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1. 发明专利

BR122021013836B1 Composto e seu uso, composição farmacêutica 未知
公开(公告)号：BR122021013836B1
公开(公告)日：2022-05-24
申请号：BR122021013836
申请日：2010-12-03
申请人： PGI DRUG DISCOVERY LLC , PSYCHOGENICS INC , SUNOVION PHARMACEUTICALS INC
发明人： JOHN EMMERSON CAMPBELL , SHAO LIMING , MICHAEL CHARLES HEWITT , TALEEN G HANANIA , CAMPBELL UNA
IPC分类号： C07D333/56 , A61K31/381 , A61P25/00 , A61P25/18 , C07D495/04 , C07D495/20
摘要： são fornecidos aqui compostos multicíclicos, métodos para a sua síntese, composições farmacêuticas compreendendo os mesmos, e métodos para o seu uso. os compostos aqui providos são úteis no tratamento, prevenção e/ou administração de vários transtornos neurológicos, incluindo, mas não limitando a psicose e/ou esquizofrenia.

2. 发明专利

NZ731621A Multicyclic compounds and methods of use thereof 未知
公开(公告)号：NZ731621A
公开(公告)日：2019-01-25
申请号：NZ73162110
申请日：2010-12-03
申请人： SUNOVION PHARMACEUTICALS INC , PGI DRUG DISCOVERY LLC
发明人： SHAO LIMING , CAMPBELL JOHN , HEWITT MICHAEL , CAMPBELL UNA , HANANIA TALEEN
IPC分类号： C07D495/04 , A61K31/35 , A61K31/381
摘要： Disclosed is a process for preparing (S)-7-((methylamino)methyl)-4,7-dihydro-5H-thieno[2,3-c]pyran and analogues thereof as represented by general formula (IVa), or a pharmaceutically acceptable salt or stereoisomer thereof, the method comprising: (a) treating a hydroxyalkyl thiophene such as 3-(2-hydroxyethyl)thiophene with an amino-aldehyde acetal (such as 2-(methylamino)acetaldehyde diethyl acetal) in the presence of an acid, wherein m is 0; n is 1; R1 and R2 are each independently hydrogen or alkyl; R3 and R4 are each independently hydrogen or alkyl; R5 is hydrogen; and R6 and R7 are each independently hydrogen, halo, or alkyl. The process may further include a step of isolating one stereoisomer of the compound of formula (IVa) or a pharmaceutically acceptable salt thereof by resolution of the mixture (e.g. by using chiral chromatography).

3. 发明专利

HK1247911A1 多環化合物及其使用方法未知
公开(公告)号：HK1247911A1
公开(公告)日：2018-10-05
申请号：HK18107195
申请日：2018-05-31
申请人： SUNOVION PHARMACEUTICALS INC , PGI DRUG DISCOVERY LLC
发明人： SHAO LIMING , CAMPBELL JOHN EMERSON , HEWITT MICHAEL CHARLES , CAMPBELL UNA , HANANIA TALEEN G
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101

4. 发明专利

AU2016200448C1 MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF 未知
公开(公告)号：AU2016200448C1
公开(公告)日：2018-05-10
申请号：AU2016200448
申请日：2016-01-27
申请人： PGI DRUG DISCOVERY LLC , SUNOVION PHARMACEUTICALS INC
发明人： SHAO LIMING , CAMPBELL JOHN EMERSON , HEWITT MICHAEL CHARLES , CAMPBELL UNA , HANANIA TALEEN G
IPC分类号： C07D333/56 , A61K31/381 , A61P25/00 , A61P25/18 , C07D495/04 , C07D495/20
摘要： Provided herein are multicyclic compounds, methods or their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

5. 发明专利

AU2016200448A1 MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF 未知
公开(公告)号：AU2016200448A1
公开(公告)日：2016-02-18
申请号：AU2016200448
申请日：2016-01-27
申请人： PGI DRUG DISCOVERY LLC , SUNOVION PHARMACEUTICALS INC
发明人： SHAO LIMING , CAMPBELL JOHN EMERSON , HEWITT MICHAEL CHARLES , CAMPBELL UNA , HANANIA TALEEN G
IPC分类号： C07D333/56 , A61K31/381 , A61P25/00 , A61P25/18 , C07D495/04 , C07D495/20
摘要： Provided herein are multicyclic compounds, methods or their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

6. 发明专利

AU2016200448B2 MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF 未知
公开(公告)号：AU2016200448B2
公开(公告)日：2017-11-09
申请号：AU2016200448
申请日：2016-01-27
申请人： PGI DRUG DISCOVERY LLC , SUNOVION PHARMACEUTICALS INC
发明人： SHAO LIMING , CAMPBELL JOHN EMERSON , HEWITT MICHAEL CHARLES , CAMPBELL UNA , HANANIA TALEEN G
IPC分类号： C07D333/56 , A61K31/381 , A61P25/00 , A61P25/18 , C07D495/04 , C07D495/20
摘要： Provided herein are multicyclic compounds, methods or their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

7. 发明专利

DK2507245T3 MULTICYKLISKE FORBINDELSER OG FREMGANGSMÅDER TIL ANVENDELSE HERAF 未知
公开(公告)号：DK2507245T3
公开(公告)日：2017-05-22
申请号：DK10835185
申请日：2010-12-03
申请人： SUNOVION PHARMACEUTICALS INC , PGI DRUG DISCOVERY LLC
发明人： SHAO LIMING , CAMPBELL JOHN EMERSON , HEWITT MICHAEL CHARLES , CAMPBELL UNA , HANANIA TALEEN G
IPC分类号： C07D495/04 , A61K31/381 , A61P25/00 , A61P25/18 , C07D333/56 , C07D495/20

8. 发明专利

NZ626068A Multicyclic compounds and methods of use thereof 未知
公开(公告)号：NZ626068A
公开(公告)日：2016-06-24
申请号：NZ62606810
申请日：2010-12-03
申请人： SUNOVION PHARMACEUTICALS INC , PGI DRUG DISCOVERY LLC
发明人： CAMPBELL JOHN EMMERSON , CAMPBELL UNA , HANANIA TALEEN G , HEWITT MICHAEL CHARLES , SHAO LIMING
IPC分类号： C07D495/04 , A61K31/35 , A61K31/381 , A61P25/00 , A61P25/18
摘要： Disclosed are thieno[3,2-c]pyran derivatives as represented by the general formula (IIa) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: R1 and R2 are each independently hydrogen, alkyl, or cycloalkyl, each of which is optionally substituted, or R1 and R2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclyl or heteroaryl, wherein at least one of R1 and R2 is not hydrogen; R3 and R4 are each independently (i) hydrogen or optionally substituted alkyl; or (ii) R3 and R4 together with the carbon atom to which they are attached form an optionally substituted cycloalkyl or heterocyclyl ring; or (iii) R3 and R1 together with the atoms to which they are attached form an optionally substituted heterocyclyl, and R4 is hydrogen; or (iv) R3 and R4 are combined together to form a double bond and together with R1 and/or R2 and the atoms to which they are attached form an optionally substituted heteroaryl; R5 is hydrogen or optionally substituted alkyl; R6 and R7 are each independently (i) hydrogen, halo, alkyl, alkoxyl, aminoalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or aralkyl, each of which is optionally substituted; or (ii) –(CH2)p–R11, wherein R11 is heteroaryl; m is 0; n is 1; and each occurrence of p is 0; wherein the substituents and terms such as hydrogen, alkyl, alkenyl, cycloalkyl, alkoxyl, aminoalkyl etc. are as defined herein. Representative compounds include N,N-dimethyl-6,7-dihydro-4H-thieno[3,2-c]pyran-4-methanamine, N-methyl-6,7-dihydro-4H-thieno[3,2-c]pyran-4-methanamine, N-methyl-2-(pyridin-4-yl)-6,7-dihydro-4H-thieno[3,2-c]pyran-4-methanamine, 2-methyl-4-(pyrrolidin-1-ylmethyl)-6,7-dihydro-4H-thieno[3,2-c]pyran, 4-(pyrrolidin-2-yl)-6,7-dihydro-4H-thieno[3,2-c]pyran and N-methyl-1-(6,7-dihydro-4H-thieno[3,2-c]pyran-4-yl)cyclopropylamine. Also disclosed is a pharmaceutical composition comprising a compound as defined above, or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable excipient or carrier for treating, preventing, or managing a neurological disorder in a subject, particularly where the disorder is psychosis, schizophrenia or a delusional disorder.

9. 发明专利

NZ767139A Multicyclic compounds and methods of use thereof 未知
公开(公告)号：NZ767139A
公开(公告)日：2022-08-26
申请号：NZ76713910
申请日：2010-12-03
申请人： SUNOVION PHARMACEUTICALS INC , PGI DRUG DISCOVERY LLC
发明人： SHAO LIMING , CAMPBELL JOHN , HEWITT MICHAEL , CAMPBELL UNA , HANANIA TALEEN
IPC分类号： A61K31/381 , A61P25/00 , A61P25/18 , C07D333/78
摘要： Disclosed are cyclopenta[b]thiophene compounds of general formula (I), wherein X and Y are CH2; Z2 is C; Z3 is S; Z1 is C; R5 is hydrogen; R6 and R7 are each independently hydrogen, halo or alkyl; m is 0; n is 0; and wherein the remaining substituents are as defined herein. Representative compounds include 1-(3-methyl-5,6-dihydro-4H-cyclopenta[b]thiophen-4-yl)-N-methylmethanamine. Medicaments comprising the compounds are provided for use in treating neurological disorders such as schizophrenia, psychotic disorders, Parkinson’s psychosis, bipolar disorder, Alzheimer’s disease agitation, attention deficit disorder, attention deficit hyperactivity disorder, Tourette’s syndrome, post-traumatic stress disorder, depression, obsessive compulsive disorder, narcolepsy, substance abuse or dependency, autism and the like.

10. 发明专利

NZ748531A Multicyclic compounds and methods of use thereof 未知
公开(公告)号：NZ748531A
公开(公告)日：2020-09-25
申请号：NZ74853110
申请日：2010-12-03
申请人： SUNOVION PHARMACEUTICALS INC , PGI DRUG DISCOVERY LLC
发明人： CAMPBELL JOHN , CAMPBELL UNA , HANANIA TALEEN , HEWITT MICHAEL , SHAO LIMING
IPC分类号： C07D495/04 , A61K31/35 , A61K31/381 , A61P25/00 , A61P25/18 , C07D333/56 , C07D495/20
摘要： Disclosed are 6,7-dihydro-4H-thieno[3,4-c]pyran-4-yl)methanamine derivatives and analogues as represented by the general formula (IIIa), or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 and R2 are each independently (i) hydrogen, alkyl, alkoxyl, aminoalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or aralkyl, each of which is optionally substituted; or (ii) –(CH2)p–R8; or (iii) R1 and R2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclyl or heteroaryl; R3 and R4 are each independently (i) hydrogen, alkyl, alkoxyl, aminoalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or aralkyl, each of which is optionally substituted; or (ii) –(CH2)p–R9; or (iii) R3 and R4 together with the carbon atom to which they are attached form an optionally substituted cycloalkyl or heterocyclyl; or (iv) R3 and R1 together with the atoms to which they are attached form an optionally substituted heterocyclyl, and R4 is (i) or (ii); or (v) R3 and R4 are combined together to form a double bond and together with R1 and/or R2 and the atoms to which they are attached form an optionally substituted heteroaryl; R5 is (i) hydrogen, alkyl, alkoxyl, aminoalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or aralkyl, each of which is optionally substituted; or (ii) –(CH2)p–R10; or (iii) R5 and R1 together with the atoms to which they are attached form an optionally substituted heterocyclyl; R6 and R7 are each independently (i) hydrogen, halo, alkyl, alkoxyl, aminoalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, or aralkyl, each of which is optionally substituted; or (ii) –(CH2)p–R11; or (iii) R6 and R7 together with the atoms to which they are attached form an optionally substituted aryl, heteroaryl, cycloalkyl or heterocyclyl ring; m is 0, 1, or 2; n is 0, 1, or 2; and each occurrence of p is independently 0, 1, or 2; and wherein the remaining substituents are as defined herein. Representative compounds include (6,7-dihydro-4H-thieno[3,4-c]pyran-4-yl)methanamine; N-methyl-(6,7-dihydro-4H-thieno[3,4-c]pyran-4-yl)methanamine; and (1,3-dimethyl-6,7-dihydro-4H-thieno[3,4-c]pyran-4-yl)methanamine. Also disclosed are methods for making the compounds and pharmaceutical compositions comprising them for the treatment, prevention, or management of a neurological disorders such as psychosis, schizophrenia, bipolar disorder, Alzheimer’s disease agitation, attention deficit disorder or attention deficit hyperactivity disorder.

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