公开(公告)号：US20240091371A1

公开(公告)日：2024-03-21

申请号：US18497645

申请日：2023-10-30

申请人： Tagworks Pharmaceuticals B.V.

发明人： Marc Stefan ROBILLARD ,  Hendricus Marie JANSSEN ,  Wolter TEN HOEVE ,  Ronny Mathieu VERSTEEGEN ,  Raffaella ROSSIN

IPC分类号： A61K47/68 ,  A61K31/435 ,  A61K31/444 ,  A61K31/704 ,  A61K38/05 ,  A61K39/395 ,  A61K47/22 ,  A61K47/54 ,  B82Y5/00 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08

CPC分类号： A61K47/6803 ,  A61K31/435 ,  A61K31/444 ,  A61K31/704 ,  A61K38/05 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/22 ,  A61K47/545 ,  A61K47/555 ,  A61K47/558 ,  A61K47/6897 ,  B82Y5/00 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08 ,  Y02A50/30

摘要： The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

公开(公告)号：US20160214917A1

公开(公告)日：2016-07-28

申请号：US14978924

申请日：2015-12-22

申请人： SynAffix B.V.

发明人： Floris Louis VAN DELFT ,  Floris Petrus Johannes Theodorus RUTJES ,  Frederik Jan DOMMERHOLT

IPC分类号： C07C33/16 ,  C07D311/82 ,  G01N21/64 ,  C07C67/347 ,  A61K49/00 ,  G01N33/58 ,  C07D495/04 ,  C07C29/147

CPC分类号： C07C33/16 ,  A61K47/54 ,  A61K49/0052 ,  C07C29/147 ,  C07C29/58 ,  C07C29/62 ,  C07C62/30 ,  C07C67/347 ,  C07C269/06 ,  C07C271/12 ,  C07C271/20 ,  C07C2602/24 ,  C07D311/82 ,  C07D495/04 ,  C07K14/47 ,  G01N21/6428 ,  G01N33/532 ,  G01N33/582 ,  G01N33/585 ,  G01N2021/6439 ,  C07C33/44 ,  C07C69/753

摘要： The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.

公开(公告)号：US5235076A

公开(公告)日：1993-08-10

申请号：US706950

申请日：1991-05-28

申请人： Alfred E. Asato ,  Robert S. H. Liu

发明人： Alfred E. Asato ,  Robert S. H. Liu

IPC分类号： A61K31/045 ,  A61K31/07 ,  A61K31/11 ,  A61K31/19 ,  A61K31/20 ,  A61K31/215 ,  A61K31/275 ,  A61P17/00 ,  A61P35/00 ,  C07C33/16 ,  C07C33/34 ,  C07C33/38 ,  C07C33/44 ,  C07C33/50 ,  C07C45/29 ,  C07C45/44 ,  C07C45/51 ,  C07C45/67 ,  C07C45/74 ,  C07C47/225 ,  C07C47/24 ,  C07C47/445 ,  C07C47/548 ,  C07C47/57 ,  C07C49/23 ,  C07C57/26 ,  C07C57/42 ,  C07C63/331 ,  C07C63/66 ,  C07C69/608 ,  C07C69/65 ,  C07C69/76 ,  C07C69/78 ,  C07C233/10 ,  C07C251/18

CPC分类号： C07C251/18 ,  A61K31/07 ,  A61K31/19 ,  A61K31/20 ,  A61K31/215 ,  A61K31/275 ,  C07C33/16 ,  C07C33/34 ,  C07C33/44 ,  C07C45/298 ,  C07C45/44 ,  C07C45/515 ,  C07C45/67 ,  C07C45/74 ,  C07C47/225 ,  C07C47/24 ,  C07C47/445 ,  C07C47/548 ,  C07C49/23 ,  C07C57/42 ,  C07C63/66 ,  C07C69/608 ,  C07C69/65 ,  C07C69/76 ,  C07C2102/30

摘要： Novel azulenic retinoid compounds and therapeutic compositions are disclosed, along with method for their production and use as anti-cancer and cancer-prevention agents. The compositions of the present invention will also find use in treating dermatological disorders such as acne and psoriasis, as well as dermatologically-related conditions such as repair and effacement of wrinkles.

摘要翻译： 公开了新型az类类视色素化合物和治疗组合物，以及其生产和用作抗癌剂和癌症预防剂的方法。 本发明的组合物还可用于治疗皮肤病学疾病如痤疮和牛皮癣，以及皮肤病学相关的病症如皱纹的修复和消除。

公开(公告)号：US11857636B2

公开(公告)日：2024-01-02

申请号：US17169217

申请日：2021-02-05

申请人： TAGWORKS PHARMACEUTICALS B.V.

发明人： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

IPC分类号： C07D257/02 ,  C07D257/08 ,  C07D237/26 ,  C07C33/16 ,  A61K47/68 ,  A61K47/54 ,  B82Y5/00 ,  A61K31/704 ,  A61K38/05 ,  A61K39/395 ,  A61K47/22 ,  A61K31/435 ,  A61K31/444

CPC分类号： A61K47/6803 ,  A61K31/435 ,  A61K31/444 ,  A61K31/704 ,  A61K38/05 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/22 ,  A61K47/545 ,  A61K47/555 ,  A61K47/558 ,  A61K47/6897 ,  B82Y5/00 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08 ,  Y02A50/30

摘要： The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

公开(公告)号：US11617799B2

公开(公告)日：2023-04-04

申请号：US16312569

申请日：2017-06-27

申请人： Tagworks Pharmaceuticals B.V. ,  Syncom B.V.

发明人： Marc Stefan Robillard ,  Wolter Ten Hoeve ,  Freek Johannes Maria Hoeben ,  Ronny Mathieu Versteegen ,  Hendricus Marie Janssen ,  Arthur Henry Antoon Marie Van Onzen ,  Raffaella Rossin

IPC分类号： C07D257/02 ,  C07D257/08 ,  C07D237/26 ,  C07C33/16 ,  A61K31/495 ,  A61K31/502 ,  A61K47/68 ,  A61K47/54 ,  C07K16/30 ,  A61K47/66 ,  A61K47/60 ,  A61K47/64 ,  A61K39/00

摘要： Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit having a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine having a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of the Construct.

公开(公告)号：US10967069B2

公开(公告)日：2021-04-06

申请号：US16512038

申请日：2019-07-15

申请人： TAGWORKS PHARMACEUTICALS B.V.

发明人： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

IPC分类号： C07D237/26 ,  C07D257/08 ,  C07C33/16 ,  A61K31/704 ,  A61K31/502 ,  A61K31/444 ,  A61K31/435 ,  A61K47/00 ,  A61K47/68 ,  A61K47/44 ,  A61K47/22 ,  A61K47/54 ,  B82Y5/00 ,  A61K38/05 ,  A61K39/395

摘要： The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

公开(公告)号：US20200048174A1

公开(公告)日：2020-02-13

申请号：US16358272

申请日：2019-03-19

申请人： SynAffix B.V.

发明人： Floris Louis VAN DELFT ,  Floris Petrus Johannes Theodorus RUTJES ,  Frederik Jan DOMMERHOLT

IPC分类号： C07C33/16 ,  A61K49/00 ,  C07C29/147 ,  C07C29/58 ,  C07C29/62 ,  C07C67/347 ,  C07C271/12 ,  G01N33/532 ,  G01N33/58 ,  A61K47/54 ,  C07C62/30 ,  C07C269/06 ,  C07C271/20 ,  C07D311/82 ,  C07D495/04 ,  C07K14/47 ,  G01N21/64

摘要： The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.

公开(公告)号：US10004810B2

公开(公告)日：2018-06-26

申请号：US15233283

申请日：2016-11-23

申请人： TAGWORKS PHARMACEUTICALS B.V.

发明人： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen

IPC分类号： C07D257/08 ,  C07D237/26 ,  A61K47/48 ,  C07C33/16 ,  B82Y5/00 ,  A61K31/704 ,  A61K38/05 ,  A61K39/395 ,  A61K47/22 ,  A61K31/435 ,  A61K31/444 ,  A61K47/54 ,  A61K47/68

CPC分类号： A61K47/6803 ,  A61K31/435 ,  A61K31/444 ,  A61K31/704 ,  A61K38/05 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/22 ,  A61K47/545 ,  A61K47/555 ,  A61K47/558 ,  A61K47/6897 ,  B82Y5/00 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08 ,  Y02A50/471

摘要： The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

公开(公告)号：US20080139848A1

公开(公告)日：2008-06-12

申请号：US11609075

申请日：2006-12-11

申请人： Satyam S. Nampalli ,  Brijesh Patel ,  Peter Xavier Tharial ,  Ravishanker Kovi

发明人： Satyam S. Nampalli ,  Brijesh Patel ,  Peter Xavier Tharial ,  Ravishanker Kovi

IPC分类号： C07C33/16 ,  C07C211/31

CPC分类号： C07C29/32 ,  C07C209/22 ,  C07C303/28 ,  C07C2603/32 ,  C07C211/32 ,  C07C309/66 ,  C07C33/38

摘要： A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.

摘要翻译： 在惰性气氛下，在四氢呋喃中，在过量的正丁基锂存在下，用氯丙醇与氯丙醇偶合制备式（1）的5-二氢苯并环庚三烯的方法，然后制备式（3）的甲磺酸酯衍生物， 通过使甲胺溶液在甲醇中反应，得到式（4）的无游离碱，从而亲核取代甲磺酸酯基。 此外，本发明方法显示盐酸盐形成和纯化，得到纯度为0.1％w / w的杂质的药物级羟基替康林盐酸盐。

公开(公告)号：US4393245A

公开(公告)日：1983-07-12

申请号：US326597

申请日：1981-12-02

申请人： Werner Hoffman ,  Karl von Fraunberg ,  Manfred Baumann

发明人： Werner Hoffman ,  Karl von Fraunberg ,  Manfred Baumann

IPC分类号： C07C29/143 ,  C07C29/17 ,  C07C29/40 ,  C07C31/133 ,  C07C33/16 ,  C07C35/205 ,  C07C49/547 ,  C07C49/307

CPC分类号： C07C49/547 ,  C07C29/143 ,  C07C29/175 ,  C07C29/40 ,  C07C31/133 ,  C07C33/16 ,  C07C35/205 ,  C07C45/512 ,  C07C2101/20

摘要： New 1-acyl- and 1-hydroxymethyl-cyclododecanes and -cyclododecenes. The new 1-acyl-cyclododecenes and -cyclododecanes are obtained by a Rupe or Meyer-Schuster rearrangement, with or without subsequent hydrogenation in the presence of Ni, Pd and Pt catalysts. The 1-acyl-cyclododecenes and -cyclododecanes are valuable scents of the basic type of the sought-after macrocyclic musk scents. Furthermore, they are used for the manufacture of numerous other new 1-substituted or 1-and 2-substituted cyclododecenes and cyclododecanes having good scent characteristics.

摘要翻译： 新的1-酰基和1-羟甲基 - 环十二烷和环十二碳烯。 通过Rupe或Meyer-Schuster重排获得新的1-酰基 - 十二碳烯和 - 环十二烷，在Ni，Pd和Pt催化剂的存在下进行或不进行随后的氢化。 1-酰基 - 环十二碳烯和环十二烷是所寻求的大环麝香香气的基本类型的有价值的气味。 此外，它们用于制造许多其它新的具有良好香味特征的1-取代或1-取代的环十二碳烯和环十二烷。