公开(公告)号：US20140163032A1

公开(公告)日：2014-06-12

申请号：US14182994

申请日：2014-02-18

申请人： BRADLEY TEEGARDEN ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  HONNAPPA JAYAKUMAR ,  THUY-ANH Tran ,  Sonja Strah-Pleynet ,  Jay Xu

发明人： BRADLEY TEEGARDEN ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  HONNAPPA JAYAKUMAR ,  THUY-ANH Tran ,  Sonja Strah-Pleynet ,  Jay Xu

IPC分类号： C07D207/335 ,  C07D207/34 ,  C07D417/12 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D405/12

CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D207/335 ,  C07D207/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，进行性多灶性脑白质病等。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US5380904A

公开(公告)日：1995-01-10

申请号：US169641

申请日：1993-12-20

申请人： Dennis Chapman ,  Aziz A. Durrani

发明人： Dennis Chapman ,  Aziz A. Durrani

IPC分类号： A61L33/00 ,  C07C43/315 ,  C07F5/00 ,  C07F9/09 ,  C07F9/6584 ,  C07F9/146 ,  A01N1/02 ,  B01J16/00 ,  C07F9/10

CPC分类号： C07F9/65844 ,  A61L33/0082 ,  C07C43/315 ,  C07F5/003 ,  C07F9/091 ,  Y10S128/912

摘要： A compound of formula: ##STR1## in which X.sup.1 is a reactive group that can react to form a covalent bond with a reactive group on the surface of a material to be rendered biocompatible, X.sup.2 is a group --O.sup..crclbar. or a precursor of such a group, n is 2, 3 or 4, Y is a group --N.sup..sym. R.sub.3 A.sup..crclbar. wherein each R, which may be the same or different, is a C.sub.1 -C.sub.4 alkyl group and A.sup..crclbar. is an anion present when X.sup.2 is an electrically neutral group or Y is ##STR2## wherein R.sup.1 together with X.sup.2 forms a direct bond between the nitrogen and the phosphorus atoms.

摘要翻译： 下式的化合物：其中X1是能与反应性基团反应形成与要生物相容的材料的表面上的反应性基团的反应性基团，X 2是基团-O（ - ）或 这种基团的前体，n为2,3或4，Y为-N（+）R 3A（ - ）基团，其中各R可以相同或不同，为C1-C4烷基，A（ - ）是当X2是电中性基团时存在的阴离子或Y是其中R 1与X 2一起形成氮和磷原子之间的直接键。

公开(公告)号：US5229162A

公开(公告)日：1993-07-20

申请号：US789894

申请日：1991-11-12

申请人： Dennis Chapman ,  Aziz A. Durrani

发明人： Dennis Chapman ,  Aziz A. Durrani

IPC分类号： A61L33/00 ,  C07C43/315 ,  C07F5/00 ,  C07F9/09 ,  C07F9/6584

CPC分类号： C07F9/65844 ,  A61L33/0082 ,  C07C43/315 ,  C07F5/003 ,  C07F9/091 ,  Y10S128/912 ,  Y10S525/937 ,  Y10S623/924 ,  Y10T428/1352

摘要： A compound of formula: ##STR1## in which X.sup.1 is a reactive group that can react to form a covalent bond with a reactive group on the surface of a material to be rendered biocompatible, X.sup.2 is a group -O.sup..crclbar. or a precursor of such a group, n is 2, 3 or 4, Y is a group --N.sup..sym. R.sub.3 A.sup..crclbar. wherein each R, which may be the same or different, is a C.sub.1 -C.sub.4 alkyl group and A.sup..crclbar. is an anion present when X.sup.2 is an electrically neutral group or Y is ##STR2## wherein R.sup.1 together with X.sup.2 forms a direct bond between the nitrogen and the phosphorus atoms.

摘要翻译： 下式的化合物：其中X1是能与反应性基团反应形成与要生物相容的材料的表面上的反应性基团的反应性基团，X 2是基团-O（ - ）或 这种基团的前体，n为2,3或4，Y为-N（+）R 3A（ - ）基团，其中各R可以相同或不同，为C1-C4烷基，A（ - ）是当X2是电中性基团时存在的阴离子或Y是其中R 1与X 2一起形成氮和磷原子之间的直接键。

公开(公告)号：US4937369A

公开(公告)日：1990-06-26

申请号：US328709

申请日：1989-03-27

申请人： Dennis Chapman ,  Aziz A. Durrani

发明人： Dennis Chapman ,  Aziz A. Durrani

IPC分类号： A61L26/00 ,  A61L33/00 ,  C07C43/315 ,  C07F5/00 ,  C07F9/09 ,  C07F9/14 ,  C07F9/6584 ,  C07F9/146

CPC分类号： C07F9/65844 ,  A61L33/0082 ,  C07C43/315 ,  C07F5/003 ,  C07F9/091

摘要： A compound of formula: ##STR1## in which X.sup.1 is a reactive group that can react to form a covalent bond with a reactive group on the surface of a material to be rendered biocompatible, X.sup.2 is a group -0.sup..crclbar. or a precursor of such a group, n is 2, 3 or 4, Y is a group --N.sup..sym. R.sub.3 A.sup..crclbar. wherein each R, which may be the same or different, is a C.sub.1 -C.sub.4 alkyl group and A.sup..crclbar. is an anion present when X.sup.2 is an electrically neutral group or Y is ##STR2## wherein R.sup.1 together with X.sup.2 forms a direct bond between the nitrogen and the phosphorus atoms.

公开(公告)号：US4675310A

公开(公告)日：1987-06-23

申请号：US803404

申请日：1985-11-21

申请人： Dennis Chapman ,  James A. Hayward

发明人： Dennis Chapman ,  James A. Hayward

IPC分类号： A61K38/00 ,  A61K9/00 ,  A61K9/127 ,  A61K38/42 ,  A61K37/14 ,  A61K31/685

CPC分类号： A61K38/42 ,  A61K9/1273

摘要： The invention herein involves the use of ligands and phospholipid liposomes as a carrier for the transport of various gases.

摘要翻译： PCT No.PCT / GB85 / 00114 Sec。 371日期：1985年11月21日 102（e）1985年11月21日PCT PCT。 出版物WO85 / 04326 1985年10月10日。本发明涉及使用配体和磷脂脂质体作为运输各种气体的载体。

公开(公告)号：US4348329A

公开(公告)日：1982-09-07

申请号：US218556

申请日：1980-12-22

申请人： Dennis Chapman

发明人： Dennis Chapman

IPC分类号： A61K9/127 ,  A61L15/44 ,  A61L27/16 ,  A61L29/08 ,  A61L33/00 ,  A61L33/06 ,  B01D67/00 ,  C07C51/353 ,  C07C57/18 ,  C07F9/10 ,  C08F38/00 ,  C07F9/02 ,  A23J7/00

CPC分类号： B01D67/0088 ,  A61K9/1273 ,  A61L15/44 ,  A61L27/16 ,  A61L29/085 ,  A61L33/00 ,  A61L33/064 ,  B01D67/0093 ,  C07C51/353 ,  C07C57/18 ,  C07F9/10 ,  C08F38/00 ,  A61L2300/626 ,  B01D2323/30 ,  B01D2323/34 ,  Y10S623/92

摘要： New phospholipids containing a conjugated di-yne system have the formula: ##STR1## wherein at least one of B.sub.1 and B.sub.2 is a group of the formula--(CO).sub.p --X.sub.1 --C.tbd.C--C.tbd.C--Y.sub.1wherein p is 0 or 1, X.sub.1 is a direct bond or a divalent aliphatic or cycloaliphatic group, Y.sub.1 is H or a monovalent aliphatic or cycloaliphatic group, the total number of carbon atoms in X.sub.1 and Y.sub.1 in each of B.sub.1 and/or B.sub.2 being 8 to 26; and the other of B.sub.1 and B.sub.2 is either (a) the same or a different group of the formula:--(CO).sub.p --X.sub.1 --C.tbd.C--C.tbd.C--Y.sub.1where X.sub.1, Y.sub.1 or p are as defined above;or (b) is an aliphatic or cycloaliphatic group containing at least 8 carbon atoms; n is 0 or 1, m is 2, 3 or 4 and each R independently represents an alkyl group containing 1 to 4 carbon atoms, and are prepared by esterification and/or etherification of glycerol by conventional techniques. The conjugated di-yne systems can be cross-linked by actinic radiation to give intermolecular and, in certain cases, also intramolecular cross-linking. Thin layers of the phospholipids can be coated onto substrates subsequently to be brought into contact with blood or other body fluids and then cross-linked to give polymer coated surfaces which have a reduced tendency to initiate blood coagulation, for example, compared to untreated surfaces. Artificial lenses for the human eye treated in this way have a reduced tendency to cause endothelial damage. The phospholipids of the invention can also be formed into liposomes and the conjugated di-yne system then cross-linked. Physiologically active materials such as drugs, enzymes or antigens can be incorporated into the liposomes which can then be used as prolonged release formulations.

摘要翻译： 含有共轭二烯体系的新型磷脂具有下式：其中B1和B2中的至少一个是式 - （CO）p-X1-C 3BOND CC 3BOND C-Y1的基团，其中p为0或 1，X1是直接键或二价脂族或脂环族基团，Y1是H或一价脂族或脂环族基团，B1和/或B2各自的X1和Y1中的碳原子总数为8-26; B1和B2中的另一个是（a）相同或不同的下式： - （CO）p-X1-C 3BOND C-C 3BOND C-Y1，其中X1，Y1或p如上定义; 或（b）是含有至少8个碳原子的脂族或脂环族基团; n为0或1，m为2,3或4，各R独立地表示含有1至4个碳原子的烷基，并且通过常规技术酯化和/或醚化甘油来制备。 共轭二烯系统可以通过光化辐射交联以产生分子间，在某些情况下也是分子内的交联。 磷脂的薄层可以涂覆在基底上，随后与血液或其他体液接触，然后交联以得到例如与未处理的表面相比具有降低的凝血发生倾向的聚合物涂覆的表面。 以这种方式处理的人眼的人造镜片具有降低的引起内皮损伤的倾向。 本发明的磷脂也可以形成脂质体，然后共轭二烯系统交联。 可以将生理活性物质如药物，酶或抗原掺入脂质体中，然后将其用作延长释放制剂。

公开(公告)号：US20140235622A1

公开(公告)日：2014-08-21

申请号：US14166511

申请日：2014-01-28

申请人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

发明人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jay Xu ,  Ning Zou

IPC分类号： C07D417/12 ,  C07D401/12 ,  C07D231/16 ,  C07D413/12 ,  C07D403/12 ,  C07D409/12 ,  C07D405/12 ,  C07D231/12

CPC分类号： A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板凝集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，进行性多灶性脑白质病等。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US08148418B2

公开(公告)日：2012-04-03

申请号：US12301180

申请日：2007-05-17

申请人： Bradley Teegarden ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Sonja Strah-Pleynet ,  Jay Xu

发明人： Bradley Teegarden ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Sonja Strah-Pleynet ,  Jay Xu

IPC分类号： A61K31/415 ,  C07D231/12 ,  A61P25/24

CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D207/335 ,  C07D207/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板凝集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，进行性多灶性脑白质病等。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US20090197935A1

公开(公告)日：2009-08-06

申请号：US12301172

申请日：2007-05-17

申请人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jingdong Xu ,  Ning Zou

发明人： Bradley Teegarden ,  Dennis Chapman ,  Juyi Choi ,  Konrad Feichtinger ,  Sangdon Han ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Jingdong Xu ,  Ning Zou

IPC分类号： A61K31/415 ,  C07D231/12 ,  A61P25/24

CPC分类号： A61K31/415 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板聚集，冠状动脉疾病，心肌梗死，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，进行性多灶性脑白质病等。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体相关疾病的方法。

公开(公告)号：US20090186895A1

公开(公告)日：2009-07-23

申请号：US12301180

申请日：2007-05-17

申请人： Bradley Teegarden ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Sonja Strah-Pleynet ,  Jingdong Xu

发明人： Bradley Teegarden ,  Dennis Chapman ,  Marc Decaire ,  Peter I. Dosa ,  Konrad Feichtinger ,  Honnappa Jayakumar ,  Thuy-Anh Tran ,  Sonja Strah-Pleynet ,  Jingdong Xu

IPC分类号： A61K31/5377 ,  C07D231/12 ,  A61K31/415 ,  C07D413/12 ,  A61K31/422 ,  C07D401/12 ,  A61K31/454 ,  C07D403/12 ,  A61K31/4196 ,  C07D417/12 ,  A61K31/427 ,  C07D405/12 ,  A61K31/4155 ,  A61K31/41 ,  A61P11/06 ,  A61P3/10 ,  A61P7/02 ,  A61P29/00 ,  A61P25/00 ,  A61P9/12

CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D207/335 ,  C07D207/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.

摘要翻译： 本发明涉及某些调节5-HT2A 5-羟色胺受体活性的式（Ia）化合物及其药物组合物。 化合物及其药物组合物涉及可用于治疗血小板凝集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法， 精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病， 相关疾病，进行性多灶性脑白质病等。 本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体相关疾病的方法。