CN102405047B - 结晶型的n-{(1s)-2-氨基-1-[(3-氟苯基)甲基]乙基}-5-氯-4-(4-氯-1-甲基-1h-吡唑-5-基)-2-噻吩甲酰胺盐酸盐 - Google Patents
结晶型的n-{(1s)-2-氨基-1-[(3-氟苯基)甲基]乙基}-5-氯-4-(4-氯-1-甲基-1h-吡唑-5-基)-2-噻吩甲酰胺盐酸盐 Download PDFInfo
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- CN102405047B CN102405047B CN201080015363.2A CN201080015363A CN102405047B CN 102405047 B CN102405047 B CN 102405047B CN 201080015363 A CN201080015363 A CN 201080015363A CN 102405047 B CN102405047 B CN 102405047B
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- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14849009P | 2009-01-30 | 2009-01-30 | |
| US61/148,490 | 2009-01-30 | ||
| PCT/US2010/022323 WO2010088331A1 (en) | 2009-01-30 | 2010-01-28 | Crystalline n-{(1-s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102405047A CN102405047A (zh) | 2012-04-04 |
| CN102405047B true CN102405047B (zh) | 2014-07-09 |
Family
ID=42395995
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080015363.2A Active CN102405047B (zh) | 2009-01-30 | 2010-01-28 | 结晶型的n-{(1s)-2-氨基-1-[(3-氟苯基)甲基]乙基}-5-氯-4-(4-氯-1-甲基-1h-吡唑-5-基)-2-噻吩甲酰胺盐酸盐 |
Country Status (25)
| Country | Link |
|---|---|
| US (5) | US8609711B2 (enExample) |
| EP (2) | EP4242206A1 (enExample) |
| JP (4) | JP2012516344A (enExample) |
| KR (1) | KR101420484B1 (enExample) |
| CN (1) | CN102405047B (enExample) |
| AR (1) | AR075153A1 (enExample) |
| AU (1) | AU2010208265B2 (enExample) |
| BR (1) | BRPI1006896B1 (enExample) |
| CA (1) | CA2750565C (enExample) |
| CL (1) | CL2011001830A1 (enExample) |
| CO (1) | CO6400189A2 (enExample) |
| CR (1) | CR20110422A (enExample) |
| EA (1) | EA018907B1 (enExample) |
| IL (1) | IL214023A (enExample) |
| MA (1) | MA32998B1 (enExample) |
| MX (1) | MX2011008073A (enExample) |
| MY (1) | MY161598A (enExample) |
| NZ (1) | NZ594064A (enExample) |
| PE (1) | PE20120003A1 (enExample) |
| SG (1) | SG172926A1 (enExample) |
| TW (1) | TWI503317B (enExample) |
| UA (1) | UA106740C2 (enExample) |
| UY (1) | UY32407A (enExample) |
| WO (1) | WO2010088331A1 (enExample) |
| ZA (1) | ZA201105033B (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2011008073A (es) | 2009-01-30 | 2011-11-18 | Glaxosmithkline Llc | Hidrocloruro de n-{(1-s)-2-amino -1-[(3-fluorofenil)metil]etil}-5- cloro-4-(4-cloro-1-metil-1h-pirazol-5-il)-2-tiofenocarboxamida cristalino. |
| US20130072507A1 (en) * | 2010-05-21 | 2013-03-21 | Glaxosmithkline Llc | Combination |
| WO2011150044A1 (en) * | 2010-05-26 | 2011-12-01 | Glaxosmithkline Llc | Combination |
| SG10201600077RA (en) * | 2011-01-11 | 2016-02-26 | Glaxosmithkline Llc | Combination |
| PE20142356A1 (es) | 2012-04-24 | 2015-01-30 | Glaxosmithkline Intellectual Property (N 2) Limited | Metodo de tratamiento de las dermatosis sensibles a los esteroides |
| CA2909434A1 (en) * | 2013-04-18 | 2014-10-23 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and pharmaceutical compositions for inhibiting lymphocyte proliferation in a subject in need thereof |
| US20160235714A1 (en) * | 2013-10-01 | 2016-08-18 | Novartis Ag | Enzalutamide in combination with afuresertib for the treatment of cancer |
| WO2015049649A1 (en) | 2013-10-01 | 2015-04-09 | Gbglaxosmithkline Intellectual Property (No.2) Limited | Combination |
| KR20160127754A (ko) * | 2014-03-12 | 2016-11-04 | 노파르티스 아게 | Btk 억제제 및 akt 억제제를 포함하는 조합물 |
| IL284875B (en) | 2016-10-11 | 2022-07-01 | Univ Duke | Zofoxifene treatment for breast cancer |
| JP6515944B2 (ja) | 2016-12-20 | 2019-05-22 | 株式会社デンソー | 半導体装置およびその製造方法 |
| EP3773524B1 (en) | 2018-04-10 | 2025-04-09 | Duke University | Lasofoxifene for the treatment of er+ breast cancer carrying the mutation d538g or y537s |
| BR112022001508A2 (pt) * | 2019-08-08 | 2022-07-12 | Laekna Ltd | Método de tratamento de câncer |
| US11915283B1 (en) | 2019-08-13 | 2024-02-27 | Splitcart Llc | Cost sharing platform and system |
| US12067592B2 (en) | 2019-08-13 | 2024-08-20 | Splitcart Llc | Co-purchasing system and method |
| GB202116903D0 (en) | 2021-11-18 | 2022-01-05 | Sermonix Pharmaceuticals Inc | Lasofoxifene treatment of aromatase-resistant er+ cancer |
| EP4493189A1 (en) | 2022-03-14 | 2025-01-22 | Laekna Limited | Combination treatment for cancer |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5369124A (en) * | 1992-10-02 | 1994-11-29 | Bayer Aktiengesellschaft | Substituted thiophenecarboxamides |
| CA2396561A1 (en) * | 1999-12-24 | 2001-07-05 | Bayer Aktiengesellschaft | Substituted oxazolidinones and their use in the field of blood coagulation |
| WO2002088107A1 (fr) * | 2001-04-26 | 2002-11-07 | Eisai Co., Ltd. | Compose azote a anneaux condenses possedant un groupe pyrazolyle et servant de substituant, et composition medicale le comprenant |
| US6982279B2 (en) * | 2000-12-12 | 2006-01-03 | Aventis Pharm Deutschland Gmbh | Arylated furan- and thiophenecarboxamides, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them |
| WO2008098104A1 (en) * | 2007-02-07 | 2008-08-14 | Smithkline Beecham Corporation | Inhibitors of akt activity |
Family Cites Families (137)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE758350A (fr) * | 1969-12-30 | 1971-05-03 | Pfizer | Procede de fabrication des sels mono- et bi-metalliques alcalins de l'alpha-carboxybenzylpenicilline |
| US4432987A (en) * | 1982-04-23 | 1984-02-21 | Pfizer Inc. | Crystalline benzenesulfonate salts of sultamicillin |
| CN1030415A (zh) | 1987-02-20 | 1989-01-18 | 山之内制药株式会社 | 饱和的杂环碳酰胺衍生物和它的制备方法 |
| ES2005163A6 (es) | 1987-04-14 | 1989-03-01 | Lilly S A E | Un procedimiento para la produccion de derivados de tiofen-2-carboxamida. |
| IE67334B1 (en) | 1988-03-16 | 1996-03-20 | Smithkline Beecham Farma | Heterocyclic derivatives |
| DE3810848A1 (de) | 1988-03-30 | 1989-10-19 | Boehringer Ingelheim Kg | Neue 2,3,4-substituierte imidazole und 3,4,5-substituierte 1,2,4-triazole, ihre herstellung und verwendung |
| US4999059A (en) * | 1989-08-11 | 1991-03-12 | Bagno Robert G | Universal solar concentrator panel |
| DE3927483A1 (de) | 1989-08-19 | 1991-02-21 | Boehringer Ingelheim Kg | Neue substituierte heterocyclische fuenfringe, ihre herstellung und verwendung |
| DE3933573A1 (de) | 1989-10-07 | 1991-04-18 | Basf Ag | Carbonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
| US5258357A (en) | 1989-10-07 | 1993-11-02 | Basf Aktiengesellschaft | Carboxamides, their preparation and their use as herbicides |
| US6645969B1 (en) | 1991-05-10 | 2003-11-11 | Aventis Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase |
| US5559235A (en) | 1991-10-29 | 1996-09-24 | Glaxo Wellcome Inc. | Water soluble camptothecin derivatives |
| US5595872A (en) | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| US5342947A (en) | 1992-10-09 | 1994-08-30 | Glaxo Inc. | Preparation of water soluble camptothecin derivatives |
| AU674553B2 (en) | 1992-10-14 | 1997-01-02 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| CA2146019A1 (en) | 1992-10-23 | 1994-05-11 | Howard B. Broughton | Dopamine receptor subtype ligands |
| ES2157254T3 (es) * | 1993-03-12 | 2001-08-16 | Upjohn Co | Ceftiofur (acido libre) cristalino. |
| DE69418045T2 (de) | 1993-08-06 | 1999-10-07 | Smithkline Beecham P.L.C., Brentford | Amidderivate als 5ht1d rezeptor antagonisten |
| US5681835A (en) | 1994-04-25 | 1997-10-28 | Glaxo Wellcome Inc. | Non-steroidal ligands for the estrogen receptor |
| US5491237A (en) | 1994-05-03 | 1996-02-13 | Glaxo Wellcome Inc. | Intermediates in pharmaceutical camptothecin preparation |
| US5668148A (en) | 1995-04-20 | 1997-09-16 | Merck & Co., Inc. | Alpha1a adrenergic receptor antagonists |
| JP3964478B2 (ja) | 1995-06-30 | 2007-08-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬 |
| CA2502764A1 (en) | 1995-08-22 | 1997-03-06 | Japan Tobacco Inc. | Amide compounds |
| US6001866A (en) | 1995-10-05 | 1999-12-14 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| WO1997012613A1 (en) | 1995-10-05 | 1997-04-10 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| US5972980A (en) | 1995-10-05 | 1999-10-26 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| AU6320998A (en) | 1997-02-21 | 1998-09-09 | Bristol-Myers Squibb Company | Benzoic acid derivatives and related compounds as antiarrhythmic agents |
| US5998336A (en) | 1997-02-26 | 1999-12-07 | The Board Of Trustees Of The Leland Stanford Junior University | Ceramic/metal and A15/metal superconducting composite materials exploiting the superconducting proximity effect and method of making the same |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
| AU751139B2 (en) | 1997-10-13 | 2002-08-08 | Astellas Pharma Inc. | Amide derivative |
| KR100349385B1 (ko) | 1997-12-12 | 2002-08-24 | 유로-셀티크 소시에떼 아노뉨 | 2-티오크산틴으로부터 얻어진 3-치환 아데닌 |
| US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
| AUPP433398A0 (en) | 1998-06-25 | 1998-07-16 | Australian National University, The | Compounds and processes |
| US6192967B1 (en) | 1998-10-19 | 2001-02-27 | Sunny En Liung Huang | Collapsible auto shade |
| US6130333A (en) | 1998-11-27 | 2000-10-10 | Monsanto Company | Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use |
| DE19904397A1 (de) | 1999-02-04 | 2000-08-10 | Bayer Ag | Verwendung von Pyrazol-Carbonsäureamiden |
| DE19904396A1 (de) | 1999-02-04 | 2000-08-10 | Bayer Ag | Substituierte Pyrazolbenzylamin-Derivate |
| JP2000256358A (ja) | 1999-03-10 | 2000-09-19 | Yamanouchi Pharmaceut Co Ltd | ピラゾール誘導体 |
| CN1353706A (zh) | 1999-04-13 | 2002-06-12 | 巴斯福股份公司 | 整合素受体配体 |
| AU5283900A (en) | 1999-05-24 | 2000-12-12 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
| AU5283800A (en) | 1999-05-24 | 2000-12-12 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
| JP2001247569A (ja) | 1999-08-12 | 2001-09-11 | Japan Tobacco Inc | ピロリジン誘導体又はピペリジン誘導体及びその医薬用途 |
| SK1812002A3 (en) * | 1999-08-12 | 2003-02-04 | Pharmacia Italia Spa | 3(5)-Amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| US6632815B2 (en) | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| US6770666B2 (en) | 1999-12-27 | 2004-08-03 | Japan Tobacco Inc. | Fused-ring compounds and use thereof as drugs |
| TR200103147T1 (tr) | 1999-12-27 | 2002-06-21 | Japan Tobacco Inc. | Kaynaşık halkalı bileşikler ve bunların ilaç olarak kullanımı. |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| GB0011098D0 (en) | 2000-05-08 | 2000-06-28 | Black James Foundation | Pharmaceutical compositions comprising protpn pump inhibitors and gastrin/cholecystokinin receptor ligands |
| EP1282418B1 (en) | 2000-05-19 | 2005-08-17 | Applied Research Systems ARS Holding N.V. | Use of pyrazole derivatives for treating infertility |
| US6589195B1 (en) * | 2000-05-26 | 2003-07-08 | Orthomerica Products, Inc. | Modular adjustable prophylactic hip orthosis and adduction/abduction joint |
| WO2002000647A1 (en) | 2000-06-23 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Heteroaryl-phenyl substituted factor xa inhibitors |
| US6624039B1 (en) * | 2000-07-13 | 2003-09-23 | Lucent Technologies Inc. | Alignment mark having a protective oxide layer for use with shallow trench isolation |
| AU2001277143A1 (en) | 2000-07-24 | 2002-02-05 | Davide Riccardo Grassetti | Inhibition of mutagenic effects of carcinogens |
| JO2654B1 (en) | 2000-09-04 | 2012-06-17 | شركة جانسين فارماسوتيكا ان. في | Multiple aryl caroxa amides are useful as lipid - lowering agents |
| WO2002064136A2 (en) | 2001-01-26 | 2002-08-22 | Chugai Seiyaku Kabushiki Kaisha | Malonyl-coa decarboxylase inhibitors useful as metabolic modulators |
| JP2004532234A (ja) | 2001-04-27 | 2004-10-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | トリアゾール由来キナーゼインヒビターおよびその使用 |
| MXPA04001087A (es) | 2001-08-03 | 2004-07-08 | Vertex Pharma | Derivados de pirazol como inhibidores de cinasa y uso de los mismos. |
| MXPA04001088A (es) | 2001-08-03 | 2004-05-20 | Vertex Pharma | Derivados de pirazol como inhibidores de cinasa y uso de los mismos. |
| JP2005508321A (ja) * | 2001-09-26 | 2005-03-31 | メルク エンド カムパニー インコーポレーテッド | 結晶形態のエルタペネムナトリウム |
| EP1441724B8 (en) | 2001-09-27 | 2007-10-17 | Laboratoires Serono SA | Methods of increasing endogenous testosterone levels |
| US6794252B2 (en) * | 2001-09-28 | 2004-09-21 | Texas Instruments Incorporated | Method and system for forming dual work function gate electrodes in a semiconductor device |
| US6897208B2 (en) | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
| WO2003039529A1 (en) | 2001-11-07 | 2003-05-15 | 4Sc A.G. | Selective antibacterial agents |
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| WO2003066629A2 (en) | 2002-02-06 | 2003-08-14 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| US7335779B2 (en) | 2002-03-08 | 2008-02-26 | Quonova, Llc | Modulation of pathogenicity |
| GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
| GB0206861D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Medicaments |
| US20050154202A1 (en) | 2002-04-05 | 2005-07-14 | Hagmann William K. | Substituted aryl amides |
| GB0216224D0 (en) | 2002-07-12 | 2002-08-21 | Glaxo Group Ltd | Compounds |
| BR0313160A (pt) | 2002-08-08 | 2005-07-12 | Smithkline Beecham Corp | Composto, composição farmacêutica, métodos para tratar uma condição e um neoplasmo suscetìvel em um animal em um animal, processo para preparar um composto e uso de um composto |
| US20040132726A1 (en) | 2002-08-09 | 2004-07-08 | Astrazeneca Ab And Nps Pharmaceuticals, Inc. | New compounds |
| US6649638B1 (en) | 2002-08-14 | 2003-11-18 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| WO2004016592A1 (en) | 2002-08-14 | 2004-02-26 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| ATE477251T1 (de) | 2002-08-23 | 2010-08-15 | Novartis Vaccines & Diagnostic | Pyrrolverbindungen als glykogen synthase kinase 3 inhibitoren |
| WO2004069805A1 (en) | 2003-02-10 | 2004-08-19 | Bayer Healthcare Ag | Bis(hetero)aryl carboxamide derivatives for use as pgi2 antagonists |
| WO2004072018A1 (ja) | 2003-02-12 | 2004-08-26 | Takeda Pharmaceutical Company Limited | アミン誘導体 |
| US7223788B2 (en) | 2003-02-14 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Substituted N-aryl heterocycles, process for their preparation and their use as medicaments |
| CA2512886A1 (en) | 2003-02-28 | 2004-09-10 | Galderma Research & Development, S.N.C. | Ligands that modulate lxr-type receptors |
| US7517887B2 (en) | 2003-04-09 | 2009-04-14 | General Atomics | Reversible inhibitors of S-adenosyl-L-homocysteine hydrolase and uses thereof |
| CA2523232A1 (en) | 2003-04-21 | 2004-11-04 | Elan Pharmaceuticals, Inc. | (hetero) arylamide 2-hydroxy-3-diaminoalkanes for use in the treatment of alzheimer's disease |
| BRPI0411674A (pt) | 2003-06-20 | 2006-08-29 | Galderma Res & Dev | compostos, composição cosmética, uso cosmético de uma composição, uso de um composto, composição farmacêutica, e processo cosmético para o embelezamento da pele |
| FR2857666B1 (fr) | 2003-07-15 | 2005-08-26 | Oreal | Composition tinctoriale comprenant a titre de coupleur un derive du furane et nouveaux derives du furane |
| DE602004030689D1 (de) | 2003-07-23 | 2011-02-03 | Synta Pharmaceuticals Corp | Verbindungen gegen entzündungen und immun-relevante verwendungen |
| ATE389651T1 (de) | 2003-08-15 | 2008-04-15 | Vertex Pharma | Als inhibitoren von c-met geeignete pyrrolzusammensetzungen |
| WO2005037198A2 (en) | 2003-10-06 | 2005-04-28 | Glaxo Group Limited | Preparation of 1,7-disubstituted azabenzimidazoles as kinase inhibitors |
| EP1670466A4 (en) | 2003-10-06 | 2007-04-25 | Glaxo Group Ltd | PREPARATION OF 1,6,7-TRISUBSTITUTED AZABENIC ZIMIDAZOLES AS KINASE-INHIBITORS |
| US7750160B2 (en) | 2003-11-13 | 2010-07-06 | Ambit Biosciences Corporation | Isoxazolyl urea derivatives as kinase modulators |
| NZ547327A (en) | 2003-11-21 | 2009-08-28 | Array Biopharma Inc | AKT protein kinase inhibitors |
| US20050145202A1 (en) * | 2004-01-05 | 2005-07-07 | James Bonner | Rigid dog leash |
| WO2005077435A1 (en) | 2004-01-19 | 2005-08-25 | Atul Kumar | A system for distending body tissue cavities by continuous flow irrigation |
| WO2005081954A2 (en) | 2004-02-25 | 2005-09-09 | Wyeth | Inhibitors of protein tyrosine phosphatase 1b |
| ES2551293T3 (es) | 2004-03-24 | 2015-11-17 | Abbvie Inc. | Inhibidores de quinasas de pirazol tricíclicos |
| WO2005095386A1 (en) | 2004-03-30 | 2005-10-13 | Chiron Corporation | Substituted thiophene derivatives as anti-cancer agents |
| JP2008502595A (ja) | 2004-03-31 | 2008-01-31 | エグゼリクシス, インコーポレイテッド | 未分化リンパ腫キナーゼモジュレータおよびその使用方法 |
| JP2005336172A (ja) | 2004-04-26 | 2005-12-08 | Japan Tobacco Inc | 腎虚血再灌流障害治療又は予防薬 |
| CA2568742A1 (en) | 2004-05-29 | 2005-12-08 | 7Tm Pharma A/S | Substituted thiazoleacetic as crth2 ligands |
| US20060135773A1 (en) | 2004-06-17 | 2006-06-22 | Semple Joseph E | Trisubstituted nitrogen modulators of tyrosine phosphatases |
| US7671077B2 (en) * | 2004-07-19 | 2010-03-02 | Leu-Fen Hou Lin | Neuroprotective small organic molecules, compositions and uses related thereto |
| JP2006066488A (ja) * | 2004-08-25 | 2006-03-09 | Mitsubishi Electric Corp | 半導体受光素子およびその製造方法 |
| US7365385B2 (en) * | 2004-08-30 | 2008-04-29 | Micron Technology, Inc. | DRAM layout with vertical FETs and method of formation |
| US20060043513A1 (en) * | 2004-09-02 | 2006-03-02 | Deok-Hoon Kim | Method of making camera module in wafer level |
| TW200616969A (en) | 2004-09-17 | 2006-06-01 | Tanabe Seiyaku Co | Imidazole compound |
| US20060062453A1 (en) * | 2004-09-23 | 2006-03-23 | Sharp Laboratories Of America, Inc. | Color highlighting document image processing |
| JP4937129B2 (ja) * | 2004-10-13 | 2012-05-23 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | 3−[5−クロロ−4−[(2,4−ジフルオロベンジル)オキシ]−6−オキソピリミジン−1(6h)−イル]−n−(2−ヒドロキシエチル)−4−メチルベンズアミドの結晶形 |
| DE102004051277A1 (de) | 2004-10-21 | 2006-04-27 | Merck Patent Gmbh | Heterocyclische Carbonylverbindungen |
| DE102004054666A1 (de) | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| MX2007003331A (es) | 2004-11-30 | 2007-06-05 | Neurosearch As | Nuevos derivados de arilo diazabiciclico. |
| JP2006232707A (ja) | 2005-02-23 | 2006-09-07 | Japan Tobacco Inc | 癌転移抑制剤 |
| CA2605603A1 (en) | 2005-04-22 | 2006-11-02 | Kalypsys, Inc. | Ortho-terphenyl inhibitors of p38 kinase and methods of treating inflammatory disorders |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| WO2006136823A1 (en) | 2005-06-21 | 2006-12-28 | Astex Therapeutics Limited | Heterocyclic containing amines as kinase b inhibitors |
| US20060288588A1 (en) | 2005-06-22 | 2006-12-28 | Frank Morabito | Garden tool |
| MA28394B1 (fr) | 2005-06-24 | 2007-01-02 | Genelabs Tech Inc | Derives d'heteroaryle pour traitement des virus |
| NZ564916A (en) | 2005-06-27 | 2011-03-31 | Exelixis Inc | Imidazole based LXR modulators |
| CN100494167C (zh) | 2005-08-02 | 2009-06-03 | 天津大学 | 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用 |
| GB0518237D0 (en) | 2005-09-07 | 2005-10-19 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| WO2007052843A1 (ja) | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
| US7838676B2 (en) | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
| JP2009519966A (ja) | 2005-12-14 | 2009-05-21 | ブリストル−マイヤーズ スクイブ カンパニー | セリンプロテアーゼ阻害剤として有用な6員ヘテロ環 |
| EP1968568A4 (en) | 2005-12-22 | 2011-04-13 | Glaxosmithkline Llc | HEMMER OF NUTS ACTIVITY |
| EP1962830B1 (en) | 2005-12-23 | 2013-03-27 | GlaxoSmithKline LLC | Azaindole inhibitors of aurora kinases |
| NZ595571A (en) | 2006-02-28 | 2013-04-26 | Helicon Therapeutics Inc | Pyrazole compounds and uses thereof |
| JP2007277230A (ja) | 2006-03-15 | 2007-10-25 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| EP1840114A1 (en) * | 2006-03-30 | 2007-10-03 | LTB4 Sweden AB | Crystalline Leukotriene B4 |
| WO2007122686A1 (ja) * | 2006-04-14 | 2007-11-01 | Eisai R & D Management Co., Ltd. | ベンズイミダゾール化合物 |
| US20080027044A1 (en) * | 2006-06-13 | 2008-01-31 | Kim Lewis | Prodrug antibiotic screens |
| MY149140A (en) * | 2006-10-13 | 2013-07-15 | Basf Se | Hydrates of 2-chloro 5-y3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoro-methyl)-1-(2h)-pyrimidinyl"-4-fluoro-n- yymethyl-(1-methylethyl)-amino"sulphonyl"benzamide |
| CN101616667A (zh) | 2006-10-27 | 2009-12-30 | 百时美施贵宝公司 | 可用作激酶抑制剂的杂环酰胺化合物 |
| CN101611008A (zh) | 2006-12-22 | 2009-12-23 | 恩希赛弗制药公司 | C3a受体调节剂及其使用方法 |
| WO2008091532A1 (en) * | 2007-01-19 | 2008-07-31 | Panacos Pharmaceuticals, Inc. | Salts of 3-o-(3',3'-dimethylsuccinyl)betulinic acid and solid state forms thereof |
| US8420690B2 (en) | 2007-02-07 | 2013-04-16 | Glaxosmithkline Llc | Inhibitors of Akt activity |
| WO2008121685A1 (en) | 2007-03-28 | 2008-10-09 | Smithkline Beecham Corporation | Methods of use for inhibitors of akt activity |
| JP2010522770A (ja) | 2007-03-29 | 2010-07-08 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Akt活性の阻害物質 |
| MX2011008073A (es) | 2009-01-30 | 2011-11-18 | Glaxosmithkline Llc | Hidrocloruro de n-{(1-s)-2-amino -1-[(3-fluorofenil)metil]etil}-5- cloro-4-(4-cloro-1-metil-1h-pirazol-5-il)-2-tiofenocarboxamida cristalino. |
| US8977217B1 (en) | 2013-02-20 | 2015-03-10 | Triquint Semiconductor, Inc. | Switching device with negative bias circuit |
-
2010
- 2010-01-28 MX MX2011008073A patent/MX2011008073A/es active IP Right Grant
- 2010-01-28 SG SG2011050143A patent/SG172926A1/en unknown
- 2010-01-28 US US12/695,331 patent/US8609711B2/en active Active
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- 2016-12-05 JP JP2016235681A patent/JP2017061559A/ja not_active Withdrawn
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- 2019-03-26 JP JP2019057789A patent/JP6924794B2/ja active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5369124A (en) * | 1992-10-02 | 1994-11-29 | Bayer Aktiengesellschaft | Substituted thiophenecarboxamides |
| CA2396561A1 (en) * | 1999-12-24 | 2001-07-05 | Bayer Aktiengesellschaft | Substituted oxazolidinones and their use in the field of blood coagulation |
| US6982279B2 (en) * | 2000-12-12 | 2006-01-03 | Aventis Pharm Deutschland Gmbh | Arylated furan- and thiophenecarboxamides, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them |
| WO2002088107A1 (fr) * | 2001-04-26 | 2002-11-07 | Eisai Co., Ltd. | Compose azote a anneaux condenses possedant un groupe pyrazolyle et servant de substituant, et composition medicale le comprenant |
| WO2008098104A1 (en) * | 2007-02-07 | 2008-08-14 | Smithkline Beecham Corporation | Inhibitors of akt activity |
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