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1. 发明申请

WO2003024943A3 ARYL DERIVATIVES FOR THE TREATMENT OF DIABETES, HYPERLIPIDEMIA, HYPERCHOLESTEROLEMIA AND ATHEROSCLEROSIS 审中-公开
公开(公告)号：WO2003024943A3
公开(公告)日：2003-03-27
申请号：PCT/US2002/030017
申请日：2002-09-20
申请人： ARYX THERAPEUTICS , DRUZGALA, Pascal , MILNER, Peter, G. , PFISTER, Jurg, R.
发明人： DRUZGALA, Pascal , MILNER, Peter, G. , PFISTER, Jurg, R.
IPC分类号： C07D277/34
摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

2. 发明申请

WO0238557A2 NOVEL COMPOUND FOR TREATMENT OF CARDIAC ARRHYTHMIA, SYNTHESIS AND METHODS OF USE 审中-公开
标题翻译：治疗心脑血管病的新型化合物，合成和使用方法
公开(公告)号：WO0238557A2
公开(公告)日：2002-05-16
申请号：PCT/US0131305
申请日：2001-10-04
申请人： ARYX THERAPEUTICS , DRUZGALA PASCAL , MILNER PETER G
发明人： DRUZGALA PASCAL , MILNER PETER G
IPC分类号： A61K31/343 , A61K31/36 , A61K31/381 , A61K31/405 , A61P9/06 , C07D209/12 , C07D209/18 , C07D307/00 , C07D307/80 , C07D333/54 , C07D333/60
CPC分类号： C07D307/80
摘要： The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
摘要翻译：本发明涉及用于治疗心律失常的新化合物和包含该化合物的组合物。本发明还涉及制备新化合物的方法。新化合物是胺碘酮的快速代谢类似物，其具有被代谢为较低亲油性化合物的独特且有利的特征。新化合物可用于治疗危及生命的室性快速性心律失常，特别是在患有充血性心力衰竭（CHF）的患者中。该产品还可以为室性心律失常和室上性心律失常提供有效的管理，包括心房颤动和涉及辅助途径的进入性快速性心律失常。

3. 发明申请

WO2001093849A3 TREATMENT OF GASTROESOPHAGEAL REFLUX DISEASE USING PIPERIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2001093849A3
公开(公告)日：2001-12-13
申请号：PCT/US2001/018365
申请日：2001-06-07
申请人： ARYX THERAPEUTICS , DRUZGALA, Pascal , MILNER, Peter, G. , PFISTER, Jurg , BECKER, Cyrus
发明人： DRUZGALA, Pascal , MILNER, Peter, G. , PFISTER, Jurg , BECKER, Cyrus
IPC分类号： A61K31/4468
摘要： The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate. Said compounds are also useful in Alzheimer's disease, schizophrenia, mania, obsessive-compulsive disorder, depression and anxiety, essential hypertension and sleep disorders.

4. 发明申请

WO0117614A2 METHODS AND COMPOSITIONS FOR PRODUCING LONG LASTING ANTINEOPLASTIC AGENTS 审中-公开
标题翻译：用于生产长期激素抗生素的方法和组合物
公开(公告)号：WO0117614A2
公开(公告)日：2001-03-15
申请号：PCT/IB0001427
申请日：2000-09-07
申请人： CONJUCHEM INC , BRIDON DOMINIQUE P , LEGER ROGER , HUANG XICAI , MILNER PETER G , SMITH DAMON , EZRIN ALAN M
发明人： BRIDON DOMINIQUE P , LEGER ROGER , HUANG XICAI , MILNER PETER G , SMITH DAMON , EZRIN ALAN M
IPC分类号： C07D473/10 , A61K9/00 , A61K9/12 , A61K9/14 , A61K31/138 , A61K31/192 , A61K31/401 , A61K31/4015 , A61K31/4025 , A61K31/407 , A61K31/437 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/519 , A61K31/522 , A61K38/00 , A61K38/22 , A61K38/55 , A61K47/42 , A61K47/48 , A61P3/10 , A61P5/10 , A61P5/14 , A61P5/16 , A61P5/38 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P25/00 , A61P25/04 , A61P25/24 , A61P29/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/06 , A61P37/08 , A61P41/00 , A61P43/00 , C07D207/452 , C07D401/12 , C07D401/14 , C07D405/12 , C07D475/08 , C07D487/14 , C07D519/04 , A61K31/135 , A61K31/235 , A61K31/33 , A61K31/4045
CPC分类号： A61K9/0075 , A61K31/704 , A61K47/643
摘要： Derivatives of antineoplastic agents are prepared. The derivatives are capable of forming covalent bonds with one or more blood components, preferably a mobile blood component.
摘要翻译：制备抗肿瘤药物的衍生物。衍生物能够与一种或多种血液成分，优选移动血液成分形成共价键。

5. 发明申请

WO0238557A9 BENZOYLBENZOFURANE DERIVATIVES FOR TREATMENT OF CARDIAC ARRHYTHMIA 审中-公开
标题翻译：用于治疗心脏病的苯并噻吩类衍生物
公开(公告)号：WO0238557A9
公开(公告)日：2003-09-18
申请号：PCT/US0131305
申请日：2001-10-04
申请人： ARYX THERAPEUTICS , DRUZGALA PASCAL , MILNER PETER G
发明人： DRUZGALA PASCAL , MILNER PETER G
IPC分类号： A61K31/343 , A61K31/36 , A61K31/381 , A61K31/405 , A61P9/06 , C07D209/12 , C07D209/18 , C07D307/00 , C07D307/80 , C07D333/54 , C07D333/60
CPC分类号： C07D307/80
摘要： The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.
摘要翻译：本发明涉及用于治疗心律失常的新化合物和包含该化合物的组合物。本发明还涉及制备新化合物的方法。新化合物是胺碘酮的快速代谢类似物，其具有被代谢为较低亲油性化合物的独特且有利的特征。新化合物可用于治疗危及生命的室性快速性心律失常，特别是在患有充血性心力衰竭（CHF）的患者中。该产品还可以为室性心律失常和室上性心律失常提供有效的管理，包括心房颤动和涉及辅助途径的进入性快速性心律失常。

6. 发明申请

WO0193849A2 MATERIALS AND METHODS FOR THE TREATMENT OF GASTROESOPHAGEAL REFLUX DISEASE 审中-公开
标题翻译：治疗胃食管反流病的材料与方法
公开(公告)号：WO0193849A2
公开(公告)日：2001-12-13
申请号：PCT/US0118365
申请日：2001-06-07
申请人： ARYX THERAPEUTICS , DRUZGALA PASCAL , MILNER PETER G , PFISTER JUERG , BECKER CYRUS
发明人： DRUZGALA PASCAL , MILNER PETER G , PFISTER JURG , BECKER CYRUS
IPC分类号： A61K31/4468 , A61P1/00 , A61P1/04 , A61P1/14 , A61P9/12 , A61P25/00 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D211/46 , C07D211/58 , A61K31/00
CPC分类号： C07D211/58 , A61K31/4468 , C07D211/46
摘要： The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.
摘要翻译：本发明提供了用于安全有效地治疗胃食管反流和相关病症的新型化合物和组合物。在优选的实施方案中，本发明的组合物包含酯化的西沙必利衍生物。这些组合物在治疗胃食管反流疾病中具有有效的活性，并且显着减少与西沙必利施用相关的不良反应。这些不良影响包括但不限于腹泻，腹部绞痛和血压升高和心率升高。

7. 发明申请

WO0069900A9 PROTECTION OF ENDOGENOUS THERAPEUTIC PEPTIDES FROM PEPTIDASE ACTIVITY THROUGH CONJUGATION TO BLOOD COMPONENTS 审中-公开
标题翻译：通过与血液成分结合从肽活性中保护内源性治疗肽
公开(公告)号：WO0069900A9
公开(公告)日：2002-07-04
申请号：PCT/US0013576
申请日：2000-05-17
申请人： CONJUCHEM INC , BRIDON DOMINIQUE P , EZRIN ALAN M , MILNER PETER G , HOLMES DARREN L , THIBAUDEAU KAREN
发明人： BRIDON DOMINIQUE P , EZRIN ALAN M , MILNER PETER G , HOLMES DARREN L , THIBAUDEAU KAREN
IPC分类号： A61K47/42 , A61K38/00 , A61K38/02 , A61K47/48 , A61P1/18 , A61P5/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07K1/107 , C07K1/113 , C07K1/14 , C07K2/00 , C07K7/00 , C07K14/00 , C07K14/16 , C07K14/465 , C07K14/575 , C07K14/605 , C07K14/645 , C07K14/135 , C07K14/46 , C07K14/655 , C12N9/68
CPC分类号： C07K14/645 , A61K38/00 , A61K47/62 , C07K14/00 , C07K14/005 , C07K14/465 , C07K14/575 , C07K14/57545 , C07K14/605 , C07K14/62 , C07K14/76 , C07K2319/31 , C12N2740/16122
摘要： A method for protecting a peptide from peptidase activity in vivo , the peptide being composed of between 2 and 50 amino acids and having a C-terminus and an N-terminus and a C-terminus amino acid and an N-terminus amino acid is described. In the first step of the method, the peptide is modified by attaching a reactive group to the C-terminus amino acid, to the N-terminus amino acid, or to an amino acid located between the N-terminus and the C-terminus, such that the modified peptide is capable of forming a covalent bond in vivo with a reactive functionality on a blood component. In the next step, a covalent bond is formed between the reactive group and a reactive functionality on a blood component to form a peptide-blood component conjugate, thereby protecting said peptide from peptidase activity. The final step of the method involves the analyzing of the stability of the peptide-blood component conjugate to assess the protection of the peptide from peptidase activity.
摘要翻译：描述了一种在体内保护肽免受肽酶活性的方法，所述肽由2-50个氨基酸组成且具有C末端和N末端以及C末端氨基酸和N-末端氨基酸。在该方法的第一步中，通过将反应性基团连接到C末端氨基酸，N末端氨基酸或位于N末端和C末端之间的氨基酸来修饰肽，使得修饰的肽能够在体内与血液成分上的反应性官能团形成共价键。在下一步骤中，在反应性基团和血液成分上的反应性官能团之间形成共价键以形成肽 - 血液成分缀合物，从而保护所述肽免受肽酶活性。该方法的最后步骤包括分析肽 - 血液成分缀合物的稳定性，以评估肽对肽酶活性的保护。

8. 发明申请

WO0129018A3 NOVEL ENANTIOMERIC COMPOUNDS FOR TREATMENT OF CARDIAC ARRHYTHMIAS AND METHODS OF USE 审中-公开
标题翻译：用于治疗心脑血管疾病的新型光学化合物及其使用方法
公开(公告)号：WO0129018A3
公开(公告)日：2001-11-29
申请号：PCT/US0028636
申请日：2000-10-13
申请人： ARYX THERAPEUTICS , DRUZGALA PASCAL , MILNER PETER G
发明人： DRUZGALA PASCAL , MILNER PETER G
IPC分类号： C07D307/80 , A61K31/343 , A61P9/04 , A61P9/06 , A61P9/10 , C07D307/54
CPC分类号： C07D307/80
摘要： The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.
摘要翻译：本发明涉及新颖的对映异构体纯的化合物和包含该化合物的组合物，用于治疗心律失常。本发明还涉及制备和纯化化合物的方法。与化合物的外消旋混合物相比，对映异构体纯化的化合物和这些化合物的组合物显示出意想不到的和有利的特征，例如显着优异的降低或抑制心室过早搏动的能力。

9. 发明申请

WO9948536A3 DELIVERY OF LONG LASTING THERAPEUTIC AGENTS BY FORMING COVALENT ATTACHMENTS IN VIVO 审中-公开
标题翻译：通过在体检中形成共同的附件来提供长期的治疗药物
公开(公告)号：WO9948536A3
公开(公告)日：2001-05-17
申请号：PCT/US9906344
申请日：1999-03-23
申请人： CONJUCHEM INC , EZRIN ALAN M , MILNER PETER G , BRIDON DOMINIQUE P , HOLMES DARREN L
发明人： EZRIN ALAN M , MILNER PETER G , BRIDON DOMINIQUE P , HOLMES DARREN L
IPC分类号： A61K9/00 , A61K38/00 , A61K45/00 , A61K47/42 , A61K47/48 , A61K51/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/02 , A61P31/18 , A61P35/00 , A61K39/385 , A61K51/04 , A61K51/08
CPC分类号： A61K47/54
摘要： This invention relates to the field of therapeutic agents in medicine. In particular, this invention relates to the field of localized delivery of therapeutic agents wherein the agents are capable of covalently bonding to a site of interest in vivo , to provide increased tissue retention and pharmacodynamic duration of therapeutic benefit for the given drug. In addition, the invention includes the non-specific labeling of fixed blood proteins and tissues with N-Hydroxy-Succinimide (NHS)-drugs and sulfo-NHS drugs, although other reactive groups, which are functional in an aqueous medium such as blood, may also be employed.
摘要翻译：本发明涉及药物治疗剂领域。特别地，本发明涉及治疗剂的局部递送领域，其中所述试剂能够在体内共价键合到感兴趣的位点，以提供增加的组织保留和药效学持续时间以获得治疗益处给药。此外，本发明包括固定血液蛋白质和组织与N-羟基琥珀酰亚胺（NHS） - 药物和磺基-NOS药物的非特异性标记，尽管其它反应性基团在水性介质如血液中起作用，也可以被使用。

10. 发明申请

WO2003031415A1 MIBEFRADIL-BASED COMPOUNDS AS CALCIUM CHANNEL BLOCKERS USEFUL IN THE TREATMENT OF HYPERTENSION AND ANGINA 审中-公开
标题翻译：基于MIBEFRADIL的化合物作为钙通道阻滞剂有效治疗高血压和血管紧张素
公开(公告)号：WO2003031415A1
公开(公告)日：2003-04-17
申请号：PCT/US2002/032562
申请日：2002-10-10
申请人： ARYX THERAPEUTICS , DRUZGALA, Pascal , MILNER, Peter, G. , PFISTER, Jurg, R. , ZHANG, Xiaoming
发明人： DRUZGALA, Pascal , MILNER, Peter, G. , PFISTER, Jurg, R. , ZHANG, Xiaoming
IPC分类号： C07D235/08
CPC分类号： C07D235/14
摘要： The subject invention provides novel calcium channel blockers based upon mibefradil: (I) wherein: X = a bond, (CH 2 ) n , O, S, or O(CH 2 ) n wherein = 1-6; R 1 = C 1-6 alkyl, optionally substituted with OH or NH 2 ; R 2 = F or COOR 5 , wherein R 5 is C 1-6 alkyl, optionally substituted with OH or NH 2 ; R 3 = CH 3 or (CH 2 )„ - COOR 6 , wherein n =1-6 and R 6 is C 1-6 alkyl, optionally substituted with OH or NH 2 ; R 4 = (CH 2 ) n - COR 7 R 8 -(CH 2 ) n -R 10 R 11 or (II) R 7 = 0, NH, or NR 9 , R 8 = optionally substituted aryl or heterocycle, R 9 = C 1-6 alkyl, R 10 = 0, S, SO, S0 2 , NH, NR 12 or N(CH 2 ) m COOR 13 R 11 = aryl of heterocyclyl optionally substituted with (CH 2 ) n, COOR 14 , R 12 = C 1-6 alkyl, optionally substituted with OH or NH 2 , R 13 = C 1-6 alkyl, optionally substituted with OH or NH 2 , R 14 = C 1-6 alkyl, optionally substituted with OH or NH 2 , R 15 = (CH 2 ) n COOR 16 , R 16 = C 1-6 alkyl, optionally substituted with OH or NH 2 , R 17 = not present or COOR 18 wherein R 18 is C 1-6 alkyl, optionally substituted with OH or NH 2 , and wherein n =1-6, useful in the treatment of hypertension, angina pectoris, ischemia, arrhythmias and cardiaq, insufficiency.
摘要翻译：本发明提供了基于mibefradil的新型钙通道阻断剂：（I）其中：X =一个键，（CH 2）s，n，s，O，S或O（CH 2 ） n 其中= 1-6; 任选被OH或NH 2 b取代的C 1 -C 6烷基; 其中R 15是任选被OH取代的C 1-6烷基，其中R 5是C 1-6烷基，或NH 2 ; 或者（CH 2 s）> - COOR 6，其中n = 1-6和 R 6是C 1-6烷基，任选被OH或NH 2 b取代; 4 =（CH 2 ） n 或者（II）R sb> 7 = 0，NH或NR 9 R 8，R 8为任选取代的芳基或杂环，R 9为C 1-6烷基， / sb>烷基，R 11 = 0，S，SO，S 0 ，NH，NR 12 S或N（CH 2）2 sb> n， COOR 14 ，R s 12> = C 6-18烷基，任选被OH或NH b取代， 2，任选被OH或NH，R b取代的烷基，R 15，R 13，任选被OH或NH 2 S 2取代的C 1 -C 6烷基，R 15和R 15独立地是（CH 2） sb>） COOR 16 ，R 16 = C 6-18烷基，任选被OH或NH 2 ，R 17 =不存在或其中R 17为C 16〜 / sb>烷基，任选被OH取代或NH 2 s，其中n = 1-6，可用于治疗高血压，心绞痛，局部缺血，心律失常和心律不齐。

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