A1 (en) | 2005-01-19 | 2006-07-27 | Biolipox Ab | Indoles useful in the treatment of inflammation |
| EP2308839B1 (en) | 2005-04-20 | 2017-03-01 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compounds |
| FR2888847B1 (fr) * | 2005-07-22 | 2007-08-31 | Sanofi Aventis Sa | Derives de n-(heteriaryl)-1-heteorarylalkyl-1h-indole-2- carboxamides, leur preparation et application en therapeutique |
| US8399666B2 (en) | 2005-11-04 | 2013-03-19 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| GB2431927B (en) | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| US7977359B2 (en) | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
| WO2007077435A1 (en) | 2005-12-30 | 2007-07-12 | Astex Therapeutics Limited | Pharmaceutical compounds |
| HRP20130058T1 (hr) * | 2006-01-24 | 2013-02-28 | Eli Lilly & Company | Indolsulfonamidni modulatori progesteronskih receptora |
| US7943622B2 (en) | 2006-06-06 | 2011-05-17 | Cornerstone Therapeutics, Inc. | Piperazines, pharmaceutical compositions and methods of use thereof |
| WO2008001115A2 (en) | 2006-06-29 | 2008-01-03 | Astex Therapeutics Limited | Pharmaceutical combinations of 1-cyclopropyl-3- [3- (5-m0rphoolin-4-ylmethyl-1h-benzoimidazol-2-yl) -lh-1-pyrazol- 4-yl] -urea |
| CA2682356C (en) * | 2007-04-16 | 2016-06-14 | Abbott Laboratories | 7-substituted indole mcl-1 inhibitors |
| BRPI0812594A2 (pt) * | 2007-08-10 | 2015-06-23 | Lundbeck & Co As H | Composto ou sal ou hidrato do mesmo, composição farmacêutica, métodos para modulação da atividade de um receptor p2x7, para tratamento de uma condição responsiva á modulação do receptor p2x7 em um paciente, para inibição de morte de células gangliônicas retinais em um paciente, para determinação da presença ou ausência de receptor p2x7 em uma amostra, preparação farmacêutica acondicionada, e, uso de um composto ou sal ou hidrato do mesmo. |
| TW200920369A (en) | 2007-10-26 | 2009-05-16 | Amira Pharmaceuticals Inc | 5-lipoxygenase activating protein (flap) inhibitor |
| NZ586651A (en) * | 2007-12-07 | 2012-06-29 | Abbott Gmbh & Co Kg | 5-halogen-substituted oxindole derivatives and use thereof for treating vasopressine-dependent diseases |
| EP2227463B1 (de) * | 2007-12-27 | 2016-08-17 | AbbVie Deutschland GmbH & Co KG | Substituierte oxindol-derivate und ihre verwendung zur behandlung von vasopressin-abhängigen erkrankungen |
| KR101247840B1 (ko) | 2008-02-22 | 2013-03-26 | 에프. 호프만-라 로슈 아게 | 아밀로이드 베타 조절제 |
| BRPI0912267A2 (pt) | 2008-05-23 | 2015-10-13 | Amira Pharmaceuticals Inc | sal farmaceuticamente aceitável, composição farmacêutica, artigo de fabricação, métodos para tratar asma, rinite alérgica, doença, lesões gástricas e dor, métodos para prevenir broncoconstrição e rinite alérgica, uso de um sal farmaceuticamente aceitável, e, processo para a preparação de um sal farmaceuticamente aceitável. |
| GB0813142D0 (en) | 2008-07-17 | 2008-08-27 | Glaxo Group Ltd | Novel compounds |
| GB0813144D0 (en) | 2008-07-17 | 2008-08-27 | Glaxo Group Ltd | Novel compounds |
| US8546431B2 (en) | 2008-10-01 | 2013-10-01 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| EP2448938B9 (en) | 2009-06-29 | 2015-06-10 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
| WO2011075643A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted heteroaryl fused derivatives as pi3k inhibitors |
| US8486967B2 (en) * | 2010-02-17 | 2013-07-16 | Hoffmann-La Roche Inc. | Heteroaryl substituted piperidines |
| EP2558463A1 (en) | 2010-04-14 | 2013-02-20 | Incyte Corporation | Fused derivatives as i3 inhibitors |
| US9062055B2 (en) | 2010-06-21 | 2015-06-23 | Incyte Corporation | Fused pyrrole derivatives as PI3K inhibitors |
| TW201249844A (en) | 2010-12-20 | 2012-12-16 | Incyte Corp | N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors |
| WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| FR2974576B1 (fr) * | 2011-04-29 | 2013-07-19 | Sanofi Aventis | Derives de n-[(1h-pyrazol-1-yl)aryl]-1h-indole ou 1h- indazole-3-carboxamide, leur preparation et leurs applications en therapeutique |
| KR102030609B1 (ko) | 2011-09-02 | 2019-10-11 | 인사이트 홀딩스 코포레이션 | Ｐｉ３ｋ 억제제로서 헤테로시클릴아민 |
| EP2819671A4 (en) * | 2012-02-29 | 2016-05-11 | Baruch S Blumberg Inst | INHIBITORS OF HEPATITIS B VIRUS WITH COVALENT CLOSED CIRCULAR DNA PREPARATION AND ITS USE METHOD |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| JP6325078B2 (ja) | 2013-03-15 | 2018-05-16 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | ヘテロ環式化合物およびその使用 |
| CN105829293B (zh) * | 2013-12-20 | 2018-11-09 | 中国人民解放军军事医学科学院毒物药物研究所 | 新型哌啶氨甲酰类化合物、制备方法及其用途 |
| WO2015176625A1 (zh) | 2014-05-22 | 2015-11-26 | 南京明德新药研发股份有限公司 | 作为凝血因子Xa抑制剂的酰肼类化合物 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| MX2017002985A (es) * | 2014-09-10 | 2017-11-17 | Epizyme Inc | Inhibidores de smyd. |
| JP6903580B2 (ja) | 2014-12-29 | 2021-07-14 | ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ | 乳酸脱水素酵素の小分子阻害剤及びその使用方法 |
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