ZA200105055B - Method of using cyclooxygenase-2-inhibitor and a matrix metalloproteinase inhibitor as a combination therapy in the treatment of neoplasia. - Google Patents
Method of using cyclooxygenase-2-inhibitor and a matrix metalloproteinase inhibitor as a combination therapy in the treatment of neoplasia. Download PDFInfo
- Publication number
- ZA200105055B ZA200105055B ZA200105055A ZA200105055A ZA200105055B ZA 200105055 B ZA200105055 B ZA 200105055B ZA 200105055 A ZA200105055 A ZA 200105055A ZA 200105055 A ZA200105055 A ZA 200105055A ZA 200105055 B ZA200105055 B ZA 200105055B
- Authority
- ZA
- South Africa
- Prior art keywords
- hydroxy
- phenyl
- sulfonyl
- trifluoromethyl
- piperidinecarboxamide
- Prior art date
Links
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- 229940121386 matrix metalloproteinase inhibitor Drugs 0.000 title claims description 45
- 239000003771 matrix metalloproteinase inhibitor Substances 0.000 title claims description 45
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 title claims description 40
- 229940093444 Cyclooxygenase 2 inhibitor Drugs 0.000 title claims description 38
- 238000011282 treatment Methods 0.000 title claims description 35
- 238000000034 method Methods 0.000 title claims description 27
- 230000009826 neoplastic cell growth Effects 0.000 title claims description 23
- 238000002648 combination therapy Methods 0.000 title description 3
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Families Citing this family (118)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6794511B2 (en) | 1997-03-04 | 2004-09-21 | G. D. Searle | Sulfonyl aryl or heteroaryl hydroxamic acid compounds |
| US6696449B2 (en) | 1997-03-04 | 2004-02-24 | Pharmacia Corporation | Sulfonyl aryl hydroxamates and their use as matrix metalloprotease inhibitors |
| US7115632B1 (en) * | 1999-05-12 | 2006-10-03 | G. D. Searle & Co. | Sulfonyl aryl or heteroaryl hydroxamic acid compounds |
| US6077850A (en) * | 1997-04-21 | 2000-06-20 | G.D. Searle & Co. | Substituted benzopyran analogs for the treatment of inflammation |
| US20030225150A1 (en) * | 1997-04-21 | 2003-12-04 | Pharmacia Corporation | Method of using a COX-2 inhibitor and a topoisomerase II inhibitor as a combination therapy in the treatment of neoplasia |
| US20040072889A1 (en) * | 1997-04-21 | 2004-04-15 | Pharmacia Corporation | Method of using a COX-2 inhibitor and an alkylating-type antineoplastic agent as a combination therapy in the treatment of neoplasia |
| US7029652B2 (en) * | 1998-09-16 | 2006-04-18 | The Regents Of The University Of California | Method of treating tumors |
| US20040053900A1 (en) * | 1998-12-23 | 2004-03-18 | Pharmacia Corporation | Method of using a COX-2 inhibitor and an aromatase inhibitor as a combination therapy |
| US20020103141A1 (en) * | 1998-12-23 | 2002-08-01 | Mckearn John P. | Antiangiogenic combination therapy for the treatment of cancer |
| EA005500B1 (ru) | 1999-02-08 | 2005-02-24 | Дж.Д. Сирл Ллк | Сульфаматогидроксамовая кислота как ингибитор металлопротеаз |
| US6800646B1 (en) | 1999-02-08 | 2004-10-05 | Pharmacia Corporation | Sulfamato hydroxamic acid metalloprotease inhibitor |
| KR20020009610A (ko) * | 1999-05-12 | 2002-02-01 | 윌리암스 로저 에이 | 매트릭스 메탈로프로테아제 억제제로서의 히드록삼산 유도체 |
| US6573290B1 (en) | 1999-05-17 | 2003-06-03 | Ilex Oncology, Inc. | DFMO and celecoxib in combination for cancer chemoprevention and therapy |
| US7141581B2 (en) | 1999-07-02 | 2006-11-28 | Agouron Pharmaceuticals, Inc. | Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use |
| GB9920548D0 (en) * | 1999-08-31 | 1999-11-03 | Rhone Poulenc Rorer Sa | Treatment of hepatocellular carcinoma |
| US7465754B1 (en) | 1999-09-15 | 2008-12-16 | Wyeth | Method of potentiating chemotherapy and treating solid tumors |
| EP1214092A2 (en) * | 1999-09-15 | 2002-06-19 | Wyeth | Method of potentiating chemotherapy and treating solid tumors |
| CA2392093A1 (en) * | 1999-11-15 | 2001-05-25 | Advanced Research And Technology Institute, Inc. | Use of nsaids for the treatment of pancreatic cancer |
| ATE464892T1 (de) * | 2000-02-03 | 2010-05-15 | Eisai R&D Man Co Ltd | Inhibitoren der integrinexpression |
| AU2000237154A1 (en) * | 2000-02-28 | 2001-09-12 | Zila, Inc. | Method for detecting and killing epithelial cancer cells |
| CN100398153C (zh) | 2000-03-24 | 2008-07-02 | 诺瓦提斯公司 | 抗血管生成药与光敏剂的联合制药用途 |
| EP1138680A1 (en) * | 2000-03-29 | 2001-10-04 | Pfizer Products Inc. | Gem substituted sulfonyl hydroxamic acids as MMP inhibitors |
| US6900232B2 (en) | 2000-06-15 | 2005-05-31 | Pharmacia Corporation | Cycloalkyl alkanoic acids as integrin receptor antagonists |
| CA2414247C (en) | 2000-06-29 | 2012-11-27 | Quick-Med Technologies, Inc. | Cosmetic composition and method comprising a hydroxamate mmpi and a triterpenoid glycoside |
| US6531494B1 (en) | 2001-08-29 | 2003-03-11 | Pharmacia Corporation | Gem-substituted αvβ3 antagonists |
| AR034142A1 (es) * | 2000-09-08 | 2004-02-04 | Sloan Kettering Inst Cancer | Una composicion farmaceutica, metodo para fabricar un medicamento en base a dicha composicion y uso de la composicion |
| US20040024044A1 (en) * | 2000-09-08 | 2004-02-05 | Di Salle Enrico | Exemestane as chemopreventing agent |
| CA2434611A1 (en) * | 2001-01-26 | 2002-09-19 | Pharmacia Italia Spa | Combined method for treating hormono-dependent disorders |
| EP1383490B1 (en) | 2001-03-14 | 2012-04-25 | Bristol-Myers Squibb Company | Combination of an epothilone analog and chemotherapeutic agents for the treatment of proliferative diseases |
| US20030105144A1 (en) * | 2001-04-17 | 2003-06-05 | Ping Gao | Stabilized oral pharmaceutical composition |
| US20040136949A1 (en) | 2001-04-24 | 2004-07-15 | Matthias Grell | Combination therapy using anti-angiogenic agents and tnf alpha |
| US6872730B2 (en) | 2001-04-27 | 2005-03-29 | 3-Dimensional Pharmaceuticals, Inc. | Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists |
| WO2002089824A1 (en) * | 2001-05-03 | 2002-11-14 | F. Hoffmann-La Roche Ag | Combination of a gelatinase inhibitor and an anti-tumor agent, and uses thereof |
| US6995171B2 (en) | 2001-06-21 | 2006-02-07 | Agouron Pharmaceuticals, Inc. | Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents |
| US6683078B2 (en) | 2001-07-19 | 2004-01-27 | Pharmacia Corporation | Use of sulfonyl aryl or heteroaryl hydroxamic acids and derivatives thereof as aggrecanase inhibitors |
| AU2002328952A1 (en) * | 2001-07-23 | 2003-02-24 | Epidauros Biotechnologie Ag | Irinotecan for treatment of cancer |
| PT1443942E (pt) * | 2001-10-19 | 2008-04-07 | Novartis Ag | Composição farmacêutica para utilização no tratamento de patologias malignas incluindo em combinação um bisfosfonato, um inibidor de cox-2 e um taxol |
| NZ552335A (en) * | 2001-10-25 | 2008-11-28 | Novartis Ag | Combinations comprising a selective COX-2 inhibitor and a microtubule interfering agent |
| ES2275931T5 (es) * | 2001-12-03 | 2018-10-23 | Bayer Healthcare Llc | Compuestos de aril-urea en combinación con otros agentes citostáticos o citotóxicos para tratamiento de cánceres humanos |
| US20030143165A1 (en) * | 2002-01-25 | 2003-07-31 | Allan Evans | NSAID-containing topical formulations that demonstrate chemopreventive activity |
| GB0204756D0 (en) * | 2002-02-28 | 2002-04-17 | Novartis Ag | Organic compounds |
| JP2005527511A (ja) | 2002-03-01 | 2005-09-15 | ファイザー インコーポレイテッド | 抗血管形成剤として有用なチエノピリジンのインドリル−尿素誘導体およびその使用法 |
| JP2005533001A (ja) * | 2002-03-04 | 2005-11-04 | メディミューン，インコーポレーテッド | インテグリンαｖβ３アンタゴニストを他の物質と併用投与する癌の予防または治療方法 |
| EP1485131A1 (en) * | 2002-03-08 | 2004-12-15 | Novartis AG | Matrix metalloproteinase inhibitors in combination with hypothermia and/or radiotherapy for the treatment of cancer |
| CA2479744A1 (en) | 2002-03-28 | 2003-10-09 | Paul E. Finke | Substituted 2,3-diphenyl pyridines |
| WO2003091247A2 (en) | 2002-04-25 | 2003-11-06 | Pharmacia Corporation | Piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors |
| UA77303C2 (en) | 2002-06-14 | 2006-11-15 | Pfizer | Derivatives of thienopyridines substituted by benzocondensed heteroarylamide useful as therapeutic agents, pharmaceutical compositions and methods for their use |
| MXPA05000754A (es) * | 2002-07-17 | 2005-04-19 | Warner Lambert Co | Combinacion de un inhibidor carboxilico alosterico de la metaloproteinasa de matriz-13 con celecoxib o valdecoxib. |
| MXPA05000722A (es) * | 2002-07-17 | 2005-04-08 | Warner Lambert Co | Combinacion de un inhibidor alosterico carboxilico de la metaloproteinasa-13 de la matriz con un inhibidor selectivo de la ciclooxigenasa-2 que no es celecoxib o valdecoxib. |
| CN1681495B (zh) * | 2002-08-19 | 2010-05-12 | 辉瑞产品公司 | 用于治疗过度增生性疾病的组合物 |
| CN102516417B (zh) | 2002-09-06 | 2014-12-10 | 天蓝制药公司 | 用于传递治疗剂的以环糊精为基础的聚合物 |
| MXPA05006676A (es) | 2002-12-19 | 2005-08-16 | Pfizer | Compuestos de indazol y composiciones farmaceuticas para inhibir proteinquinasas, y procedimientos para su uso. |
| AU2004222527A1 (en) * | 2003-03-18 | 2004-09-30 | Pharmacia Italia Spa | Combined therapy comprising nemorubicin and a cyclooxygenase-2-inhibitor |
| DE10313272A1 (de) * | 2003-03-24 | 2004-10-21 | Baxter Healthcare S.A. | Verwendung von Miltefosine zur Behandlung von aktinischer oder multiplen aktinischer Keratosen |
| US20050043233A1 (en) | 2003-04-29 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis |
| CA2519189C (en) | 2003-05-07 | 2012-07-17 | Osteologix A/S | Water-soluble strontium salts for use in treatment of cartilage and/or bone conditions |
| US7008953B2 (en) | 2003-07-30 | 2006-03-07 | Agouron Pharmaceuticals, Inc. | 3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| MXPA06002296A (es) | 2003-08-29 | 2006-05-22 | Pfizer | Tienopiridina-fenilacetamidas y sus derivados utiles como nuevos agentes antiangiogenicos. |
| GB0321999D0 (en) * | 2003-09-19 | 2003-10-22 | Cancer Rec Tech Ltd | Anti-cancer combinations |
| WO2005043155A1 (en) | 2003-10-21 | 2005-05-12 | Cedars-Sinai Medical Center | System and method for the treatment of cancer, including cancers of the central nervous system |
| MXPA06007242A (es) | 2003-12-23 | 2006-08-18 | Pfizer | Nuevos derivados de quinolina. |
| WO2006004795A2 (en) | 2004-06-25 | 2006-01-12 | The Johns Hopkins University | Angiogenesis inhibitors |
| PL1786785T3 (pl) | 2004-08-26 | 2010-08-31 | Pfizer | Enancjomerycznie czyste związki aminoheteroarylowe jako kinazy białkowe |
| WO2006090931A1 (ja) * | 2005-02-28 | 2006-08-31 | Eisai R & D Management Co., Ltd. | スルホンアミド化合物の抗癌剤との新規併用 |
| US7399335B2 (en) * | 2005-03-22 | 2008-07-15 | H.C. Starck Inc. | Method of preparing primary refractory metal |
| EP2338518A1 (en) | 2006-01-18 | 2011-06-29 | Merck Patent GmbH | Specific therapy using integrin ligands for treating cancer |
| DE102006037158A1 (de) * | 2006-08-02 | 2008-02-14 | Bioxsys Gmbh | Verfahren zur Feststellung der Sensitivität von Tumoren gegenüber Capecitabin und Testkit |
| US20080051380A1 (en) | 2006-08-25 | 2008-02-28 | Auerbach Alan H | Methods and compositions for treating cancer |
| CA2700573C (en) | 2006-09-26 | 2016-11-22 | Cedars-Sinai Medical Center | Cancer stem cell antigen vaccines and methods |
| CA2700579A1 (en) | 2006-09-28 | 2008-04-03 | Cedars-Sinai Medical Center | Cancer vaccines and vaccination methods |
| MX2009007597A (es) | 2007-01-18 | 2009-07-22 | Merck Patent Gmbh | Terapia especifica y medicamento que utilizan ligandos de integrina para tratar el cancer. |
| US20100111858A1 (en) * | 2007-01-19 | 2010-05-06 | Howard Carol P | Diangostic and Therapeutic Cyclooxygenase-2 Binding Ligands |
| US20080176958A1 (en) | 2007-01-24 | 2008-07-24 | Insert Therapeutics, Inc. | Cyclodextrin-based polymers for therapeutics delivery |
| EP2130048B1 (en) * | 2007-03-23 | 2012-04-18 | F. Hoffmann-La Roche AG | Apex as a marker for lung cancer |
| CN101730706B (zh) * | 2007-05-11 | 2015-04-15 | 生物科技研究有限公司 | 具有神经保护和增强记忆活性的受体拮抗剂 |
| JP5359879B2 (ja) * | 2007-11-16 | 2013-12-04 | 宇部興産株式会社 | ベンズアゼピノン化合物 |
| WO2009092381A1 (en) | 2008-01-23 | 2009-07-30 | Herlev Hospital, Region Hovedstaden | Ykl-40 as a general marker for non-specific disease |
| JP2011510308A (ja) * | 2008-01-23 | 2011-03-31 | リグスホスピタル | バイオマーカーｙｋｌ−４０のレベルの測定により見出される生存予後に基く心血管疾患を患う個体の分類 |
| JP5564490B2 (ja) | 2008-04-18 | 2014-07-30 | リアタ ファーマシューティカルズ インコーポレイテッド | 抗炎症性ファルマコアを含む化合物および使用法 |
| EP2328923B1 (en) | 2008-09-02 | 2016-01-13 | Cedars-Sinai Medical Center | Cd133 epitopes |
| NZ592241A (en) | 2008-09-15 | 2012-11-30 | Herlev Hospital | Ykl-40 as a marker for gastrointestinal cancers |
| US11298113B2 (en) | 2008-10-01 | 2022-04-12 | Covidien Lp | Device for needle biopsy with integrated needle protection |
| US9186128B2 (en) * | 2008-10-01 | 2015-11-17 | Covidien Lp | Needle biopsy device |
| US9332973B2 (en) | 2008-10-01 | 2016-05-10 | Covidien Lp | Needle biopsy device with exchangeable needle and integrated needle protection |
| US8968210B2 (en) | 2008-10-01 | 2015-03-03 | Covidien LLP | Device for needle biopsy with integrated needle protection |
| US9782565B2 (en) | 2008-10-01 | 2017-10-10 | Covidien Lp | Endoscopic ultrasound-guided biliary access system |
| EP2427485B1 (en) | 2009-05-07 | 2016-12-07 | ImmunoCellular Therapeutics, Ltd. | Cd133 epitopes |
| PT2430452E (pt) * | 2009-05-14 | 2014-09-30 | Univ Arizona State | Diagnóstico e tratamentos de carcinoma com base no genótipo odc1 |
| JP5572996B2 (ja) * | 2009-05-15 | 2014-08-20 | 宇部興産株式会社 | ベンズアゼピノン化合物を有効成分として含有する医薬 |
| BRPI1011206A2 (pt) | 2009-05-25 | 2016-03-15 | Merck Patent Gmbh | administração contínua de ligantes de integrina para tratar câncer |
| CA3024216C (en) | 2010-02-12 | 2021-03-30 | Pfizer Inc. | Salts and polymorphs of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one |
| US8515525B2 (en) * | 2011-08-16 | 2013-08-20 | Women's Imaging Solutions Enterprises Llc | Skin adhesive agent for mammography procedures |
| JP6426001B2 (ja) | 2011-11-17 | 2018-11-21 | グリア エスピー ゼット．オー．オー． | 神経膠腫を治療するための組成物および方法 |
| CN104640857B (zh) | 2012-07-18 | 2017-07-04 | 圣路易斯大学 | 作为整合素拮抗剂的β氨基酸衍生物 |
| US8716226B2 (en) | 2012-07-18 | 2014-05-06 | Saint Louis University | 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists |
| WO2014055493A1 (en) | 2012-10-02 | 2014-04-10 | Cerulean Pharma Inc. | Methods and systems for polymer precipitation and generation of particles |
| TWI646091B (zh) | 2012-12-28 | 2019-01-01 | 日商衛斯克慧特股份有限公司 | 鹽類及晶形 |
| EP2956544B1 (en) | 2013-02-14 | 2017-11-01 | Immunocellular Therapeutics Ltd. | Cancer vaccines and vaccination methods |
| WO2014127785A1 (en) | 2013-02-20 | 2014-08-28 | Ganymed Pharmaceuticals Ag | Combination therapy involving antibodies against claudin 18.2 for treatment of cancer |
| WO2014150996A1 (en) * | 2013-03-15 | 2014-09-25 | Cba Pharma, Inc. | Cancer treatment |
| PT3929196T (pt) | 2013-09-24 | 2023-09-11 | Fujifilm Corp | Composição farmacêutica de um novo composto contendo azoto ou seu sal, ou seu complexo de metal |
| EP3049078B1 (en) * | 2013-09-27 | 2018-06-27 | BlueLink Pharmaceuticals, Inc. | Treatment of cancer |
| EP3094342A4 (en) | 2014-01-15 | 2017-12-27 | Nikolai Khodarev | Anti-tumor therapy |
| EP3233829B1 (en) | 2014-12-18 | 2019-08-14 | Pfizer Inc | Pyrimidine and triazine derivatives and their use as axl inhibitors |
| MX2018005350A (es) | 2015-10-30 | 2018-08-14 | Cancer Prevention Pharmaceuticals Inc | Formulacion de combinacion de dosis fija, eflornitina y sulindaco. |
| US9782370B2 (en) * | 2015-12-21 | 2017-10-10 | Gongwin Biopharm Holdings Co., Ltd. | Pharmaceutical compositions of benzenesulfonamide derivatives for treatment of adenoid cystic carcinoma |
| WO2017117130A1 (en) | 2015-12-28 | 2017-07-06 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Methods for inhibiting human immunodeficiency virus (hiv) release from infected cells |
| SG11201805387RA (en) | 2015-12-30 | 2018-07-30 | Univ Saint Louis | Meta-azacyclic amino benzoic acid derivatives as pan integrin antagonists |
| US10888549B2 (en) | 2016-03-07 | 2021-01-12 | The Johns Hopkins University | Pharmaceutical agents targeting cancer stem cells |
| US20170273926A1 (en) * | 2016-03-24 | 2017-09-28 | Orbus Therapeutics, Inc. | Compositions and methods for use of eflornithine and derivatives and analogs thereof to treat cancers, including gliomas |
| JP2019522032A (ja) | 2016-07-29 | 2019-08-08 | ヤンセン ファーマシューティカ エヌ．ベー． | 前立腺癌の治療方法 |
| US10668039B2 (en) | 2016-09-02 | 2020-06-02 | The Children's Medical Center Corporation | Methods for treatment of adenoid cystic carcinoma |
| CN110191876A (zh) | 2016-10-06 | 2019-08-30 | 奥巴斯治疗股份有限公司 | 用于施用依氟鸟氨酸的制剂 |
| CN106389429A (zh) * | 2016-12-02 | 2017-02-15 | 郑州莉迪亚医药科技有限公司 | 一种治疗老年痴呆症的西药组合物及其应用 |
| US11426385B2 (en) | 2017-08-25 | 2022-08-30 | The Regents Of The University Of California | Methods of improving cancer chemotherapy |
| CN111777615B (zh) * | 2020-07-20 | 2022-04-19 | 济南大学 | 一种检测环氧合酶2的光动力治疗探针及其制备 |
| CN114767868B (zh) * | 2022-03-30 | 2023-04-18 | 宁夏医科大学 | Cox-2抑制剂与化疗药物在制备抗肿瘤药物中的应用 |
| WO2024184889A1 (en) * | 2023-03-08 | 2024-09-12 | Ariel Scientific Innovations Ltd. | Methods of treating |
Family Cites Families (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2465486A1 (fr) | 1979-09-21 | 1981-03-27 | Roussel Uclaf | Nouvelle application utilisant la lh-rh ou des agonistes |
| DE3121153A1 (de) | 1981-05-22 | 1982-12-09 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | "verwendung von aromatase-hemmern zur prophylaxe und therapie der prostatahyperplasie" |
| US4659695A (en) | 1985-02-08 | 1987-04-21 | Fernand Labrie | Method of treatment of prostate cancer |
| US4775660A (en) | 1984-08-02 | 1988-10-04 | Fernand Labrie | Treatment of breast cancer by combination therapy |
| US4760053A (en) | 1984-08-02 | 1988-07-26 | Fernand Labrie | Combination therapy for selected sex steroid dependent cancers |
| US5039805A (en) | 1988-12-08 | 1991-08-13 | Hoffmann-La Roche Inc. | Novel benzoic and phenylacetic acid derivatives |
| US5084466A (en) | 1989-01-31 | 1992-01-28 | Hoffmann-La Roche Inc. | Novel carboxamide pyridine compounds which have useful pharmaceutical utility |
| CA2008116C (en) | 1989-02-23 | 2001-11-20 | Thomas Weller | Glycine derivatives |
| US5686568A (en) | 1989-06-16 | 1997-11-11 | Cor Therapeutics, Inc. | Platelet aggregration inhibitors |
| US5061693A (en) | 1989-07-28 | 1991-10-29 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| CA2037153A1 (en) | 1990-03-09 | 1991-09-10 | Leo Alig | Acetic acid derivatives |
| US5612311A (en) | 1990-04-06 | 1997-03-18 | La Jolla Cancer Research Foundation | Method and composition for treating thrombosis |
| US5721210A (en) | 1990-07-09 | 1998-02-24 | Tanabe Seiyaku Co., Ltd. | Cyclic cell adhesion modulation compounds |
| US5229366A (en) | 1990-10-23 | 1993-07-20 | Fuji Photo Film Co., Ltd. | Peptide-containing polyethylene glycol derivatives and application thereof |
| AU646966B2 (en) | 1991-08-23 | 1994-03-10 | Takeda Chemical Industries Ltd. | 2-piperazinone compounds, their production and use |
| CA2078817A1 (en) | 1991-10-18 | 1993-04-19 | Beat A. Imhof | Anti-.alpha.6-integrin-antibodies |
| US5565449A (en) | 1991-10-18 | 1996-10-15 | Genentech, Inc. | Nonpeptidyl integrin inhibitors having specificity for the GPIIb IIIa receptor |
| JPH07103148B2 (ja) | 1991-12-16 | 1995-11-08 | 株式会社ディ・ディ・エス研究所 | アントラサイクリン−マクロライド複合体 |
| US5965132A (en) | 1992-03-05 | 1999-10-12 | Board Of Regents, The University Of Texas System | Methods and compositions for targeting the vasculature of solid tumors |
| US5225531A (en) | 1992-04-09 | 1993-07-06 | Washington University | Hexapeptide Lys Gly Ala Gly Asp Val |
| EP0589181A3 (en) | 1992-07-30 | 1995-02-22 | Yeda Res & Dev | Synthetic vitronectin derivatives and their pharmaceutical compositions. |
| WO1994007481A1 (en) * | 1992-10-02 | 1994-04-14 | Merck & Co., Inc. | N-(mercaptoacyl)peptidyl derivatives as antidegenerative agents |
| JPH06116289A (ja) | 1992-10-09 | 1994-04-26 | Fuji Photo Film Co Ltd | 細胞接着性ペプチド配列複合体とその用途 |
| JPH08503475A (ja) * | 1992-11-25 | 1996-04-16 | メルク エンド カンパニー インコーポレーテッド | 抗変性活性剤としてのカルボキシ−ペプチジル誘導体 |
| TW301607B (es) | 1993-03-09 | 1997-04-01 | Takeda Pharm Industry Co Ltd | |
| DE4310643A1 (de) | 1993-04-01 | 1994-10-06 | Merck Patent Gmbh | Cyclische Adhäsionsinhibitoren |
| DE4310632A1 (de) | 1993-04-01 | 1994-10-06 | Merck Patent Gmbh | Lineare Adhäsionsinhibitoren |
| EP0623615B1 (de) | 1993-05-01 | 1999-06-30 | MERCK PATENT GmbH | Substituierte 1-Phenyl-oxazolidin-2-on Derivate, deren Herstellung und deren Verwendung als Adhäsionsrezeptor-Antagonisten |
| DE4332384A1 (de) | 1993-09-23 | 1995-03-30 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten III |
| US5536814A (en) | 1993-09-27 | 1996-07-16 | La Jolla Cancer Research Foundation | Integrin-binding peptides |
| DE4336758A1 (de) | 1993-10-28 | 1995-05-04 | Merck Patent Gmbh | Lineare Adhäsionsinhibitoren |
| EP0656348B1 (de) | 1993-12-03 | 2000-05-03 | F. Hoffmann-La Roche Ag | Essigsäurederivate als Arzneimittel |
| JP3750144B2 (ja) | 1994-01-14 | 2006-03-01 | 大正製薬株式会社 | ３−アリールチアゾリン誘導体 |
| JP3235319B2 (ja) | 1994-01-14 | 2001-12-04 | 大正製薬株式会社 | チアゾリン誘導体 |
| DE4405378A1 (de) | 1994-02-19 | 1995-08-24 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten |
| JPH07285992A (ja) | 1994-02-25 | 1995-10-31 | Snow Brand Milk Prod Co Ltd | 新規ペプチド |
| US5753230A (en) * | 1994-03-18 | 1998-05-19 | The Scripps Research Institute | Methods and compositions useful for inhibition of angiogenesis |
| US5770565A (en) | 1994-04-13 | 1998-06-23 | La Jolla Cancer Research Center | Peptides for reducing or inhibiting bone resorption |
| DE4415310A1 (de) | 1994-04-30 | 1995-11-02 | Merck Patent Gmbh | Cyclopeptide |
| CA2190870A1 (en) | 1994-05-27 | 1995-12-07 | George D. Hartman | Compounds for inhibiting osteoclast-mediated bone resorption |
| US5990112A (en) * | 1996-06-18 | 1999-11-23 | Affymax Technologies N.V. | Inhibitors of metalloproteases pharmaceutical compositions comprising same and methods of their use |
| US5510332A (en) | 1994-07-07 | 1996-04-23 | Texas Biotechnology Corporation | Process to inhibit binding of the integrin α4 62 1 to VCAM-1 or fibronectin and linear peptides therefor |
| US5464855A (en) | 1994-08-09 | 1995-11-07 | Warner-Lambert Company | Thiophene-2-carboxamidotetrazoles and pharmaceutical use thereof |
| US5639726A (en) | 1994-09-30 | 1997-06-17 | The Regents Of The University Of Michigan | Peptide mediated enhancement of thrombolysis methods and compositions |
| ES2123889T3 (es) | 1994-11-02 | 1999-01-16 | Merck Patent Gmbh | Antagonistas de receptores de adhesion. |
| DE4439846A1 (de) | 1994-11-08 | 1996-05-09 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten |
| US5574026A (en) | 1994-12-13 | 1996-11-12 | American Cyanamid Company | Methods for inhibiting angiogenesis proliferation of endothelial or tumor cells and tumor growth |
| JPH08183752A (ja) | 1994-12-28 | 1996-07-16 | Sumitomo Pharmaceut Co Ltd | シクロヘキサン誘導体 |
| JPH08183788A (ja) | 1994-12-28 | 1996-07-16 | Sumitomo Pharmaceut Co Ltd | １−オキサ−６−アザスピロ〔２．５〕オクタン誘導体 |
| DE19504954A1 (de) | 1995-02-15 | 1996-08-22 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten |
| DE19516483A1 (de) | 1995-05-05 | 1996-11-07 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten |
| US5817750A (en) | 1995-08-28 | 1998-10-06 | La Jolla Cancer Research Foundation | Structural mimics of RGD-binding sites |
| US6100423A (en) | 1995-08-30 | 2000-08-08 | G. D. Searle & Co. | Amino benzenepropanoic acid compounds and derivatives thereof |
| ATE203234T1 (de) | 1995-08-30 | 2001-08-15 | Searle & Co | Meta-guanidine, harnstoff, thioharnstoff oder azacyklische aminobenzoesäure-derivate als integrin antagonisten |
| US6013651A (en) | 1995-08-30 | 2000-01-11 | G. D. Searle & Co. | Meta-azacyclic amino benzoic acid compounds and derivatives thereof |
| DE19534016A1 (de) | 1995-09-14 | 1997-03-20 | Merck Patent Gmbh | Biotinderivate |
| DE19534177A1 (de) | 1995-09-15 | 1997-03-20 | Merck Patent Gmbh | Cyclische Adhäsionsinhibitoren |
| EP0765660A3 (en) | 1995-09-28 | 1998-09-23 | Takeda Chemical Industries, Ltd. | Microcapsules comprising 2-piperazinone-1-acetic acid compounds |
| DE19539091A1 (de) | 1995-10-20 | 1997-04-24 | Thomae Gmbh Dr K | 5-gliedrige Heterocyclen, diese Verbindungen enthaltende Arzneimittel und deren Verwendung sowie Verfahren zur ihrer Herstellung |
| ATE230275T1 (de) | 1995-10-25 | 2003-01-15 | Senju Pharma Co | Angiogense-inhibitor |
| EP1095936B1 (en) * | 1995-12-08 | 2004-11-24 | Agouron Pharmaceuticals, Inc. | Intermediates useful for the preparation of metallproteinase inhibitors |
| US5760028A (en) | 1995-12-22 | 1998-06-02 | The Dupont Merck Pharmaceutical Company | Integrin receptor antagonists |
| PT796855E (pt) | 1996-03-20 | 2002-07-31 | Hoechst Ag | Inibicao da reabsorcao nos ossos e antagonistas de vitronectina |
| DE19626701A1 (de) | 1996-07-03 | 1998-01-08 | Hoechst Ag | Neue Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten |
| JP2000515493A (ja) | 1996-03-29 | 2000-11-21 | ジー．ディー．サール アンド カンパニー | パラ―置換フェニレン誘導体 |
| JP2000506538A (ja) | 1996-03-29 | 2000-05-30 | ジー．ディー．サール アンド カンパニー | メタ―置換フェニレン誘導体 |
| PT889876E (pt) | 1996-03-29 | 2001-11-30 | Searle & Co | Derivados de fenilenossulfonamidas meta-substituidas |
| PT894084E (pt) | 1996-03-29 | 2002-11-29 | Searle & Co | Derivados de acido cinamico e sua utilizacao como antagonistas de integrina |
| DE69705300T2 (de) | 1996-03-29 | 2002-05-02 | G.D. Searle & Co., Chicago | Cyclopropylalkansäurederivate |
| DE19613933A1 (de) | 1996-04-06 | 1997-10-09 | Merck Patent Gmbh | Cyclische Adhäsionsinhibitoren |
| US5925655A (en) | 1996-04-10 | 1999-07-20 | Merck & Co., Inc. | αv β3 antagonists |
| AU2438297A (en) * | 1996-05-09 | 1997-11-26 | Alcon Laboratories, Inc. | Combinations of angiostatic compounds |
| DE19654483A1 (de) | 1996-06-28 | 1998-01-02 | Merck Patent Gmbh | Phenylalanin-Derivate |
| ES2167758T3 (es) | 1996-07-12 | 2002-05-16 | Searle & Co | Sintesis asimetrica de beta-aminoacidos quirales. |
| DE19629816A1 (de) | 1996-07-24 | 1998-01-29 | Hoechst Ag | Neue Cycloalkyl-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten |
| DE19629817A1 (de) | 1996-07-24 | 1998-01-29 | Hoechst Ag | Neue Imino-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten |
| UA60311C2 (uk) * | 1996-10-02 | 2003-10-15 | Смітклайн Бічам Корпорейшн | Антагоністи рецептора вітронектину, спосіб одержання цих сполук та фармацевтична композиція |
| DK0932402T3 (da) * | 1996-10-15 | 2004-11-08 | Searle Llc | Metode til anvendelse af cyclooxygenase-2-inhibitorer ved behandling og forebyggelse af neoplasi |
| US5919792A (en) | 1996-10-30 | 1999-07-06 | Merck & Co., Inc. | Integrin antagonists |
| TR199901703T2 (xx) * | 1996-11-19 | 2000-07-21 | G.D. Searle & Co. | Siklooksijenaz-2 inhibit�rlerini anti-anjiyojenik ajanlar olarak kullanma y�ntemi. |
| EP0846702B1 (en) | 1996-12-09 | 2009-03-11 | MERCK PATENT GmbH | Soluble recombinant alphaV beta3 adhesion receptor |
| DE19653647A1 (de) | 1996-12-20 | 1998-06-25 | Hoechst Ag | Vitronectin - Rezeptorantagonisten, deren Herstellung sowie deren Verwendung |
| DE19653646A1 (de) | 1996-12-20 | 1998-06-25 | Hoechst Ag | Substituierte Purinderivate, Verfahren zu deren Herstellung, sie enthaltende Mittel und deren Verwendung |
| DE19653645A1 (de) | 1996-12-20 | 1998-06-25 | Hoechst Ag | Vitronectin - Rezeptorantagonisten, deren Herstellung sowie deren Verwendung |
| US5837696A (en) * | 1997-01-15 | 1998-11-17 | The Research Foundation Of State University Of New York | Method of inhibiting cancer growth |
| US6017925A (en) * | 1997-01-17 | 2000-01-25 | Merck & Co., Inc. | Integrin antagonists |
| CA2277273C (en) * | 1997-01-17 | 2008-03-25 | Merck & Co., Inc. | Integrin antagonists |
| AU1110799A (en) * | 1997-10-29 | 1999-05-17 | Warner-Lambert Company | Method of inhibiting metastases of cancer cells |
| EP1042290A1 (en) * | 1997-11-14 | 2000-10-11 | G.D. SEARLE & CO. | Aromatic sulfone hydroxamic acid metalloprotease inhibitor |
| ATE298338T1 (de) * | 1997-12-17 | 2005-07-15 | Merck & Co Inc | Integrin-rezeptor-antagonisten |
| NZ333399A (en) * | 1997-12-24 | 2000-05-26 | Sankyo Co | Cyclooxygenase-2 inhibitors (COX-2) for the prevention and treatment of tumors, cachexia and tumor-metastasis |
| SI0928793T1 (en) | 1998-01-02 | 2002-10-31 | F. Hoffmann-La Roche Ag | Thiazole derivatives |
| US6372719B1 (en) * | 1998-03-04 | 2002-04-16 | Jay Cunningham | ανβ3 integrin antagonists in combination with chemotherapeutic agents |
| CZ20003672A3 (cs) * | 1998-04-10 | 2001-08-15 | G. D. Searle & Co. | Heterocyklické glycyl-beta-alaninové deriváty jako agonisté vitronektinu |
| EP1100506A4 (en) * | 1998-07-29 | 2002-06-26 | Merck & Co Inc | INTEGRIN RECEPTOR ANTAGONISTS |
| US6277878B1 (en) * | 1998-09-07 | 2001-08-21 | Pfizer Inc | Substituted indole compounds as anti-inflammatory and analgesic agents |
-
1999
- 1999-12-22 CZ CZ20012320A patent/CZ20012320A3/cs unknown
- 1999-12-22 WO PCT/US1999/030776 patent/WO2000037107A2/en not_active Application Discontinuation
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