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1. 发明授权

US5889058A Peptidyl derivatives 失效
标题翻译：肽基衍生物
公开(公告)号：US5889058A
公开(公告)日：1999-03-30
申请号：US335957
申请日：1994-11-03
申请人： John Robert Porter , Thomas Andrew Millican , John Richard Morphy , Nigel Robert Arnold Beeley
发明人： John Robert Porter , Thomas Andrew Millican , John Richard Morphy , Nigel Robert Arnold Beeley
IPC分类号： A61K31/19 , A61K31/195 , C07C229/04 , C07C229/24 , C07C229/28 , C07C233/05 , C07C233/08 , C07C237/06
CPC分类号： A61K31/195
摘要： Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastases. ##STR1##
摘要翻译：其中R代表-CONHOH，羧基（-CO 2 H）或酯化的羧基;式（I）化合物的使用方法; R 1表示氢原子或任选取代的烷基，烯基，芳基，芳烷基，杂芳烷基或杂芳硫基烷基; R2表示任选取代的苯乙基，苯基丙基或苯基丁基; R3表示氢原子或烷基; R4表示氢原子或烷基; R5表示任选被一个或多个-O-或-S-原子或-N（R 7） - 基团（其中R 7是氢原子或C 1-6烷基）间隔的任选取代的烷基或烯基; X表示氨基（-NH 2）或取代的氨基，羟基或取代的羟基; 及其盐，溶剂化物和水合物。化合物是金属蛋白酶抑制剂，特别是具有选择性明胶酶作用，并且可用于治疗癌症以控制肿瘤转移的发展。（一）

2. 发明授权

US07807686B2 2-(4-oxo-4H-quinazolin-3-yl)acetamides and their use as vasopressin V3 antagonists 有权
标题翻译： 2-（4-氧代-4H-喹唑啉-3-基）乙酰胺及其作为血管加压素V3拮抗剂的用途
公开(公告)号：US07807686B2
公开(公告)日：2010-10-05
申请号：US11908221
申请日：2006-03-10
申请人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Hoc , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
发明人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Hoc , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
IPC分类号： A61K31/517
CPC分类号： C07D409/04 , C07D239/91 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04
摘要： The present invention relates to 2-(4-oxo4H-quinazolin-3-yl) acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
摘要翻译：本发明涉及式（I）的2-（4-氧代-4-喹唑啉-3-基）乙酰胺衍生物及其作为加压素V3拮抗剂的用途，特别是用于治疗抑郁症。

3. 发明授权

US07126027B2 N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives 失效
标题翻译： N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物
公开(公告)号：US07126027B2
公开(公告)日：2006-10-24
申请号：US10484410
申请日：2002-07-11
申请人： John Richard Morphy , Zoran Rankovoc
发明人： John Richard Morphy , Zoran Rankovoc
IPC分类号： C07C233/65 , A61K31/165
CPC分类号： C07D333/16 , C07C235/50 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18
摘要： The present invention relates to N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives having the general formula I wherein n is 0, 1, 2 or 3; R1 and R2 are independently H, (C1-4)alkyl or (C1-4)alkyloxy; R3 is (C3-8)alkyl, (C4-7)cycloalkyl, (C4-7)cycloalkyl (C1-3)alkyl, (C6-12)aryl(C1-3)alkyl (wherein the aryl moiety is optionally substituted with 1–3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, halogen, trifluoromethyl and methoxycarbonyl), or (C4-9)heteroaryl(C1-3)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives in the treatment of disorders or conditions which are responsive to inhibition of the GlyT-2 transporter, such as muscle spasticity, epilepsy and, particularly, acute, chronic and neuropathic pain.
摘要翻译：本发明涉及具有通式I的N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物，其中n为0,1,2或3; R 1和R 2独立地是H，（C 1-4烷基）烷基或（C 1-4））烷氧基; R 3是（C 3-8）烷基，（C 1-4-7）环烷基，（C 1-4 - （C 1-3）烷基，（C 6-12）芳基（C 1-3-2烷基）烷基（其中芳基部分任选被1-3个选自（C 1-4烷基）烷基，（C 1-4 - 烷基）烷氧基，卤素，三氟甲基和甲氧基羰基的取代基取代）或（C 1-4 - ）杂芳基（C 1-3-3烷基）烷基; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物用于治疗对抑制GlyT-2转运蛋白有反应的病症或病症的用途，例如肌肉痉挛，癫痫，特别是急性，慢性和神经性疼痛。

4. 发明申请

US20080214553A1 2-(4-Oxo-4H-Quinazolin-3-Yl) Acetamides and Their Use as Vasopressin V3 Antagonists 有权
标题翻译： 2-（4-氧代-4H-喹唑啉-3-基）乙酰胺及其作为加压素V3拮抗剂的用途
公开(公告)号：US20080214553A1
公开(公告)日：2008-09-04
申请号：US11908221
申请日：2006-03-10
申请人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Ho , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
发明人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Ho , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
IPC分类号： A61K31/517 , C07D403/02
CPC分类号： C07D409/04 , C07D239/91 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04
摘要： The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
摘要翻译：本发明涉及式（I）的2-（4-氧代-4-喹唑啉-3-基）乙酰胺衍生物及其作为加压素V3拮抗剂的用途，特别是用于治疗抑郁症。

5. 发明授权

US07084154B2 2-(aminomethyl) arylamide analgesics 有权
标题翻译： 2-（氨基甲基）芳基酰胺镇痛药
公开(公告)号：US07084154B2
公开(公告)日：2006-08-01
申请号：US10364039
申请日：2003-02-11
申请人： Koc-Kan Ho , John J. Baldwin , Adolph C. Bohnstedt , Steven G. Kultgen , Edward McDonald , Tao Guo , John Richard Morphy , Zoran Rankovic , Robert Horlick , Kenneth C. Appell
发明人： Koc-Kan Ho , John J. Baldwin , Adolph C. Bohnstedt , Steven G. Kultgen , Edward McDonald , Tao Guo , John Richard Morphy , Zoran Rankovic , Robert Horlick , Kenneth C. Appell
IPC分类号： A61P25/00 , A61K31/44 , C07D471/02
CPC分类号： C07C237/30 , C07C237/32 , C07C311/08 , C07C311/37 , C07C323/42 , C07C2602/10 , C07C2602/12 , C07D207/08 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/22 , C07D213/81 , C07D217/04 , C07D223/16 , C07D295/155 , C07D401/06 , C07D401/12 , C07D471/04
摘要： A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed. The genus is represented by the formula I: A representative example is:
摘要翻译：公开了可用作止痛剂的2-（氨基甲基）芳基酰胺的化学属。该属由式I表示：代表性的例子是：

6. 发明授权

US06486354B1 Solid phase supports 失效
标题翻译：固相支持
公开(公告)号：US06486354B1
公开(公告)日：2002-11-26
申请号：US09485613
申请日：2000-04-17
申请人： David Gani , Friedrich Erich Karl Kroll , Michael John Plater , John Richard Morphy , David Rees
发明人： David Gani , Friedrich Erich Karl Kroll , Michael John Plater , John Richard Morphy , David Rees
IPC分类号： C07C31500
CPC分类号： G01N33/545 , C07K1/042 , C08F8/30 , C08F8/34
摘要： Embodiments of the present invention generally relate to carrying out organic chemistry on solid supports comprising derivatised functionalities, methods for synthesizing said supports, methods for synthesizing compounds comprising amine groups or N-containing heterocycles using said solid supports, intermediate compounds linked to said supports and uses thereof.
摘要翻译：本发明的实施方案通常涉及在包含衍生化官能团的固体支持物上进行有机化学，用于合成所述载体的方法，使用所述固体支持物合成包含胺基或含N杂环的化合物的方法，与所述载体连接的中间体化合物和用途其中。

7. 发明授权

US5714491A Peptidyl derivatives as metalloproteinase inhibitors 失效
标题翻译：肽基衍生物作为金属蛋白酶抑制剂
公开(公告)号：US5714491A
公开(公告)日：1998-02-03
申请号：US356315
申请日：1995-02-06
申请人： John Richard Morphy , Thomas Andrew Millican
发明人： John Richard Morphy , Thomas Andrew Millican
IPC分类号： A61K31/66 , A61K31/19 , A61K41/00 , A61P35/00 , C07C233/45 , C07C237/04 , C07C259/06 , C07C317/50 , C07C323/60 , C07C323/61 , C07D285/38 , C07F9/38 , C07F9/40 , C07C259/04 , A61K31/505
CPC分类号： C07D285/38 , A61K41/00 , C07C317/50 , C07C323/60 , C07C323/61 , C07C2101/02
摘要： Peptidyl derivatives are disclosed that are orally active metalloproteinase inhibitors. The peptidyl derivatives have a selective gelatinase action, have a long duration of action, and are useful in the prophylaxis or treatment of diseases or disorders in which stromelysis, collagenase or gelatinase have a role, for example, in the treatment of cancer to control the development of tumor metastases.
摘要翻译： PCT No.PCT / GB94 / 00895 Sec。 371日期：1995年2月6日 102（e）日期1995年2月6日PCT 1994年4月27日PCT PCT。公开号WO94 / 25434 日期：1994年11月10日公开了作为口服活性金属蛋白酶抑制剂的肽基衍生物。肽基衍生物具有选择性明胶酶作用，具有长的作用持续时间，并且可用于预防或治疗其中溶质，胶原酶或明胶酶具有作用的疾病或病症，例如用于治疗癌症以控制肿瘤转移的发展。

8. 发明授权

US07960365B2 Compounds with medicinal effects due to interaction with the glucocorticoid receptor 有权
标题翻译：与糖皮质激素受体相互作用具有药效的化合物
公开(公告)号：US07960365B2
公开(公告)日：2011-06-14
申请号：US11641524
申请日：2006-12-19
申请人： Niall Morton Hamilton , Simon James Anthony Grove , Michael John Kiczun , John Richard Morphy , Brad Sherborne , Peter Thomas Albert Littlewood , Angus Richard Brown , Celia Kingsbury , Michael Ohhlmeyer , Koc-Kan Ho , Steven G. Kultgen
发明人： Niall Morton Hamilton , Simon James Anthony Grove , Michael John Kiczun , John Richard Morphy , Brad Sherborne , Peter Thomas Albert Littlewood , Angus Richard Brown , Celia Kingsbury , Michael Ohhlmeyer , Koc-Kan Ho , Steven G. Kultgen
IPC分类号： C07D401/00 , A01N57/00
CPC分类号： C07C311/17 , C07C311/29 , C07D213/61 , C07D261/10 , C07D307/64 , C07D333/34 , C07D401/12
摘要： The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.
摘要翻译：本发明提供具有式I结构的化合物，其中：X是碳原子或氮原子; Ar是苯基或杂芳环; R1是氢，卤素，CN或（1C-4C）烷基; R2是氢，卤素或任选氟化的（1C-3C）烷氧基; 任选卤代（1C-4C）烷氧基，任选卤代芳基（1C-4C）烷氧基，任选卤代（1C-4C）烯基或羟甲基; R4是氢，卤素，任选卤代（1C-4C）烷氧基或任选的卤代芳基（1C-4C）烷氧基; R6是氢，苄基，任选被一个或多个卤素或（1C-4C）烷基取代，或R6任选被卤代（1C-4C）烷基取代; 每个R 7独立地是氢，卤素，任选卤代（1C-4C）烷基或任选卤代（1C-4C）烷氧基及其药学上合适的酸加成盐，用作糖皮质激素受体调节剂，特别是用于治疗中枢神经系统疾病。

9. 发明授权

US07906504B2 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives 有权
标题翻译： 2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物
公开(公告)号：US07906504B2
公开(公告)日：2011-03-15
申请号：US11852737
申请日：2007-09-10
申请人： Jeffrey Letourneau , Jui-Hsiang Chan , Patrick Jokiel , Michael Ohlmeyer , Irina Neagu , Christopher Riviello , John Richard Morphy , Susan Elizabeth Napier , Koc-Kan Ho
发明人： Jeffrey Letourneau , Jui-Hsiang Chan , Patrick Jokiel , Michael Ohlmeyer , Irina Neagu , Christopher Riviello , John Richard Morphy , Susan Elizabeth Napier , Koc-Kan Ho
IPC分类号： C07D217/24 , A61K31/472
CPC分类号： C07D217/24 , C07D401/12
摘要： Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.
摘要翻译：本文公开了式I的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物或其药学上可接受的盐或溶剂合物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义。还公开了包含根据本发明的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物及其在治疗中的用途的药物组合物。

10. 发明授权

US07893088B2 6-substituted isoquinoline derivatives 有权
标题翻译： 6-取代的异喹啉衍生物
公开(公告)号：US07893088B2
公开(公告)日：2011-02-22
申请号：US11839703
申请日：2007-08-16
申请人： Peter Christopher Ray , Steven Laats , John Richard Morphy , Brad Sherborne
发明人： Peter Christopher Ray , Steven Laats , John Richard Morphy , Brad Sherborne
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D217/22 , C07D217/24
摘要： The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
摘要翻译：本发明涉及具有通式I的6-取代的异喹啉衍生物，其中X是O，S或NH; Y是OH或NH 2; m为0,1或2; n为0或1; o为0或1; 当Y为NH 2时，R 1为H; 或者当Y为OH时，R 1为H，（C 1-4）烷基或卤素; R2和R3独立地是H，（C1-4）烷基或卤素; R4是H或（C 1-6）烷基，任选地被卤素，（C 3-7）环烷基，（C 6-10）芳基或饱和的5-或6-元杂环包含1-3个独立地选自O， S和N，（C 6-10）芳基和杂环任选被（C 1-4）烷基，（C 1-4）烷氧基或卤素取代; R5是H或（C1-4）烷基; 或其药学上可接受的盐，条件是其中X为O，Y为OH，n为0且m + o = 2的式I化合物排除于包含该化合物的药物组合物中，以及使用的所述6-取代的异喹啉衍生物用于制备用于治疗ROCK-1相关疾病如青光眼，高血压和动脉粥样硬化的药物。

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