JP2016529321A - 改変されたグリコシル基を含む糖脂質を用いたヒトiNKT細胞の活性化 - Google Patents
改変されたグリコシル基を含む糖脂質を用いたヒトiNKT細胞の活性化 Download PDFInfo
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Abstract
Description
本発明は、一般的に免疫療法薬の分野に関する。特に、本開示は、ヒトにおいてインバリアントナチュラルキラーT(iNKT)細胞をモジュレートしてサイトカインおよび/またはケモカインの生成を刺激し、したがって下流の免疫細胞をトランス活性化し、それにより先天性免疫と適応免疫の橋渡しをする糖脂質およびそのバリアントに関する。
ナチュラルキラー様T(NKT)細胞は、がんおよび自己免疫障害などの疾患の処置において数多くの治療的潜在性を有する区別可能なTリンパ球集団である。インバリアントナチュラルキラーT(iNKT)細胞は、先天性免疫と適応免疫の両方の特長を有する調節性T細胞のサブセットを構成している。MHCクラスIまたはII分子によって提示されたペプチドによって活性化される通常のT細胞とは対照的に、iNKT細胞は、抗原提示細胞(APC)上に発現される非古典的MHC I分子であるCD1dと関連して存在する脂質誘導体を認識する。
α−GalCer(α−ガラクトシルセラミド)は、a−結合型ガラクトース、スフィンゴシンおよびアシル尾部で構成された糖脂質であり、アゲラスフィン(海綿Agelas mauritianusから単離)の構造の最適化によって得られた。これは、インビトロおよびインビボの両方で抗腫瘍活性を示すことがわかっており、マウスとヒトの両方のインバリアントナチュラルキラーT細胞(iNKT細胞)について、これまで知られている最も強力なリガンドであることが示されている。
したがって、iNKT細胞の選択的Th1またはTh2サイトカイン応答を刺激するための多くの類似体が設計された。糖脂質は、マウスおよび人間の両方において著しいTh1偏向を有し、インビボ卓越した腫瘍防除をもたらす。例えば、切断型スフィンゴシン尾部を有するスフィンゴ糖脂質(GSL)はTh2方向に免疫応答を誘導することができ、自己免疫性脳脊髄炎が予防された17。Miyamoto,K.;Miyake,S.;Yamamura,T.Nature 2001,413,531.他方で、アシル鎖上にフェニル環を有するGSLによりマウスおよびヒトにおいてTh1偏向サイトカインが誘導され、マウスでは乳房、肺および黒色腫腫瘍に対してより強力な抗がん活性が示された18,19。(18)(Chang,Y.J.;Huang,J.R.;Tsai,Y.C.;Hung,J.T.;Wu,D.;Fujio,M.;Wong,C.H.;Yu,A.L.Proc.Natl.Acad.Sci.U.S.A.2007,104,10299および(19)Wu,T.N.;Lin,K.H.;Chang,Y.J.;Huang,J.R.;Cheng,J.Y.;Yu,A.L.;Wong,C.H.Proc.Natl.Acad.Sci.U.S.A.2011,108,17275.
ナチュラルキラーT細胞(NKT)は、固有の特性、例えば、CD1dによって提示された天然または合成の糖脂質に対する反応性およびインバリアントT細胞抗原受容体(TCR)アルファ鎖の発現を有するTリンパ球のサブセットを表す。NKTは、機能的に区別される通常のαβT細胞と、ナチュラルキラー細胞とT細胞の両方の特性を共有しており、リガンドにより刺激されると(先天性免疫)、TH1型応答およびTH2型応答の両方を速やかにもたらし得るという点で異なる。逆説的に、NKTの活性化は免疫応答の抑制または刺激のいずれかをもたらすことがあり得る。例えば、TH1サイトカインの生成は、抗腫瘍、抗ウイルス/抗菌およびアジュバント活性を伴う細胞性免疫を促進すると考えられているが、TH2サイトカインの生成は、自己免疫疾患を抑制し、抗体産生を促進すると考えられている。NKTは免疫系において調節的役割を果たしているため、免疫療法の魅力的な標的である。
−N3、−SO2H、−SO3H、−OH、−OC1〜6アルキル、−ON(C1〜6アルキル)2、−N(C1〜6アルキル)2、−N(C1〜6アルキル)3 +X−、−NH(C1〜6アルキル)2 +X−、−NH2(C1〜6アルキル)+X−、−NH3 +X−、−N(OC1〜6アルキル)(C1〜6アルキル)、−N(OH)(C1〜6アルキル)、−NH(OH)、−SH、−SC1〜6アルキル、−SS(C1〜6アルキル)、−C(=O)(C1〜6アルキル)、−CO2H、−CO2(C1〜6アルキル)、−OC(=O)(C1〜6アルキル)、−OCO2(C1〜6アルキル)、−C(=O)NH2、−C(=O)N(C1〜6アルキル)2、−OC(=O)NH(C1〜6アルキル)、−NHC(=O)(C1〜6アルキル)、−N(C1〜6アルキル)C(=O)(C1〜6アルキル)、−NHCO2(C1〜6アルキル)、−NHC(=O)N(C1〜6アルキル)2、−NHC(=O)NH(C1〜6アルキル)、−NHC(=O)NH2、−C(=NH)O(C1〜6アルキル)、−OC(=NH)(C1〜6アルキル)、−OC(=NH)OC1〜6アルキル、−C(=NH)N(C1〜6アルキル)2、−C(=NH)NH(C1〜6アルキル)、−C(=NH)NH2、−OC(=NH)N(C1〜6アルキル)2、−OC(NH)NH(C1〜6アルキル)、−OC(NH)NH2、−NHC(NH)N(C1〜6アルキル)2、−NHC(=NH)NH2、−NHSO2(C1〜6アルキル)、−SO2N(C1〜6アルキル)2、−SO2NH(C1〜6アルキル)、−SO2NH2,−SO2C1〜6アルキル、−SO2OC1〜6アルキル、−OSO2C1〜6アルキル、−SOC1〜6アルキル、−Si(C1〜6アルキル)3、−Osi(C1〜6アルキル)3−C(=S)N(C1〜6アルキル)2、C(=S)NH(C1〜6アルキル)、C(=S)NH2、−C(=O)S(C1〜6アルキル)、−C(=S)SC1〜6アルキル、−SC(=S)SC1〜6アルキル、−P(=O)2(C1〜6アルキル)、−P(=O)(C1〜6アルキル)2、−OP(=O)(C1〜6アルキル)2、−OP(=O)(OC1〜6アルキル)2、C1〜6アルキル、C1〜6ペルハロアルキル、C2〜6アルケニル、C2〜6アルキニル、C3〜10カルボシクリル、C6〜10アリール、3〜10員のヘテロシクリル、5〜10員のヘテロアリールであるか;または2つのRgg置換基が連接されて=Oもしくは=Sを形成していてもよく;ここで、X−は対イオンである。
以下の実施例は、当業者に完全な本発明ならびに本発明による実施形態をどのようにして作製および使用するかの説明をもたらすために示しており、本発明者らが発見とみなす範囲の限定を意図するものではない。使用した数値(例えば、量、温度など)に関して精度が確実になるよう努力を行なったが、いくらかの実験誤差および偏差を考慮されたい。特に記載のない限り、部は重量部であり、分子量は重量平均分子量であり、温度はセ氏度であり、圧力は大気圧またはほぼ大気圧である。
によってコンピュータ計算した。
Claims (48)
- 式(I):
R1は−OHまたはハロゲンであり;
R2は−OH、水素またはハロゲンであり;
R3は水素またはハロゲンであり;
各場合のR4およびR5は独立して、水素、ハロゲン、任意選択的に置換されたアルキル、任意選択的に置換されたアルケニル、任意選択的に置換されたアルキニル、任意選択的に置換されたカルボシクリル、任意選択的に置換されたアリール、任意選択的に置換されたヘテロシクリル、任意選択的に置換されたヘテロアリール、任意選択的に置換されたアルコキシ、任意選択的に置換されたアミノ基または任意選択的に置換されたアシルからなる群より選択され;
nは1〜15(両端を含む)の整数であり;
mは1〜20(両端を含む)の整数である)
を有する免疫アジュバント化合物またはその薬学的に許容され得る塩。 - R2が−OHである、請求項1に記載の化合物。
- R2がハロゲンである、請求項1に記載の化合物。
- R1が−OHである、請求項1〜3のいずれか1項に記載の化合物。
- R1がハロゲンである、請求項1〜3のいずれか1項に記載の化合物。
- R6がハロゲンである、請求項6に記載の化合物。
- R6がFである、請求項6に記載の化合物。
- 各場合のR7およびR8が独立して、水素またはハロゲンである、請求項9に記載の化合物。
- R7が水素であり;R8がFであり;kが1、2または3である、請求項9に記載の化合物。
- R7がFであり;R8が水素であり;jが1、2または3である、請求項9に記載の化合物。
- R7およびR8がともにFであり;kが1、2または3であり;jが1、2または3である、請求項9に記載の化合物。
- (i)抗原とともにヒト被験体に共投与した場合、免疫応答を刺激するのに充分な量の請求項1〜14のいずれかに記載の化合物および(ii)薬学的に許容され得る賦形剤を含む医薬組成物。
- 抗原の免疫原性の増大を、それを必要とする被験体において行なうための方法であって、該抗原を、一般式IのGSL化合物を含むアジュバント組成物とともに共投与することを含む方法。
- 免疫応答の刺激を、それを必要とするヒト被験体において行なうための方法であって、該被験体に、薬学的に許容され得る担体中の治療有効量の免疫アジュバント組成物を投与することを含み、該組成物が請求項1〜14のいずれかに記載の化合物を含むものである方法。
- 前記アジュバント組成物がワクチンアジュバントである、請求項16に記載の方法。
- 前記アジュバント組成物が、ヒトにおいてインバリアントナチュラルキラーT(iNKT)細胞を上昇させることが可能な量で投与される、請求項16に記載の方法。
- 前記アジュバント組成物の投与により、ヒトにおいてサイトカインおよび/またはケモカインの生成が増大する、請求項19に記載の方法。
- 前記サイトカインの生成が下流の免疫細胞をトランス活性化するのに充分なものである、請求項20に記載の方法。
- 前記下流の免疫細胞が、樹状細胞(DC)、ナチュラルキラー細胞(NK)、B細胞、CD4+ TおよびCD8+ T細胞のうちの1種類またはそれより多くを含む、請求項21に記載の方法。
- 前記サイトカインがTh1サイトカインを含む、請求項20に記載の方法。
- 前記Th1サイトカインが:インターフェロン−ガンマ(IFN−γ)、GM−CSF、TNFα、インターロイキン2、インターロイキン12およびインターロイキン10を含む群のうちの少なくとも1種類から選択される、請求項23に記載の方法。
- 前記ケモカインが、RANTES、MIP−1α、KC、MCP−1、IP−10およびMIGを含む群のうちの少なくとも1種類から選択される、請求項20に記載の方法。
- 前記組成物の投与が抗がん効果を有する、請求項16に記載の方法。
- 前記がんが、肺がん、乳がん、肝細胞癌、白血病、充実性腫瘍および癌からなる群より選択される、請求項26に記載の方法。
- 式Iの化合物のR4が置換または非置換のアリールおよび置換または非置換のヘテロアリールから選択され、ヒトにおけるTh1サイトカインの増加がTh2サイトカインのいずれかの増加を超えている、請求項16に記載の方法。
- インバリアントナチュラルキラーT(iNKT)細胞の生成の上昇を、それを必要とするヒト被験体において行なうための方法であって:該被験体に治療有効量の医薬組成物を投与することを含み、該組成物が請求項1〜14のいずれかに記載の化合物を含むものである方法。
- 前記iNKTレベルの上昇が、グリコシル頭部基としてアルファ−ガラクトース(αGal)を含む等量の糖脂質類似体の投与により得られる上昇と比べた場合、大きくなる、請求項29に記載の方法。
- サイトカインおよび/またはケモカインの生成の刺激を、それを必要とするヒト被験体において行なうための方法であって:該被験体に治療有効量の医薬組成物を投与することを含み、該組成物が、サイトカイン/ケモカインの生成を増大させるのに充分な量の請求項1〜14のいずれかに記載の化合物を含むものである方法。
- 前記サイトカインの生成が下流の免疫細胞をトランス活性化するのに充分なものである、請求項31に記載の方法。
- 前記下流の免疫細胞が、樹状細胞(DC)、ナチュラルキラー細胞(NK)、B細胞、CD4+ TおよびCD8+ T細胞のうちの1種類またはそれより多くを含む、請求項32に記載の方法。
- 前記サイトカインがTh1サイトカインを含む、請求項31に記載の方法。
- 前記サイトカインが:インターフェロン−ガンマ(IFN−γ)、GM−CSF、TNFα、インターロイキン2、インターロイキン12およびインターロイキン10から選択される、請求項34に記載の方法。
- 前記ケモカインが:RANTES、MIP−1α、KC、MCP−1、IP−10およびMIGから選択される、請求項31に記載の方法。
- ワクチンアジュバントである、請求項15に記載の医薬組成物。
- 抗がん治療薬である、請求項15に記載の医薬組成物。
- 前記化合物のR4が置換または非置換のアリールおよび置換または非置換のヘテロアリールから選択され、該化合物が、ヒトにおいてTh1サイトカインを、付随するTh2サイトカイン増加を最小限にして増加させることが可能である、請求項16に記載の医薬組成物。
- 被験体において抗原による免疫応答を増大させるための方法であって、該被験体に、1種類またはそれより多くの抗原と免疫原性有効量の請求項15に記載のアジュバント組成物とを含む有効量のワクチンを投与することを含む方法。
- 前記1種類またはそれより多くの抗原が、細菌抗原、ウイルス抗原、真菌抗原、原生動物抗原、プリオン抗原、新生抗原、腫瘍抗原および自己抗原からなる群より選択される、請求項40に記載の方法。
- 前記ワクチンが、核酸、タンパク質、ペプチド、糖タンパク質、炭水化物、融合タンパク質、脂質、糖脂質、炭水化物−タンパク質コンジュゲート;細胞もしくはその抽出物;死細胞もしくは弱毒化細胞もしくはその抽出物;腫瘍細胞もしくはその抽出物;ウイルス粒子;アレルゲンまたはその混合物からなる群より選択される、請求項40に記載の方法。
- 前記投与される抗原が腫瘍抗原である、請求項40に記載の方法。
- 前記抗原の量が0.1μg〜100mg/kg体重の範囲で投与される、請求項40に記載の方法。
- 前記アジュバントの量が10〜100μg/kg体重の範囲である、請求項40に記載の方法。
- 前記共投与される組成物が、式IのGSLと薬学的に許容され得る担体とを含む共製剤化された薬学的に許容され得る組成物である、請求項40に記載の方法。
- 式IのGSLを含む製造物品。
- 請求項1〜14のいずれか1項に記載のGSLおよび使用のための説明書を備えたキット。
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2023153527A1 (ja) * | 2022-02-14 | 2023-08-17 | 国立研究開発法人理化学研究所 | Nkt細胞リガンド含有リポソーム組成物 |
Families Citing this family (32)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7960139B2 (en) | 2007-03-23 | 2011-06-14 | Academia Sinica | Alkynyl sugar analogs for the labeling and visualization of glycoconjugates in cells |
US8680020B2 (en) | 2008-07-15 | 2014-03-25 | Academia Sinica | Glycan arrays on PTFE-like aluminum coated glass slides and related methods |
US11377485B2 (en) | 2009-12-02 | 2022-07-05 | Academia Sinica | Methods for modifying human antibodies by glycan engineering |
US10087236B2 (en) | 2009-12-02 | 2018-10-02 | Academia Sinica | Methods for modifying human antibodies by glycan engineering |
WO2011130332A1 (en) | 2010-04-12 | 2011-10-20 | Academia Sinica | Glycan arrays for high throughput screening of viruses |
US10130714B2 (en) | 2012-04-14 | 2018-11-20 | Academia Sinica | Enhanced anti-influenza agents conjugated with anti-inflammatory activity |
WO2014031498A1 (en) | 2012-08-18 | 2014-02-27 | Academia Sinica | Cell-permeable probes for identification and imaging of sialidases |
WO2014210397A1 (en) | 2013-06-26 | 2014-12-31 | Academia Sinica | Rm2 antigens and use thereof |
US9981030B2 (en) | 2013-06-27 | 2018-05-29 | Academia Sinica | Glycan conjugates and use thereof |
CA2923579C (en) | 2013-09-06 | 2023-09-05 | Academia Sinica | Human inkt cell activation using glycolipids with altered glycosyl groups |
US10150818B2 (en) | 2014-01-16 | 2018-12-11 | Academia Sinica | Compositions and methods for treatment and detection of cancers |
JP2017507118A (ja) | 2014-01-16 | 2017-03-16 | アカデミア シニカAcademia Sinica | がんの処置および検出のための組成物および方法 |
CN106415244B (zh) | 2014-03-27 | 2020-04-24 | 中央研究院 | 反应性标记化合物及其用途 |
EP3149045B1 (en) | 2014-05-27 | 2023-01-18 | Academia Sinica | Compositions and methods relating to universal glycoforms for enhanced antibody efficacy |
WO2015184004A1 (en) | 2014-05-27 | 2015-12-03 | Academia Sinica | Anti-cd20 glycoantibodies and uses thereof |
JP7062361B2 (ja) | 2014-05-27 | 2022-05-06 | アカデミア シニカ | 抗her2糖操作抗体群およびその使用 |
US10118969B2 (en) | 2014-05-27 | 2018-11-06 | Academia Sinica | Compositions and methods relating to universal glycoforms for enhanced antibody efficacy |
CA2950433A1 (en) | 2014-05-28 | 2015-12-03 | Academia Sinica | Anti-tnf-alpha glycoantibodies and uses thereof |
EP3191500A4 (en) * | 2014-09-08 | 2018-04-11 | Academia Sinica | HUMAN iNKT CELL ACTIVATION USING GLYCOLIPIDS |
WO2016109880A1 (en) | 2015-01-06 | 2016-07-14 | Immunovaccine Technologies Inc. | Lipid a mimics, methods of preparation, and uses thereof |
US9975965B2 (en) | 2015-01-16 | 2018-05-22 | Academia Sinica | Compositions and methods for treatment and detection of cancers |
US10495645B2 (en) | 2015-01-16 | 2019-12-03 | Academia Sinica | Cancer markers and methods of use thereof |
EP3248005B1 (en) | 2015-01-24 | 2020-12-09 | Academia Sinica | Novel glycan conjugates and methods of use thereof |
CA3016170A1 (en) | 2016-03-08 | 2017-09-14 | Academia Sinica | Methods for modular synthesis of n-glycans and arrays thereof |
SG11201809402VA (en) | 2016-04-28 | 2018-11-29 | Riken | Technology for efficient activation of nkt cells |
KR102588027B1 (ko) | 2016-08-22 | 2023-10-12 | 초 파마 인크. | 항체, 결합 단편 및 사용 방법 |
CN108070011A (zh) * | 2018-01-05 | 2018-05-25 | 河南科技大学 | 一种半乳糖糖酯基供体化合物及其制备方法 |
CN110872575A (zh) * | 2019-10-21 | 2020-03-10 | 中冠赛尔生物科技(北京)有限公司 | 一种iNKT细胞的体外扩增方法 |
US11718565B2 (en) * | 2020-01-31 | 2023-08-08 | Champion Link International Corporation | Panel for forming a floor covering and such floor covering |
CA3212136A1 (en) | 2021-03-01 | 2022-09-09 | Deciduous Therapeutics, Inc. | Compounds for activating invariant natural killer t-cells and methods of use in eliminating inflammatory senescent cells |
CN113750229A (zh) * | 2021-10-18 | 2021-12-07 | 浙江省农业科学院 | 人参茎叶皂苷纳米粒及其制备方法和用途 |
EP4174074A1 (en) | 2021-10-29 | 2023-05-03 | Consejo Superior de Investigaciones Científicas (CSIC) | Multiantennary glycolipid mimetics |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP3717512B2 (ja) * | 1992-10-22 | 2005-11-16 | 麒麟麦酒株式会社 | 新規スフィンゴ糖脂質およびその使用 |
JP2008511634A (ja) * | 2004-08-27 | 2008-04-17 | アルバート アインシュタイン カレッジ オブ メディシン オブ イエシバ ユニバーシティ | 免疫及び自己免疫の調節因子としてのセラミド誘導体 |
JP2008525495A (ja) * | 2004-12-28 | 2008-07-17 | ザ ロックフェラー ユニバーシティ | Nkt細胞に対する抗原としての糖脂質及びその類似体 |
WO2008133801A1 (en) * | 2007-04-23 | 2008-11-06 | Albert Einstein College Of Medicine Of Yeshiva University | Ceramide derivatives as modulators of immunity and autoimmunity |
WO2009119692A1 (ja) * | 2008-03-25 | 2009-10-01 | 独立行政法人理化学研究所 | 新規糖脂質及びその用途 |
US20120178705A1 (en) * | 2011-01-05 | 2012-07-12 | National Taiwan University | Methods for preparation of glycosphingolipids and uses thereof |
Family Cites Families (374)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
US3896111A (en) | 1973-02-20 | 1975-07-22 | Research Corp | Ansa macrolides |
US4151042A (en) | 1977-03-31 | 1979-04-24 | Takeda Chemical Industries, Ltd. | Method for producing maytansinol and its derivatives |
US4137230A (en) | 1977-11-14 | 1979-01-30 | Takeda Chemical Industries, Ltd. | Method for the production of maytansinoids |
USRE30985E (en) | 1978-01-01 | 1982-06-29 | Serum-free cell culture media | |
US4265814A (en) | 1978-03-24 | 1981-05-05 | Takeda Chemical Industries | Matansinol 3-n-hexadecanoate |
US4307016A (en) | 1978-03-24 | 1981-12-22 | Takeda Chemical Industries, Ltd. | Demethyl maytansinoids |
JPS5562090A (en) | 1978-10-27 | 1980-05-10 | Takeda Chem Ind Ltd | Novel maytansinoid compound and its preparation |
JPS5566585A (en) | 1978-11-14 | 1980-05-20 | Takeda Chem Ind Ltd | Novel maytansinoid compound and its preparation |
US4256746A (en) | 1978-11-14 | 1981-03-17 | Takeda Chemical Industries | Dechloromaytansinoids, their pharmaceutical compositions and method of use |
JPS55164687A (en) | 1979-06-11 | 1980-12-22 | Takeda Chem Ind Ltd | Novel maytansinoid compound and its preparation |
JPS55102583A (en) | 1979-01-31 | 1980-08-05 | Takeda Chem Ind Ltd | 20-acyloxy-20-demethylmaytansinoid compound |
JPS55162791A (en) | 1979-06-05 | 1980-12-18 | Takeda Chem Ind Ltd | Antibiotic c-15003pnd and its preparation |
JPS55164685A (en) | 1979-06-08 | 1980-12-22 | Takeda Chem Ind Ltd | Novel maytansinoid compound and its preparation |
JPS55164686A (en) | 1979-06-11 | 1980-12-22 | Takeda Chem Ind Ltd | Novel maytansinoid compound and its preparation |
US4309428A (en) | 1979-07-30 | 1982-01-05 | Takeda Chemical Industries, Ltd. | Maytansinoids |
JPS5645483A (en) | 1979-09-19 | 1981-04-25 | Takeda Chem Ind Ltd | C-15003phm and its preparation |
JPS5645485A (en) | 1979-09-21 | 1981-04-25 | Takeda Chem Ind Ltd | Production of c-15003pnd |
EP0028683A1 (en) | 1979-09-21 | 1981-05-20 | Takeda Chemical Industries, Ltd. | Antibiotic C-15003 PHO and production thereof |
US4270537A (en) | 1979-11-19 | 1981-06-02 | Romaine Richard A | Automatic hypodermic syringe |
US4376110A (en) | 1980-08-04 | 1983-03-08 | Hybritech, Incorporated | Immunometric assays using monoclonal antibodies |
WO1982001188A1 (en) | 1980-10-08 | 1982-04-15 | Takeda Chemical Industries Ltd | 4,5-deoxymaytansinoide compounds and process for preparing same |
US4450254A (en) | 1980-11-03 | 1984-05-22 | Standard Oil Company | Impact improvement of high nitrile resins |
US4419446A (en) | 1980-12-31 | 1983-12-06 | The United States Of America As Represented By The Department Of Health And Human Services | Recombinant DNA process utilizing a papilloma virus DNA as a vector |
US4315929A (en) | 1981-01-27 | 1982-02-16 | The United States Of America As Represented By The Secretary Of Agriculture | Method of controlling the European corn borer with trewiasine |
US4313946A (en) | 1981-01-27 | 1982-02-02 | The United States Of America As Represented By The Secretary Of Agriculture | Chemotherapeutically active maytansinoids from Trewia nudiflora |
JPS57192389A (en) | 1981-05-20 | 1982-11-26 | Takeda Chem Ind Ltd | Novel maytansinoid |
US4596792A (en) | 1981-09-04 | 1986-06-24 | The Regents Of The University Of California | Safe vaccine for hepatitis containing polymerized serum albumin |
US4741900A (en) | 1982-11-16 | 1988-05-03 | Cytogen Corporation | Antibody-metal ion complexes |
US4601978A (en) | 1982-11-24 | 1986-07-22 | The Regents Of The University Of California | Mammalian metallothionein promoter system |
US4560655A (en) | 1982-12-16 | 1985-12-24 | Immunex Corporation | Serum-free cell culture medium and process for making same |
US4657866A (en) | 1982-12-21 | 1987-04-14 | Sudhir Kumar | Serum-free, synthetic, completely chemically defined tissue culture media |
US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
US4767704A (en) | 1983-10-07 | 1988-08-30 | Columbia University In The City Of New York | Protein-free culture medium |
US4599230A (en) | 1984-03-09 | 1986-07-08 | Scripps Clinic And Research Foundation | Synthetic hepatitis B virus vaccine including both T cell and B cell determinants |
US4599231A (en) | 1984-03-09 | 1986-07-08 | Scripps Clinic And Research Foundation | Synthetic hepatitis B virus vaccine including both T cell and B cell determinants |
US4965199A (en) | 1984-04-20 | 1990-10-23 | Genentech, Inc. | Preparation of functional human factor VIII in mammalian cells using methotrexate based selection |
US4970198A (en) | 1985-10-17 | 1990-11-13 | American Cyanamid Company | Antitumor antibiotics (LL-E33288 complex) |
US4596556A (en) | 1985-03-25 | 1986-06-24 | Bioject, Inc. | Hypodermic injection apparatus |
US4601903A (en) | 1985-05-01 | 1986-07-22 | The United States Of America As Represented By The Department Of Health And Human Services | Vaccine against Neisseria meningitidis Group B serotype 2 invasive disease |
GB8516415D0 (en) | 1985-06-28 | 1985-07-31 | Celltech Ltd | Culture of animal cells |
US4676980A (en) | 1985-09-23 | 1987-06-30 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Target specific cross-linked heteroantibodies |
US4927762A (en) | 1986-04-01 | 1990-05-22 | Cell Enterprises, Inc. | Cell culture medium with antioxidant |
US5567610A (en) | 1986-09-04 | 1996-10-22 | Bioinvent International Ab | Method of producing human monoclonal antibodies and kit therefor |
US5075109A (en) | 1986-10-24 | 1991-12-24 | Southern Research Institute | Method of potentiating an immune response |
US6024983A (en) | 1986-10-24 | 2000-02-15 | Southern Research Institute | Composition for delivering bioactive agents for immune response and its preparation |
CA1283827C (en) | 1986-12-18 | 1991-05-07 | Giorgio Cirelli | Appliance for injection of liquid formulations |
IL85035A0 (en) | 1987-01-08 | 1988-06-30 | Int Genetic Eng | Polynucleotide molecule,a chimeric antibody with specificity for human b cell surface antigen,a process for the preparation and methods utilizing the same |
US5079233A (en) | 1987-01-30 | 1992-01-07 | American Cyanamid Company | N-acyl derivatives of the LL-E33288 antitumor antibiotics, composition and methods for using the same |
GB8704027D0 (en) | 1987-02-20 | 1987-03-25 | Owen Mumford Ltd | Syringe needle combination |
JP3101690B2 (ja) | 1987-03-18 | 2000-10-23 | エス・ビィ・2・インコーポレイテッド | 変性抗体の、または変性抗体に関する改良 |
US4849222A (en) | 1987-03-24 | 1989-07-18 | The Procter & Gamble Company | Mixtures for treating hypercholesterolemia |
US4940460A (en) | 1987-06-19 | 1990-07-10 | Bioject, Inc. | Patient-fillable and non-invasive hypodermic injection device assembly |
US4941880A (en) | 1987-06-19 | 1990-07-17 | Bioject, Inc. | Pre-filled ampule and non-invasive hypodermic injection device assembly |
US4790824A (en) | 1987-06-19 | 1988-12-13 | Bioject, Inc. | Non-invasive hypodermic injection device |
US4975278A (en) | 1988-02-26 | 1990-12-04 | Bristol-Myers Company | Antibody-enzyme conjugates in combination with prodrugs for the delivery of cytotoxic agents to tumor cells |
US5004697A (en) | 1987-08-17 | 1991-04-02 | Univ. Of Ca | Cationized antibodies for delivery through the blood-brain barrier |
US5606040A (en) | 1987-10-30 | 1997-02-25 | American Cyanamid Company | Antitumor and antibacterial substituted disulfide derivatives prepared from compounds possessing a methyl-trithio group |
US5770701A (en) | 1987-10-30 | 1998-06-23 | American Cyanamid Company | Process for preparing targeted forms of methyltrithio antitumor agents |
US5053394A (en) | 1988-09-21 | 1991-10-01 | American Cyanamid Company | Targeted forms of methyltrithio antitumor agents |
JP2670680B2 (ja) | 1988-02-24 | 1997-10-29 | 株式会社ビーエムジー | 生理活性物質含有ポリ乳酸系微小球およびその製造法 |
US5339163A (en) | 1988-03-16 | 1994-08-16 | Canon Kabushiki Kaisha | Automatic exposure control device using plural image plane detection areas |
JPH01287029A (ja) | 1988-05-13 | 1989-11-17 | Mect Corp | 新規抗ウィルス剤 |
ATE135397T1 (de) | 1988-09-23 | 1996-03-15 | Cetus Oncology Corp | Zellenzuchtmedium für erhöhtes zellenwachstum, zur erhöhung der langlebigkeit und expression der produkte |
GB8823869D0 (en) | 1988-10-12 | 1988-11-16 | Medical Res Council | Production of antibodies |
FR2638359A1 (fr) | 1988-11-03 | 1990-05-04 | Tino Dalto | Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau |
US5175384A (en) | 1988-12-05 | 1992-12-29 | Genpharm International | Transgenic mice depleted in mature t-cells and methods for making transgenic mice |
US5530101A (en) | 1988-12-28 | 1996-06-25 | Protein Design Labs, Inc. | Humanized immunoglobulins |
DE3920358A1 (de) | 1989-06-22 | 1991-01-17 | Behringwerke Ag | Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung |
ATE144793T1 (de) | 1989-06-29 | 1996-11-15 | Medarex Inc | Bispezifische reagenzien für die aids-therapie |
US5690938A (en) | 1989-07-07 | 1997-11-25 | Oravax, Inc. | Oral immunization with multiple particulate antigen delivery system |
US5518725A (en) | 1989-09-25 | 1996-05-21 | University Of Utah Research Foundation | Vaccine compositions and method for induction of mucosal immune response via systemic vaccination |
US5208020A (en) | 1989-10-25 | 1993-05-04 | Immunogen Inc. | Cytotoxic agents comprising maytansinoids and their therapeutic use |
CA2026147C (en) | 1989-10-25 | 2006-02-07 | Ravi J. Chari | Cytotoxic agents comprising maytansinoids and their therapeutic use |
US5238843A (en) | 1989-10-27 | 1993-08-24 | Genencor International, Inc. | Method for cleaning a surface on which is bound a glycoside-containing substance |
US5064413A (en) | 1989-11-09 | 1991-11-12 | Bioject, Inc. | Needleless hypodermic injection device |
US5312335A (en) | 1989-11-09 | 1994-05-17 | Bioject Inc. | Needleless hypodermic injection device |
DE69120146T2 (de) | 1990-01-12 | 1996-12-12 | Cell Genesys Inc | Erzeugung xenogener antikörper |
US5061620A (en) | 1990-03-30 | 1991-10-29 | Systemix, Inc. | Human hematopoietic stem cell |
US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
KR100186783B1 (ko) | 1990-04-24 | 1999-05-01 | 게리 왁톤; 산티노 디-지아코모 | 적혈구와 표면-결합된 항원을 포함하는 경구용 백신 |
SK282950B6 (sk) | 1990-04-24 | 2003-01-09 | Biota Scientific Management Pty Ltd | Deriváty alfa-D-neuramínovej kyseliny, spôsob ich prípravy, ich použitie a farmaceutické prípravky na ich báze |
US5229275A (en) | 1990-04-26 | 1993-07-20 | Akzo N.V. | In-vitro method for producing antigen-specific human monoclonal antibodies |
US5427908A (en) | 1990-05-01 | 1995-06-27 | Affymax Technologies N.V. | Recombinant library screening methods |
AU8295491A (en) | 1990-06-29 | 1992-01-23 | Biosource Technologies Incorporated | Melanin production by transformed microorganisms |
US5190521A (en) | 1990-08-22 | 1993-03-02 | Tecnol Medical Products, Inc. | Apparatus and method for raising a skin wheal and anesthetizing skin |
US5633425A (en) | 1990-08-29 | 1997-05-27 | Genpharm International, Inc. | Transgenic non-human animals capable of producing heterologous antibodies |
DK0814159T3 (da) | 1990-08-29 | 2005-10-24 | Genpharm Int | Transgene, ikke-humane dyr, der er i stand til at danne heterologe antistoffer |
US5625126A (en) | 1990-08-29 | 1997-04-29 | Genpharm International, Inc. | Transgenic non-human animals for producing heterologous antibodies |
US5545806A (en) | 1990-08-29 | 1996-08-13 | Genpharm International, Inc. | Ransgenic non-human animals for producing heterologous antibodies |
US5661016A (en) | 1990-08-29 | 1997-08-26 | Genpharm International Inc. | Transgenic non-human animals capable of producing heterologous antibodies of various isotypes |
US5714374A (en) | 1990-09-12 | 1998-02-03 | Rutgers University | Chimeric rhinoviruses |
US5122469A (en) | 1990-10-03 | 1992-06-16 | Genentech, Inc. | Method for culturing Chinese hamster ovary cells to improve production of recombinant proteins |
WO1992006691A1 (en) | 1990-10-19 | 1992-04-30 | Biota Scientific Management Pty. Ltd. | Anti-viral compounds that bind the active site of influenza neuramidase and display in vivo activity against orthomyxovirus and paramyxovirus |
US5508192A (en) | 1990-11-09 | 1996-04-16 | Board Of Regents, The University Of Texas System | Bacterial host strains for producing proteolytically sensitive polypeptides |
US5264365A (en) | 1990-11-09 | 1993-11-23 | Board Of Regents, The University Of Texas System | Protease-deficient bacterial strains for production of proteolytically sensitive polypeptides |
WO1992009690A2 (en) | 1990-12-03 | 1992-06-11 | Genentech, Inc. | Enrichment method for variant proteins with altered binding properties |
US5527288A (en) | 1990-12-13 | 1996-06-18 | Elan Medical Technologies Limited | Intradermal drug delivery device and method for intradermal delivery of drugs |
US5571894A (en) | 1991-02-05 | 1996-11-05 | Ciba-Geigy Corporation | Recombinant antibodies specific for a growth factor receptor |
EP0586515B1 (en) | 1991-04-30 | 1997-09-17 | Eukarion, Inc. | Cationized antibodies against intracellular proteins |
LU91067I2 (fr) | 1991-06-14 | 2004-04-02 | Genentech Inc | Trastuzumab et ses variantes et dérivés immuno chimiques y compris les immotoxines |
GB9114948D0 (en) | 1991-07-11 | 1991-08-28 | Pfizer Ltd | Process for preparing sertraline intermediates |
GB9118204D0 (en) | 1991-08-23 | 1991-10-09 | Weston Terence E | Needle-less injector |
SE9102652D0 (sv) | 1991-09-13 | 1991-09-13 | Kabi Pharmacia Ab | Injection needle arrangement |
US7018809B1 (en) | 1991-09-19 | 2006-03-28 | Genentech, Inc. | Expression of functional antibody fragments |
DE69229477T2 (de) | 1991-09-23 | 1999-12-09 | Cambridge Antibody Technology Ltd., Melbourn | Methoden zur Herstellung humanisierter Antikörper |
ES2136092T3 (es) | 1991-09-23 | 1999-11-16 | Medical Res Council | Procedimientos para la produccion de anticuerpos humanizados. |
US5362852A (en) | 1991-09-27 | 1994-11-08 | Pfizer Inc. | Modified peptide derivatives conjugated at 2-hydroxyethylamine moieties |
US5587458A (en) | 1991-10-07 | 1996-12-24 | Aronex Pharmaceuticals, Inc. | Anti-erbB-2 antibodies, combinations thereof, and therapeutic and diagnostic uses thereof |
US5288502A (en) | 1991-10-16 | 1994-02-22 | The University Of Texas System | Preparation and uses of multi-phase microspheres |
WO1993008829A1 (en) | 1991-11-04 | 1993-05-13 | The Regents Of The University Of California | Compositions that mediate killing of hiv-infected cells |
WO1993009764A1 (en) | 1991-11-19 | 1993-05-27 | Center For Innovative Technology | Combined virustatic antimediator (covam) treatment of common colds |
JPH0826057B2 (ja) | 1992-01-16 | 1996-03-13 | 株式会社ディ・ディ・エス研究所 | シアル酸オリゴ糖誘導体及び微粒子キャリヤー |
US5667988A (en) | 1992-01-27 | 1997-09-16 | The Scripps Research Institute | Methods for producing antibody libraries using universal or randomized immunoglobulin light chains |
CA2372813A1 (en) | 1992-02-06 | 1993-08-19 | L.L. Houston | Biosynthetic binding protein for cancer marker |
US5328483A (en) | 1992-02-27 | 1994-07-12 | Jacoby Richard M | Intradermal injection device with medication and needle guard |
US5733743A (en) | 1992-03-24 | 1998-03-31 | Cambridge Antibody Technology Limited | Methods for producing members of specific binding pairs |
US5326856A (en) | 1992-04-09 | 1994-07-05 | Cytogen Corporation | Bifunctional isothiocyanate derived thiocarbonyls as ligands for metal binding |
ZA932522B (en) | 1992-04-10 | 1993-12-20 | Res Dev Foundation | Immunotoxins directed against c-erbB-2(HER/neu) related surface antigens |
JP2904647B2 (ja) | 1992-06-12 | 1999-06-14 | 株式会社蛋白工学研究所 | 5−ブロム−4−クロロインド−3−イル−2−シアル酸の製造方法 |
CA2137558A1 (en) | 1992-07-17 | 1994-02-03 | Wayne A. Marasco | Method of intracellular binding of target molecules |
US5383851A (en) | 1992-07-24 | 1995-01-24 | Bioject Inc. | Needleless hypodermic injection device |
CA2141216A1 (en) | 1992-07-27 | 1994-02-03 | Michael J. Micklus | Targeting of liposomes to the blood-brain barrier |
EP0656064B1 (en) | 1992-08-17 | 1997-03-05 | Genentech, Inc. | Bispecific immunoadhesins |
US5569189A (en) | 1992-09-28 | 1996-10-29 | Equidyne Systems, Inc. | hypodermic jet injector |
US5807722A (en) | 1992-10-30 | 1998-09-15 | Bioengineering Resources, Inc. | Biological production of acetic acid from waste gases with Clostridium ljungdahlii |
US5334144A (en) | 1992-10-30 | 1994-08-02 | Becton, Dickinson And Company | Single use disposable needleless injector |
US5736137A (en) | 1992-11-13 | 1998-04-07 | Idec Pharmaceuticals Corporation | Therapeutic application of chimeric and radiolabeled antibodies to human B lymphocyte restricted differentiation antigen for treatment of B cell lymphoma |
ATE196606T1 (de) | 1992-11-13 | 2000-10-15 | Idec Pharma Corp | Therapeutische verwendung von chimerischen und markierten antikörpern, die gegen ein differenzierung-antigen gerichtet sind, dessen expression auf menschliche b lymphozyt beschränkt ist, für die behandlung von b-zell-lymphoma |
US5635483A (en) | 1992-12-03 | 1997-06-03 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Tumor inhibiting tetrapeptide bearing modified phenethyl amides |
JP3523285B2 (ja) | 1993-01-22 | 2004-04-26 | 雪印乳業株式会社 | 糖分解酵素の製造法 |
US5780588A (en) | 1993-01-26 | 1998-07-14 | Arizona Board Of Regents | Elucidation and synthesis of selected pentapeptides |
US5374541A (en) | 1993-05-04 | 1994-12-20 | The Scripps Research Institute | Combined use of β-galactosidase and sialyltransferase coupled with in situ regeneration of CMP-sialic acid for one pot synthesis of oligosaccharides |
US20020037517A1 (en) | 1993-05-28 | 2002-03-28 | Hutchens T. William | Methods for sequencing biopolymers |
EP0714409A1 (en) | 1993-06-16 | 1996-06-05 | Celltech Therapeutics Limited | Antibodies |
DK0724432T3 (da) | 1993-10-22 | 2003-01-27 | Genentech Inc | Fremgangsmåder og præparater til mikroindkapsling af antigener til brug som vacciner |
US5369017A (en) | 1994-02-04 | 1994-11-29 | The Scripps Research Institute | Process for solid phase glycopeptide synthesis |
JPH09509664A (ja) | 1994-02-25 | 1997-09-30 | イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー | 4−n−置換シアル酸およびそれらのシアロシド類 |
WO1995024176A1 (en) | 1994-03-07 | 1995-09-14 | Bioject, Inc. | Ampule filling device |
US5466220A (en) | 1994-03-08 | 1995-11-14 | Bioject, Inc. | Drug vial mixing and transfer device |
US5773001A (en) | 1994-06-03 | 1998-06-30 | American Cyanamid Company | Conjugates of methyltrithio antitumor agents and intermediates for their synthesis |
US5622701A (en) | 1994-06-14 | 1997-04-22 | Protein Design Labs, Inc. | Cross-reacting monoclonal antibodies specific for E- and P-selectin |
WO1996004925A1 (en) | 1994-08-12 | 1996-02-22 | Immunomedics, Inc. | Immunoconjugates and humanized antibodies specific for b-cell lymphoma and leukemia cells |
US5639635A (en) | 1994-11-03 | 1997-06-17 | Genentech, Inc. | Process for bacterial production of polypeptides |
EP1241264A1 (en) | 1994-12-02 | 2002-09-18 | Chiron Corporation | Monoclonal antibodies to colon cancer antigen |
US5663149A (en) | 1994-12-13 | 1997-09-02 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides |
US5599302A (en) | 1995-01-09 | 1997-02-04 | Medi-Ject Corporation | Medical injection system and method, gas spring thereof and launching device using gas spring |
US5731168A (en) | 1995-03-01 | 1998-03-24 | Genentech, Inc. | Method for making heteromultimeric polypeptides |
US5840523A (en) | 1995-03-01 | 1998-11-24 | Genetech, Inc. | Methods and compositions for secretion of heterologous polypeptides |
US6673533B1 (en) | 1995-03-10 | 2004-01-06 | Meso Scale Technologies, Llc. | Multi-array multi-specific electrochemiluminescence testing |
US5641870A (en) | 1995-04-20 | 1997-06-24 | Genentech, Inc. | Low pH hydrophobic interaction chromatography for antibody purification |
US5869046A (en) | 1995-04-14 | 1999-02-09 | Genentech, Inc. | Altered polypeptides with increased half-life |
AU707444B2 (en) | 1995-04-25 | 1999-07-08 | Irori | Remotely programmable matrices with memories and uses thereof |
EP1709970A1 (en) | 1995-04-27 | 2006-10-11 | Abgenix, Inc. | Human antibodies against EGFR, derived from immunized xenomice |
AU2466895A (en) | 1995-04-28 | 1996-11-18 | Abgenix, Inc. | Human antibodies derived from immunized xenomice |
US5730723A (en) | 1995-10-10 | 1998-03-24 | Visionary Medical Products Corporation, Inc. | Gas pressured needle-less injection device and method |
US5837234A (en) | 1995-06-07 | 1998-11-17 | Cytotherapeutics, Inc. | Bioartificial organ containing cells encapsulated in a permselective polyether suflfone membrane |
US5712374A (en) | 1995-06-07 | 1998-01-27 | American Cyanamid Company | Method for the preparation of substantiallly monomeric calicheamicin derivative/carrier conjugates |
US5714586A (en) | 1995-06-07 | 1998-02-03 | American Cyanamid Company | Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates |
US6265150B1 (en) | 1995-06-07 | 2001-07-24 | Becton Dickinson & Company | Phage antibodies |
WO1997005267A2 (en) | 1995-07-26 | 1997-02-13 | Maxim Pharmaceuticals | Mucosal delivery of polynucleotides |
DE19544393A1 (de) | 1995-11-15 | 1997-05-22 | Hoechst Schering Agrevo Gmbh | Synergistische herbizide Mischungen |
US5893397A (en) | 1996-01-12 | 1999-04-13 | Bioject Inc. | Medication vial/syringe liquid-transfer apparatus |
ATE238552T1 (de) | 1996-03-01 | 2003-05-15 | Biota Scient Management | Verfahren zum nachweis von influenza-virus und dazu verwendbare verbindungen |
WO1997038123A1 (en) | 1996-04-05 | 1997-10-16 | Board Of Regents, The University Of Texas System | Methods for producing soluble, biologically-active disulfide bond-containing eukaryotic proteins in bacterial cells |
GB9607549D0 (en) | 1996-04-11 | 1996-06-12 | Weston Medical Ltd | Spring-powered dispensing device |
US5922845A (en) | 1996-07-11 | 1999-07-13 | Medarex, Inc. | Therapeutic multispecific compounds comprised of anti-Fcα receptor antibodies |
US6340702B1 (en) | 1996-07-22 | 2002-01-22 | Sankyo Company, Limited | Neuraminic acid derivatives, their preparation and their medical use |
US6506564B1 (en) | 1996-07-29 | 2003-01-14 | Nanosphere, Inc. | Nanoparticles having oligonucleotides attached thereto and uses therefor |
KR20000068986A (ko) | 1996-11-14 | 2000-11-25 | 리차드웨드레이 | 신규 용도 화합물 및 그 제조방법 |
CA2273194C (en) | 1996-12-03 | 2011-02-01 | Abgenix, Inc. | Transgenic mammals having human ig loci including plural vh and vk regions and antibodies produced therefrom |
TW555562B (en) | 1996-12-27 | 2003-10-01 | Kirin Brewery | Method for activation of human antigen-presenting cells, activated human antigen-presenting cells and use thereof |
DE69835201T2 (de) | 1997-04-18 | 2007-06-14 | Novartis Ag | Neoglycoproteine |
US5993412A (en) | 1997-05-19 | 1999-11-30 | Bioject, Inc. | Injection apparatus |
US6083715A (en) | 1997-06-09 | 2000-07-04 | Board Of Regents, The University Of Texas System | Methods for producing heterologous disulfide bond-containing polypeptides in bacterial cells |
JPH1135593A (ja) | 1997-07-18 | 1999-02-09 | Daikin Ind Ltd | 2−フルオロフコシル−n−アロイルグルコサミン誘導体及びその中間物、並びにそれらの製造方法 |
TW477783B (en) | 1997-12-12 | 2002-03-01 | Gilead Sciences Inc | Novel compounds useful as neuraminidase inhibitors and pharmaceutical compositions containing same |
IT1298087B1 (it) | 1998-01-08 | 1999-12-20 | Fiderm S R L | Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni |
AU765703B2 (en) | 1998-03-27 | 2003-09-25 | Bruce J. Bryan | Luciferases, fluorescent proteins, nucleic acids encoding the luciferases and fluorescent proteins and the use thereof in diagnostics, high throughput screening and novelty items |
DK1068241T3 (da) | 1998-04-02 | 2008-02-04 | Genentech Inc | Antistofvarianter og fragmenter deraf |
US20030175884A1 (en) | 2001-08-03 | 2003-09-18 | Pablo Umana | Antibody glycosylation variants having increased antibody-dependent cellular cytotoxicity |
AU3657899A (en) | 1998-04-20 | 1999-11-08 | James E. Bailey | Glycosylation engineering of antibodies for improving antibody-dependent cellular cytotoxicity |
US6455571B1 (en) | 1998-04-23 | 2002-09-24 | Abbott Laboratories | Inhibitors of neuraminidases |
DK1308456T3 (da) | 1998-05-06 | 2007-12-27 | Genentech Inc | Antistofoprensning ved ionbytterkromatografi |
US6528286B1 (en) | 1998-05-29 | 2003-03-04 | Genentech, Inc. | Mammalian cell culture process for producing glycoproteins |
JP3773153B2 (ja) | 1998-05-29 | 2006-05-10 | 独立行政法人理化学研究所 | シアル酸誘導体 |
EP2306195A3 (en) | 1998-09-18 | 2012-04-25 | Massachusetts Institute of Technology | Biological applications of semiconductor nanocrystals |
FR2783523B1 (fr) | 1998-09-21 | 2006-01-20 | Goemar Lab Sa | Fuco-oligosaccharides, enzyme pour leur preparation a partir des fucanes, bacterie productrice de l'enzyme et applications des fuco-oligosaccharides a la protection des plantes |
US6696304B1 (en) | 1999-02-24 | 2004-02-24 | Luminex Corporation | Particulate solid phase immobilized protein quantitation |
AUPP913999A0 (en) | 1999-03-12 | 1999-04-01 | Biota Scientific Management Pty Ltd | Novel chemical compounds and their use |
US7090973B1 (en) | 1999-04-09 | 2006-08-15 | Oscient Pharmaceuticals Corporation | Nucleic acid sequences relating to Bacteroides fragilis for diagnostics and therapeutics |
US7854934B2 (en) | 1999-08-20 | 2010-12-21 | Sloan-Kettering Institute For Cancer Research | Glycoconjugates, glycoamino acids, intermediates thereto, and uses thereof |
US6824780B1 (en) | 1999-10-29 | 2004-11-30 | Genentech, Inc. | Anti-tumor antibody compositions and methods of use |
AUPQ422399A0 (en) | 1999-11-24 | 1999-12-16 | University Of New South Wales, The | Method of screening transformed or transfected cells |
US6727356B1 (en) | 1999-12-08 | 2004-04-27 | Epoch Pharmaceuticals, Inc. | Fluorescent quenching detection reagents and methods |
US20020098513A1 (en) | 2000-02-17 | 2002-07-25 | Glycominds Ltd. | Combinatorial complex carbohydrate libraries and methods for the manufacture and uses thereof |
US7019129B1 (en) | 2000-05-09 | 2006-03-28 | Biosearch Technologies, Inc. | Dark quenchers for donor-acceptor energy transfer |
US7863020B2 (en) | 2000-06-28 | 2011-01-04 | Glycofi, Inc. | Production of sialylated N-glycans in lower eukaryotes |
US6514221B2 (en) | 2000-07-27 | 2003-02-04 | Brigham And Women's Hospital, Inc. | Blood-brain barrier opening |
US20020065259A1 (en) | 2000-08-30 | 2002-05-30 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
AUPR001000A0 (en) | 2000-09-08 | 2000-10-05 | Biota Scientific Management Pty Ltd | Novel chemical compounds and their use |
US7034036B2 (en) | 2000-10-30 | 2006-04-25 | Pain Therapeutics, Inc. | Inhibitors of ABC drug transporters at the blood-brain barrier |
US20030083299A1 (en) | 2000-11-04 | 2003-05-01 | Ferguson Ian A. | Non-invasive delivery of polypeptides through the blood-brain barrier |
JP2002153272A (ja) | 2000-11-24 | 2002-05-28 | Inst Of Physical & Chemical Res | 生体分子マイクロアレイ |
US7754208B2 (en) | 2001-01-17 | 2010-07-13 | Trubion Pharmaceuticals, Inc. | Binding domain-immunoglobulin fusion proteins |
AU2002338446A1 (en) | 2001-01-23 | 2002-11-05 | University Of Rochester Medical Center | Methods of producing or identifying intrabodies in eukaryotic cells |
US6884869B2 (en) | 2001-04-30 | 2005-04-26 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
DE10121982B4 (de) | 2001-05-05 | 2008-01-24 | Lts Lohmann Therapie-Systeme Ag | Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung |
JP2002371087A (ja) | 2001-06-15 | 2002-12-26 | Mitsubishi Chemicals Corp | 有機ホスホン酸 |
US20030113316A1 (en) | 2001-07-25 | 2003-06-19 | Kaisheva Elizabet A. | Stable lyophilized pharmaceutical formulation of IgG antibodies |
DE60234057D1 (de) | 2001-07-25 | 2009-11-26 | Raptor Pharmaceutical Inc | Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke |
WO2003009812A2 (en) | 2001-07-25 | 2003-02-06 | New York University | Use of glycosylceramides as adjuvants for vaccines against infections and cancer |
CN101724075B (zh) | 2001-10-10 | 2014-04-30 | 诺和诺德公司 | 肽的重构和糖缀合 |
KR20040077655A (ko) | 2001-10-19 | 2004-09-06 | 슈페리어 마이크로파우더스 엘엘씨 | 전자 형상 증착용 테잎 조성물 |
AUPR879601A0 (en) | 2001-11-09 | 2001-12-06 | Biota Scientific Management Pty Ltd | Novel chemical compounds and their use |
US20040023295A1 (en) | 2001-11-21 | 2004-02-05 | Carol Hamilton | Methods and systems for analyzing complex biological systems |
AU2003208415B2 (en) | 2002-02-14 | 2009-05-28 | Immunomedics, Inc. | Anti-CD20 antibodies and fusion proteins thereof and methods of use |
US20030162695A1 (en) | 2002-02-27 | 2003-08-28 | Schatzberg Alan F. | Glucocorticoid blocking agents for increasing blood-brain barrier permeability |
US7317091B2 (en) | 2002-03-01 | 2008-01-08 | Xencor, Inc. | Optimized Fc variants |
WO2003077945A1 (en) | 2002-03-14 | 2003-09-25 | Medical Research Council | Intracellular antibodies |
DE60328481D1 (de) | 2002-05-14 | 2009-09-03 | Novartis Vaccines & Diagnostic | Schleimhautapplizierter impfstoff, der das adjuvanz chitosan und menigokokkenantigene enthält |
RS20050006A (en) | 2002-07-08 | 2007-09-21 | Glaxo Smith Kline Istraživački Centar Zagreb D.O.O., | Novel compounds,compositions as carriers for steroid/non- steroid anti-inflammatory,antineoplastic and antiviral active molecules |
US20080070324A1 (en) | 2002-07-15 | 2008-03-20 | Floyd Alton D | Quantity control device for microscope slide staining assays |
EP1391213A1 (en) | 2002-08-21 | 2004-02-25 | Boehringer Ingelheim International GmbH | Compositions and methods for treating cancer using maytansinoid CD44 antibody immunoconjugates and chemotherapeutic agents |
US20040062682A1 (en) | 2002-09-30 | 2004-04-01 | Rakow Neal Anthony | Colorimetric sensor |
PL218660B1 (pl) | 2002-10-17 | 2015-01-30 | Genmab As | Izolowane ludzkie przeciwciało monoklonalne wiążące ludzki CD20, związane z tym przeciwciałem transfektoma, komórka gospodarza, transgeniczne zwierzę lub roślina, kompozycja, immunokoniugat, cząsteczka bispecyficzna, wektor ekspresyjny, kompozycja farmaceutyczna, zastosowanie medyczne, zestaw oraz przeciwciało antyidiotypowe i jego zastosowanie |
KR101186210B1 (ko) | 2002-12-03 | 2012-10-08 | 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 | 혈뇌장벽을 통과하는 물질 수송용 인공 저밀도 지단백질 운반체 |
EP2301966A1 (en) | 2002-12-16 | 2011-03-30 | Genentech, Inc. | Immunoglobulin variants and uses thereof |
ES2897506T3 (es) | 2003-01-09 | 2022-03-01 | Macrogenics Inc | Identificación y modificación de anticuerpos con regiones Fc variantes y métodos de utilización de los mismos |
US8088387B2 (en) | 2003-10-10 | 2012-01-03 | Immunogen Inc. | Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates |
AR044388A1 (es) | 2003-05-20 | 2005-09-07 | Applied Molecular Evolution | Moleculas de union a cd20 |
US20040259142A1 (en) | 2003-06-04 | 2004-12-23 | Imperial College Innovations Limited | Products and methods |
US20060019256A1 (en) | 2003-06-09 | 2006-01-26 | The Regents Of The University Of Michigan | Compositions and methods for treating and diagnosing cancer |
JP4148844B2 (ja) | 2003-06-11 | 2008-09-10 | ソニー・エリクソン・モバイルコミュニケーションズ株式会社 | 情報端末装置及び音声付画像ファイルの出力方法 |
EP1663239A4 (en) | 2003-09-10 | 2008-07-23 | Cedars Sinai Medical Center | KALIUM CHANNEL-MEDIATED FEEDING OF MEDICINES BY THE BLOOD BRAIN BARRIER |
JP2007505697A (ja) | 2003-09-15 | 2007-03-15 | ウィックストローム、エリック | シリル化治療剤を結合したインプラント |
EP1689439A2 (en) | 2003-09-22 | 2006-08-16 | Acidophil LLC | Small molecule compositions and methods for increasing drug efficiency using compositions thereof |
WO2005033663A2 (en) | 2003-09-30 | 2005-04-14 | Sequenom, Inc. | Methods of making substrates for mass spectrometry analysis and related devices |
US20050221337A1 (en) | 2003-10-02 | 2005-10-06 | Massachusetts Institute Of Technology | Microarrays and microspheres comprising oligosaccharides, complex carbohydrates or glycoproteins |
LT2348051T (lt) | 2003-11-05 | 2019-02-25 | Roche Glycart Ag | Cd20 antikūnai su padidintu fc receptoriaus prisijungimo giminingumu ir efektorine funkcija |
BR122018071808B8 (pt) | 2003-11-06 | 2020-06-30 | Seattle Genetics Inc | conjugado |
WO2005050224A2 (en) | 2003-11-13 | 2005-06-02 | Epitome Biosystems Inc. | Small molecule and peptide arrays and uses thereof |
EP1723422A2 (en) | 2004-03-05 | 2006-11-22 | The Scripps Research Institute | High throughput glycan microarrays |
US20050221397A1 (en) | 2004-03-30 | 2005-10-06 | Northern Advancement Center For Science & Technology | RM2 antigen (beta1,4-GalNAc-disialyl-Lc4) as prostate cancer-associated antigen |
US7850962B2 (en) | 2004-04-20 | 2010-12-14 | Genmab A/S | Human monoclonal antibodies against CD20 |
ITMI20040928A1 (it) | 2004-05-07 | 2004-08-07 | Uni Di Bologna Dipartiment O D | Procedura per la preparazione di coniugati della doxorubicina con l'albumina umana lattosaminata |
WO2006002382A2 (en) | 2004-06-24 | 2006-01-05 | The Scripps Research Institute | Arrays with cleavable linkers |
SI1771482T1 (sl) | 2004-07-22 | 2014-12-31 | Genentech, Inc. | Sestavek HER2 protitelesa |
WO2006055925A2 (en) | 2004-11-19 | 2006-05-26 | Swiss Federal Institute Of Technology | Microarrays for analyte detection |
WO2006064983A1 (en) | 2004-12-14 | 2006-06-22 | Korea Research Institute Of Bioscience And Biotechnology | Monoclonal antibody specific human embryonic stem cell |
US7923013B2 (en) | 2004-12-28 | 2011-04-12 | The Rockefeller University | Glycolipids and analogues thereof as antigens for NKT cells |
DK1835937T3 (da) | 2005-01-06 | 2012-07-23 | Novo Nordisk As | Sammensætninger og fremgangsmåder til behandling af virusinfektion |
US7837990B2 (en) | 2005-03-28 | 2010-11-23 | The Rockefeller University | In vivo expanded NKT cells and methods of use thereof |
PL2143795T3 (pl) | 2005-03-31 | 2011-12-30 | Biomedics Inc | Przeciwciało monoklonalne skierowane przeciwko CD20 |
CA2609731A1 (en) | 2005-05-24 | 2006-11-30 | Avestha Gengraine Technologies Pvt Ltd. | A method for the production of a monoclonal antibody to cd20 for the treatment of b-cell lymphoma |
AU2006252733A1 (en) | 2005-06-02 | 2006-12-07 | Astrazeneca Ab | Antibodies directed to CD20 and uses thereof |
US7723112B2 (en) | 2005-10-31 | 2010-05-25 | The Regents Of The University Of Michigan | Compositions and methods for treating and diagnosing cancer |
MY149159A (en) | 2005-11-15 | 2013-07-31 | Hoffmann La Roche | Method for treating joint damage |
US7781203B2 (en) | 2005-12-29 | 2010-08-24 | Corning Incorporated | Supports for assaying analytes and methods of making and using thereof |
US20090060921A1 (en) | 2006-01-17 | 2009-03-05 | Biolex Therapeutics, Inc. | Glycan-optimized anti-cd20 antibodies |
CA2647632C (en) | 2006-03-27 | 2017-06-27 | University Of Maryland Biotechnology Institute | Glycoprotein synthesis and remodeling by enzymatic transglycosylation |
KR20090031362A (ko) | 2006-05-18 | 2009-03-25 | 페터리내르메디찌니쉐 우니버지태트 빈 | 인플루엔자 바이러스의 검출 방법 |
EP2035034A4 (en) | 2006-06-09 | 2009-11-18 | Univ Maryland | GLYCOSYLATION-CONTROLLED ANTIBODY THERAPY |
US8445288B2 (en) | 2006-07-12 | 2013-05-21 | Merck Patent Gmbh | Solid-phase detection of terminal monosaccharides cleaved from glycosylated substrates |
JP2008025989A (ja) | 2006-07-15 | 2008-02-07 | Keio Gijuku | 局在表面プラズモン共鳴法と質量分析法によるリガンドの分析方法及びそのためのセンサー素子 |
WO2008020596A2 (en) | 2006-08-18 | 2008-02-21 | Oncotherapy Science, Inc. | Treating or preventing cancers over-expressing reg4 or kiaa0101 |
JP5391073B2 (ja) | 2006-11-27 | 2014-01-15 | ディアデクサス インコーポレーテッド | Ovr110抗体組成物および使用方法 |
US8765390B2 (en) | 2006-12-08 | 2014-07-01 | The Board Of Trustees Of The Leland Stanford Junior University | Identification and isolation of squamous carcinoma stem cells |
CA2591496C (en) | 2006-12-18 | 2014-09-02 | Japan Science And Technology Agency | Method of measuring interaction between biomaterial and sugar chain, method of evaluating biomaterial in sugar chain selectivity, method of screening biomaterial, method of patterning biomaterials, and kits for performing these methods |
CA2676323A1 (en) | 2007-01-18 | 2008-07-24 | Suomen Punainen Risti, Veripalvelu | Novel methods and reagents directed to production of cells |
EP2115461A4 (en) | 2007-01-18 | 2010-01-13 | Suomen Punainen Risti Veripalv | NEW SPECIFIC CELL BINDING AGENTS |
JP2010516259A (ja) | 2007-01-22 | 2010-05-20 | レイベン バイオテクノロジーズ | ヒトがん幹細胞 |
PT2123271E (pt) | 2007-03-07 | 2011-12-20 | Daiichi Sankyo Co Ltd | Fármaco para o tratamento de gripe |
US20080220988A1 (en) | 2007-03-07 | 2008-09-11 | Ada Technologies, Inc. | Preparing carbohydrate microarrays and conjugated nanoparticles |
PL2308514T3 (pl) | 2007-03-23 | 2013-11-29 | To Bbb Holding B V | Koniugaty do ukierunkowanego dostarczania leku poprzez barierę krew-mózg |
US7943330B2 (en) | 2007-03-23 | 2011-05-17 | Academia Sinica | Tailored glycoproteomic methods for the sequencing, mapping and identification of cellular glycoproteins |
US7960139B2 (en) | 2007-03-23 | 2011-06-14 | Academia Sinica | Alkynyl sugar analogs for the labeling and visualization of glycoconjugates in cells |
WO2008128207A1 (en) | 2007-04-13 | 2008-10-23 | Academia Sinica | Alpha-galactosyl ceramide analogs and their use as immunotherapies |
CN101986783A (zh) | 2007-04-23 | 2011-03-16 | 先灵公司 | 抗mdl-1抗体 |
WO2009009086A2 (en) | 2007-07-12 | 2009-01-15 | Sangamo Biosciences, Inc. | Methods and compositions for inactivating alpha 1,6 fucosyltransferase (fut 8) gene expression |
EP2022848A1 (en) | 2007-08-10 | 2009-02-11 | Hubrecht Institut | A method for identifying, expanding, and removing adult stem cells and cancer stem cells |
JP5345059B2 (ja) | 2007-08-24 | 2013-11-20 | Lsipファンド運営合同会社 | 婦人科癌の検出方法 |
US7888337B2 (en) | 2007-08-31 | 2011-02-15 | Academia Sinica | Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity |
FR2921387B1 (fr) | 2007-09-26 | 2012-04-20 | Sanofi Pasteur | Procede de production du virus de la grippe |
US8647626B2 (en) | 2007-10-02 | 2014-02-11 | Avaxia Biologics, Incorporated | Compositions comprising TNF-specific antibodies for oral delivery |
US20090123439A1 (en) | 2007-11-09 | 2009-05-14 | The Jackson Laboratory | Diagnostic and prognosis methods for cancer stem cells |
US8399627B2 (en) | 2007-12-31 | 2013-03-19 | Bayer Pharma AG | Antibodies to TNFα |
DK2268804T3 (en) | 2008-03-21 | 2017-12-11 | Danisco Us Inc | HEMICELLULASE-ENRICHED COMPOSITIONS FOR IMPROVED BIOMASS HYDROLYSE |
CN102016585B (zh) | 2008-04-09 | 2017-10-10 | 贝克顿·迪金森公司 | 使用包被的纳米颗粒的灵敏的免疫测定 |
US8383554B2 (en) | 2008-04-14 | 2013-02-26 | Academia Sinica | Quantitative microarray of intact glycolipid CD1d interaction and correlation with cell-based cytokine production |
US8906832B2 (en) | 2008-04-30 | 2014-12-09 | Academia Sinica | Quantitative analysis of carbohydrate-protein interactions using glycan microarrays: determination of surface and solution dissociation constants |
WO2009140853A1 (en) | 2008-05-23 | 2009-11-26 | The University Of Hong Kong | Combination therapy for the treatment of influenza |
WO2009154964A2 (en) | 2008-05-30 | 2009-12-23 | Glycome Technologies Inc. | Methods for structural analysis of glycans |
KR20110031949A (ko) | 2008-06-16 | 2011-03-29 | 아카데미아 시니카 | Globo h 및 ssea3에 특이적인 면역 반응을 유도하기 위한 조성물 및 암 치료에서의 이의 용도 |
KR101324109B1 (ko) | 2008-06-16 | 2013-10-31 | 아카데미아 시니카 | Globo h 및 그의 절편들에 대한 항체의 양에 따른 암 진단방법 |
JP2010014691A (ja) | 2008-06-20 | 2010-01-21 | Igaku Seibutsugaku Kenkyusho:Kk | 腹水中のメソテリン及び/又は巨核球増強因子を検出するための方法、キット、試薬及び装置 |
US20100003674A1 (en) | 2008-07-03 | 2010-01-07 | Cope Frederick O | Adult stem cells, molecular signatures, and applications in the evaluation, diagnosis, and therapy of mammalian conditions |
US7928077B2 (en) * | 2008-07-11 | 2011-04-19 | Academia Sinica | Alpha-galactosyl ceramide analogs and their use as immunotherapies |
US8680020B2 (en) | 2008-07-15 | 2014-03-25 | Academia Sinica | Glycan arrays on PTFE-like aluminum coated glass slides and related methods |
US20100022916A1 (en) | 2008-07-24 | 2010-01-28 | Javanbakhsh Esfandiari | Method and Apparatus for Collecting and Preparing Biological Samples for Testing |
GB0816679D0 (en) | 2008-09-11 | 2008-10-22 | Univ Bath | Compounds for treating viral infections |
JP2012503656A (ja) | 2008-09-26 | 2012-02-09 | エウレカ セラピューティクス,インコーポレイテッド | 変異体グリコシル化パターンを有する細胞株およびタンパク質 |
CN104971341B (zh) | 2008-10-27 | 2019-12-13 | 北海道公立大学法人札幌医科大学 | 肿瘤干细胞分子标记 |
ES2555220T3 (es) | 2009-03-27 | 2015-12-29 | Academia Sinica | Donantes de sialil-fosfato selectivos para la preparación de sialósidos y matrices de sialósidos para la detección del virus de la gripe |
WO2011005756A1 (en) | 2009-07-06 | 2011-01-13 | Puretech Ventures, Llc | Delivery of agents targeted to microbiota niches |
CA2767453C (en) | 2009-07-15 | 2018-10-09 | The University Of British Columbia | Neuraminidase inhibitor compounds, compositions and methods for the use thereof as anti-virals |
US20120171201A1 (en) | 2009-07-22 | 2012-07-05 | Enzon Pharmaceuticals, Inc. | Methods of treating her2 positive cancer with her2 receptor antagonist in combination with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin |
US20120172329A1 (en) | 2009-09-14 | 2012-07-05 | Thailand Excellence Center For Tissue Engineering | Phytochemical compositions including xanthones for anti-inflammatory, anti-cytokine storm, and other uses |
US10087236B2 (en) | 2009-12-02 | 2018-10-02 | Academia Sinica | Methods for modifying human antibodies by glycan engineering |
WO2011074621A1 (ja) | 2009-12-18 | 2011-06-23 | 株式会社医学生物学研究所 | メソセリン(msln)に対する抗体及びその用途 |
EP2347769A1 (en) | 2010-01-20 | 2011-07-27 | Glycotope GmbH | Cancer stem cell markers and uses thereof |
SG182823A1 (en) | 2010-02-11 | 2012-09-27 | Alexion Pharma Inc | Therapeutic methods using an ti-cd200 antibodies |
KR101930961B1 (ko) | 2010-02-24 | 2018-12-19 | 머크 샤프 앤드 돔 코포레이션 | 피키아 파스토리스에서 생산된 치료 당단백질 상의 n-글리코실화 부위 점유를 증가시키는 방법 |
EP3620467A1 (en) | 2010-03-12 | 2020-03-11 | Debiopharm International SA | Cd37-binding molecules and immunoconjugates thereof |
WO2011130332A1 (en) | 2010-04-12 | 2011-10-20 | Academia Sinica | Glycan arrays for high throughput screening of viruses |
WO2011130624A2 (en) | 2010-04-16 | 2011-10-20 | Immune Disease Institute, Inc. | Sustained polypeptide expression from synthetic, modified rnas and uses thereof |
DK2568976T3 (en) | 2010-05-10 | 2016-01-11 | Academia Sinica | Zanamivir-phosphonate congener with the anti-influenza activity, and determining the sensitivity oseltamivir in influenza viruses |
WO2011145957A1 (en) | 2010-05-20 | 2011-11-24 | Auckland Uniservices Limited | Agents and methods for detection and/or imaging of hypoxia |
NZ603883A (en) | 2010-05-27 | 2015-01-30 | Merck Sharp & Dohme | Method for preparing antibodies having improved properties |
GB201015569D0 (en) | 2010-09-16 | 2010-10-27 | Medical Res Council | Blood assay for prions |
WO2012082635A1 (en) | 2010-12-13 | 2012-06-21 | Ancora Pharmaceuticals, Inc. | Synthetic oligosaccharide group a streptococcus |
US20130331381A1 (en) | 2011-02-28 | 2013-12-12 | Mcmaster University | Treatment of Cancer WIth Dopamine Receptor Antagonists |
US10851174B2 (en) | 2011-03-03 | 2020-12-01 | University Of Maryland, Baltimore | Core fucosylated glycopeptides and glycoproteins: chemoenzymatic synthesis and uses thereof |
EP2714732A4 (en) | 2011-05-25 | 2014-12-10 | Merck Sharp & Dohme | PROCESS FOR PREPARING FC-CONTAINING POLYPEPTIDES WITH IMPROVED PROPERTIES |
EP3418300B1 (en) | 2011-07-18 | 2020-10-28 | Institute for Research in Biomedicine | Neutralizing anti-influenza a virus antibodies and uses thereof |
JP5795067B2 (ja) | 2011-07-21 | 2015-10-14 | 京セラ株式会社 | 照明装置、イメージセンサヘッドおよびこれを備える読取装置 |
IN2014MN00228A (ja) | 2011-08-12 | 2015-09-25 | Nissan Chemical Ind Ltd | |
IN2014CN03072A (ja) | 2011-10-31 | 2015-07-31 | Merck Sharp & Dohme | |
WO2013074598A1 (en) | 2011-11-18 | 2013-05-23 | Merck Sharp & Dohme Corp. | Fc CONTAINING POLYPEPTIDES HAVING INCREASED ANTI-INFLAMMATORY PROPERTIES AND INCREASED FcRN BINDING |
EP2604281B1 (en) | 2011-12-14 | 2014-07-30 | Centre National de la Recherche Scientifique (CNRS) | Clicked somatostatin conjugated analogs for biological applications |
WO2013106937A1 (en) | 2012-01-19 | 2013-07-25 | The University Of British Columbia | 3' equatorial-fluorine-substituted neuraminidase inhibitor compounds, compositions and methods for the use thereof as anti-virals |
GB201201314D0 (en) | 2012-01-26 | 2012-03-07 | Isis Innovation | Composition |
CA2862925C (en) | 2012-02-10 | 2020-01-21 | University Of Maryland, Baltimore | Chemoenzymatic glycoengineering of antibodies and fc fragments thereof |
US9846160B2 (en) | 2012-02-27 | 2017-12-19 | Board Of Regents, The University Of Texas Systems | Ganglioside GD2 as a marker and target on cancer stem cells |
WO2013152034A1 (en) | 2012-04-02 | 2013-10-10 | Merrimack Pharmaceuticals, Inc. | Dosage and administration of monospecific and bispecific anti-igf-1r and anti-erbb3 antibodies |
WO2013151649A1 (en) | 2012-04-04 | 2013-10-10 | Sialix Inc | Glycan-interacting compounds |
US10130714B2 (en) | 2012-04-14 | 2018-11-20 | Academia Sinica | Enhanced anti-influenza agents conjugated with anti-inflammatory activity |
EP2855745A4 (en) | 2012-06-01 | 2016-01-20 | Momenta Pharmaceuticals Inc | METHODS RELATING TO ADALIMUM AB |
WO2014031498A1 (en) | 2012-08-18 | 2014-02-27 | Academia Sinica | Cell-permeable probes for identification and imaging of sialidases |
TWI510627B (zh) | 2012-08-20 | 2015-12-01 | Academia Sinica | 寡醣之大規模酵素合成 |
CA2883168A1 (en) | 2012-08-21 | 2014-02-27 | Academia Sinica | Benzocyclooctyne compounds and uses thereof |
KR102460297B1 (ko) | 2012-10-30 | 2022-10-28 | 에스퍼란스 파마슈티컬스, 인코포레이티드 | 항체/약물 컨쥬게이트 및 이의 사용 방법 |
US20150284452A1 (en) | 2012-11-13 | 2015-10-08 | Iogenetics, Llc | Antimicrobial compositions |
GB201305986D0 (en) | 2013-04-03 | 2013-05-15 | Asociaci N Ct De Investigaci N Cooperativa En Biomateriales | Synthesis and use of isotopically-labelled glycans |
WO2014167126A2 (en) | 2013-04-13 | 2014-10-16 | Universidade De Coimbra | Platform for targeted delivery to stem cells and tumor cells and methods thereof |
CN104225616A (zh) | 2013-06-08 | 2014-12-24 | 中南大学 | 一种靶向卵巢癌干细胞的抗肿瘤生物制剂 |
WO2014210397A1 (en) | 2013-06-26 | 2014-12-31 | Academia Sinica | Rm2 antigens and use thereof |
US9981030B2 (en) | 2013-06-27 | 2018-05-29 | Academia Sinica | Glycan conjugates and use thereof |
TWI599370B (zh) | 2013-07-26 | 2017-09-21 | 中央研究院 | 靈芝多醣誘發之抗體介導抗腫瘤活性 |
CA2923579C (en) | 2013-09-06 | 2023-09-05 | Academia Sinica | Human inkt cell activation using glycolipids with altered glycosyl groups |
WO2015038963A1 (en) | 2013-09-12 | 2015-03-19 | Teva Pharmaceutical Industries, Ltd. | Gene expression biomarkers of laquinimod responsiveness |
CN103436627B (zh) | 2013-09-13 | 2016-02-03 | 四川大学华西医院 | 一种恶性乳腺癌干细胞的筛查试剂盒 |
WO2015054039A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Fc CONTAINING POLYPEPTIDES HAVING INCREASED BINDING TO FcGammaRIIB |
US10150818B2 (en) | 2014-01-16 | 2018-12-11 | Academia Sinica | Compositions and methods for treatment and detection of cancers |
JP2017507118A (ja) | 2014-01-16 | 2017-03-16 | アカデミア シニカAcademia Sinica | がんの処置および検出のための組成物および方法 |
CN106415244B (zh) | 2014-03-27 | 2020-04-24 | 中央研究院 | 反应性标记化合物及其用途 |
WO2015184004A1 (en) | 2014-05-27 | 2015-12-03 | Academia Sinica | Anti-cd20 glycoantibodies and uses thereof |
JP7062361B2 (ja) | 2014-05-27 | 2022-05-06 | アカデミア シニカ | 抗her2糖操作抗体群およびその使用 |
US10118969B2 (en) | 2014-05-27 | 2018-11-06 | Academia Sinica | Compositions and methods relating to universal glycoforms for enhanced antibody efficacy |
EP3149045B1 (en) | 2014-05-27 | 2023-01-18 | Academia Sinica | Compositions and methods relating to universal glycoforms for enhanced antibody efficacy |
CA2950433A1 (en) | 2014-05-28 | 2015-12-03 | Academia Sinica | Anti-tnf-alpha glycoantibodies and uses thereof |
MX2017002333A (es) | 2014-08-22 | 2017-08-28 | Academia Sinica | Conjugados novedosos de glicano y uso de los mismos. |
EP3191500A4 (en) | 2014-09-08 | 2018-04-11 | Academia Sinica | HUMAN iNKT CELL ACTIVATION USING GLYCOLIPIDS |
WO2016040683A1 (en) | 2014-09-12 | 2016-03-17 | The Regents Of The University Of California | Macropinocytosing human anti-cd46 antibodies and targeted cancer therapeutics |
US9975965B2 (en) | 2015-01-16 | 2018-05-22 | Academia Sinica | Compositions and methods for treatment and detection of cancers |
US10495645B2 (en) | 2015-01-16 | 2019-12-03 | Academia Sinica | Cancer markers and methods of use thereof |
WO2016118090A1 (en) | 2015-01-23 | 2016-07-28 | Agency For Science, Technology And Research | Cancer specific antigen-binding proteins |
EP3248005B1 (en) | 2015-01-24 | 2020-12-09 | Academia Sinica | Novel glycan conjugates and methods of use thereof |
US20170283878A1 (en) | 2015-12-11 | 2017-10-05 | Academia Sinica | Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers |
CA3016170A1 (en) | 2016-03-08 | 2017-09-14 | Academia Sinica | Methods for modular synthesis of n-glycans and arrays thereof |
CA3019560A1 (en) | 2016-03-29 | 2017-10-05 | Obi Pharma, Inc. | Antibodies, pharmaceutical compositions and methods |
KR102588027B1 (ko) | 2016-08-22 | 2023-10-12 | 초 파마 인크. | 항체, 결합 단편 및 사용 방법 |
TWI767959B (zh) | 2016-11-21 | 2022-06-21 | 台灣浩鼎生技股份有限公司 | 共軛生物分子、醫藥組成物及方法 |
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Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP3717512B2 (ja) * | 1992-10-22 | 2005-11-16 | 麒麟麦酒株式会社 | 新規スフィンゴ糖脂質およびその使用 |
JP2008511634A (ja) * | 2004-08-27 | 2008-04-17 | アルバート アインシュタイン カレッジ オブ メディシン オブ イエシバ ユニバーシティ | 免疫及び自己免疫の調節因子としてのセラミド誘導体 |
JP2008525495A (ja) * | 2004-12-28 | 2008-07-17 | ザ ロックフェラー ユニバーシティ | Nkt細胞に対する抗原としての糖脂質及びその類似体 |
WO2008133801A1 (en) * | 2007-04-23 | 2008-11-06 | Albert Einstein College Of Medicine Of Yeshiva University | Ceramide derivatives as modulators of immunity and autoimmunity |
WO2009119692A1 (ja) * | 2008-03-25 | 2009-10-01 | 独立行政法人理化学研究所 | 新規糖脂質及びその用途 |
US20120178705A1 (en) * | 2011-01-05 | 2012-07-12 | National Taiwan University | Methods for preparation of glycosphingolipids and uses thereof |
Non-Patent Citations (1)
Title |
---|
RAJU,R. ET AL.: "Synthesis and evaluation of 3''- and 4''-deoxy-fluoro analogs of the immunostimulatory glycolipid, K", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 19, no. 15, JPN6018029303, 2009, pages 4122 - 4125, XP026301649, DOI: doi:10.1016/j.bmcl.2009.06.005 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2023153527A1 (ja) * | 2022-02-14 | 2023-08-17 | 国立研究開発法人理化学研究所 | Nkt細胞リガンド含有リポソーム組成物 |
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