公开(公告)号：WO2004014307A3

公开(公告)日：2004-12-29

申请号：PCT/US0324869

申请日：2003-08-07

Applicant: SYNAPTIC PHARMA CORP

Inventor： BLACKBURN THOMAS

IPC: A61K31/435 ,  A61K31/44 ,  A61K31/505

CPC classification number: H04M3/2281 ,  A61K31/435 ,  A61K31/44 ,  A61K31/505

Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor and are useful for the treatment of neuropathic pain and other abnormalities. This invention also provides a method of treating a subject suffering from an abnormality which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's abnormality. This invention also provides a method of treating an abnormality in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

Abstract translation: 本发明涉及嘧啶和吲哚酮衍生物，它们是GAL3受体的选择性拮抗剂，可用于治疗神经性疼痛和其他异常。 本发明还提供了治疗患有异常的受试者的方法，该方法包括给受试者施用有效治疗受试者异常的量的本发明化合物。 本发明还提供了治疗受试者异常的方法，该方法包括给受试者施用包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂的组合物。

公开(公告)号：WO2004060282A2

公开(公告)日：2004-07-22

申请号：PCT/US0339465

申请日：2003-12-10

Applicant: SYNAPTIC PHARMA CORP

Inventor： DELGADO LILIANA ,  BERRADA KARIM ,  ARTYMYSHYN ROMAN

IPC: A61K20060101 ,  C07K14/00 ,  G01N33/53 ,  G01N33/566 ,  G01N33/574 ,  A61K

CPC classification number: G01N33/566

Abstract: The invention provides methods of treating an abnormality that is linked to the activity of the mammalian SNORF207 receptor, as well as methods of determining binding of compounds to the mammalian SNORF207 receptor, methods of identifying agonists and antagonists of the SNORF207 receptor, and agonists and antagonists so identified.

Abstract translation: 本发明提供了治疗与哺乳动物SNORF207受体的活性相关的异常的方法，以及确定化合物与哺乳动物SNORF207受体的结合的方法，鉴定SNORF207受体的激动剂和拮抗剂的方法，以及激动剂和拮抗剂 如此确定。

公开(公告)号：WO02060392A2

公开(公告)日：2002-08-08

申请号：PCT/US0204608

申请日：2002-01-31

Applicant: SYNAPTIC PHARMA CORP

Inventor： BLACKBURN THOMAS P ,  KONKEL MICHAEL

IPC: A61K31/407 ,  A61K31/506 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12 ,  A61K

CPC classification number: C07D405/14 ,  A61K31/407 ,  A61K31/506 ,  C07D209/40 ,  C07D239/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D417/12

Abstract: This invention is directed to pyrimidine and indolone derivatives which are selective antagonists for the GAL3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and apharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GAL3 receptor antagonist.

Abstract translation: 本发明涉及作为GAL3受体的选择性拮抗剂的嘧啶和吲哚酮衍生物。 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。 本发明还提供通过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而制备的药物组合物。 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与可药用载体组合。 本发明还提供了治疗患有抑郁症和/或焦虑症的受试者的方法，其包括给予受试者一定量的有效治疗受试者的抑郁症和/或焦虑症的本发明化合物。 本发明还提供了治疗受试者的抑郁症和/或焦虑的方法，其包括向受试者施用包含药学上可接受的载体和治疗有效量的GAL3受体拮抗剂的组合物。

公开(公告)号：WO0073449B1

公开(公告)日：2001-03-01

申请号：PCT/US0014654

申请日：2000-05-26

Applicant: SYNAPTIC PHARMA CORP ,  BOROWSKY BETH E ,  OGOZALEK KRISTINE L ,  JONES KENNETH A

Inventor： BOROWSKY BETH E ,  OGOZALEK KRISTINE L ,  JONES KENNETH A

IPC: A01K67/027 ,  A61K31/7088 ,  A61K38/00 ,  A61K39/395 ,  A61K45/00 ,  A61K48/00 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10 ,  A61P3/12 ,  A61P5/00 ,  A61P5/06 ,  A61P7/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P15/00 ,  A61P19/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P27/02 ,  A61P37/00 ,  A61P43/00 ,  C07K14/705 ,  C07K16/28 ,  C12N5/10 ,  C12N15/09 ,  C12N15/12 ,  C12P21/08 ,  C12Q1/02 ,  C12Q1/68 ,  G01N33/15 ,  G01N33/50 ,  G01N33/566 ,  C07K14/47 ,  C12P21/02 ,  G01N33/53 ,  G01N33/567

CPC classification number: C07K14/705 ,  A61K38/00 ,  A61K48/00

Abstract: This invention provides isolated nucleic acids encoding mammalian SNORF33 receptors, purified mammalian SNORF33 receptors, vectors comprising nucleic acid encoding mammalian SNORF33 receptors, cells comprising such vectors, antibodies directed to mammalian SNORF33 receptors, nucleic acid probes useful for detecting nucleic acid encoding mammalian SNORF33 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding mammalian SNORF33 receptors, transgenic, nonhuman animals which express DNA encoding normal or mutant mammalian SNORF33 receptors, methods of isolating mammalian SNORF33 receptors, methods of treating an abnormality that is linked to the activity of the mammalian SNORF33 receptors, as well as methods of determining binding of compounds to mammalian SNORF33 receptors, methods of identifying agonists and antagonists of SNORF33 receptors, and agonists and antagonists so identified.

Abstract translation: 本发明提供编码哺乳动物SNORF33受体的分离的核酸，纯化的哺乳动物SNORF33受体，包含编码哺乳动物SNORF33受体的核酸的载体，包含此类载体的细胞，针对哺乳动物SNORF33受体的抗体，用于检测编码哺乳动物SNORF33受体的核酸的核酸探针， 与编码哺乳动物SNORF33受体的核酸的独特序列互补的反义寡核苷酸，表达编码正常或突变的哺乳动物SNORF33受体的DNA的转基因非人动物，分离哺乳动物SNORF33受体的方法，治疗与哺乳动物的活性相关的异常的方法 SNORF33受体以及确定化合物与哺乳动物SNORF33受体结合的方法，识别SNORF33受体的激动剂和拮抗剂的方法，以及如此确定的激动剂和拮抗剂。

公开(公告)号：WO2004034967A3

公开(公告)日：2004-07-15

申请号：PCT/US0325134

申请日：2003-08-07

Applicant: SYNAPTIC PHARMA CORP

Inventor： PACKIARAJAN MATHIVANAN

IPC: A61K47/10 ,  A61K47/26 ,  C07D239/50 ,  A61K31/506 ,  A61K31/5377 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04

CPC classification number: C07D239/50 ,  A61K47/10 ,  A61K47/26

Abstract: This invention is directed to pyrimidine derivatives which are selective antagonists for the GalR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering the subject an amount of a compound of the invention effective to treat the subject's depression and/or anxiety. This invention also provides a method of treating depression and/or anxiety in a subject which comprises administering to the subject a composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a GalR3 receptor antagonist.

Abstract translation: 本发明涉及作为GalR3受体的选择性拮抗剂的嘧啶衍生物。 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。 本发明还提供了通过组合治疗有效量的本发明化合物和药学上可接受的载体制成的药物组合物。 本发明进一步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。 本发明还提供了治疗患有抑郁症和/或焦虑症的对象的方法，其包括给予对象有效治疗对象抑郁症和/或焦虑的量的本发明化合物。 本发明还提供了治疗受试者中的抑郁症和/或焦虑症的方法，其包括给受试者施用包含药学上可接受的载体和治疗有效量的GalR3受体拮抗剂的组合物。

公开(公告)号：WO0039279A2

公开(公告)日：2000-07-06

申请号：PCT/US9931169

申请日：1999-12-30

Applicant: SYNAPTIC PHARMA CORP ,  SALON JOHN A ,  LAZ THOMAS M ,  NAGORNY RAISA ,  WILSON AMY E

Inventor： SALON JOHN A ,  LAZ THOMAS M ,  NAGORNY RAISA ,  WILSON AMY E

IPC: G01N33/50 ,  A61K31/7088 ,  A61K45/00 ,  A61K48/00 ,  A61M1/36 ,  A61P1/00 ,  A61P3/10 ,  A61P3/12 ,  A61P5/06 ,  A61P9/00 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P15/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/06 ,  A61P25/36 ,  A61P37/00 ,  A61P43/00 ,  C07K14/72 ,  C07K16/28 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N15/09 ,  C12P21/02 ,  C12P21/08 ,  C12Q1/02 ,  C12Q1/68 ,  G01N33/15 ,  G01N33/53 ,  G01N33/566 ,  C12N

CPC classification number: A61M1/3621 ,  C07K14/72

Abstract: This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense aligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors.

Abstract translation: 本发明提供编码人MCH1受体的分离核酸，纯化的人MCH1受体，包含编码人MCH1受体的分离核酸的载体，包含此类载体的细胞，针对人MCH1受体的抗体，用于检测核酸的核酸探针 编码人MCH1受体的酸，与编码人MCH1受体的核酸的独特序列互补的反义寡核苷酸，表达编码正常或突变人MCH1受体的DNA的转基因非人动物，分离人MCH1受体的方法，治疗异常 与人MCH1受体的活性有关，以及确定化合物与哺乳动物MCH1受体结合的方法。

公开(公告)号：WO9422829A3

公开(公告)日：1995-01-05

申请号：PCT/US9403852

申请日：1994-04-05

Applicant: SYNAPTIC PHARMA CORP ,  GLUCHOWSKI CHARLES ,  WETZEL JOHN M ,  CHIU GEORGE ,  MARZABADI MOHAMMAD R ,  WONG WAI C ,  NAGARATHNAM DHANAPALAN

Inventor： GLUCHOWSKI CHARLES ,  WETZEL JOHN M ,  CHIU GEORGE ,  MARZABADI MOHAMMAD R ,  WONG WAI C ,  NAGARATHNAM DHANAPALAN

IPC: C07D211/90 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/10 ,  C07F7/08 ,  A61K31/435 ,  C07D211/84 ,  C07D401/00

CPC classification number: C07D401/12 ,  C07D211/90 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/10 ,  C07F7/0812

Abstract: The invention provides a method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound having structure (I) wherein Y is -(CH2)n-, where n is 1, 2, 3, 4 or 5; -(CH2)h-O-(CH2)k-, where h and k are independently the same or different and are 2, 3 or 4; -(CH2)h-CH=CH-(CH2)k-; or -(CH2)h-C C-(CH2)k-, where h and k are independently the same or different and are 1, 2, 3 or 4; wherein Z is 0, NH, or CH2; wherein R1 is a linear or branched chain alkyl, alkoxyalkyl or arylalkyl group; wherein R?2 and R4¿ are independently the same or different and are H, or a linear or branched chain alkyl group; wherein R3 is H, a linear or branched chain alkyl, alkoxy, alkoxyalkyl or acyl group; and wherein R?5 and R6¿ are independently the same or different and are H, OH, Cl, Br, F, No¿2?, CN, CF3, or NH2, or a linear or branched chain alkyl, alkoxy, alkoxycarbonyl, acyl, alkylsulfoxide, alkylsulfone, or mono- or dialkylamino group. Other active compounds containing one, two or three rings are also disclosed as well as pharmaceutical compositions prepared therefrom and methods of use in the treatment of BPH, inhibition of cholesterol synthesis, and reduction of intraocular pressure.

公开(公告)号：WO2004050853A3

公开(公告)日：2005-06-02

申请号：PCT/US0338529

申请日：2003-12-03

Applicant: SYNAPTIC PHARMA CORP

Inventor： ARTYMYSHYN ROMAN ,  DELGADO LILLIANA ,  VAYSSE PIERRE J-J ,  BERRADA KARIM ,  SMITH KELLI E ,  GERALD CHRISTOPHE

IPC: C07K14/705 ,  G01N33/53 ,  C07K14/00 ,  G01N33/566 ,  G01N33/567 ,  G01N33/574

CPC classification number: C07K14/705

Abstract: This invention provides methods of treating an abnormality that is linked to the activity of the mammalian SNORF55 receptor, as well as methods of determining binding of compounds to the mammalian SNORF55 receptor, methods of identifying agonists and antagonists of the SNORF55 receptor, and agonists and antagonists so identified.

Abstract translation: 本发明提供了治疗与哺乳动物SNORF55受体的活性相关的异常的方法，以及确定化合物与哺乳动物SNORF55受体的结合的方法，识别SNORF55受体的激动剂和拮抗剂的方法以及激动剂和拮抗剂 如此确定。

公开(公告)号：WO03050263A3

公开(公告)日：2003-10-09

申请号：PCT/US0239616

申请日：2002-12-11

Applicant: SYNAPTIC PHARMA CORP

Inventor： SMITH KELLI E ,  QUAN YONG

IPC: C07K14/705 ,  C07H21/04

CPC classification number: C07K14/705

Abstract: This invention provides a recombinant nucleic acid comprising a nucleic acid encoding a mammalian SNORF49 receptor, wherein the mammalian receptor-encoding nucleic acid hybridizes under high stringency conditions to a nucleic acid encoding a human SNORF49 receptor and having a sequence identical to the sequence of the human SNORF49 receptor-encoding nucleic acid contained in plasmid pEXJ.T73BS-hSNORF49-f (ATCC Patent Deposit Designation PTA-659). This invention further provides a recombinant nucleic acid comprising a nucleic acid encoding a human SNORF49 receptor, wherein the human SNORF49 receptor comprises an amino acid sequence identical to the sequence of the human SNORF49 receptor encoded by the shortest open reading frame indicated in Figures 1A-1B (SEQ ID NO: 1).

Abstract translation: 本发明提供了包含编码哺乳动物SNORF49受体的核酸的重组核酸，其中编码哺乳动物受体的核酸在高度严格条件下与编码人类SNORF49受体的核酸杂交并具有与人类序列相同的序列 包含在质粒pEXJ.T73BS-hSNORF49-f（ATCC专利保藏名称PTA-659）中的SNORF49受体编码核酸。 本发明还提供了包含编码人类SNORF49受体的核酸的重组核酸，其中人类SNORF49受体包含与图1A-1B所示的最短开放阅读框编码的人类SNORF49受体序列相同的氨基酸序列 （SEQ ID NO：1）。

公开(公告)号：WO0202744A2

公开(公告)日：2002-01-10

申请号：PCT/US0121350

申请日：2001-07-05

Applicant: SYNAPTIC PHARMA CORP

Inventor： SALON JOHN A ,  LAZ THOMAS M ,  NAGORNY RAISA ,  WILSON AMY E

IPC: A01K67/027 ,  A61K31/165 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/438 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/7088 ,  A61K39/395 ,  A61K45/00 ,  A61K48/00 ,  A61P1/00 ,  A61P3/10 ,  A61P3/12 ,  A61P5/00 ,  A61P5/06 ,  A61P5/38 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P15/00 ,  A61P19/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/36 ,  A61P37/00 ,  C07D211/52 ,  C07D211/58 ,  C07D239/36 ,  C07D249/18 ,  C07D295/02 ,  C07D295/10 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/048 ,  C07D491/107 ,  C07K14/72 ,  C07K16/18 ,  C07K16/28 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N15/09 ,  C12P21/08 ,  C12Q1/02 ,  C12Q1/68 ,  C40B30/04 ,  C40B40/02 ,  C40B40/04 ,  C40B50/06 ,  G01N33/15 ,  G01N33/50 ,  G01N33/53 ,  G01N33/566 ,  C12N

CPC classification number: C07K14/72

Abstract: This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequence of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors. This invention provides a method of modifying the feeding behavior of a subject which comprises administering to the subject an amount of an MCH1 antagonist effective to decrease the body mass of the subject and/or decrease the consumption of food by the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of an MCH1 antagonist effective to treat the subject's depression and/or anxiety.

Abstract translation: 本发明提供编码人MCH1受体的纯化的人MCH1受体的核酸，纯化的人MCH1受体，包含分离的编码人MCH1受体的核酸的载体，包含该载体的细胞，针对人MCH1受体的抗体，用于检测核酸的核酸探针 编码人MCH1受体的酸，与编码人MCH1受体的唯一核酸序列互补的反义寡核苷酸，表达编码正常或突变型人MCH1受体的DNA的转基因非人动物，分离人MCH1受体的方法，治疗异常的方法 与人MCH1受体的活性相关，以及确定化合物与哺乳动物MCH1受体结合的方法。 本发明提供了改变受试者的喂养行为的方法，其包括向受试者施用一定量的有效降低受试者体重的MCH1拮抗剂和/或降低受试者的食物消耗。 本发明进一步提供了治疗患有抑郁症和/或焦虑症的受试者的方法，其包括向受试者施用一定量的有效治疗受试者的抑郁症和/或焦虑症的MCH1拮抗剂。