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51. 发明授权

US07091313B2 Synthesis of template-fixed β-hairpin loop mimetics 有权
标题翻译：模板固定β-发夹环模拟物的合成
公开(公告)号：US07091313B2
公开(公告)日：2006-08-15
申请号：US11029331
申请日：2005-01-05
申请人： John A. Robinson , Daniel Obrecht
发明人： John A. Robinson , Daniel Obrecht
IPC分类号： A61K38/00
CPC分类号： C07K7/06 , C07K1/04 , C07K7/02 , C07K7/08 , C07K7/64
摘要： Template-fixed β-hairpin loop mimetics comprising a template corresponding to one of the structures (a), (b), (c), (d), (e), (f), (g), (h) and a template-fixed chain of 4 to 20 α-amino acid residues which, if their α-C atom is asymmetric, have L-configuration can be manufactured by a novel process which is based on a mixed solid- and solution phase synthetic strategy. If desired, this process can be modified to give the enantiomers of these template-fixed β-hairpin loop mimetics. These enantiomers are novel compounds, and many of said template-fixed β-hairpin loop mimetics themselves are also novel compounds. The template-fixed β-hairpin loop mimetics and their enantiomers can mimic flat surfaces of proteins and thus be used to probe large surface protein-protein interactions. Accordingly they can serve as lead finding tools for protein targets where it is difficult to find small-molecular-weight lead compounds.
摘要翻译：模板固定的β-发夹环模拟物，其包含对应于结构（a），（b），（c），（d），（e），（f），（g），（h）和 4至20个α-氨基酸残基的模板固定链，如果它们的α-C原子是不对称的，则具有L-构型可以通过基于混合固相和溶液相合成策略的新方法制备。如果需要，可以修饰该方法以得到这些模板固定的β-发夹环模拟物的对映异构体。这些对映体是新化合物，许多所述模板固定的β-发夹环模拟物本身也是新的化合物。模板固定的β-发夹环模拟物及其对映体可以模拟蛋白质的平坦表面，因此可用于探测大的表面蛋白质 - 蛋白质相互作用。因此，它们可以作为难以发现小分子量铅化合物的蛋白质靶标的主要发现工具。

52. 发明授权

US5837807A Tetrahydronaphthalene compounds 失效
标题翻译：四氢萘化合物
公开(公告)号：US5837807A
公开(公告)日：1998-11-17
申请号：US607734
申请日：1996-02-27
申请人： Christine Abrecht , Alfred Grieder , Klaus Muller , Daniel Obrecht
发明人： Christine Abrecht , Alfred Grieder , Klaus Muller , Daniel Obrecht
IPC分类号： A61K38/00 , C07K1/107 , C07K7/06 , C07K7/08 , C07K4/00 , C07D285/00 , C07K5/12
CPC分类号： C07K7/08
摘要： This invention is directed to tetrahydronaphthalene compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, bromine, cyano, formyl, hydroxy, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, aryloxy, lower aralkoxy or aryl; R.sup.2 is an amino acid residue or a chain of 2 to 20 amino acid residues wherein reactive moieties in the side chains of the amino acid residue(s) is/are protected or unprotected, and wherein the amino group of the N-terminal amino acid is a free or protected amino group; A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each are .alpha.-amino acid residues wherein A.sup.1 and A.sup.2 are in the L configuration and A.sup.3 and A.sup.4 are in the D configuration when the .alpha.-C atom of said .alpha.-amino acid residue is asymmetric; X is oxygen or sulphur; Y is a residue of the formula ##STR2## n is 0 or 1; R.sup.3 is hydrogen or lower alkyl; R.sup.4 is hydrogen or lower alkyl; and Z and the two C atoms together are an aromatic ring selected from the group of benzene, furan, thiophene, pyridine or pyrimidine, wherein said aromatic ring is substituted or unsubstituted; and salts thereof and their intermediates. The compounds are useful as mimetics of exposed helical domains of proteins in order to clarify their role with respect to interactions with other proteins or with DNA or RNA through .alpha.-helical conformation. They are therefore valuable aids in the determination of biologically active peptide sequences and are accordingly so-called "research tools". They are also potentially useful as medicaments.
摘要翻译：本发明涉及下式的四氢化萘化合物，其中R 1是氢，溴，氰基，甲酰基，羟基，低级烷基，低级烯基，低级炔基，低级烷氧基，芳氧基，低级芳烷氧基或芳基。 R2是氨基酸残基或2至20个氨基酸残基的链，其中氨基酸残基的侧链中的活性部分被保护或未被保护，并且其中N-末端氨基酸的氨基是一个游离或保护的氨基; A1，A2，A3和A4各自为α-氨基酸残基，其中A1和A2为L构型，当所述α-氨基酸残基的α-C原子不对称时，A3和A4为D构型; X是氧或硫; （a）下式的残基：（a）（b）n为0或1; R3是氢或低级烷基; R4是氢或低级烷基; Z和两个C原子一起是选自苯，呋喃，噻吩，吡啶或嘧啶的芳环，其中所述芳环是取代或未取代的; 及其盐及其中间体。这些化合物可用作蛋白质暴露的螺旋结构域的模拟物，以便澄清其在与其他蛋白质的相互作用或通过α-螺旋构象与DNA或RNA的作用。因此，它们是测定生物活性肽序列的有价值的辅助因素，因此是所谓的“研究工具”。它们也可能用作药物。

53. 发明授权

US5644024A Tetrahydronaphthalene derivatives 失效
标题翻译：四氢萘衍生物
公开(公告)号：US5644024A
公开(公告)日：1997-07-01
申请号：US292128
申请日：1994-08-17
申请人： Christine Abrecht , Klaus Muller , Daniel Obrecht , Arnold Trzeciak
发明人： Christine Abrecht , Klaus Muller , Daniel Obrecht , Arnold Trzeciak
IPC分类号： G01N33/68 , A61K38/00 , C07K5/062 , C07K7/06 , C07K7/08 , C07K7/54 , C07D285/00 , C07K4/00
CPC分类号： C07K7/08 , Y02P20/55
摘要： The present invention is concerned with tetrahydronaphthalene derivatives which are mimics of domains of peptides or proteins which can interact with other proteins or with DNA or RNA through .alpha.-helical conformation, said tetrahydronaphthalene derivatives having the formulae: ##STR1## are valuable aids in the determination of biologically active peptide sequences and are accordingly so-called "research tools". They are, however, also potentially suitable as medicaments.
摘要翻译：本发明涉及四氢萘衍生物，其是模拟可通过α-螺旋构象与其他蛋白质或与其它蛋白质或DNA或RNA相互作用的肽或蛋白质的结构域，所述四氢萘衍生物具有下列结构式：有用的帮助确定生物活性肽序列，因此是所谓的“研究工具”。然而，它们也可能适合作为药物。

54. 发明授权

US4927958A Styryl ketones 失效
标题翻译：苯乙烯酮
公开(公告)号：US4927958A
公开(公告)日：1990-05-22
申请号：US169570
申请日：1988-03-17
申请人： Albert Fischli , Eva-Maria Gutknecht , Daniel Obrecht
发明人： Albert Fischli , Eva-Maria Gutknecht , Daniel Obrecht
IPC分类号： C07C45/29 , C07C45/45 , C07C45/63 , C07C45/67 , C07C45/74 , C07C49/255 , C07C59/84 , C07C59/88 , C07C59/90 , C07C69/618 , C07C69/738 , C07D317/60
CPC分类号： C07D317/60 , C07C323/00 , C07C45/298 , C07C45/455 , C07C45/63 , C07C45/673 , C07C45/74 , C07C49/255 , C07C59/88 , C07C59/90
摘要： Styryl ketones of the formula ##STR1## wherein R.sup.8 and R.sup.9 are independently hydrogen or lower alkyl or together represent an additional carbon-carbon bond andR.sup.10 is a group of the formula ##STR2## as well as corresponding compounds of the formula ##STR3## wherein R.sup.10' is a group of formula (a), (b), (d) or (e) or a group of the formula--C(R.sup.18)(R.sup.19)OR.sup.20' ; (f') have mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers or duodenal ulcers.
摘要翻译：式IMA的苯乙烯基酮其中R 8和R 9独立地是氢或低级烷基或一起代表额外的碳 - 碳键，并且R 10是下式的基团：以及相应的化合物其中R 10'是式（a），（b），（d）或（e）的基团或式-C（R 18）（R 19）OR 20'的基团; （f'）具有粘膜保护性和/或胃酸分泌抑制性质，使得它们可用于控制或预防胃肠道疾病，特别是胃溃疡或十二指肠溃疡。

55. 发明授权

US08835437B2 Piperidine/piperazine derivatives 有权
标题翻译：哌啶/哌嗪衍生物
公开(公告)号：US08835437B2
公开(公告)日：2014-09-16
申请号：US12663009
申请日：2008-06-05
申请人： Jean-Pierre André Marc Bongartz , Lieven Meerpoel , Gustaaf Maria Boeckx , Guy Rosalia Eugeen Van Lommen , Christophe Francis Robert Nestor Buyck , Daniel Obrecht , Philipp Ermert , Anatol Luther
发明人： Jean-Pierre André Marc Bongartz , Lieven Meerpoel , Gustaaf Maria Boeckx , Guy Rosalia Eugeen Van Lommen , Christophe Francis Robert Nestor Buyck , Daniel Obrecht , Philipp Ermert , Anatol Luther
IPC分类号： A61K31/496 , C07D487/04 , C07D513/04 , C07D239/42 , C07D239/26 , A61K31/506 , A61K31/454 , C07D231/12 , C07D249/08 , C07D249/12 , C07D271/06 , C07D401/10
CPC分类号： C07D513/04 , C07D231/12 , C07D239/26 , C07D239/42 , C07D249/08 , C07D249/12 , C07D271/06 , C07D271/10 , C07D271/107 , C07D401/04 , C07D401/10 , C07D401/12 , C07D487/04
摘要： The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p—; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
摘要翻译：本发明还涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含1或2个N原子的6元芳族杂环，其中所述C3 6-环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 其N-氧化物，其药学上可接受的盐或其溶剂合物。本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。

56. 发明申请

US20100056432A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIBACTERIAL ACTIVITY 审中-公开
标题翻译：具有抗菌活性的模板固定肽
公开(公告)号：US20100056432A1
公开(公告)日：2010-03-04
申请号：US12506794
申请日：2009-07-21
申请人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
发明人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
IPC分类号： A61K38/12 , C07K5/12 , A61P11/00 , A61P17/02 , A61P1/00 , A61P27/16 , A61P35/00
CPC分类号： C07K5/06165 , A61K38/00 , C07K1/047 , C07K7/64 , Y02A50/473
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 α-amino acid residues which, depend on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa and Acinetobacter. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. In a specific embodiment, the template is based on the D-Pro-L-Pro dipeptides. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid—and solution phase synthetic strategy.
摘要翻译：通式（I）的模板固定和半透明肽模拟物，其中Z是12个α-氨基酸残基的模板固定链，其取决于它们在链中的位置（从N-末端氨基酸开始计数）是Gly或Pro，或某些类型，作为上述式中的其余符号在说明书和权利要求及其盐中定义，其具有选择性抑制微生物生长或杀死诸如假单胞菌属（Pseudomonas）铜绿假单胞菌和不动杆菌。它们可以用作食品，化妆品，药物或其他含营养材料的消毒剂，或用作治疗或预防感染的药物。在具体实施方案中，模板基于D-Pro-L-Pro二肽。这些＆bair-Hairpin肽模拟物可以通过基于混合固相和溶液相合成策略的方法制造。

57. 发明授权

US07612064B2 Sulfopyrroles 有权
标题翻译：硫磺吡咯
公开(公告)号：US07612064B2
公开(公告)日：2009-11-03
申请号：US10557664
申请日：2004-05-24
申请人： Martin Eberle , Philipp Ermert , Daniel Obrecht , Frank Lach , Anatol Luther , Felix Bachmann , Allessandro Strebel
发明人： Martin Eberle , Philipp Ermert , Daniel Obrecht , Frank Lach , Anatol Luther , Felix Bachmann , Allessandro Strebel
IPC分类号： C07D233/00 , C07D249/08 , C07D413/00 , A61K31/535 , A01N43/50 , A01N43/64
CPC分类号： C07D401/04 , C07D207/48 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
摘要翻译：本发明涉及式（I）化合物，其中R 1表示芳基，芳烷基或杂芳基，R 2为芳基或杂芳基，R 3为芳基，杂芳基或任选取代的氨基甲基，合成这些化合物的方法为含有式（I）化合物用于制备用于治疗肿瘤和自身免疫性疾病的药物组合物的式（I）化合物的使用，以及使用式（I）或式（I）化合物治疗肿瘤和自身免疫性疾病的方法，含有该组合物的药物组合物。

58. 发明授权

US07582604B2 Template-fixed peptidomimetics with antibacterial activity 有权
标题翻译：具有抗菌活性的模板固定肽模拟物
公开(公告)号：US07582604B2
公开(公告)日：2009-09-01
申请号：US11062021
申请日：2005-02-18
申请人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
发明人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
IPC分类号： A61K38/12 , C07K7/64
CPC分类号： C07K5/06165 , A61K38/00 , C07K1/047 , C07K7/64 , Y02A50/473
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I), wherein Z is a template-fixed chain of 12 α-amino acid residues which, depend on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa and Acinetobacter. They can be used as disinfectants for foodstuff, cosmetics, medicaments or other nutrient-containing materials, or as medicaments or treat or prevent infections. In a specific embodiment, the template is based on the D-Pro-L-Pro dipeptide. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
摘要翻译：通式（I）的模板固定的β-发夹肽模拟物，其中Z是12个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基酸开始计数）是Gly或Pro，或某些类型，作为上述式中的其余符号在说明书和权利要求及其盐中定义，其具有选择性抑制微生物生长或杀死诸如假单胞菌属（Pseudomonas）铜绿假单胞菌和不动杆菌。它们可用作食品，化妆品，药物或其他含营养物质的消毒剂，或用作药物或治疗或预防感染。在具体实施方案中，模板基于D-Pro-L-Pro二肽。这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。

59. 发明授权

US07253146B2 Template-fixed peptidomimetics with antimicrobial activity 有权
标题翻译：具有抗菌活性的模板固定肽模拟物
公开(公告)号：US07253146B2
公开(公告)日：2007-08-07
申请号：US10469060
申请日：2002-02-18
申请人： Daniel Obrecht , John Anthony Robinson , Jan Wim Vrijbloed
发明人： Daniel Obrecht , John Anthony Robinson , Jan Wim Vrijbloed
IPC分类号： A61K38/12 , C07K5/12 , C07K2/00 , C07K1/00 , A61K38/00 , A61K38/02
CPC分类号： C07K7/06 , A61K38/00 , C07K1/047 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formulae (I) and (II) wherein Z, Z1 and Z2 are template-fixed chains of 8 to 16 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms and cancer cells. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials or as medicaments to treat or prevent infections or diseases related to such infections and/or cancer. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy
摘要翻译：通式（I）和（II）的模板固定的β-发夹肽模拟物，其中Z，Z1和Z2是8至16个α-氨基酸残基的模板固定链，这取决于它们在链中的位置（开始计数来自N-末端氨基酸）是Gly或Pro，或某些类型，其作为上述式中的其余符号在说明书和权利要求书中定义，及其盐具有抑制生长的性质或杀死微生物和癌细胞。它们可以用作食品，化妆品，药物或其他含营养材料的消毒剂，或用作治疗或预防与这种感染和/或癌症相关的感染或疾病的药物。这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备

60. 发明授权

US5811389A Tri- and tetracyclic compounds 失效
标题翻译：三环和四环化合物
公开(公告)号：US5811389A
公开(公告)日：1998-09-22
申请号：US668871
申请日：1996-06-24
申请人： Wilhelm Bannwarth , Fernand Gerber , Alfred Grieder , Andreas Knierzinger , Klaus Muller , Daniel Obrecht , Arnold Trzeciak
发明人： Wilhelm Bannwarth , Fernand Gerber , Alfred Grieder , Andreas Knierzinger , Klaus Muller , Daniel Obrecht , Arnold Trzeciak
IPC分类号： A61K31/38 , A61K31/382 , A61K31/435 , A61K31/535 , A61K31/538 , A61K31/54 , A61K31/5415 , A61K38/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P37/08 , C07D265/38 , C07D279/20 , C07D279/22 , C07D279/30 , C07D311/82 , C07D335/12 , C07D413/06 , C07D417/06 , C07D498/06 , C07D513/06 , C07K1/113 , C07K5/04 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/103 , C07K7/06 , C07K7/08 , C07K14/75 , A61K38/03 , C07K4/00
CPC分类号： C07D413/06 , C07D265/38 , C07D279/22 , C07D311/82 , C07D417/06 , C07D513/06 , C07K14/75 , C07K5/04 , C07K5/06026 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06086 , C07K5/06104 , C07K5/0808 , C07K5/1008 , C07K5/101 , C07K5/1019 , C07K7/06 , A61K38/00 , Y02P20/55
摘要： There are described compounds of the formula ##STR1## Wherein the variables have been defined herein. The compounds are useful as research tools in the determination of biologically active peptides sequences and also potentially suitable as medicaments, some of them being useful in the prevention or control of the formation of blood platelet thrombi, and some compounds are useful as intermediates.
摘要翻译：描述了本文定义的变量的化合物。这些化合物可用作测定生物活性肽序列的研究工具，并且也可用作药物，其中一些可用于预防或控制血小板血栓的形成，一些化合物可用作中间体。

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