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1. 发明授权

US10398665B2 Compounds as modulators of a mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction 有权
公开(公告)号：US10398665B2
公开(公告)日：2019-09-03
申请号：US14969573
申请日：2015-12-15
申请人： INSTYTUT BIOCHEMII I BIOFIZYKI PAN
发明人： Norbert Odolczyk , Piotr Zielenkiewicz , Grzegorz Wieczorek , Aleksander Edelman , Danielle Tondelier , Janine Fritsch
IPC分类号： A61K31/663 , A61K31/194 , C07C233/65 , C07D219/10 , C07D473/30 , C07F9/30 , C07C235/84 , C07D401/12 , C07D473/22 , A61K31/496 , A61K31/52
摘要： An exemplary embodiment relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. An exemplary embodiment provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation ΔF508-CFTR, or another mutation of class II.

2. 发明授权

US08026244B2 Thioxanthine derivatives and their use as inhibitors of MPO 失效
标题翻译：硫代黄嘌呤衍生物及其作为MPO抑制剂的用途
公开(公告)号：US08026244B2
公开(公告)日：2011-09-27
申请号：US12295306
申请日：2007-04-12
申请人： Anna-Karin Tiden , Jenny Viklund
发明人： Anna-Karin Tiden , Jenny Viklund
IPC分类号： C07D473/22 , A61K31/522 , A61P9/10 , A61P11/00 , A61P11/08 , A61P25/16 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12
CPC分类号： C07D473/20 , C07D473/22
摘要： There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.
摘要翻译：公开了式（I）的新化合物，其中L，R 1，X和Y如说明书中所定义，及其药学上可接受的盐; 以及其制备方法，含有它们的组合物及其在治疗中的用途。这些化合物是MPO酶的抑制剂，因此特别可用于治疗或预防神经炎症性疾病，心脑血管动脉粥样硬化性疾病和外周动脉疾病和呼吸系统疾病。

3. 发明授权

US07002012B2 Substituted (1,3-bis(cyclohexylmethyl)-1,2,3,6-tetrahydro-2,6-dioxo-9h-purin-8-YI)phenyl derivatives, their preparation and their use in the treatment of inflammatory conditions and immune disorders 失效
标题翻译：取代的（1,3-双（环己基甲基）-1,2,3,6-四氢-2,6-二氧代-9H-嘌呤-8-基）苯基衍生物，其制备及其用于治疗炎性病症和免疫疾病
公开(公告)号：US07002012B2
公开(公告)日：2006-02-21
申请号：US10174414
申请日：2002-06-17
申请人： Susan Mary Daluge , Gerald Wolberg , Douglas Alan Livingston
发明人： Susan Mary Daluge , Gerald Wolberg , Douglas Alan Livingston
IPC分类号： C07D473/06 , C07D473/22 , A61P29/02 , A61P37/06 , A61K31/522
CPC分类号： C07D473/06
摘要： A method for the prophylaxis of an inflammatory condition or immune disorder associated with infiltration of leukocytes into inflamed tissue in a subject in need thereof, which method comprises administering to the subject a therapeutically effective amount of a compound of formula (I) or a solvate thereof wherein: X is —O— or —NH—; Q is (—CH2—)p, (—CH═CH—)p, (—C≡C—)p where p is an integer of from 0 to 4; R1 is hydrogen or methyl; R2 and R3 independently represent O or S; n is an integer of 1 to 50; and R is hydrogen or methyl.
摘要翻译：用于预防与有需要的受试者相关的白细胞浸润到发炎组织中的炎性病症或免疫病症的方法，所述方法包括向受试者施用治疗有效量的式（I）化合物，化学式= “CHEM-US-00001”num =“000”

4. 发明授权

US06998484B2 Synthesis of purine locked nucleic acid analogues 有权
公开(公告)号：US06998484B2
公开(公告)日：2006-02-14
申请号：US09971364
申请日：2001-10-04
申请人： Troels Koch , Flemming Ressig Jensen
发明人： Troels Koch , Flemming Ressig Jensen
IPC分类号： C07D473/18 , C07D473/40 , C07D473/16 , C07D473/22
CPC分类号： C07H19/04
摘要： The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.

5. 发明授权

US06949559B2 Nitrogen substituted biaryl purine derivatives as potent antiproliferative agents 有权
标题翻译：氮取代的联芳基嘌呤衍生物作为有效的抗增殖剂
公开(公告)号：US06949559B2
公开(公告)日：2005-09-27
申请号：US10680832
申请日：2003-10-07
申请人： Michael Peter Trova
发明人： Michael Peter Trova
IPC分类号： A61P35/00 , A61P35/02 , C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34 , C07D473/22 , A61K31/52 , A61K31/522
CPC分类号： C07D473/34 , C07D473/16 , C07D473/18 , C07D473/24
摘要： The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: with X, Y, D, Q, V, A, R1, R2, R3, R4, and n1 defined herein.
摘要翻译：本发明的化合物是2,6,9-三取代的嘌呤衍生物，其是细胞周期蛋白/ cdk复合物的抑制剂。本发明的化合物也是人细胞增殖的有效抑制剂。因此，本发明的化合物构成具有药学上可接受的载体的药物组合物。通过向这些哺乳动物施用有效量的该化合物，这些化合物可用于治疗与哺乳动物相比，通过升高的哺乳动物细胞增殖水平介导的病症。本发明化合物的实例由以下化学结构表示：X，Y，D，Q，V，A，R 1，R 2，R 本文定义的3，3，R 4和n 1个。

6. 发明申请

US20030143561A1 Nucleoside derivatives for library preparation 审中-公开
标题翻译：用于文库制备的核苷衍生物
公开(公告)号：US20030143561A1
公开(公告)日：2003-07-31
申请号：US10175500
申请日：2002-06-20
申请人： Nuevolution A/S
发明人： Henrik Pedersen , Christian Klarner Sams , Frank Abilgaard Slok , Lene Hyldtoft , Michael Anders Godskesen
IPC分类号： C12Q001/68 , C07H021/04 , C07H019/04 , C07D413/14 , C07D473/34 , C07D473/22 , C07K014/00
CPC分类号： C07H21/00 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H23/00 , C12N15/1068 , C40B40/00
摘要： Nucleoside derivatives as building blocks for templated libraries are described.
摘要翻译：描述了核苷衍生物作为模板文库的构建块

7. 发明授权

US5929046A Pyrimidine and purine derivatives and their use in treating tumour cells 失效
标题翻译：嘧啶和嘌呤衍生物及其在治疗肿瘤细胞中的应用
公开(公告)号：US5929046A
公开(公告)日：1999-07-27
申请号：US572966
申请日：1995-12-15
申请人： Thomas Brian Hamilton McMurry , Robert Stanley McElhinney , Dorothy Josephine Donnelly , Paul Murray , Christophe Carola , Rhoderick Hugh Elder , Jane Kelly , Geoffrey Paul Margison , Joseph Anthony Rafferty , Amanda Jean Watson , Mark Andrew Willington
发明人： Thomas Brian Hamilton McMurry , Robert Stanley McElhinney , Dorothy Josephine Donnelly , Paul Murray , Christophe Carola , Rhoderick Hugh Elder , Jane Kelly , Geoffrey Paul Margison , Joseph Anthony Rafferty , Amanda Jean Watson , Mark Andrew Willington
IPC分类号： C07D239/47 , A61K31/00 , A61K31/17 , A61K31/505 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/529 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61K31/708 , A61P35/00 , A61P43/00 , C07D239/46 , C07D239/48 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D473/00 , C07D473/18 , C07D473/22 , C07D473/30 , C07D473/40 , C07D475/02 , C07D475/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07H19/04 , C07H19/06 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/19 , C07H19/23
CPC分类号： C07D239/47 , C07D471/04 , C07D473/00 , C07D473/18 , C07D473/22 , C07D473/30 , C07D473/40 , C07D475/04 , C07D487/04 , C07H19/04
摘要： The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom chosen from O, N, or S, or a substituted derivative thereof; or (ii) phenyl or a substituted derivative thereof,R.sup.2 is selected from H, C.sub.1 -C.sub.5 alkyl, halogen or NH.sub.2,R.sup.4 and R.sup.5 which are the same or different are selected fromH, NH.sub.2 or NO.sub.n where n=1 or 2, or R.sup.4 and R.sup.5 together with the pyrimidine ring form a 5-or 6-membered ring structure containing one or more heterocyclic atoms, and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.
摘要翻译：本发明提供了一些式II的6-芳基烷氧基嘧啶衍生物，其中R是（i）具有至少一个5-或6-元杂环的环状基团，任选地与其中稠合的碳环或杂环，该杂环或每个杂环具有至少一个选自O，N或S的杂原子或其取代的衍生物; 或（ii）苯基或其取代衍生物，R2选自H，C1-C5烷基，卤素或NH2，R4和R5相同或不同，选自H，NH2或NON，其中n = 1或2，或R4和R5与嘧啶环一起形成含有一个或多个杂环原子的5-或6-元环结构及其药学上可接受的盐，表现出消耗+ E，非O + EE6-烷基鸟嘌呤-DNA烷基转移酶的能力（ATase）活动。

8. 发明授权

US5220024A Process for the preparation of purine derivatives as antiviral agents 失效
标题翻译：用于制备作为抗病毒剂的嘌呤衍生物的方法
公开(公告)号：US5220024A
公开(公告)日：1993-06-15
申请号：US588569
申请日：1990-09-26
申请人： Graham R. Geen , Trevor J. Grinter , Stephen Moore
发明人： Graham R. Geen , Trevor J. Grinter , Stephen Moore
IPC分类号： C07D473/18 , C07D473/00 , C07D473/22 , C07D473/24 , C07D473/32 , C07D473/36 , C07D473/40 , C07F9/6561
CPC分类号： C07D473/00
摘要： A process for the preparation of a compound of formula (A): ##STR1## wherein X is hydrogen, hydroxy, chloro, C.sub.1-6 alkoxy or phenyl C.sub.1-6 alkoxy and R.sub.a and R.sub.b are hydrogen, including acyl and phosphate derivatives thereof; which process comprises:i) the preparation of a compound of formula (I): ##STR2## wherein R.sub.1 is C.sub.1-6 alkyl, or phenyl C.sub.1-6 alkyl in which the phenyl group is optionally substituted; R.sub.2 is hydrogen, hydroxy, chlorine, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy or amino; and R.sub.3 is halogen, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which process comprises the reaction of a compound of formula (II): ##STR3## with a compound of formula (VII): ##STR4## wherein Q is a leaving group, J is hydrogen or halo and R.sub.1 is as hereinbefore defined; to give a compound of formula (VIII): ##STR5## followed by reduction of the compound of formula (VIII) to give a compound of formula (I) as hereinbefore defined; and, as necessary or desired, interconverting variables R.sub.1, R.sub.2 and R.sub.3 to further values of R.sub.1, R.sub.2 and R.sub.3 ;(ii) the conversion of the resulting compound of formula (I) to a compound of formula (A) by converting variable R.sub.3, when other than amino, to amino, reducing the ester groups CO.sub.2 R.sub.1 to CH.sub.2 OH and optionally forming acyl or phosphate derivatives thereof, and as necessary or desired converting variable R.sub.2 in the compound of formula (I) to variable X in the compound of formula (A).

9. 发明授权

US3437661A Process of producing purine derivatives 失效
标题翻译：生产嘌呤衍生物的方法
公开(公告)号：US3437661A
公开(公告)日：1969-04-08
申请号：US42593765
申请日：1965-01-15
申请人： KYOWA HAKKO KOGYO KK
发明人： FUJIMOTO YASUO , TERANISHI MASAYUKI
IPC分类号： C07D473/00 , C07D473/04 , C07D473/18 , C07D473/22 , C07D473/30 , C07D57/38 , C07C113/00
CPC分类号： C07D473/00 , C07D473/04 , C07D473/18 , C07D473/22 , C07D473/30

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