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公开(公告)号：WO2007039462A3
公开(公告)日：2007-06-21
申请号：PCT/EP2006066540
申请日：2006-09-20
Applicant: HOFFMANN LA ROCHE , BERTHEL STEVEN JOSEPH , ERICKSON SHAWN DAVID , FOTOUHI NADER , KESTER ROBERT FRANCIS , KIM KYUNGJIN , MISCHKE STEVEN GREGORY , QIAN YIMIN , THAKKAR KSHITIJ CHHABILBHAI , TILLEY JEFFERSON WRIGHT , WANG HONG
Inventor： BERTHEL STEVEN JOSEPH , ERICKSON SHAWN DAVID , FOTOUHI NADER , KESTER ROBERT FRANCIS , KIM KYUNGJIN , MISCHKE STEVEN GREGORY , QIAN YIMIN , THAKKAR KSHITIJ CHHABILBHAI , TILLEY JEFFERSON WRIGHT , WANG HONG
IPC: C07D401/06 , A61K31/4184
CPC classification number: C07D401/04 , C07D401/14 , C07D471/04
Abstract: Provided herein are compounds of the formula (I): wherein A, R 1 , R 2 , R 4 , R a and R b are as those disclosed in the specification, as well as pharmaceutically acceptable salts thereof. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of obesity, hyperphagia, anxiety, depression and related disorders and diseases.
Abstract translation: 本文提供了式（I）的化合物：其中A，R 1，R 2，R 4，R 5， 并且如本说明书中公开的那些，以及其药学上可接受的盐。 这些化合物和含有它们的药物组合物可用于治疗肥胖症，食欲过盛，焦虑症，抑郁症和相关病症和疾病。
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2.发明申请DISUBSTITUTED PYRAZOLOBENZODIAZEPINES USEFUL AS INHIBITORS FOR CDK2 AND ANGIOGESIS, AND FOR THE TREATMENT OF BREAST, COLON, LUNG AND PROSTATE CANCER 审中-公开作为CDK2和ANGIOGESIS的抑制剂，用于治疗乳腺癌，结肠癌，肺癌和前列腺癌的有用的吡唑嗪酮
公开(公告)号：WO2006040036A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/010653
申请日：2005-10-04
Applicant: F. HOFFMANN-LA ROCHE AG , LIU, Jin-Jun , LUK, Kin-Chun , PIZZOLATO, Giacomo , REN, Yi , THAKKAR, Kshitij Chhabilbhai , WOVKULICH, Peter, Michael , ZHANG, Zhuming
Inventor： LIU, Jin-Jun , LUK, Kin-Chun , PIZZOLATO, Giacomo , REN, Yi , THAKKAR, Kshitij Chhabilbhai , WOVKULICH, Peter, Michael , ZHANG, Zhuming
IPC: C07D487/04 , A61K31/5517 , A61P35/00
CPC classification number: C07D487/04
Abstract: The present invention provides compounds of the formula (I) wherein R 1 , R 2 , R 3 and R 4 are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.
Abstract translation: 本发明提供式（I）化合物，其中R
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公开(公告)号：WO2013092463A1
公开(公告)日：2013-06-27
申请号：PCT/EP2012/075716
申请日：2012-12-17
Applicant: F. HOFFMANN-LA ROCHE AG , ALAM, Muzaffar , DU BOIS, Daisy, Joe , HAWLEY, Ronald, Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana, Elena , THAKKAR, Kshitij, Chhabilbhai , WILHELM, Robert, Stephen
Inventor： ALAM, Muzaffar , DU BOIS, Daisy, Joe , HAWLEY, Ronald, Charles , KENNEDY-SMITH, Joshua , MINATTI, Ana, Elena , THAKKAR, Kshitij, Chhabilbhai , WILHELM, Robert, Stephen
IPC: C07D471/04 , A61K31/437 , A61P29/00
CPC classification number: C07D471/04
Abstract: Disclosed are compounds of Formula (I), useful for treatment of autoimmune and inflammatory diseases associated with IL-2 inhibition via modulation of calcium release-activated calcium (CRAC) channels. Also disclosed are methods of making and using the compounds for treatment of diseases associated with CRAC channels.
Abstract translation: 公开了式（I）化合物，其可用于通过调节钙释放激活的钙（CRAC）通道治疗与IL-2抑制相关的自身免疫性和炎性疾病。 还公开了制备和使用化合物治疗与CRAC通道相关疾病的方法。
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4.发明申请BIPHENYL CARBOXYLIC ACIDS AND BIOISOSTERES AS GLYCOGEN SYNTHASE ACTIVATORS 审中-公开作为GLYCOGEN SYNTHASE激活剂的联苯羧酸和生物活性成分
公开(公告)号：WO2011058154A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/067423
申请日：2010-11-15
Applicant: F. HOFFMANN-LA ROCHE AG , BOLIN, David, Robert , QIAN, Yimin , THAKKAR, Kshitij, Chhabilbhai , YI, Lin , YUN, Weiya
Inventor： BOLIN, David, Robert , QIAN, Yimin , THAKKAR, Kshitij, Chhabilbhai , YI, Lin , YUN, Weiya
IPC: C07C235/42 , C07C311/51 , C07D207/16 , C07D277/30 , C07D403/04 , A61K31/426 , A61K31/41 , A61K31/401 , A61K31/18 , A61K31/166
CPC classification number: C07C235/42 , C07C311/51 , C07C2601/02 , C07D207/16 , C07D277/56 , C07D403/04
Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Abstract translation: 本文提供式（I）化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。
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5.发明申请PYRIDO [2 , 3-D] PYRIMIDINE-2 , 4-DIAMINE COMPOUNDS AS PTPlB INHIBITORS 审中-公开PYRIDO [2，3-D] PYRIMIDINE-2，4-DIAMINE化合物作为PTPlB抑制剂
公开(公告)号：WO2007009911A1
公开(公告)日：2007-01-25
申请号：PCT/EP2006/064091
申请日：2006-07-11
Applicant: F. HOFFMANN-LA ROCHE AG , BERTHEL, Steven, Joseph , CHEUNG, Adrian, Wai-Hing , KIM, Kyungjin , LI, Shiming , THAKKAR, Kshitij, Chhabilbhai , YUN, Weiya
Inventor： BERTHEL, Steven, Joseph , CHEUNG, Adrian, Wai-Hing , KIM, Kyungjin , LI, Shiming , THAKKAR, Kshitij, Chhabilbhai , YUN, Weiya
IPC: C07D471/04 , A61P3/00 , A61K31/519
CPC classification number: C07D471/04
Abstract: The present invention is concerned with compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and X are as described in the description and claims. The compounds are inhibitors of PTP1B. Accordingly, the compounds can be used for treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 4，R 4， SUP>和X如说明书和权利要求中所述。 这些化合物是PTP1B的抑制剂。 因此，该化合物可用于治疗或预防PTP-1B介导的疾病，包括糖尿病，肥胖症和糖尿病相关疾病。
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Patent Agency Ranking
公开(公告)号：WO2012123467A1
公开(公告)日：2012-09-20
申请号：PCT/EP2012/054409
申请日：2012-03-14
Applicant: F. HOFFMANN-LA ROCHE AG , GILLESPIE, Paul , MICHOUD, Christophe , RUPERT, Kenneth Carey , THAKKAR, Kshitij Chhabilbhai , YI, Lin
Inventor： GILLESPIE, Paul , MICHOUD, Christophe , RUPERT, Kenneth Carey , THAKKAR, Kshitij Chhabilbhai , YI, Lin
IPC: C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
CPC classification number: C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14
Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.
Abstract translation: 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗炎性疾病和病症，例如哮喘和COPD。
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7.发明申请
公开(公告)号：WO2011067266A1
公开(公告)日：2011-06-09
申请号：PCT/EP2010/068590
申请日：2010-12-01
Applicant: F. HOFFMANN-LA ROCHE AG , BOLIN, David Robert , HAYDEN, Stuart , QIAN, Yimin , THAKKAR, Kshitij Chhabilbhai
Inventor： BOLIN, David Robert , HAYDEN, Stuart , QIAN, Yimin , THAKKAR, Kshitij Chhabilbhai
IPC: C07C229/14 , C07C233/47 , C07C233/48 , C07C233/51 , C07C233/63 , C07C233/83 , C07C235/12 , C07C271/22 , C07C311/06 , C07C311/14 , C07C311/19 , C07D207/16 , C07D207/28 , C07D211/60 , C07D213/81
CPC classification number: C07C233/47 , C07C229/14 , C07C233/48 , C07C233/51 , C07C233/63 , C07C233/83 , C07C235/12 , C07C271/22 , C07C311/06 , C07C311/14 , C07C311/19 , C07C2601/02 , C07C2601/04 , C07D207/16 , C07D207/28 , C07D211/60 , C07D213/81 , C07D213/82 , C07D233/90 , C07D275/02 , C07D277/56 , C07D279/02 , C07D295/215 , C07D307/24 , C07D417/06
Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
Abstract translation: 本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。
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公开(公告)号：WO2007039462A2
公开(公告)日：2007-04-12
申请号：PCT/EP2006/066540
申请日：2006-09-20
Applicant: F. HOFFMANN-LA ROCHE AG , BERTHEL, Steven Joseph , ERICKSON, Shawn David , FOTOUHI, Nader , KESTER, Robert Francis , KIM, Kyungjin , MISCHKE, Steven Gregory , QIAN, Yimin , THAKKAR, Kshitij Chhabilbhai , TILLEY, Jefferson Wright , WANG, Hong
Inventor： BERTHEL, Steven Joseph , ERICKSON, Shawn David , FOTOUHI, Nader , KESTER, Robert Francis , KIM, Kyungjin , MISCHKE, Steven Gregory , QIAN, Yimin , THAKKAR, Kshitij Chhabilbhai , TILLEY, Jefferson Wright , WANG, Hong
CPC classification number: C07D401/04 , C07D401/14 , C07D471/04
Abstract: Provided herein are compounds of the formula (I): wherein A, R 1 , R 2 , R 4 , R a and R b are as those disclosed in the specification, as well as pharmaceutically acceptable salts thereof. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of obesity, hyperphagia, anxiety, depression and related disorders and diseases.
Abstract translation: 本文提供式（I）的化合物：其中A，R 1，R 2，R 4，R a， / SUB和R bb如本说明书中公开的那些，以及其药学上可接受的盐。 这些化合物和含有它们的药物组合物可用于治疗肥胖，食欲过盛，焦虑，抑郁和相关疾病和疾病。
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公开(公告)号：WO2006050843A1
公开(公告)日：2006-05-18
申请号：PCT/EP2005/011682
申请日：2005-11-02
Applicant: F. HOFFMANN-LA ROCHE AG , BERTHEL, Steven, Joseph , CHEUNG, Adrian, Wai-Hing , THAKKAR, Kshitij, Chhabilbhai , YUN, Weiya
Inventor： BERTHEL, Steven, Joseph , CHEUNG, Adrian, Wai-Hing , THAKKAR, Kshitij, Chhabilbhai , YUN, Weiya
IPC: C07D239/42 , A61K31/517
CPC classification number: C07D401/12 , C07D239/95 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/12 , C07D409/04 , C07D413/04
Abstract: The present invention is concerned with compounds of formula (1), wherein R 1 , R 2 and X are as defined in the description and claims. The compounds of the present invention are PTP-1B inhibitors and can be used as medicaments.
Abstract translation: 本发明涉及式（1）的化合物，其中R 1，R 2和X如说明书和权利要求中所定义。 本发明的化合物是PTP-1B抑制剂，可用作药物。
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10.发明申请DIAMINOPYRROLOQUINAZOLINES COMPOUNDS AS PROTEIN TYROSINE PHOSPHATASE INHIBITORS 审中-公开作为蛋白酪氨酸磷酸酶抑制剂的二氨基吡咯烷酮化合物
公开(公告)号：WO2004101569A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/004978
申请日：2004-05-10
Inventor： BERTHEL, Steven, Joseph , THAKKAR, Kshitij, Chhabilbhai
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: This Invention relates to diaminopyrroloquinazoline compounds of formula (I) wherein R1, R2, R3, Ra, Rb, Rc, Rd, Re, Rf and A are as defined in the description and Claims, which are useful for inhibiting protein tyrosine phosphatases, particularly PTP1B, and are useful for lowering blood glucose concentrations in mammals.
Abstract translation: 本发明涉及式（I）的二氨基吡咯并喹唑啉化合物，其中R1，R2，R3，Ra，Rb，Rc，Rd，Re，Rf和A如说明书和权利要求中所定义，其可用于抑制蛋白酪氨酸磷酸酶，特别是 PTP1B，可用于降低哺乳动物血糖浓度。
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