公开(公告)号：US08629147B2

公开(公告)日：2014-01-14

申请号：US11593191

申请日：2006-11-02

Applicant: Alexey Vyacheslavovich Anikin ,  Vidyasagar Reddy Gantla ,  Vlad Edward Gregor ,  Luyong Jiang ,  Yahua Liu ,  Danny Peter Claude McGee ,  Charles Chamchoumis Mikel ,  Jason Conrad Pickens ,  Thomas Roy Webb ,  Zheng Yan ,  Tong Zhu ,  Aleksander Kadushkin ,  Sergey Sviridov ,  Sergey Zozulya ,  Alexander Chucholowski ,  Douglas Eric McGrath

Inventor： Alexey Vyacheslavovich Anikin ,  Vidyasagar Reddy Gantla ,  Vlad Edward Gregor ,  Luyong Jiang ,  Yahua Liu ,  Danny Peter Claude McGee ,  Charles Chamchoumis Mikel ,  Jason Conrad Pickens ,  Thomas Roy Webb ,  Zheng Yan ,  Tong Zhu ,  Aleksander Kadushkin ,  Sergey Sviridov ,  Sergey Zozulya ,  Alexander Chucholowski ,  Douglas Eric McGrath

IPC: A61K31/497 ,  A61K31/47 ,  A61K31/445

CPC classification number: C07D401/04 ,  C07D235/18 ,  C07D235/20 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/04 ,  C07D495/04

Abstract: The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.

Abstract translation: 本发明提供了能够调节酪氨酸激酶的化合物，包含该化合物的组合物及其使用方法。

公开(公告)号：US08063225B2

公开(公告)日：2011-11-22

申请号：US11891604

申请日：2007-08-10

Applicant: Vlad E. Gregor ,  Yahua Liu ,  Alexey Anikin ,  Danny Peter Claude McGee ,  Charles Mikel ,  Douglas Eric McGrath ,  Goverdhan Reddy Vavilala ,  Jason C. Pickens ,  Alexander Kadushkin ,  Luyong Jiang ,  Mohan Santhanam Thiruvazhi ,  Sergey Zozulya ,  Rajendran Vairagoundar ,  Tong Zhu ,  Alexander Chucholowski ,  Thomas Webb ,  Vidyasagar Reddy Gantla ,  Zheng Yan

Inventor： Vlad E. Gregor ,  Yahua Liu ,  Alexey Anikin ,  Danny Peter Claude McGee ,  Charles Mikel ,  Douglas Eric McGrath ,  Goverdhan Reddy Vavilala ,  Jason C. Pickens ,  Alexander Kadushkin ,  Luyong Jiang ,  Mohan Santhanam Thiruvazhi ,  Sergey Zozulya ,  Rajendran Vairagoundar ,  Tong Zhu ,  Alexander Chucholowski ,  Thomas Webb ,  Vidyasagar Reddy Gantla ,  Zheng Yan

IPC: C07D401/00 ,  A61K31/44

CPC classification number: C07D487/04

Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.

Abstract translation: 提供式（I）化合物或其调节酪氨酸激酶活性的立体异构体，互变异构体，盐，水合物或前药，包含该化合物的组合物及其使用方法。

公开(公告)号：US20100056475A1

公开(公告)日：2010-03-04

申请号：US12536455

申请日：2009-08-05

Applicant: Alexander Chucholowski ,  Thomas Hermann ,  Benjamin Ayida ,  Tingmin Wang ,  Alisher Khasanov

Inventor： Alexander Chucholowski ,  Thomas Hermann ,  Benjamin Ayida ,  Tingmin Wang ,  Alisher Khasanov

IPC: A61K31/724 ,  C08B37/16 ,  C07K9/00 ,  C07H21/00 ,  C12N5/00 ,  C07H1/00 ,  A61P43/00

CPC classification number: A61K48/0041 ,  A61K47/62 ,  A61K47/6951 ,  B82Y5/00 ,  C08B37/0012 ,  C08B37/0015 ,  C12N15/111 ,  C12N2310/351 ,  C12N2320/32

Abstract: It has been discovered that the uptake of anionic charged species into cells can be enhanced by noncovalently associating such species with specifically modified forms of cyclodextrin. The invention modified forms of cyclodextrin form well defined stoichiometric complexes with anionic charged molecules. This discovery enables one to produce various compositions containing anionic charged molecules and facilitates methods for enhancing the cellular uptake of double-stranded or hairpin nucleic acid.

Abstract translation: 已经发现，通过非特异性地将这些物质与特定的修饰形式的环糊精缔合，可以增强阴离子带电物质进入细胞的摄取。 本发明改性形式的环糊精与阴离子带电分子形成了明确的化学计量络合物。 该发现使得人们可以生产含有阴离子带电分子的各种组合物，并且有利于增强双链或发夹核酸的细胞摄取的方法。

公开(公告)号：US20080021027A1

公开(公告)日：2008-01-24

申请号：US11821265

申请日：2007-06-22

Applicant: Gregory Benson ,  Konrad Bleicher ,  Alexander Chucholowski ,  Henrietta Dehmlow ,  Uwe Grether ,  Bernd Kuhn ,  Rainer Martin ,  Eric Niesor ,  Narendra Panday ,  Hans Richter ,  Franz Schuler ,  Xavier Warot ,  Matthew Wright ,  Minmin Yang

Inventor： Gregory Benson ,  Konrad Bleicher ,  Alexander Chucholowski ,  Henrietta Dehmlow ,  Uwe Grether ,  Bernd Kuhn ,  Rainer Martin ,  Eric Niesor ,  Narendra Panday ,  Hans Richter ,  Franz Schuler ,  Xavier Warot ,  Matthew Wright ,  Minmin Yang

IPC: A61K31/4184 ,  A61K31/41 ,  A61K31/422 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/47 ,  A61K31/5377 ,  A61P1/16 ,  C07D211/12 ,  C07D215/20 ,  C07D235/26 ,  C07D257/04 ,  C07D261/12 ,  C07D285/06 ,  C07D401/04 ,  C07D413/10 ,  C07D413/14

CPC classification number: C07D235/18 ,  C07D235/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/10 ,  C07D413/04 ,  C07D417/06

Abstract: The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to Farnesoid-X-receptors (FXR) and can be used to treat diseases which are modulated by FXR agonists such as diabetes and dyslipidemia.

Abstract translation: 本发明涉及式（I）的新的苯并咪唑衍生物，其中R 1至R 8如在说明书和权利要求书中所定义，以及生理上可接受的盐 及其酯。 这些化合物与法呢型-X受体（FXR）结合，可用于治疗由FXR激动剂如糖尿病和血脂异常调节的疾病。

公开(公告)号：US07071212B2

公开(公告)日：2006-07-04

申请号：US10639030

申请日：2003-08-12

Applicant: Jean Ackermann ,  Leo Alig ,  Alexander Chucholowski ,  Katrin Groebke ,  Kurt Hilpert ,  Holger Kuehne ,  Ulrike Obst ,  Lutz Weber ,  Hans Peter Wessel

Inventor： Jean Ackermann ,  Leo Alig ,  Alexander Chucholowski ,  Katrin Groebke ,  Kurt Hilpert ,  Holger Kuehne ,  Ulrike Obst ,  Lutz Weber ,  Hans Peter Wessel

IPC: A61K31/445 ,  C07D265/30

CPC classification number: C07D207/27 ,  C07C257/18 ,  C07C259/18 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/12 ,  C07D209/48 ,  C07D211/46 ,  C07D211/58 ,  C07D211/96 ,  C07D213/30 ,  C07D213/55 ,  C07D213/65 ,  C07D213/74 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D261/04 ,  C07D271/06 ,  C07D277/24 ,  C07D295/155 ,  C07D307/12 ,  C07D307/20 ,  C07D307/54 ,  C07D309/12 ,  C07D309/14 ,  C07D317/64 ,  C07D319/18 ,  C07D321/10 ,  C07D333/24 ,  C07D335/04 ,  C07D403/12

Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.

Abstract translation: 本发明涉及下式的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物：其中R 1，E，X 1至X 4 本说明书和权利要求书中所定义的，以及其水合物或溶剂合物及其生理上可用的盐。

公开(公告)号：US06964974B2

公开(公告)日：2005-11-15

申请号：US09939872

申请日：2001-08-27

Applicant: Jean Ackermann ,  Johannes Aebi ,  Alexander Chucholowski ,  Henrietta Dehmlow ,  Olivier Morand ,  Sabine Wallbaum ,  Thomas Weller

Inventor： Jean Ackermann ,  Johannes Aebi ,  Alexander Chucholowski ,  Henrietta Dehmlow ,  Olivier Morand ,  Sabine Wallbaum ,  Thomas Weller

IPC: A61K31/445 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/55 ,  A61P1/16 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P31/10 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00 ,  C07D211/18 ,  C07D211/22 ,  C07D211/26 ,  C07D211/44 ,  C07D211/46 ,  C07D211/96 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

CPC classification number: C07D211/46 ,  C07D211/22 ,  C07D211/26 ,  C07D211/96

Abstract: The present invention relates to piperidine derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract translation: 本发明涉及可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，胆结石，肿瘤和/或过度增殖性疾病相关的疾病的哌啶衍生物 ，以及治疗和/或预防糖耐量异常和糖尿病。

公开(公告)号：US06660738B2

公开(公告)日：2003-12-09

申请号：US09906983

申请日：2001-07-17

Applicant: Johannes Aebi ,  Daniel Bur ,  Alexander Chucholowski ,  Henrietta Dehmlow

Inventor： Johannes Aebi ,  Daniel Bur ,  Alexander Chucholowski ,  Henrietta Dehmlow

IPC: C07D40104

CPC classification number: C07D401/04 ,  C07D403/04

Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.

公开(公告)号：US5521160A

公开(公告)日：1996-05-28

申请号：US368519

申请日：1995-01-04

Applicant: Alexander Chucholowski ,  Jurgen Fingerle ,  Niggi Iberg ,  Hans P. Marki ,  Rita Muller ,  Michael Pech ,  Marianne Rouge ,  Gerard Schmid ,  Thomas Tschopp ,  Hans P. Wessel

Inventor： Alexander Chucholowski ,  Jurgen Fingerle ,  Niggi Iberg ,  Hans P. Marki ,  Rita Muller ,  Michael Pech ,  Marianne Rouge ,  Gerard Schmid ,  Thomas Tschopp ,  Hans P. Wessel

IPC: C07D307/42 ,  A61K31/17 ,  A61K31/225 ,  A61K31/255 ,  A61K31/7024 ,  A61P9/10 ,  A61P9/14 ,  C07C31/18 ,  C07C31/27 ,  C07C305/04 ,  C07C305/06 ,  C07C305/10 ,  C07C305/16 ,  C07C309/02 ,  C07C311/17 ,  C07C311/23 ,  C07C317/22 ,  C07C317/36 ,  C07C317/44 ,  C07C335/06 ,  C07C335/16 ,  C07D303/46 ,  C07D307/68 ,  C07D311/82 ,  C07H7/00 ,  C07H11/00 ,  C07H5/04

CPC classification number: C07C305/10 ,  C07C305/06 ,  C07C311/17 ,  C07C317/22 ,  C07C317/36 ,  C07C317/44 ,  C07C335/16 ,  C07D307/68 ,  C07D311/82

Abstract: The present invention is concerned with novel sulfuric acid esters of sugar alcohols and sugar alcohol-like compounds of the formula ##STR1## Also described are methods for the treatment and/or prophylaxis of arteriosclerotic changes in the vascular wall as well as a process for the manufacture of the compounds of formula I and their salts.

Abstract translation: 本发明涉及糖醇的新型硫酸酯和下式的糖醇类化合物（I）。还描述了治疗和/或预防血管壁动脉硬化变化的方法以及 用于制备式I化合物及其盐的方法。

公开(公告)号：US20120149732A1

公开(公告)日：2012-06-14

申请号：US13215109

申请日：2011-08-22

Applicant: Alexander Chucholowski ,  Alisher Khasanov ,  Gregory Parker ,  Tong Zhu

Inventor： Alexander Chucholowski ,  Alisher Khasanov ,  Gregory Parker ,  Tong Zhu

IPC: A61K31/4545 ,  C07F7/18 ,  C07D213/71 ,  C07D401/12 ,  C07D305/14 ,  A61K31/4402 ,  A61K31/337 ,  A61K31/4025 ,  A61P35/00 ,  A61P29/00 ,  A61P31/00 ,  A61P37/00 ,  A61P37/08 ,  A61P25/00 ,  A61P17/00 ,  A61P9/00 ,  A61P3/10 ,  A61P1/00 ,  C07F7/12

CPC classification number: C07D213/71 ,  A61K47/50 ,  A61K47/542 ,  A61K47/60 ,  C07D305/14 ,  C07D405/12 ,  C07F7/1804

Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.

Abstract translation: 根据本发明，已经开发了在其上具有正交反应性基团的新型多官能化合物，从而有利于制备具有多种功能性质的化合物（例如靶向部分和生物活性部分）。 这样的构建体可用于各种应用，例如用于递送生物相容性材料并以活性形式释放。 因此，根据本发明，提供了具有限定结构的多功能接头以及其上具有一种或多种生物活性组分的各种衍生物。 根据本发明还提供了制备这种构建体的方法及其各种用途。

公开(公告)号：US20100056612A1

公开(公告)日：2010-03-04

申请号：US12536456

申请日：2009-08-05

Applicant: Alexander Chucholowski ,  Thomas Hermann

Inventor： Alexander Chucholowski ,  Thomas Hermann

IPC: A61K31/7052 ,  C07K7/64 ,  C07K2/00 ,  C07K9/00 ,  C08B37/16 ,  C12N5/00 ,  C07H21/00 ,  A61P43/00

CPC classification number: C12N15/87

Abstract: In accordance with the present invention, it has been discovered that the uptake of charged molecules into cells can be enhanced by noncovalently associating such molecules with molecular entities comprising an amphiphilic core with oppositely charged arms. The molecular entities form well defined stoichiometric complexes with charged molecules. Various compositions and methods for stabilizing anionic charged molecules and for enhancing the cellular uptake of any anionic charged molecules, e.g. double-stranded or hairpin nucleic acid, are provided.

Abstract translation: 根据本发明，已经发现，通过将这样的分子与包含具有相反电荷的臂的两亲核心的分子实体非共价结合，可以增强带电分子进入细胞的摄取。 分子实体与带电分子形成明确的化学计量络合物。 用于稳定阴离子带电分子和增强任何阴离子带电分子的细胞摄取的各种组合物和方法，例如， 双链或发夹核酸。