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1.发明申请PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开作为β-分泌酶抑制剂的全氟化环丙氯联-1,3-氧化物-2-胺化合物及其使用方法公开(公告)号：US20150252011A1
公开(公告)日：2015-09-10
申请号：US14691715
申请日：2015-04-21
Applicant: AMGEN INC.
Inventor： Ana Elena Minatti , Jonathan D. LOW , Jennifer R. ALLEN , Albert AMEGADZIE , James BROWN , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Patricia LOPEZ , Vu Van MA , Nobuko NISHIMURA , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Kelvin SHAM , Adrian L. SMITH , Ryan WHITE , Qiufen XUE
IPC: C07D265/12 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D413/12 , C07D471/04
CPC classification number: C07D413/12 , C07D265/12 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的每个R a，R b，R 1，R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。
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2.发明申请PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 有权作为β-分泌酶抑制剂的全氟化环丙氯联-1,3-氧化物-2-胺化合物及其使用方法公开(公告)号：US20140275058A1
公开(公告)日：2014-09-18
申请号：US14199844
申请日：2014-03-06
Applicant: AMGEN INC.
Inventor： Ana Elena MINATTI , Jonathan D. LOW , Jennifer R. ALLEN , Albert AMEGADZIE , James BROWN , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Patricia LOPEZ , Vu Van MA , Nobuko NISHIMURA , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Kelvin SHAM , Adrian L. SMITH , Ryan WHITE , Qiufen XUE
IPC: C07D471/04 , C07D265/12 , C07D417/12 , C07D417/14 , C07D413/12 , C07D413/14
CPC classification number: C07D413/12 , C07D265/12 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的每个R a，R b，R 1，R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。
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3.发明申请公开(公告)号：US20170267673A1
公开(公告)日：2017-09-21
申请号：US15354877
申请日：2016-11-17
Applicant: AMGEN INC.
Inventor： Jennifer R. ALLEN , Albert AMEGADZIE , Matthew P. BOURBEAU , James A. BROWN , Jian J. CHEN , Yuan CHENG , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Longbin LIU , Qingyian LIU , Jonathan D. LOW , Vu Van MA , James R. MANNING , Ana Elena MINATTI , Thomas T. NGUYEN , Nobuko NISHIMURA , Mark H. NORMAN , Liping H. PETTUS , Alexander J. PICKRELL , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Aaron C. SIEGMUND , Markian M. STEC , Ryan D. WHITE , Qiufen XUE
IPC: C07D417/12 , C07D417/14 , C07D471/04 , C07D279/08 , C07D417/04 , C07D513/10
CPC classification number: C07D417/12 , C07D279/08 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/10
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
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4.发明申请Cyclopropyl Fused Thiazin-2-Amine Compounds as Beta-Secretase Inhibitors and Methods of Use 有权环丙基稠合噻嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法公开(公告)号：US20160046618A1
公开(公告)日：2016-02-18
申请号：US14819256
申请日：2015-08-05
Applicant: AMGEN INC.
Inventor： Jennifer R. ALLEN , Albert AMEGADZIE , Matthew P. BOURBEAU , James A. BROWN , Jian J. CHEN , Yuan CHENG , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Longbin LIU , Qingyian LIU , Jonathan D. LOW , Vu Van MA , James MANNING , Ana Elena MINATTI , Thomas T. NGUYEN , Nobuko NISHIMURA , Mark H. NORMAN , Liping H. PETTUS , Alexander J. PICKRELL , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Aaron C. SIEGMUND , Markian M. STEC , Ryan D. WHITE , Qiufen XUE
IPC: C07D417/12 , C07D471/04 , C07D513/10 , C07D417/14
CPC classification number: C07D417/12 , C07D279/08 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/10
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 所述化合物具有通式I：其中式I中的变量A4，A5，A6，A8以及R 1，R b，R 1，R 2，R 3和R 7各自独立地定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。
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公开(公告)号：US20150045361A1
公开(公告)日：2015-02-12
申请号：US14520899
申请日：2014-10-22
Applicant: AMGEN INC.
Inventor： Yi CHEN , Timothy D. CUSHING , Jason A. DUQUETTE , Felix GONZALEZ LOPEZ DE TURISO , Xiaolin HAO , Xiao HE , Brian S. LUCAS , Lawrence R. MCGEE , Andreas REICHELT , Robert M. RZASA , Jennifer L. SEGANISH , Youngsook SHIN , Dawei ZHANG
IPC: C07D487/04 , C07D471/04
CPC classification number: C07D487/04 , C07D471/04 , C07D473/30 , C07D473/34
Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
Abstract translation: 取代的双环杂芳基和含有它们的组合物，用于治疗一般炎症，关节炎，风湿性疾病，骨关节炎，炎性肠病，炎症性眼病，炎症性或不稳定性膀胱病，牛皮癣，皮肤炎症成分的投诉，慢性炎性病症 不限于自身免疫疾病如系统性红斑狼疮（SLE），重症肌无力，类风湿性关节炎，急性播散性脑脊髓炎，特发性血小板减少性紫癜，多发性硬化症，Sjoegren综合征和自身免疫性溶血性贫血，包括所有形式的超敏反应的过敏症状 包括但不限于白血病，如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增生性疾病（MPD）慢性骨髓性白血病（MPD），介导，依赖或与p110δ活性相关的癌症的方法 （CML）T细胞急性淋巴细胞白血病（T-ALL）B细胞急性淋巴细胞白血病（B-ALL）非霍奇金淋巴瘤（NHL）B细胞淋巴瘤和实体瘤如乳腺癌。
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Patent Agency Ranking
6.发明申请PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 审中-公开作为β-分泌酶抑制剂的全氟化环丙氯联-1,3-氧化物-2-胺化合物及其使用方法公开(公告)号：US20160280695A1
公开(公告)日：2016-09-29
申请号：US14932787
申请日：2015-11-04
Applicant: AMGEN INC.
Inventor： Ana Elena MINATTI , Jonathan D. LOW , Jennifer R. ALLEN , Albert AMEGADZIE , James BROWN , Michael J. FROHN , Angel GUZMAN-PEREZ , Paul E. HARRINGTON , Patricia LOPEZ , Vu Van MA , Nobuko NISHIMURA , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Kelvin SHAM , Adrian L. SMITH , Ryan WHITE , Qiufen XUE
IPC: C07D413/12
CPC classification number: C07D413/12 , C07D265/12 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Abstract translation: 其中式I的Ra，Rb，R1，R2，R3和R7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及该化合物和组合物用于治疗由BACE的生物学活性产生的与A-β斑块形成和沉积有关的病症和/或病症的用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明还提供式II和III的化合物及其分子式实施方案，用于制备本发明化合物的中间体和方法。
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公开(公告)号：US20160176874A1
公开(公告)日：2016-06-23
申请号：US15058023
申请日：2016-03-01
Applicant: AMGEN INC.
Inventor： Jennifer R. ALLEN , Jian J. CHEN , Michael J. FROHN , Matthew R. KALLER , Qingyian LIU , Thomas T. NGUYEN , Alexander J. PICKRELL , Wenyuan QIAN , Robert M. RZASA , Wenge ZHONG
IPC: C07D471/04 , C07D403/14 , C07D401/14
CPC classification number: C07D471/04 , A61K31/497 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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8.发明申请PERFLUORINATED 5,6-DIHYDRO-4H-1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE 有权全氟化的5,6-二氢-4H-1,3-氧杂环丁-2-胺化合物作为β-分泌酶抑制剂和使用方法公开(公告)号：US20140249104A1
公开(公告)日：2014-09-04
申请号：US14192710
申请日：2014-02-27
Applicant: AMGEN INC.
Inventor： Ana Elena MINATTI , Jonathan D. LOW , Jennifer R. ALLEN , Jian CHEN , Ning CHEN , Yuan CHENG , Ted JUDD , Qingyian LIU , Patricia LOPEZ , Wenyuan QIAN , Shannon RUMFELT , Robert M. RZASA , Nuria A. TAMAYO , Qiufen XUE , Bryant YANG , Wenge ZHONG
IPC: C07D413/14 , C07F7/08 , C07D513/04 , C07D413/12 , C07D471/04
CPC classification number: C07D413/14 , C07D265/08 , C07D413/04 , C07D413/10 , C07D413/12 , C07D471/04 , C07D498/04 , C07D513/04 , C07F7/0812
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of R1 and R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.
Abstract translation: 本发明提供了一类可用于调节β-分泌酶（BACE）活性的化合物。 化合物具有通式I：其中式I中的各个R 1和R 2，R 3和R 7各自独立地定义的变量A4，A5，A6，A8在本文中定义。 本发明还提供包含该化合物的药物组合物，以及用于治疗由BACE的生物学活性产生的A-β斑块形成和沉积相关的病症和/或病症的化合物和组合物的相应用途。 这种BACE介导的疾病包括例如阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。 本发明进一步提供式II和III的化合物及其分式实施方案，可用于制备式I-III化合物的中间体和方法和方法。
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公开(公告)号：US20200048265A1
公开(公告)日：2020-02-13
申请号：US16656328
申请日：2019-10-17
Applicant: AMGEN INC.
Inventor： Yi CHEN , Timothy D. CUSHING , Jason A. DUQUETTE , Felix GONZALEZ LOPEZ DE TURISO , Xiaolin HAO , Xiao HE , Brian S. LUCAS , Lawrence R. MCGEE , Andreas REICHELT , Robert M. RZASA , Jennifer L. SEGANISH , Youngsook SHIN , Dawei ZHANG
IPC: C07D487/04 , C07D473/30 , C07D473/34 , C07D471/04
Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
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公开(公告)号：US20180105532A1
公开(公告)日：2018-04-19
申请号：US15841153
申请日：2017-12-13
Applicant: AMGEN INC.
Inventor： Yi CHEN , Timothy D. CUSHING , Jason A. DUQUETTE , Felix GONZALEZ LOPEZ DE TURISO , Xiaolin HAO , Xiao HE , Brian S. LUCAS , Lawrence R. MCGEE , Andreas REICHELT , Robert M. RZASA , Jennifer L. SEGANISH , Youngsook SHIN , Dawei ZHANG
IPC: C07D487/04 , C07D471/04 , C07D473/30 , C07D473/34
CPC classification number: C07D487/04 , C07D471/04 , C07D473/30 , C07D473/34
Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
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