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1. 发明公开

EP2435424A1 ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C 失效转让
标题翻译： THREE彼此相关芳基单元组合抗病毒化合物FOR疾病，如肝炎C的治疗
公开(公告)号：EP2435424A1
公开(公告)日：2012-04-04
申请号：EP10721906.5
申请日：2010-05-28
申请人： Schering Corporation
发明人： ZENG, Qingbei , CHEN, Kevin, X. , ANILKUMAR, Gopinadhan, N. , ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George
IPC分类号： C07D403/14 , A61P31/12 , A61K31/4184
CPC分类号： C07D403/14
摘要： The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56

2. 发明授权

EP1902046B1 PIPERIDINE DERIVATIVES USEFUL AS HISTAMINE H3 ANTAGONISTS 有权
标题翻译：作为组胺H3 SUITABLE哌啶拮抗剂
公开(公告)号：EP1902046B1
公开(公告)日：2009-12-02
申请号：EP06773528.2
申请日：2006-06-19
申请人： Schering Corporation
发明人： ASLANIAN, Robert, G. , BERLIN, Michael, Y. , BOYCE, Christopher, W. , CHAO, Jianhua , DE LERA RUIZ, Manuel , MANGIARACINA, Pietro , MCCORMICK, Kevin, D. , MUTAHI, Mwangi, W. , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang , SOLOMON, Daniel, M. , TOM, Wing, C. , VACCARO, Henry, A. , ZHENG, Junying , ZHU, Xiaohong
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61P3/04 , A61P29/00 , A61P37/00 , C07D409/14 , C07D471/04
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are novel compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is -C(=O)-, -C(=S)-, -(CH2)q-, -C(=NOR7)- or -SO1-2-; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula (II) where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, -C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.

3. 发明公开

EP1996577A1 HETEROCYCLIC SUBSTITUTED PYRIDINE COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 失效转让
标题翻译： WITH CXCR3拮抗剂活性的杂环取代的吡啶
公开(公告)号：EP1996577A1
公开(公告)日：2008-12-03
申请号：EP07753453.5
申请日：2007-03-19
申请人： Schering Corporation , PHARMACOPEIA, INC.
发明人： ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A. , SHIH, Neng-Yang , MCGUINNESS, Brian, F. , HOBBS, Douglas, W.
IPC分类号： C07D401/14 , C07D413/14 , A61K31/497 , A61P29/00 , A61P37/06
CPC分类号： C07D401/14 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

4. 发明公开

EP1848710A2 HETEROCYCLIC SUBSTITUTED PIPERAZINES WITH CXCR3 ANTAGONIST ACTIVITY 失效转让
标题翻译：与CXCR3拮抗剂活性的杂环取代的哌嗪
公开(公告)号：EP1848710A2
公开(公告)日：2007-10-31
申请号：EP06735000.9
申请日：2006-02-14
申请人： Schering Corporation , PHARMACOPEIA, INC.
发明人： KIM, Seong, Heon , ANILKUMAR, Gopinadhan, N. , WONG, Michael, K. C. , ZENG, Qingbei , ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A. , SHAO, Yuefei , MC GUINNESS, Brian, F. , HOBBS, Douglas, W.
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , A61K31/445 , A61K31/495
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1 or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non limiting example(s) include, psoriasis), autoimmune diseases (non limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

5. 发明授权

EP1121354B1 N-(IMIDAZOLYLALKYL)SUBSTITUTED CYCLIC AMINES AS HISTAMINE-H 3 AGONISTS OR ANTAGONISTS 有权
标题翻译： N-咪唑烷基取代的环状胺作为组胺H3激动剂或拮抗剂
公开(公告)号：EP1121354B1
公开(公告)日：2004-12-08
申请号：EP99954622.9
申请日：1999-10-15
申请人： SCHERING CORPORATION
发明人： WOLIN, Ronald , ROSENBLUM, Stuart, B. , AFONSO, Adriano
IPC分类号： C07D401/06 , C07D233/56 , A61K31/4164 , A61P25/00
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention discloses novel N(imidazolylalkyl)-substituted cyclic amine compounds of Formula (I), wherein R1 is selected from the group consisting of H,OCO-R7, andCO2R7 with R7 being a substituted or unsubstituted alkyl or aryl, the substituents on said substituted alkyl or aryl being selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, heterocyclic and halogen; R2 is selected from the group consisting of H, hydroxyl or halogen; G is spacer moiety selected from the group consisting of a C3-C7 straight chain alkyl, a C2-C7 alkene or a C2-C7 alkyne, with said straight chain alkyl, alkene or alkyne being optionally substituted with one or more R7 groups; and T which represents a cyclic amine is a ring moiety selected from the group consisting of a, b, c or d, wherein n is an integer for 0-3, and R3, R4, R5 and R6 can be the same or different with the proviso that any two of said R3, R4, R5 and R6 can be bound to the same or different carbon atom of ring T, with said R3, R4, R5 and R6 being independently selected from the group consisting of H, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C1-C6 alkenyl, substituted or unsubstituted C1-C6 alkynyl, aryl, aralkyl, alkylaryl, cycloalkyl, heterocyclic,C-O- R8,C(=O)R8, CO2R8, OC(O)R8, NH2,NHR8, N(R8)2, NR8R9, SR8, SO2R8, S(O)R8, OH,OR8, CH2OR8, CH2NH2, CH2N(R8)2, CH2NHR8, CH2SR8, C(O)-NHR8, C(O)NR8R9, CN,NO2, NR8-CO-, C(NH)-NR8, C(=NR8)NR9, NR8-C(NH)-, NHR8(CO)NHR9, (O-CR8-CR8-O)-, CX(R8)2, CX2R8, CX3,OCX3, N(R8)-S(O)R9, N(R8)-SO2R9, (=O), (=NH-OR8), C(=S)R8,NCR8, NOR8,NR8R9-SO2-NR8R9, OPO2R8, P+(R8)3X,SO3H, fused heteroaryl, and (=CR8) wherein R8 and R9 are independently H or C1-C6 alkyl, aryl, aralkyl, alkylaryl, cycloalkyl or heterocyclic, and X is a halogen which have excellent histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat allergy, inflammatory and CNS-related diseases.

6. 发明公开

EP1326858A2 PIPERIDINE COMPOUNDS AS ANTI-ALLERGIC 有权
标题翻译：哌啶使用AS抗过敏药
公开(公告)号：EP1326858A2
公开(公告)日：2003-07-16
申请号：EP01983968.7
申请日：2001-10-15
申请人： Schering Corporation
发明人： ASLANIAN, Robert, G. , SHIH, Neng-Yang , TING, Pauline, C. , BERLIN, Michael, Y. , ROSENBLUM, Stuart, B. , MC CORMICK, Kevin, D. , TOM, Wing, C. , BOYCE, Christopher, W. , MANGIARACINA, Pietro , MUTAHI, Mwangi, Wa , PIWINSKI, John, J.
IPC分类号： C07D401/14 , C07D413/14 , C07D401/12 , C07D409/14 , C07D498/04 , C07D417/14
CPC分类号： C07D213/73 , A61K31/435 , A61K31/445 , A61K31/495 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： Disclosed are novel compounds of the formula: (I) Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I). Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula (I) in combination with a H1 receptor antagonist.

7. 发明公开

EP1121354A1 N-(IMIDAZOLYLALKYL)SUBSTITUTED CYCLIC AMINES AS HISTAMINE-H 3? AGONISTS OR ANTAGONISTS 有权
标题翻译： N-咪唑烷基取代的环状胺作为组胺H3激动剂或拮抗剂
公开(公告)号：EP1121354A1
公开(公告)日：2001-08-08
申请号：EP99954622.9
申请日：1999-10-15
申请人： SCHERING CORPORATION
发明人： WOLIN, Ronald , ROSENBLUM, Stuart, B. , AFONSO, Adriano
IPC分类号： C07D401/06 , C07D233/56 , A61K31/4164 , A61P25/00
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention discloses novel N(imidazolylalkyl)-substituted cyclic amine compounds of Formula (I), wherein R1 is selected from the group consisting of H,OCO-R7, andCO2R7 with R7 being a substituted or unsubstituted alkyl or aryl, the substituents on said substituted alkyl or aryl being selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, heterocyclic and halogen; R2 is selected from the group consisting of H, hydroxyl or halogen; G is spacer moiety selected from the group consisting of a C3-C7 straight chain alkyl, a C2-C7 alkene or a C2-C7 alkyne, with said straight chain alkyl, alkene or alkyne being optionally substituted with one or more R7 groups; and T which represents a cyclic amine is a ring moiety selected from the group consisting of a, b, c or d, wherein n is an integer for 0-3, and R3, R4, R5 and R6 can be the same or different with the proviso that any two of said R3, R4, R5 and R6 can be bound to the same or different carbon atom of ring T, with said R3, R4, R5 and R6 being independently selected from the group consisting of H, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C1-C6 alkenyl, substituted or unsubstituted C1-C6 alkynyl, aryl, aralkyl, alkylaryl, cycloalkyl, heterocyclic,C-O- R8,C(=O)R8, CO2R8, OC(O)R8, NH2,NHR8, N(R8)2, NR8R9, SR8, SO2R8, S(O)R8, OH,OR8, CH2OR8, CH2NH2, CH2N(R8)2, CH2NHR8, CH2SR8, C(O)-NHR8, C(O)NR8R9, CN,NO2, NR8-CO-, C(NH)-NR8, C(=NR8)NR9, NR8-C(NH)-, NHR8(CO)NHR9, (O-CR8-CR8-O)-, CX(R8)2, CX2R8, CX3,OCX3, N(R8)-S(O)R9, N(R8)-SO2R9, (=O), (=NH-OR8), C(=S)R8,NCR8, NOR8,NR8R9-SO2-NR8R9, OPO2R8, P+(R8)3X,SO3H, fused heteroaryl, and (=CR8) wherein R8 and R9 are independently H or C1-C6 alkyl, aryl, aralkyl, alkylaryl, cycloalkyl or heterocyclic, and X is a halogen which have excellent histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat allergy, inflammatory and CNS-related diseases.

8. 发明公开

EP2430015A1 FUSED TRICYCLIC ARYL COMPOUNDS USEFUL FOR THE TREATMENT OF VIRAL DISEASES 失效转让
标题翻译：病毒性疾病的处理的合适稠合的三环芳基化合物
公开(公告)号：EP2430015A1
公开(公告)日：2012-03-21
申请号：EP10720692.2
申请日：2010-05-12
申请人： Schering Corporation
发明人： ROSENBLUM, Stuart, B. , CHEN, Kevin, X. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , COBURN, Craig, A.
IPC分类号： C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , C07D491/044 , C07D493/04 , A61P31/12 , A61K31/4178 , A61K31/437 , A61K31/55
CPC分类号： C07D403/14 , C07C403/04 , C07D403/04 , C07D471/04 , C07D487/04 , C07D491/044 , C07D493/04
摘要： The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.

9. 发明授权

EP1937666B1 SUBSTITUTED HETEROCYCLIC COMPOUNDS WITH CXCR3 ANTAGONIST ACTIVITY 失效转让
标题翻译：与CXCR3拮抗剂活性的取代的杂环化合物
公开(公告)号：EP1937666B1
公开(公告)日：2012-02-22
申请号：EP06816540.6
申请日：2006-10-10
申请人： Schering Corporation
发明人： KIM, Seong, Heon , SHANKAR, Bandarpalle, B. , KOZLOWSKI, Joseph, A. , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang
IPC分类号： C07D401/14 , C07D413/14 , A61K31/497 , A61P29/00
CPC分类号： C07D401/14 , C07D401/08 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula (1) , or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g , tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, type I diabetes, viral meningitis and tumors using a compound of Formula (1).

10. 发明公开

EP2408761A1 SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF 失效转让
标题翻译：取代的吲哚衍生物及其使用方法
公开(公告)号：EP2408761A1
公开(公告)日：2012-01-25
申请号：EP08795629.8
申请日：2008-08-27
申请人： Schering Corporation
发明人： ANILKUMAR, Gopinadhan, N. , BENNETT, Frank , CHAN, Tin-Yau , CHEN, Kevin, X. , SANNIGRAHI, Mousumi , VELAZQUEZ, Francisco , VENKATRAMAN, Srikanth , ZENG, Qingbei , DUCA, Jose, S. , LESBURG, Charles, A. , KOZLOWSKI, Joseph, A. , NJOROGE, F., George , ROSENBLUM, Stuart, B. , SHIH, Neng-Yang
IPC分类号： C07D401/04 , C07D403/04 , A61K31/513 , A61P31/12
CPC分类号： C07D403/04 , C07D401/04
摘要： The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.

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