AR054631A1 - DERIVADOS DE L-ALFA-GLUTAMINA COMO INHIBIDORES DE GLUTAMATO AGRECANASA, INTERMEDIARIOS Y MÉTODOS DE SíNTESIS DE LOS MISMOS Y COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN. - Google Patents
DERIVADOS DE L-ALFA-GLUTAMINA COMO INHIBIDORES DE GLUTAMATO AGRECANASA, INTERMEDIARIOS Y MÉTODOS DE SíNTESIS DE LOS MISMOS Y COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN.Info
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- AR054631A1 AR054631A1 ARP060102979A ARP060102979A AR054631A1 AR 054631 A1 AR054631 A1 AR 054631A1 AR P060102979 A ARP060102979 A AR P060102979A AR P060102979 A ARP060102979 A AR P060102979A AR 054631 A1 AR054631 A1 AR 054631A1
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- aryl
- heteroaryl
- alkyl
- cycloalkyl
- alkenyl
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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Abstract
Estos compuestos son inhibidores de metaloproteinasa. Reivindicacion 1: Un compuesto de la Formula (1), o una sal del mismo, farmacéuticamente aceptable, caracterizado porque W es -C(O)-, -OC(O)-, -NHC(O)-, -C(O)O-, o -C(O)NH-; R1 es fenilo, heteroarilo, bifenilo, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico, o heteroarilo tricíclico, cada uno opcionalmente sustituido con uno o más de R5 o R6, y cuando R1 es sustituido con uno más de R5 o R6, los sustituyentes pueden ser idénticos o diferentes; R2 es hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -(CH2)nR11, -OH, o alquilo -O-C1-6; R3 es CO2H, -CONH2, -CONHOH, -CONHSO2R7, tetrazol, -SO2NHR7, -SO3H, -PO(OH)NH2, -PO(OH)OR7, -CONHR7, -COOR7, un grupo mimético de ácido, o un heteroarilo o heterocicloalquilo de 5 o 6 elementos, que contiene 1 a 4 heteroátomos seleccionados de O, N, S; R4 es-CO2H, -CONH2, - (CH2)nOR7, o -CONR9R10; R5 es arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O- heteroarilo, -S-arilo, -S-heteroarilo, -NH-arilo, -NH-heteroarilo, -CO-alquilo C1-6, -CO-arilo, -CO-heteroarilo, -SO2-alquilo C1-6, -SO2-arilo, -SO2-heteroarilo, -SO2NH-arilo, -SO2NH-heteroarilo, -NHSO2-alquilo C1-6, -NHSO2-arilo, -NHSO2- heteroarilo, -NHCO-arilo, -NHCO-heteroarilo, -CONH-arilo, -CONH-heteroarilo, alquilo C1-6, -O-alquilo C1-6, -S-alquilo C1-6, -NR-alquilo C1-6, -NHCO-alquilo C1-6, -CONH alquilo C1-6, -O-cicloalquilo C3-6, -S-cicloalquilo C3-6, -NH-cicloalquilo C3-6, -NHCO-cicloalquilo C3-6 o -CONH-cicloalquilo C3-6; cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R6, y cuando R5 es sustituido con más de un R6, los sustituyentes pueden ser idénticos o diferentes; R6 y R12 son cada uno independientemente, hidrogeno, halogeno, -CN, -OCF3, -CF3, -NO2, -OH, -SH, -NR7R8, -CONR7R8, NR8COR7, NR8CO2R7, -CO2R7, -COR7-, -SO2-alquilo C1-6, -SO2-arilo, -SO2-heteroarilo, SO2R7, NR7SO2R8, SO2NR7R8; alquilo C1-6, -O-alquilo C1- 6, -S-alquilo C1-6, -NH-alquilo C1-6, -NHCO-alquilo C1-6, -CONH-alquilo C1-6, -O-cicloalquilo C3-6, -S-cicloalquilo C3-6, -NH-cicloalquilo C3-6, -NHCO-cicloalquilo C3-6. -CONH-cicloalquilo C3-6, heterocicloalquilo, -alquilo C1-6-OR7, alquinilo C2-6, alquenilo C2-6, -O-alquil-cicloalquilo C3-6, -O-alquenilo, -O-alquilo C1-6 sustituido con arilo, arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O-heteroarilo, -S-arilo, o - S-heteroarilo; cada alquilo, arilo, cicloalquilo, heterocicloalquilo, heteroarilo, alquenilo o alquinilo, opcionalmente sustituido con uno o más de R13; R7 y R8 son cada uno independientemente hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, -(CH2)n-arilo, o -(CH2)n-heteroarilo; o R7 y R8 junto con el átomo al cual están unidos, pueden formar un grupo cíclico de cinco a siete elementos que contiene hasta 3 heteroátomos seleccionados entre N, O, o S; R9 y R10 son cada uno independientemente hidrogeno, alquilo C1-6, alquilo C1-6-OH, alquilo C1-6-O-alquilo C1-6, arilo, cicloalquilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico o heteroarilo tricíclico, cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R12; o R9 y R10 juntos pueden formar un grupo cíclico de cinco a siete elementos que contienen hasta 3 heteroátomos seleccionados de N, O o S; R11 es arilo, heteroarilo o cicloalquilo; R13 es halogeno, -O-alquilo C1-6, -CO2H, -OH, -CF3. hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C1-6, cicloalquilo, cicloalquilo sustituido con -OH, arilo sustituido con -NH2, arilo sustituido con -O-alquilo C1-6, -(CH2)n-arilo, o -(CH2)n-heteroarilo; m es 0 - 4; n es 0 - 4; y p es 0 - 2. Reivindicacion 20: Un compuesto de formula (2); o una sal del mismo farmacéuticamente aceptable, caracterizado porque R1 es fenilo, heteroarilo, bifenilo, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico, o heteroarilo tricíclico, cada uno opcionalmente sustituido con uno o más de R5 o R6, y cuando R1 es sustituido con uno más de R5 o R6, los sustituyentes pueden ser idénticos o diferentes. R2 es hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -(CH2)n-R11, -OH, o alquilo -O-C1-6; R5 es arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O--heteroarilo, -S-arilo, -S- heteroarilo, -NH-arilo, -NH-heteroarilo, -CO-alquilo C1-6, -CO-arilo, - CO-heteroarilo, -SO2-alquilo C1-6, -SO2- arilo, -SO2-heteroarilo, -SO2NH-arilo, -SO2NH-heteroarilo, -NHSO2-alquilo C1-6, -NHSO2-arilo, -NHSO2-heteroarilo, -NHCO-arilo, -NHCO--heteroarilo, -CONH-arilo, -CONH-heteroarilo, alquilo C1-6, -O-alquilo C1- 6, -S-alquilo C1-6, -NH-alquilo C1-6 , -NHCO-alquilo C1-6, CONH-alquilo C1-6, -O-cicloalquilo C3-6, -S-cicloalquilo C3-6 , -NH-cicloalquilo C3-6, -NHCO-cicloalquilo C3-6, o -CONH-cicloalquilo cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R6, y cuando R5 es sustituido con más de un R6, los sustituyentes pueden ser idénticos o diferentes; R6 y R12 son cada uno independientemente, hidrogeno, halogeno, -CN, -OCF3, -CF3, -NO2, -OH, -SH, -NR7R8, - CONR7R8, NR8COR7, NR8CO2R7, -CO2R7, -COR7, -SO2-alquilo C1-6, -SO2- arilo, -SO2-heteroarilo, SO2R7, NR7SO2R8, SO2NR7R8 alquilo C1-6 , -O-alquilo C1-6, -S-alquilo C1-6, -NH-alquilo C1-6, -NHCO-alquilo C1-6, -CONH-alquilo C1-6, -O-cicloalquilo C3-6, - S-cicloalquilo C3-6, -NH-cicloalquilo C3-6, -NHCO- cicloalquilo C3-6, -CONH-cicloalquilo C3-6, heterocicloalquilo, -alquilo C1-6-OR7, alquinilo C2-6, alquenilo C2-6, -O-alquil-cicloalquilo C3-6, -O-alquenilo, -O-alquilo C1-6 sustituido con arilo, arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O-heteroarilo, -S-arilo, o -S-heteroarilo; cada alquilo, arilo, cicloalquilo, heterocicloalquilo, heteroarilo, alquenilo o alquinilo, opcionalmente sustituido con uno o más de R13; R7 y R8 son cada uno independientemente hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, -(CH2)n-arilo, o -(CH2)n-heteroarilo; o R7 y R8 junto con el átomo al cual están unidos, pueden formar un grupo cíclico de cinco a siete elementos que contiene hasta 3 heteroátomos seleccionados entre N, O, o S; R11 es arilo, heteroarilo o cicloalquilo; R13 es halogeno, -O-alquilo C1-6, -CO2H, -OH, - CF3, hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, cicloalquilo sustituido con -OH, arilo sustituido con -NH2, arilo sustituido con -O-alquilo C1-6, -(CH2)n-arilo, o -(CH2)n-heteroarilo; R14 y R15 son cada uno independientemente hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, heterocicloalquilo, -(CH2)n-arilo, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico o heteroarilo tricíclico, cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R12; o R14 y R15 juntos pueden formar un grupo cíclico de cinco a siete elementos que contienen hasta 3 heteroátomos seleccionados de N, O o S; n es 0 - 4; y p es 0 - 2.
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US9492400B2 (en) * | 2004-11-04 | 2016-11-15 | Massachusetts Institute Of Technology | Coated controlled release polymer particles as efficient oral delivery vehicles for biopharmaceuticals |
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US9267937B2 (en) | 2005-12-15 | 2016-02-23 | Massachusetts Institute Of Technology | System for screening particles |
US8623871B2 (en) | 2006-01-25 | 2014-01-07 | Synta Pharmaceuticals Corp. | Substituted biaryl compounds for inflammation and immune-related uses |
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US20110052697A1 (en) * | 2006-05-17 | 2011-03-03 | Gwangju Institute Of Science & Technology | Aptamer-Directed Drug Delivery |
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US9381477B2 (en) * | 2006-06-23 | 2016-07-05 | Massachusetts Institute Of Technology | Microfluidic synthesis of organic nanoparticles |
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US20100216886A1 (en) * | 2006-11-09 | 2010-08-26 | Wyeth | Polymorphs of n2-(1,1'-biphenyl-4-ylcarbonyl)-n1-[2-(4-fluorophenyl)-1,1-dimethylethyl]-l-alpha-glutamine |
US20100303723A1 (en) * | 2006-11-20 | 2010-12-02 | Massachusetts Institute Of Technology | Drug delivery systems using fc fragments |
US9217129B2 (en) | 2007-02-09 | 2015-12-22 | Massachusetts Institute Of Technology | Oscillating cell culture bioreactor |
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WO2010005726A2 (en) * | 2008-06-16 | 2010-01-14 | Bind Biosciences Inc. | Therapeutic polymeric nanoparticles with mtor inhibitors and methods of making and using same |
EA020753B1 (ru) | 2008-06-16 | 2015-01-30 | Бинд Терапьютикс, Инк. | Терапевтические полимерные наночастицы, содержащие алкалоиды vinca, и их применение |
US8277812B2 (en) | 2008-10-12 | 2012-10-02 | Massachusetts Institute Of Technology | Immunonanotherapeutics that provide IgG humoral response without T-cell antigen |
US8591905B2 (en) | 2008-10-12 | 2013-11-26 | The Brigham And Women's Hospital, Inc. | Nicotine immunonanotherapeutics |
JP5584696B2 (ja) * | 2008-11-17 | 2014-09-03 | 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 | Mmp−13阻害剤として有用なヘテロアリールジアミド化合物 |
US8563041B2 (en) | 2008-12-12 | 2013-10-22 | Bind Therapeutics, Inc. | Therapeutic particles suitable for parenteral administration and methods of making and using same |
WO2010075072A2 (en) * | 2008-12-15 | 2010-07-01 | Bind Biosciences | Long circulating nanoparticles for sustained release of therapeutic agents |
TR201906255T4 (tr) | 2009-12-11 | 2019-05-21 | Pfizer | Terapötik partiküllerin liyofilize edilmesine yönelik stabil formülasyonlar. |
EP2515942B1 (en) | 2009-12-15 | 2020-02-12 | Pfizer Inc. | Therapeutic polymeric nanoparticle compositions with high glass transition temperature or high molecular weight copolymers |
EP2576536B1 (en) * | 2010-06-01 | 2016-09-14 | The University of Queensland | Haematopoietic-prostaglandin d2 synthase inhibitors |
AU2013315118B2 (en) | 2012-09-17 | 2017-10-05 | Pfizer Inc. | Process for preparing therapeutic nanoparticles |
AR092971A1 (es) * | 2012-10-26 | 2015-05-06 | Lilly Co Eli | Inhibidores de agrecanasa |
CA2900116C (en) * | 2013-02-06 | 2021-08-10 | Merck Patent Gmbh | Substituted carboxylic acid derivatives as aggrecanase inhibitors for the treatment of osteoarthritis |
GB201312311D0 (en) | 2013-07-09 | 2013-08-21 | Uni I Oslo | Uses of enzyme inhibitors |
WO2015075699A1 (en) | 2013-11-25 | 2015-05-28 | Sanofi | Dotam derivatives for therapeutic use |
EP3116547B1 (en) | 2014-03-14 | 2019-06-05 | Pfizer Inc | Therapeutic nanoparticles comprising a therapeutic agent and methods of making and using same |
EP3672939A1 (en) | 2017-08-21 | 2020-07-01 | Celgene Corporation | Processes for preparation of (s)-tert-butyl 4,5-diamino-5-oxopentanoate |
CN109516925B (zh) * | 2018-10-31 | 2021-07-16 | 陕西慧康生物科技有限责任公司 | 一种谷氨酸-1-甲酯-5-叔丁酯的合成方法 |
CN109734660B (zh) * | 2019-01-18 | 2020-07-28 | 西安交通大学 | 一种含有叔丁基取代的丝氨酸的类肽类化合物及其制备方法和应用 |
CN109824584B (zh) * | 2019-01-18 | 2020-08-18 | 西安交通大学 | 一种含有叔亮氨酸的类肽类化合物及其制备方法和应用 |
CN109824581B (zh) * | 2019-01-18 | 2020-08-18 | 西安交通大学 | 一种含有丙氨酸的类肽类化合物以及其制备方法和应用 |
CN109824582B (zh) * | 2019-01-18 | 2020-06-19 | 西安交通大学 | 一种丙氨酸衍生物及其制备方法和应用 |
KR20230128503A (ko) * | 2020-12-25 | 2023-09-05 | (주)앰틱스바이오 | 신규한 아미노알칸산에 바이페닐기를 도입한 유도체 화합물 및 이를 포함하는 항염증용 조성물 |
Family Cites Families (38)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2440649A (en) | 1948-04-27 | Quinazoline | ||
GB1108819A (en) * | 1964-07-31 | 1968-04-03 | Rotta Research Lab | Derivatives of 2-acylaminobicarboxylic acids and method for preparing same |
DE3332633A1 (de) | 1983-09-09 | 1985-04-04 | Luitpold-Werk Chemisch-pharmazeutische Fabrik GmbH & Co, 8000 München | Substituierte carbonsaeurederivate, verfahren zu ihrer herstellung, und arzneimittel |
IT1215169B (it) | 1985-12-17 | 1990-01-31 | Rotta Research Lab | Derivati alchil ossigenati degli acidi glutammico ed aspartico ad attivita antagonista su polipeptidi bioattivi e procedimento per la loro preparazione |
IT1217123B (it) | 1987-02-05 | 1990-03-14 | Rotta Research Lab | Derivati otticamente attivi dell acido 5 pentilammino 5 oxo pentanoico r ad attivita antagonista della colecistochinina e procedimento per la loro preparazione |
DE4102024A1 (de) | 1991-01-24 | 1992-07-30 | Thomae Gmbh Dr K | Biphenylderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
EP0673247A4 (en) | 1992-12-01 | 1996-05-01 | Merck & Co Inc | FIBRINOGEN RECEPTOR ANTAGONISTS. |
JPH06192199A (ja) | 1992-12-25 | 1994-07-12 | Mitsubishi Kasei Corp | ケトン誘導体 |
US5563127A (en) | 1993-03-24 | 1996-10-08 | The Dupont Merck Pharmaceutical Company | Boronic acid and ester inhibitors of thrombin |
JPH09510442A (ja) | 1994-03-11 | 1997-10-21 | ファーマコペイア,インコーポレイテッド | スルホンアミド誘導体及びそれらの使用 |
GB2292149A (en) | 1994-08-09 | 1996-02-14 | Ferring Res Ltd | Peptide inhibitors of pro-interleukin-1beta converting enzyme |
US6306840B1 (en) | 1995-01-23 | 2001-10-23 | Biogen, Inc. | Cell adhesion inhibitors |
CA2227466A1 (en) | 1995-07-24 | 1997-02-06 | Fujisawa Pharmaceutical Co., Ltd. | Esters and amides as pla2 inhibitors |
DE69637307T2 (de) | 1995-11-28 | 2008-02-28 | Cephalon, Inc. | Aus d-aminosäuren abgeleitete cystein-und serinproteasehemmer |
DE69833858T2 (de) | 1997-07-08 | 2007-02-22 | Ono Pharmaceutical Co. Ltd. | Aminosäurederivate |
JP4129069B2 (ja) | 1997-09-16 | 2008-07-30 | 株式会社Adeka | アシル化ペプチド類の製造方法 |
JP4090541B2 (ja) | 1997-10-15 | 2008-05-28 | 株式会社Adeka | アシル化ペプチド類の製造方法 |
AU3366899A (en) | 1998-03-27 | 1999-10-18 | Regents Of The University Of California, The | Novel hiv integrase inhibitors and hiv therapy based on drug combinations including integrase inhibitors |
TWI245035B (en) | 1998-06-26 | 2005-12-11 | Ono Pharmaceutical Co | Amino acid derivatives and a pharmaceutical composition comprising the derivatives |
US7157430B2 (en) | 1998-10-22 | 2007-01-02 | Idun Pharmaceuticals, Inc. | (Substituted)acyl dipeptidyl inhibitors of the ICE/CED-3 family of cysteine proteases |
US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
DE19851184A1 (de) | 1998-11-06 | 2000-05-11 | Aventis Pharma Gmbh | N-Arylsulfonyl-aminosäure-omega-amide |
AU4180900A (en) * | 1999-04-02 | 2000-10-23 | Du Pont Pharmaceuticals Company | Novel amide derivatives as inhibitors of matrix metalloproteinases, tnf-alpha, and aggrecanase |
ES2228527T5 (es) | 1999-05-07 | 2013-05-23 | Encysive Pharmaceuticals, Inc. | Derivados del ácido propanoico que inhiben la unión de las integrinas a sus receptores |
US6723711B2 (en) | 1999-05-07 | 2004-04-20 | Texas Biotechnology Corporation | Propanoic acid derivatives that inhibit the binding of integrins to their receptors |
EP1081137A1 (en) * | 1999-08-12 | 2001-03-07 | Pfizer Products Inc. | Selective inhibitors of aggrecanase in osteoarthritis treatment |
JP2003146905A (ja) * | 1999-11-11 | 2003-05-21 | Yamanouchi Pharmaceut Co Ltd | アグリカナーゼ活性を有する新規な金属プロテアーゼ |
CN1366518A (zh) | 2000-04-25 | 2002-08-28 | 三星电子株式会社 | 作为基质金属蛋白酶抑制剂的联苯基丁酸衍生物 |
AU2001264595A1 (en) * | 2000-05-19 | 2001-12-03 | Guilford Pharmaceuticals Inc. | Sulfonamide and carbamide derivatives of 6(5h)phenanthridinones and their uses |
JP2002145849A (ja) | 2000-11-10 | 2002-05-22 | Kyorin Pharmaceut Co Ltd | アルキニルアミノ酸誘導体及びその製造法 |
US20050049242A1 (en) | 2000-12-21 | 2005-03-03 | W. Edward Robinson | Novel HIV integrase inhibitors and HIV therapy based on drug combinations including integrase inhibitors |
WO2003093498A1 (en) | 2002-04-29 | 2003-11-13 | The Ohio State University | Inhibition of protein tyrosine phosphatases and sh2 domains by a neutral phosphotyrosine mimetic |
CA2490646A1 (en) * | 2002-06-25 | 2003-12-31 | Pharmacia Corporation | Arylsulfonylhydroxamic acid and amide derivatives and their use as protease inhibitors |
US20040229955A1 (en) * | 2003-01-08 | 2004-11-18 | Andersen Niels H. | Antibacterial agents |
JP2007502287A (ja) | 2003-08-13 | 2007-02-08 | アムジェン インコーポレイテッド | メラニン凝集ホルモン受容体アンタゴニスト |
US20070208166A1 (en) | 2003-10-24 | 2007-09-06 | Exelixis, Inc. | Tao Kinase Modulators And Method Of Use |
JP2007525406A (ja) | 2003-12-04 | 2007-09-06 | ワイス | ビアリールスルホンアミドおよびその使用方法 |
CN1894206A (zh) * | 2003-12-15 | 2007-01-10 | 日本烟草产业株式会社 | N-取代的n-磺酰氨基环丙烷化合物和其药学应用 |
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- 2006-07-11 CN CNA2006800253865A patent/CN101223130A/zh active Pending
- 2006-07-11 KR KR1020087003025A patent/KR20080031379A/ko not_active Application Discontinuation
- 2006-07-11 EP EP06787028A patent/EP1902014A2/en not_active Withdrawn
- 2006-07-11 RU RU2007149182/04A patent/RU2436768C2/ru not_active IP Right Cessation
- 2006-07-11 CA CA002614930A patent/CA2614930A1/en not_active Abandoned
- 2006-07-11 US US11/484,005 patent/US7553873B2/en not_active Expired - Fee Related
- 2006-07-11 JP JP2008521573A patent/JP5181118B2/ja not_active Expired - Fee Related
- 2006-07-11 GT GT200600306A patent/GT200600306A/es unknown
- 2006-07-11 WO PCT/US2006/027066 patent/WO2007008994A2/en active Application Filing
- 2006-07-11 UA UAA200800409A patent/UA94412C2/ru unknown
- 2006-07-11 AU AU2006268183A patent/AU2006268183B2/en not_active Ceased
- 2006-07-11 PE PE2010000448A patent/PE20100809A1/es not_active Application Discontinuation
- 2006-07-11 BR BRPI0613030-5A patent/BRPI0613030A2/pt not_active IP Right Cessation
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CA2614930A1 (en) | 2007-01-18 |
JP5181118B2 (ja) | 2013-04-10 |
WO2007008994A2 (en) | 2007-01-18 |
EP1902014A2 (en) | 2008-03-26 |
WO2007008994A3 (en) | 2007-07-12 |
NO20076678L (no) | 2008-03-14 |
US7553873B2 (en) | 2009-06-30 |
ZA200800379B (en) | 2011-06-29 |
RU2436768C2 (ru) | 2011-12-20 |
US20100010012A1 (en) | 2010-01-14 |
BRPI0613030A2 (pt) | 2012-01-03 |
TW200800209A (en) | 2008-01-01 |
PE20100809A1 (es) | 2011-01-07 |
JP2009500456A (ja) | 2009-01-08 |
US7998965B2 (en) | 2011-08-16 |
GT200600306A (es) | 2007-03-29 |
RU2007149182A (ru) | 2009-08-20 |
AU2006268183A1 (en) | 2007-01-18 |
CN101223130A (zh) | 2008-07-16 |
AU2006268183B2 (en) | 2012-08-09 |
UA94412C2 (en) | 2011-05-10 |
US20070043066A1 (en) | 2007-02-22 |
ECSP088092A (es) | 2008-02-20 |
PE20070505A1 (es) | 2007-05-15 |
MY144590A (en) | 2011-10-14 |
KR20080031379A (ko) | 2008-04-08 |
IL188617A0 (en) | 2008-04-13 |
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