公开(公告)号：US06727257B1

公开(公告)日：2004-04-27

申请号：US09730458

申请日：2000-12-05

申请人： Dhanapalan Nagarathnam ,  George Chiu ,  T. G. Murali Dhar ,  Wai C. Wong ,  Mohammad R. Marzabadi ,  Charles Gluchowski ,  Bharat Lagu ,  Shou Wu Miao

发明人： Dhanapalan Nagarathnam ,  George Chiu ,  T. G. Murali Dhar ,  Wai C. Wong ,  Mohammad R. Marzabadi ,  Charles Gluchowski ,  Bharat Lagu ,  Shou Wu Miao

IPC分类号： C07D40106

CPC分类号： C07D239/30 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D491/04

摘要： This invention is directed to dihydropyrimidine compounds of the following formula: wherein A is which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及下式的二氢嘧啶化合物：其中A是人α1C受体的选择性拮抗剂。 本发明还涉及这些化合物用于降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ence，心律失常以及用于治疗任何α1C受体拮抗作用的疾病 有用 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US06268369B1

公开(公告)日：2001-07-31

申请号：US08836628

申请日：1997-05-16

申请人： Dhanapalan Nagarathnam ,  George Chiu ,  T. G. Murali Dhar ,  Wai C. Wong ,  Mohammad R. Marzabadi ,  Charles Gluchowski ,  Bharat Lagu ,  Shou Wu Miao

发明人： Dhanapalan Nagarathnam ,  George Chiu ,  T. G. Murali Dhar ,  Wai C. Wong ,  Mohammad R. Marzabadi ,  Charles Gluchowski ,  Bharat Lagu ,  Shou Wu Miao

IPC分类号： C07D4004

CPC分类号： C07D239/30 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D491/04

摘要： This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及下式的二氢嘧啶化合物：它们是人α1C受体的选择性拮抗剂。 本发明还涉及这些化合物用于降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ence，心律失常以及用于治疗任何α1C受体拮抗作用的疾病 有用 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US06620815B1

公开(公告)日：2003-09-16

申请号：US09636518

申请日：2000-08-10

申请人： Bharat Lagu ,  T. G. Murali Dhar ,  Dhanapalan Nagarathnam ,  Yoon T. Jeon ,  Mohammad R. Marzabadi ,  Wai C. Wong ,  Charles Gluchowski

发明人： Bharat Lagu ,  T. G. Murali Dhar ,  Dhanapalan Nagarathnam ,  Yoon T. Jeon ,  Mohammad R. Marzabadi ,  Wai C. Wong ,  Charles Gluchowski

IPC分类号： A61K31496

CPC分类号： C07D263/52 ,  A61K31/58 ,  C07D263/26 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/535 ,  A61K31/495 ,  A61K31/445 ,  A61K2300/00

摘要： This invention is directed to oxazolidinone compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及作为人α1A受体的选择性拮抗剂的恶唑烷酮化合物。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，松弛下尿路组织，治疗良性前列腺增生，阳ency，心律失常以及治疗任何α1A受体拮抗作用的疾病的用途 可能是有用的 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US06245773B1

公开(公告)日：2001-06-12

申请号：US08858017

申请日：1997-05-16

申请人： Wai C. Wong ,  Bharat Lagu ,  Dhanapalan Nagarathnam ,  Mohammad R. Marzabadi ,  Charles Gluchowski

发明人： Wai C. Wong ,  Bharat Lagu ,  Dhanapalan Nagarathnam ,  Mohammad R. Marzabadi ,  Charles Gluchowski

IPC分类号： A61K31505

CPC分类号： C07D239/22 ,  A61K31/506 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D451/06 ,  C07D491/04

摘要： This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及下式的二氢嘧啶化合物：它们是人α1A受体的选择性拮抗剂。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ency，心律失常以及用于治疗任何α1A受体拮抗作用的疾病 有用 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US6159990A

公开(公告)日：2000-12-12

申请号：US99225

申请日：1998-06-17

申请人： Bharat Lagu ,  T.G. Murali Dhar ,  Dhanapalan Nagarathnam ,  Yoon T. Jeon ,  Mohammad R. Marzabadi ,  Wai C. Wong ,  Charles Gluchowski

发明人： Bharat Lagu ,  T.G. Murali Dhar ,  Dhanapalan Nagarathnam ,  Yoon T. Jeon ,  Mohammad R. Marzabadi ,  Wai C. Wong ,  Charles Gluchowski

IPC分类号： A61K31/58 ,  C07D263/26 ,  C07D263/52 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/445

CPC分类号： C07D263/52 ,  A61K31/58 ,  C07D263/26 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/535 ,  A61K31/495 ,  A61K31/445 ,  A61K2300/00

摘要： This invention is directed to oxazolidinone compounds which are selective antagonists for human .alpha..sub.1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the .alpha..sub.1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及作为人α1A受体的选择性拮抗剂的恶唑烷酮化合物。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，松弛下尿路组织，治疗良性前列腺增生，阳ency，心律失常以及用于治疗其中α1A拮抗作用的任何疾病 受体可能是有用的。 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US06720324B2

公开(公告)日：2004-04-13

申请号：US09899635

申请日：2001-07-05

申请人： Mohammad R. Marzabadi ,  John Wetzel ,  John E. DeLeon ,  Bharat Lagu ,  Charles Gluchowski ,  Stewart Noble ,  Dhanapalan Nagarathnam

发明人： Mohammad R. Marzabadi ,  John Wetzel ,  John E. DeLeon ,  Bharat Lagu ,  Charles Gluchowski ,  Stewart Noble ,  Dhanapalan Nagarathnam

IPC分类号： C07D23932

CPC分类号： C07D211/58 ,  C07C233/79 ,  C07C2601/14 ,  C07D211/52 ,  C07D295/073 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D471/10 ,  C07D491/04 ,  C07D491/10

摘要： This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

摘要翻译： 本发明涉及作为黑色素浓缩激素-1（MCH1）受体的选择性拮抗剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。 本发明还提供了制备药物组合物的方法，其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了改变受试者进食行为的方法，其包括向受试者施用量 的有效减少受试者食物消耗的本发明化合物。 本发明进一步提供了治疗受试者进食障碍的方法，其包括向受试者施用一定量的有效降低受试者食物消耗的本发明化合物。 在本发明的一个实施方案中，喂食障碍是贪食症，神经性贪食症或肥胖症。

公开(公告)号：US6057350A

公开(公告)日：2000-05-02

申请号：US98781

申请日：1998-06-17

申请人： Michael A. Patane ,  Mark G. Bock ,  Dhanapalan Nagarathnam ,  Bharat Lagu ,  Wai C. Wong

发明人： Michael A. Patane ,  Mark G. Bock ,  Dhanapalan Nagarathnam ,  Bharat Lagu ,  Wai C. Wong

IPC分类号： C07C255/46 ,  C07D263/26 ,  C07D275/06 ,  A61K31/42 ,  A61K31/425 ,  C07D263/22

CPC分类号： C07D275/06 ,  C07C255/46 ,  C07D263/26 ,  C07C2101/02 ,  C07C2101/14 ,  C07C2103/18

摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

公开(公告)号：US06531471B2

公开(公告)日：2003-03-11

申请号：US10017263

申请日：2001-12-14

申请人： Bharat Lagu ,  Dhanapalan Nagarathnam ,  Dake Tian ,  Charles Gluchowski

发明人： Bharat Lagu ,  Dhanapalan Nagarathnam ,  Dake Tian ,  Charles Gluchowski

IPC分类号： A61K315375

CPC分类号： C07D413/12 ,  A61K31/5375 ,  A61K31/5377 ,  C07D265/32 ,  C07D413/14

摘要： This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

公开(公告)号：US06362182B1

公开(公告)日：2002-03-26

申请号：US09702015

申请日：2000-10-30

申请人： Bharat Lagu ,  Dhanapalan Nagarathnam ,  Dake Tian ,  Charles Gluchowski

发明人： Bharat Lagu ,  Dhanapalan Nagarathnam ,  Dake Tian ,  Charles Gluchowski

IPC分类号： A61K31537

CPC分类号： C07D413/12 ,  A61K31/5375 ,  A61K31/5377 ,  C07D265/32 ,  C07D413/14

摘要： This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及作为人α1a受体的选择性拮抗剂的吗啉酮和吗啉衍生物。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ency，心律失常，交感神经介导的疼痛，偏头痛以及用于治疗任何疾病的用途 其中α1a受体的拮抗作用可能是有用的。 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US06218390B1

公开(公告)日：2001-04-17

申请号：US09213539

申请日：1998-12-17

申请人： Bharat Lagu ,  Dhanapalan Nagarathnam ,  Dake Tian ,  Charles Gluchowski

发明人： Bharat Lagu ,  Dhanapalan Nagarathnam ,  Dake Tian ,  Charles Gluchowski

IPC分类号： A61K315375

CPC分类号： C07D413/12 ,  A61K31/5375 ,  A61K31/5377 ,  C07D265/32 ,  C07D413/14

摘要： This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

摘要翻译： 本发明涉及作为人α1a受体的选择性拮抗剂的吗啉酮和吗啉衍生物。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ency，心律失常，交感神经介导的疼痛，偏头痛以及用于治疗任何疾病的用途 其中α1a受体的拮抗作用可能是有用的。 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。