BR112019022445A2 - Composição de conjugado ligante-fármaco, formulação, método para inibir a multiplicação de uma célula tumoral ou célula cancerosa ou causar apoptose em uma célula tumoral ou cancerosa, e, composto de conector de fármaco - Google Patents
Composição de conjugado ligante-fármaco, formulação, método para inibir a multiplicação de uma célula tumoral ou célula cancerosa ou causar apoptose em uma célula tumoral ou cancerosa, e, composto de conector de fármaco Download PDFInfo
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- BR112019022445A2 BR112019022445A2 BR112019022445-9A BR112019022445A BR112019022445A2 BR 112019022445 A2 BR112019022445 A2 BR 112019022445A2 BR 112019022445 A BR112019022445 A BR 112019022445A BR 112019022445 A2 BR112019022445 A2 BR 112019022445A2
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- Brazil
- Prior art keywords
- unit
- drug
- compound
- optionally substituted
- alkyl
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- 0 C*(NCS*)=C* Chemical compound C*(NCS*)=C* 0.000 description 45
- OHWCAVRRXKJCRB-UHFFFAOYSA-N CC(C(C(C1O)O)O)OC1OC Chemical compound CC(C(C(C1O)O)O)OC1OC OHWCAVRRXKJCRB-UHFFFAOYSA-N 0.000 description 3
- BUKJMOUXWVEXNZ-CMDGGOBGSA-N C=C(c1cc(N)cc(C(O)=C)c1)N1CCC(CCCCNC(/C=C/c2cnccc2)=O)CC1 Chemical compound C=C(c1cc(N)cc(C(O)=C)c1)N1CCC(CCCCNC(/C=C/c2cnccc2)=O)CC1 BUKJMOUXWVEXNZ-CMDGGOBGSA-N 0.000 description 1
- CMYVMQHTXJQDJZ-UHFFFAOYSA-N C=C(c1cc(N)ccc1)N1CCC(CCCCN/C(/Nc2ccncc2)=N/C#N)CC1 Chemical compound C=C(c1cc(N)ccc1)N1CCC(CCCCN/C(/Nc2ccncc2)=N/C#N)CC1 CMYVMQHTXJQDJZ-UHFFFAOYSA-N 0.000 description 1
- RLGMRAAHZIOAPH-OUKQBFOZSA-N CC(C)(C)OC(Nc1cc(C(N2CCC(CCCCNC(/C=C/c3cnccc3)=O)CC2)=O)ccc1)=O Chemical compound CC(C)(C)OC(Nc1cc(C(N2CCC(CCCCNC(/C=C/c3cnccc3)=O)CC2)=O)ccc1)=O RLGMRAAHZIOAPH-OUKQBFOZSA-N 0.000 description 1
- DAMSURYLURICHN-SBUREZEXSA-N CC(C)[C@@H](C(N[C@@H](C)C(Nc1ccc(CO)cc1)=O)=O)NC(CCCCCN(C(C=C1)=O)C1=O)=O Chemical compound CC(C)[C@@H](C(N[C@@H](C)C(Nc1ccc(CO)cc1)=O)=O)NC(CCCCCN(C(C=C1)=O)C1=O)=O DAMSURYLURICHN-SBUREZEXSA-N 0.000 description 1
- GSWKJIWKGSPISH-LRDDRELGSA-N CC(C)[C@@H](C(N[C@@H](C)C(O)=O)=O)NC(CCCCCN(C(C=C1)=O)C1=O)=O Chemical compound CC(C)[C@@H](C(N[C@@H](C)C(O)=O)=O)NC(CCCCCN(C(C=C1)=O)C1=O)=O GSWKJIWKGSPISH-LRDDRELGSA-N 0.000 description 1
- JZHYYGXJLWRHSU-UHFFFAOYSA-N CCCCCC(C(C)=O)NC Chemical compound CCCCCC(C(C)=O)NC JZHYYGXJLWRHSU-UHFFFAOYSA-N 0.000 description 1
- DQMAEKOMFBRRSO-UHFFFAOYSA-N CCCCCCCCC(N(CC1)CCC1O)=O Chemical compound CCCCCCCCC(N(CC1)CCC1O)=O DQMAEKOMFBRRSO-UHFFFAOYSA-N 0.000 description 1
- GOVXKUCVZUROAN-UHFFFAOYSA-N CCc1c[nH]c2ccccc12 Chemical compound CCc1c[nH]c2ccccc12 GOVXKUCVZUROAN-UHFFFAOYSA-N 0.000 description 1
- ZOXDMRGAEOZEAG-UHFFFAOYSA-N CN(CCO)C(CCCCCCCN/C(/Nc1ccncc1)=N\C#N)=O Chemical compound CN(CCO)C(CCCCCCCN/C(/Nc1ccncc1)=N\C#N)=O ZOXDMRGAEOZEAG-UHFFFAOYSA-N 0.000 description 1
- IEBOWSYQQIAQHO-UHFFFAOYSA-O CNc1ccc(C[NH3+])cc1 Chemical compound CNc1ccc(C[NH3+])cc1 IEBOWSYQQIAQHO-UHFFFAOYSA-O 0.000 description 1
- KDLLZNFEWASQMJ-UHFFFAOYSA-N NC(C[IH]C(O)=O)=O Chemical compound NC(C[IH]C(O)=O)=O KDLLZNFEWASQMJ-UHFFFAOYSA-N 0.000 description 1
- AXKGIPZJYUNAIW-UHFFFAOYSA-N Nc1ccc(CO)cc1 Chemical compound Nc1ccc(CO)cc1 AXKGIPZJYUNAIW-UHFFFAOYSA-N 0.000 description 1
- AEMOLEFTQBMNLQ-JGONUKNZSA-N O[C@@H](C(C(C(O)=O)O[C@H]1O)O)C1O Chemical compound O[C@@H](C(C(C(O)=O)O[C@H]1O)O)C1O AEMOLEFTQBMNLQ-JGONUKNZSA-N 0.000 description 1
- MAZZMZJDJQVRLM-IKDMVZCSSA-N O[C@H](C(COC1C(O)=O)OO)C1O Chemical compound O[C@H](C(COC1C(O)=O)OO)C1O MAZZMZJDJQVRLM-IKDMVZCSSA-N 0.000 description 1
Classifications
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- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
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- A61K31/33—Heterocyclic compounds
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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- A61K47/6867—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from a cell of a blood cancer
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
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- Medicinal Chemistry (AREA)
- Public Health (AREA)
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- Molecular Biology (AREA)
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- Proteomics, Peptides & Aminoacids (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762490733P | 2017-04-27 | 2017-04-27 | |
| US62/490733 | 2017-04-27 | ||
| US201762573987P | 2017-10-18 | 2017-10-18 | |
| US62/573987 | 2017-10-18 | ||
| PCT/US2018/030018 WO2018201087A1 (en) | 2017-04-27 | 2018-04-27 | Quaternized nicotinamide adenine dinucleotide salvage pathway inhibitor conjugates |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112019022445A2 true BR112019022445A2 (pt) | 2020-05-12 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112019022445-9A BR112019022445A2 (pt) | 2017-04-27 | 2018-04-27 | Composição de conjugado ligante-fármaco, formulação, método para inibir a multiplicação de uma célula tumoral ou célula cancerosa ou causar apoptose em uma célula tumoral ou cancerosa, e, composto de conector de fármaco |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11931414B2 (https=) |
| EP (1) | EP3615081A1 (https=) |
| JP (2) | JP7425606B2 (https=) |
| KR (1) | KR20190141181A (https=) |
| CN (1) | CN110799217A (https=) |
| AU (2) | AU2018258687C1 (https=) |
| BR (1) | BR112019022445A2 (https=) |
| CA (1) | CA3060206A1 (https=) |
| IL (1) | IL269794A (https=) |
| MA (1) | MA51189A (https=) |
| MX (2) | MX2019012194A (https=) |
| SG (1) | SG11201909563VA (https=) |
| TW (1) | TW201904613A (https=) |
| WO (1) | WO2018201087A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2019001302A (es) | 2016-08-09 | 2019-06-12 | Seattle Genetics Inc | Conjugados de farmaco con enlazadores autoestabilizantes que tienen propiedades fisioquimicas mejoradas. |
| TWI835714B (zh) | 2016-10-18 | 2024-03-21 | 美商思進公司 | 菸鹼醯胺腺嘌呤二核苷酸補救合成(salvage pathway)抑制劑之靶向投遞 |
| WO2018201087A1 (en) | 2017-04-27 | 2018-11-01 | Seattle Genetics, Inc. | Quaternized nicotinamide adenine dinucleotide salvage pathway inhibitor conjugates |
| CN110339181A (zh) * | 2019-07-02 | 2019-10-18 | 中国药科大学 | 一种基于点击反应的pH响应型纳米制剂及其制法和应用 |
| CN111454327B (zh) * | 2020-04-02 | 2024-07-26 | 中国人民解放军第二军医大学 | 一种nampt蛋白降解靶向嵌合体及其制备方法和应用 |
| WO2021207701A1 (en) * | 2020-04-10 | 2021-10-14 | Seagen Inc. | Charge variant linkers |
| JP2025530213A (ja) | 2022-09-09 | 2025-09-11 | ミリックス ファーマ リミテッド | Nmt阻害剤を含む抗体薬物コンジュゲート及びその使用 |
| CN116092586B (zh) * | 2023-03-10 | 2025-11-04 | 西北工业大学 | 一种基于生物电子等排体搜索平台的数据处理方法 |
| WO2025162305A1 (zh) * | 2024-02-01 | 2025-08-07 | 浙江养生堂天然药物研究所有限公司 | 含季铵盐的抗体偶联药物及其医药用途 |
| CN119219604B (zh) * | 2024-09-25 | 2025-11-18 | 大连理工大学 | 一种吡啶季铵盐类fk866前药、其制备方法及应用 |
Family Cites Families (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2036891B (en) | 1978-12-05 | 1983-05-05 | Windsor Smith C | Change speed gear |
| GB8308235D0 (en) | 1983-03-25 | 1983-05-05 | Celltech Ltd | Polypeptides |
| US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
| JPS6147500A (ja) | 1984-08-15 | 1986-03-07 | Res Dev Corp Of Japan | キメラモノクロ−ナル抗体及びその製造法 |
| EP0173494A3 (en) | 1984-08-27 | 1987-11-25 | The Board Of Trustees Of The Leland Stanford Junior University | Chimeric receptors by dna splicing and expression |
| GB8422238D0 (en) | 1984-09-03 | 1984-10-10 | Neuberger M S | Chimeric proteins |
| JPS61134325A (ja) | 1984-12-04 | 1986-06-21 | Teijin Ltd | ハイブリツド抗体遺伝子の発現方法 |
| JPS63501765A (ja) | 1985-11-01 | 1988-07-21 | インタ−ナショナル、ジェネティック、エンジニアリング インコ−ポレ−テッド | 抗体遺伝子のモジュ−ル組立体、それにより産生された抗体及び用途 |
| US5225539A (en) | 1986-03-27 | 1993-07-06 | Medical Research Council | Recombinant altered antibodies and methods of making altered antibodies |
| US5530101A (en) | 1988-12-28 | 1996-06-25 | Protein Design Labs, Inc. | Humanized immunoglobulins |
| US6214345B1 (en) | 1993-05-14 | 2001-04-10 | Bristol-Myers Squibb Co. | Lysosomal enzyme-cleavable antitumor drug conjugates |
| JP4046354B2 (ja) | 1996-03-18 | 2008-02-13 | ボード オブ リージェンツ,ザ ユニバーシティ オブ テキサス システム | 増大した半減期を有する免疫グロブリン様ドメイン |
| US6451816B1 (en) | 1997-06-20 | 2002-09-17 | Klinge Pharma Gmbh | Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression |
| DE19624668A1 (de) | 1996-06-20 | 1998-02-19 | Klinge Co Chem Pharm Fab | Verwendung von Pyridylalkan-, Pyridylalken- bzw. Pyridylalkinsäureamiden |
| GB9711125D0 (en) | 1997-05-29 | 1997-07-23 | Leo Pharm Prod Ltd | Novel cyanoguanidines |
| AU4076500A (en) | 1999-04-09 | 2000-11-14 | Shionogi Bioresearch Corp. | (n)-substituted cyanoguanidine compounds |
| US7091186B2 (en) | 2001-09-24 | 2006-08-15 | Seattle Genetics, Inc. | p-Amidobenzylethers in drug delivery agents |
| CA2484671A1 (en) | 2002-05-17 | 2003-11-27 | Leo Pharma A/S | Cyanoguanidine prodrugs |
| SI1545613T1 (sl) | 2002-07-31 | 2011-11-30 | Seattle Genetics Inc | Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni |
| 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 |
| US7498298B2 (en) | 2003-11-06 | 2009-03-03 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
| EP1718667B1 (en) | 2004-02-23 | 2013-01-09 | Genentech, Inc. | Heterocyclic self-immolative linkers and conjugates |
| JP5171621B2 (ja) | 2005-07-07 | 2013-03-27 | シアトル ジェネティックス, インコーポレイテッド | フェニルアラニン側鎖修飾をc末端に有するモノメチルバリン化合物 |
| US8871720B2 (en) | 2005-07-07 | 2014-10-28 | Seattle Genetics, Inc. | Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus |
| BRPI0617546A2 (pt) | 2005-09-26 | 2011-07-26 | Medarex Inc | conjugado de fÁrmaco-anticorpo, formulaÇço farmacÊutica, mÉtodo para matar uma cÉlula de tumor, mÉtodo para retardar ou interromper o crescimento de um tumor em um sujeito mamÍfero e composto |
| US8257706B2 (en) | 2006-08-25 | 2012-09-04 | Seattle Genetics, Inc. | CD30 binding agents and uses thereof |
| RU2476441C2 (ru) | 2007-10-19 | 2013-02-27 | Сиэтл Дженетикс, Инк. | Cd19-связывающие средства и их применение |
| WO2009086835A1 (en) | 2008-01-11 | 2009-07-16 | Topotarget A/S | Novel cyanoguanidines |
| US8742076B2 (en) | 2008-02-01 | 2014-06-03 | Genentech, Inc. | Nemorubicin metabolite and analog reagents, antibody-drug conjugates and methods |
| KR20200058590A (ko) | 2008-04-30 | 2020-05-27 | 이뮤노젠 아이엔씨 | 가교제 및 그 용도 |
| US8324165B2 (en) | 2008-05-14 | 2012-12-04 | Five Prime Therapeutics, Inc. | Compositions for treating arthritis comprising HG1023575 polypeptide |
| RU2529468C2 (ru) | 2008-06-24 | 2014-09-27 | Топотаргет А/С | Производные 1, 2-дигидроциклобутендиона в качестве ингибиторов фосфорибозилтрансферазы никотинамида |
| JP5688367B2 (ja) | 2008-08-29 | 2015-03-25 | トポターゲット・アクティーゼルスカブTopoTarget A/S | 新規なウレアおよびチオウレア誘導体 |
| EP2440527A1 (en) | 2009-06-09 | 2012-04-18 | Topo Target A/S | Pyridinyl derivatives as inhibitors of enzyme nicotinamide phosphoribosyltransferase |
| CA2768338A1 (en) * | 2009-07-17 | 2011-01-20 | Topotarget A/S | Method for predicting the utility of administering nicotinic acid or a precursor or prodrug thereof to reduce the severity of side-effects of cancer treatment with nicotinamide phosphoribosyltransferase inhibitors |
| JP6038792B2 (ja) | 2010-09-03 | 2016-12-07 | フォーマ ティーエム, エルエルシー. | 癌などの疾患の治療のためのnampt阻害剤としての4−{[(ピリジン−3−イル−メチル)アミノカルボニル]アミノ}ベンゼン−スルホン誘導体 |
| PE20140011A1 (es) | 2010-09-03 | 2014-01-31 | Forma Tm Llc | Compuestos y composiciones novedosos para la inhibicion de nampt |
| AU2011329233A1 (en) | 2010-11-15 | 2013-05-23 | Abbvie Deutschland Gmbh & Co Kg | NAMPT and ROCK inhibitors |
| EP2640704A1 (en) | 2010-11-15 | 2013-09-25 | Abbvie Inc. | Nampt inhibitors |
| JP6105481B2 (ja) | 2010-12-06 | 2017-03-29 | シアトル ジェネティクス,インコーポレーテッド | Liv−1に対するヒト化抗体および癌治療のためのその使用 |
| RU2017112522A (ru) | 2011-05-04 | 2019-01-24 | ФОРМА ТиЭм, ЭлЭлСИ | Новые соединения и композиции для ингибирования nampt |
| WO2012154194A1 (en) | 2011-05-09 | 2012-11-15 | Forma Tm, Llc | Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (nampt) |
| CA2877474A1 (en) | 2011-06-20 | 2012-12-27 | Myrexis, Inc. | Compounds and therapeutic uses thereof |
| MX348311B (es) | 2011-11-11 | 2017-06-06 | Abbvie Inc | Inhibidores nampt. |
| WO2013082150A1 (en) | 2011-11-30 | 2013-06-06 | The Curators Of The University Of Missouri | Small molecule inhibitors of nicotinamide phosphoribosyltransferase (nampt) |
| CN104220094A (zh) | 2012-02-17 | 2014-12-17 | 西雅图基因公司 | 针对整联蛋白αvβ6的抗体和使用该抗体治疗癌症 |
| WO2013130935A1 (en) | 2012-03-02 | 2013-09-06 | Genentech, Inc. | Amido-benzyl sulfoxide derivatives |
| WO2013130943A1 (en) | 2012-03-02 | 2013-09-06 | Genentech, Inc. | Alkyl-and di-substituted amido-benzyl sulfonamide derivatives |
| WO2013127268A1 (en) | 2012-03-02 | 2013-09-06 | Genentech,Inc. | Amido-benzyl sulfone and sulfonamide derivatives |
| CA2873075A1 (en) | 2012-05-11 | 2013-07-14 | Abbvie Inc. | Nampt inhibitors |
| MX2014013758A (es) | 2012-05-11 | 2015-02-05 | Abbvie Inc | Derivados de tiazolcarboxamida para usarse como inhibidores de nampt. |
| WO2013170191A1 (en) | 2012-05-11 | 2013-11-14 | Genentech, Inc. | Methods of using antagonists of nad biosynthesis from nicotinamide |
| US8975398B2 (en) | 2012-05-11 | 2015-03-10 | Abbvie Inc. | NAMPT inhibitors |
| AR091022A1 (es) | 2012-05-11 | 2014-12-30 | Abbvie Inc | Inhibidores del nampt |
| US9504756B2 (en) | 2012-05-15 | 2016-11-29 | Seattle Genetics, Inc. | Self-stabilizing linker conjugates |
| US20130309223A1 (en) | 2012-05-18 | 2013-11-21 | Seattle Genetics, Inc. | CD33 Antibodies And Use Of Same To Treat Cancer |
| MX340090B (es) | 2012-11-05 | 2016-06-23 | Pfizer | Analogos de spliceostatina. |
| WO2014074715A1 (en) | 2012-11-07 | 2014-05-15 | Genentech, Inc. | Cyclopropyl amide derivatives |
| WO2014111871A1 (en) | 2013-01-17 | 2014-07-24 | Aurigene Discovery Technologies Limited | 4,5-dihydroisoxazole derivatives as nampt inhibitors |
| ITTO20130356A1 (it) | 2013-05-03 | 2014-11-04 | Uni Degli Studi Del Piemonte Orientale Ame | Inibitori di nicotinamide fosforibosil transferasi, relative composizioni, prodotti ed usi |
| CA2921532A1 (en) | 2013-10-09 | 2015-04-16 | Eli Lilly And Company | Novel pyridyloxyacetyl tetrahydroisoquinoline compounds useful as nampt inhibitors |
| ES2826398T3 (es) * | 2013-10-15 | 2021-05-18 | Seagen Inc | Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco |
| JP6701077B2 (ja) | 2013-12-19 | 2020-05-27 | シアトル ジェネティックス, インコーポレイテッド | 標的化薬物結合体と使用するためのメチレンカルバメートリンカー |
| US10144742B2 (en) | 2014-04-18 | 2018-12-04 | Millennium Pharmaceuticals, Inc. | Quinoxaline compounds and uses thereof |
| TW201625641A (zh) | 2014-05-22 | 2016-07-16 | 健臻公司 | Nampt抑制劑及方法 |
| AU2015293534A1 (en) | 2014-07-23 | 2017-02-02 | Aurigene Discovery Technologies Limited | 4,5-dihydroisoxazole derivatives as NAMPT inhibitors |
| SI3900742T1 (sl) | 2014-09-11 | 2024-10-30 | Seagen Inc. | Ciljana dostava zdravilnih snovi, ki vsebujejo terciarne amine |
| CN104557863B (zh) | 2014-12-18 | 2017-03-15 | 中国科学院广州生物医药与健康研究院 | 一种新型烟酰胺磷酸核糖转移酶抑制剂及其合成方法与应用 |
| EP3247705B1 (en) | 2015-01-20 | 2019-11-20 | Millennium Pharmaceuticals, Inc. | Quinazoline and quinoline compounds and uses thereof as nampt inhibitors |
| TWI835714B (zh) | 2016-10-18 | 2024-03-21 | 美商思進公司 | 菸鹼醯胺腺嘌呤二核苷酸補救合成(salvage pathway)抑制劑之靶向投遞 |
| WO2018201087A1 (en) | 2017-04-27 | 2018-11-01 | Seattle Genetics, Inc. | Quaternized nicotinamide adenine dinucleotide salvage pathway inhibitor conjugates |
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| AU2022246407B2 (en) | 2024-07-18 |
| CA3060206A1 (en) | 2018-11-01 |
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| CN110799217A (zh) | 2020-02-14 |
| JP7425606B2 (ja) | 2024-01-31 |
| MX2019012194A (es) | 2019-12-16 |
| TW201904613A (zh) | 2019-02-01 |
| KR20190141181A (ko) | 2019-12-23 |
| MX2023014831A (es) | 2024-01-15 |
| AU2018258687C1 (en) | 2023-02-02 |
| AU2018258687B2 (en) | 2022-07-07 |
| SG11201909563VA (en) | 2019-11-28 |
| EP3615081A1 (en) | 2020-03-04 |
| MA51189A (fr) | 2020-03-04 |
| US20240293554A1 (en) | 2024-09-05 |
| IL269794A (en) | 2019-11-28 |
| US11931414B2 (en) | 2024-03-19 |
| JP2023119064A (ja) | 2023-08-25 |
| JP2020517599A (ja) | 2020-06-18 |
| AU2018258687A1 (en) | 2019-12-05 |
| US20200197524A1 (en) | 2020-06-25 |
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