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1. 发明授权

US06369060B1 Indoline derivatives useful as 5-HT-2C receptor antagonists 失效
标题翻译：可用作5-HT-2C受体拮抗剂的二氢吲哚衍生物
公开(公告)号：US06369060B1
公开(公告)日：2002-04-09
申请号：US09202780
申请日：1998-12-21
申请人： Steven Mark Bromidge , Ian Thomson Forbes
发明人： Steven Mark Bromidge , Ian Thomson Forbes
IPC分类号： A61K31501
CPC分类号： C07D401/14
摘要： The invention relates to compounds of formula (I) or a salt thereof wherein X is CH or N; R1 is hydrogen or C1-6 alkyl; R2 and R3 groups are independently C1-6 alkyl, or trifluoromethyl, having pharmacological activity, processes for their preparation, compositions containing them and to their use in the treatment of CNS disorders such as anxiety.
摘要翻译：本发明涉及式（I）化合物或其盐，其中X是CH或N; R1是氢或C1-6烷基; R 2和R 3基团独立地为具有药理学活性的C 1-6烷基或三氟甲基，其制备方法，含有它们的组合物及其在治疗CNS疾病如焦虑症中的应用。

2. 发明授权

US06350744B1 Compounds having cytokine inhibitory activity 失效
公开(公告)号：US06350744B1
公开(公告)日：2002-02-26
申请号：US09433247
申请日：1999-11-04
申请人： David A. Claremon , Gerald S. Ponticello
发明人： David A. Claremon , Gerald S. Ponticello
IPC分类号： A61K31501
CPC分类号： C07D401/14 , C07D401/04 , C07D403/04
摘要： There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.

3. 发明授权

US06800628B2 N-substituted 4-((-4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties 有权
标题翻译：具有胃动力学性质的N-取代的4 - （（ - 4'-氨基苯甲酰基） - 氧基甲基） - 哌啶
公开(公告)号：US06800628B2
公开(公告)日：2004-10-05
申请号：US10299317
申请日：2002-11-19
申请人： Jean-Paul René Marie Bosmans , Christopher John Love , Marc Gustaaf Celine Verdonck , Joannes Adrianus Jacobus Schuurkes
发明人： Jean-Paul René Marie Bosmans , Christopher John Love , Marc Gustaaf Celine Verdonck , Joannes Adrianus Jacobus Schuurkes
IPC分类号： A61K31501
CPC分类号： C07D401/06 , C07D211/22 , C07D401/12 , C07D405/12 , C07D405/14 , C07D417/14
摘要： This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-26alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R4, —Alk—NR5R6, 1-R6-4-piperidinyl, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar—, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, Ar or Het2; X is O, S, SO2 or NR8; said R8 being hydrogen, C1-6alkyl or Ar; R9 is hydrogen, C1-6alkyl, C3-6cyclo-alkyl, Ar, ArC1-6alkyl, di(Ar)methyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, C1-6alkyl or Ar; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar or ArC1-6alkyl, or R11 and R12 combined with the nitrogen atom bearing R11 and R12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：本发明涉及配制N-氧化物形式的化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1为C 1-6烷氧基，C 2-6烯氧基或C 2-6-26炔氧基; R 2是氢或C 1-6烷氧基，或者当R 1和R 2一起可以形成下式的二价基团时，其中在所述二价基团中，一个或两个氢原子可以被C 1-6烷基取代，R 3是氢或卤素; L是C3-6环烷基，C5-6环烷酮，任选被芳基取代的C 2-6链烯基，或L是式-Alk-R 4，-Alk-NR 5 R 6，1-R 6 其中每个Alk为C1（= O）-R9，-Alk-YC（= O）-NR11R12，其中每个Alk为C1 -12烷二基; R 4是氢，C 1-6烷基磺酰基氨基，C 3-6环烷基，C 5-6环烷酮，Ar-，二（Ar）甲基，Ar-氧基或Het 1。 R 5是氢或C 1-6烷基; R 6是Het 2; R 7是氢，C 1-6烷基，羟基C 1-6烷基，C 3-6环烷基，Ar或Het 2; X是O，S，SO 2或NR 8; 所述R 8为氢，C 1-6烷基或Ar; R 9是氢，C 1-6烷基，C 3-6环烷基，Ar，ArC 1-6烷基，二（Ar）甲基，C 1-6烷氧基或羟基; Y是NR 10或直接键; 所述R 10为氢，C 1-6烷基或Ar; R 11和R 12各自独立地为氢，C 1-6烷基，C 3-6环烷基，Ar或ArC 1-6烷基，或R 11和R 12与带有R 11和R 10的氮原子结合可以形成任选被C

4. 发明授权

US06265407B1 Angiogenesis inhibiting thiadiazolyl pyridazine derivatives 失效
标题翻译：血管发生抑制噻二唑基哒嗪衍生物
公开(公告)号：US06265407B1
公开(公告)日：2001-07-24
申请号：US09446495
申请日：2000-08-14
申请人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
发明人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
IPC分类号： A61K31501
CPC分类号： C07D417/04 , C07D417/14
摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7—Alk1—X—, NR7—Alk1—X—Alk2—, O—Alk1—X—, O—Alk1—X—Alk2— or S—Alk1—X—; wherein X is a direct bond, —O—, —S—, C═O, —NR8— or Het2; R7 is hydrogen, C1-6alkyl or Ar2methyl; R8 is hydrogen, C1-6alkyl or Ar2methyl; Alk1 is C1-6alkanediyl; Alk2 is C1-4alkanediyl; Ar1 and Ar2 are optionally substituted phenyl; phenyl; Het1 and Het2 are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar1，Ar1-NH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; R4，R5和R6各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 或当R 4和R 5彼此相邻时，它们可以一起形成式-CH = CH-CH = CH-的基团; A是式NR7，NR7-Alk1-X，NR7-Alk1-X-Alk2-，O-Alk1-X，O-Alk1-X-Alk2-或S-Alk1-X-2的二价基; 其中X是直接键，-O - ， - S - ，C = O，-NR 8 - 或Het 2; R 7为氢，C 1-6烷基或Ar 2甲基; R8是氢，C1-6烷基或Ar2甲基; Alk1是C1-6烷二基; Alk2是C1-4烷二基; Ar1和Ar2是任选取代的苯基; 苯基; Het1和Het2是任选取代的杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

5. 发明授权

US06670362B2 Pyridazine endothelin antagonists 失效
标题翻译：哒嗪内皮素拮抗剂
公开(公告)号：US06670362B2
公开(公告)日：2003-12-30
申请号：US09951019
申请日：2001-09-12
申请人： Bernard Joseph Banks , Anthony Logan Chubb , Douglas James Critcher , James John Eshelby , Darren John Schulz
发明人： Bernard Joseph Banks , Anthony Logan Chubb , Douglas James Critcher , James John Eshelby , Darren John Schulz
IPC分类号： A61K31501
CPC分类号： C07D403/04
摘要： Compounds of formula (I), pharmaceutical formulations thereof and the use of such compounds for treating endothelin mediated diseases or conditions are described herein. The compounds of the present invention have affinity for endothelin receptors, are selective for ETA over ETB, and thus are useful in the treatment of conditions mediated by endothelin.
摘要翻译：本文描述了式（I）化合物，其药物制剂和这些化合物用于治疗内皮素介导的疾病或病症的用途。本发明的化合物对内皮素受体具有亲和力，对ETB具有选择性，因此是有用的在治疗由内皮素介导的病症。

6. 发明授权

US06602873B2 Angiogenesis inhibiting thiadiazolyl pyridazine derivatives 失效
标题翻译：血管发生抑制噻二唑基哒嗪衍生物
公开(公告)号：US06602873B2
公开(公告)日：2003-08-05
申请号：US09864594
申请日：2001-05-24
申请人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
发明人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
IPC分类号： A61K31501
CPC分类号： C07D417/04 , C07D417/14
摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7-Alk1-X-, NR7-Alk1-X-Alk2-, O-Alk1-X-, O-Alk1-X-Alk2- or S-Alk1-X-; wherein X is a direct bond, —O—, —S—, C═O, —NR8— or Het2; R7 is hydrogen, C1-6alkyl or Ar2methyl; R8 is hydrogen, C1-6alkyl or Ar2methyl; Alk1 is C1-6alkanediyl; Alk2 is C1-4alkanediyl; Ar1 and Ar2 are optionally substituted phenyl; phenyl; Het1 and Het2 are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar1，Ar1-NH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; R4，R5和R6各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 或当R 4和R 5彼此相邻时，它们可以一起形成式-CH = CH-CH = CH-的基团; A是式NR7，NR7-Alk1-X，NR7-Alk1-X-Alk2-，O-Alk1-X，O-Alk1-X-Alk2-或S-Alk1-X-2的二价基; 其中X是直接键，-O - ， - S - ，C = O，-NR 8 - 或Het 2; R 7为氢，C 1-6烷基或Ar 2甲基; R8是氢，C1-6烷基或Ar2甲基; Alk1是C1-6烷二基; Alk2是C1-4烷二基; Ar1和Ar2是任选取代的苯基; 苯基; Het1和Het2是任选取代的杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

7. 发明授权

US06268365B1 Src family SH2 domain inhibitors 有权
标题翻译： Src家族SH2结构域抑制剂
公开(公告)号：US06268365B1
公开(公告)日：2001-07-31
申请号：US09438629
申请日：1999-11-12
申请人： Rajashekhar Betageri , Pierre L. Beaulieu , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , Usha Patel , John R. Proudfoot , Mario Cardozo
发明人： Rajashekhar Betageri , Pierre L. Beaulieu , Jean-Marie Ferland , Montse Llinas-Brunet , Neil Moss , Usha Patel , John R. Proudfoot , Mario Cardozo
IPC分类号： A61K31501
CPC分类号： C07D213/75 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of formula (1): wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.
摘要翻译：本发明涉及式（1）的化合物：其中环a，A，B，C，D，E，R和Q在本文中定义。这些化合物具有破坏具有一个或多个SH2结构域及其天然配体的调节蛋白之间相互作用的能力。

8. 发明授权

US06177428B1 Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses 失效
公开(公告)号：US06177428B1
公开(公告)日：2001-01-23
申请号：US09247321
申请日：1999-02-10
申请人： David S. Garvey , Inigo Saenz de Tejada
发明人： David S. Garvey , Inigo Saenz de Tejada
IPC分类号： A61K31501
CPC分类号： C07D487/04 , C07D405/14
摘要： Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.

9. 发明授权

US06579879B2 Pyridazinone aldose reductase inhibitors 失效
公开(公告)号：US06579879B2
公开(公告)日：2003-06-17
申请号：US10104664
申请日：2002-03-21
申请人： Banavara L. Mylari
发明人： Banavara L. Mylari
IPC分类号： A61K31501
CPC分类号： C07D409/12 , C07D307/82 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/04 , C07D495/04
摘要： The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals. This invention also relates to other combinations with the ARIs of this invention, including combinations with adendsine agonists; NHE-1 inhibitors; glycogen phosphorylase inhibitors; selective serotonin reuptake inhibitors; GABA agonists; antihypertensive agents; 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors; phosphodiesterase-5 inhibitors; and to glucose lowering agents.

10. 发明授权

US06451797B1 Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US06451797B1
公开(公告)日：2002-09-17
申请号：US09514935
申请日：2000-02-28
申请人： Joseph A. Kozlowski , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice
发明人： Joseph A. Kozlowski , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice
IPC分类号： A61K31501
CPC分类号： C07D401/12 , C07D211/58 , C07D405/14 , C07D409/12
摘要： Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) wherein wherein one of Y and Z is —N— and the other is —N— or —CH—; X is —O—, —S—, —SO—, —SO2— or —CH2—; Q is R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R1, R2 and R3 are H or alkyl; R4 is alkyl, cyclolalkyl or R5 is H, alkyl, —C(O)alkyl, arylcarbonyl, —SO2alkyl, aryl-sulfonyl —C(O)Oalkyl, aryloxycarbonyl, —C(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted; R6 is H or alkyl; and R7 is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of treatment are also disclosed.
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代的哌啶化合物的杂环衍生物（包括所有异构体，盐和溶剂合物），其中Y和Z之一是-N-，另一个是-N-或 -CH-; X是-O - ， - S-，-SO-，-SO 2 - 或-CH 2 - ; Q是R是烷基，环烷基，任选取代的芳基或杂芳基; R 1和R 2是H或烷基; R 4 是烷基，环烷基或R 5是H，烷基，-C（O）烷基，芳基羰基，-SO 2烷基，芳基 - 磺酰基-C（O）O烷基，芳氧基羰基，-C（O）NH-烷基或芳基 - 氨基羰基，部分任选被取代; R 6是H或烷基; 和R 7是H，烷基，羟基烷基或烷氧基烷基; 是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和治疗方法。

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