Patent search ap:("SQUIBB BRISTOL MYERS CO") AND inv:"TINO JOSEPH A" Page 1

1.

发明申请
PHOSPHONATE AND PHOSPHINATE COMPOUNDS AS GLUCOKINASE ACTIVATORS 审中-公开
Title translation: 磷酸酯和磷酸酯化合物作为GLUCOKINASE激活剂

公开(公告)号：WO2008005964A3

公开(公告)日：2008-03-06

申请号：PCT/US2007072708

申请日：2007-07-03

Applicant: SQUIBB BRISTOL MYERS CO , RYONO DENNIS E , CHENG PETER T W , BOLTON SCOTT A , CHEN SEAN S , SHI YAN , MENG WEI , TINO JOSEPH A , ZHANG HAO , SULSKY RICHARD B

Inventor： RYONO DENNIS E , CHENG PETER T W , BOLTON SCOTT A , CHEN SEAN S , SHI YAN , MENG WEI , TINO JOSEPH A , ZHANG HAO , SULSKY RICHARD B

IPC: C07F9/32 , A61K31/675 , A61P3/00 , C07F9/40

CPC classification number: C07F9/6539 , C07F9/582 , C07F9/587 , C07F9/65032 , C07F9/650964 , C07F9/650982 , C07F9/65181

Abstract: Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure of Formula (I), wherein Formula (II) is a heteroaryl ring; R 4 is -(CH 2 ) n -Z-(CH 2 ) m -PO(OR 7 )(OR 8 ), -(CH 2 ) n Z-(CH 2 ) m -PO(OR 7 )R 9 , -(CH 2 ) n -Z-(CH 2 ) m -OPO(OR 7 )R 9 , -(CH 2 ) n Z-(CH 2 ) m -OPO(R 9 )(R 10 ), or -(CH 2 ) n Z-(CH 2 ) m -PO(R 9 )(R 10 ); R 5 and R 6 are independently selected from H, alkyl and halogen; Y is R 7 (CH 2 ) s or is absent; and X, n, Z, m, R 4 , R 5 , R 6 , R 7 , and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

Abstract translation: 提供了膦酸酯和次膦酸酯活化剂的化合物，因此可用于治疗糖尿病和相关疾病，并具有式（I）的结构，其中式（II）是杂芳基环; R 4是 - （CH 2 CH 2）n - （Z）（CH 2）n - （OR 7）（OR 8）， - （CH 2 CH 2）n - Z - （ CH 2 OR 2（OR 7）R 9， - （CH 2 CH 2） SUB>）_{名词 -Z-（CH _{2 ）_{米 -OPO（OR _{7 ）R _{9 - （CH 2）n - Z - （CH 2）2 - （O） - （CH 2）n - （R 10），或 - （CH 2）n - Z - （CH 2） 2 ）_{米 -PO（R _{9 ）（R _{10 ）; R 5和R 6独立地选自H，烷基和卤素; Y是R 7（CH 2）2，或不存在; 和X，n，Z，m，R 4，R 5，R 6，R 7，和 s如本文所定义; 或其药学上可接受的盐。还提供了使用上述化合物治疗糖尿病和相关疾病的方法。}}}}}}}}

2.

发明申请
HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
Title translation: 杂环芳族化合物可用作生长激素的秘密

公开(公告)号：WO0054729A3

公开(公告)日：2001-01-11

申请号：PCT/US0005704

申请日：2000-03-02

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： ROBL JEFFREY , TINO JOSEPH A , HERNANDEZ ANDRES S , LI JAMES J , LI JUN , SWARTZ STEPHEN G

IPC: C07D249/08 , A61K31/41 , A61K31/4174 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/565 , A61K31/568 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P13/12 , A61P17/02 , A61P19/10 , A61P21/00 , A61P31/18 , C07D233/54 , C07D233/64 , C07D235/10 , C07D235/14 , C07D249/12 , C07D257/04 , C07D263/32 , C07D271/06 , C07D277/20 , C07D277/28 , C07D277/56 , C07D277/64 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , A61P5/08 , A61P5/48 , C07D403/14 , C07D413/14

CPC classification number: C07D233/54 , C07D235/14 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/64 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12

Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have structure (I) including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably (a), (b) or (c) and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.

Abstract translation: 提供了可用于刺激生长激素的内源性生产或释放以及治疗肥胖症，骨质疏松症（改善骨密度）和改善肌肉质量和肌肉力量的杂环芳族化合物。杂环芳族化合物具有包括其药学上可接受的盐和其全部立体异构体的结构（I），其中X a是杂芳基，优选（a），（b）或（c）和R 1，R 1a，R 6，Y，X b，A，B ，Z，R3，R4，R4a，R5和R5a如本文所定义。

3.

发明申请
SUBSTITUTED TETRAHYDROCARBAZOLE AND CARBAZOLE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
Title translation: 用作激酶抑制剂的替代四氯化碳和卡博唑酰胺化合物

公开(公告)号：WO2014210085A9

公开(公告)日：2015-12-23

申请号：PCT/US2014043978

申请日：2014-06-25

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： TINO JOSEPH A , SRIVASTAVA ANURAG S , KO SOO SUNG , GALELLA MICHAEL A , LANGEVINE CHARLES M , DELUCCA GEORGE V , LIU QINGJIE , BATT DOUGLAS G , WATTERSON SCOTT HUNTER , SHI QING , BERTRAND MYRA BEAUDOIN

IPC: C07D403/10 , A61K31/429 , A61K31/513 , A61K31/517 , A61K31/522 , A61P29/00 , A61P37/00 , C07D471/04 , C07D513/04

CPC classification number: C07D513/04 , C07B2200/07 , C07B2200/13 , C07D209/88 , C07D239/70 , C07D403/10 , C07D471/04

Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, CN, or CH3; R2 is Cl or CH3; R3 is C(CH3)2OH or CH2CH2OH; Ra is H or CH3; each R6 is independently F, Cl, CH3, and/or OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

Abstract translation: 公开了式（I）的化合物，其中：两条虚线表示两个单键或双键; Q是：R1是F，Cl，CN或CH3; R2是Cl或CH3; R3是C（CH3）2OH或CH2CH2OH; Ra为H或CH3; 每个R 6独立地是F，Cl，CH 3和/或OCH 3; 并且n为0,1或2.还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

4.

发明申请
HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
Title translation: 杂环芳族化合物可用作生长激素的秘密

公开(公告)号：WO2004021984A3

公开(公告)日：2004-11-25

申请号：PCT/US0327513

申请日：2003-09-02

Applicant: SQUIBB BRISTOL MYERS CO , YU GUIXUE , LI JUN , EWING WILLIAM R , SULSKY RICHARD B , LI JAMES J , TINO JOSEPH A

Inventor： YU GUIXUE , LI JUN , EWING WILLIAM R , SULSKY RICHARD B , LI JAMES J , TINO JOSEPH A

IPC: A61K31/4025 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , A61P3/00 , C07D231/56 , C07D261/20 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07D519/00

CPC classification number: C07D487/04 , C07D231/56 , C07D261/20 , C07D471/04 , C07D513/04

Abstract: Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula (I) wherein R1, R1', R2, R3, R4, Xa, Y, Z, and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.

Abstract translation: 提供了可用于刺激生长激素的内源性产生或释放的新型杂环芳族化合物，所述具有式（I）的通式结构的化合物其中R1，R1'，R2，R3，R4，Xa，Y，Z和n 如本文所述。本文提供的化合物可用于治疗肥胖症，骨质疏松症（改善骨密度）和改善肌肉质量和肌肉力量。

5.

发明申请
SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTI-ATHEROSCLEROTIC, ANTI-DYSLIPIDEMIC, ANTI-DIABETIC AND ANTI-OBESITY AGENTS AND METHOD 审中-公开
Title translation: 取代的酸衍生物有助于抗甲状腺激素，抗血糖，抗糖尿病和抗胆碱药物和方法

公开(公告)号：WO2008006043A2

公开(公告)日：2008-01-10

申请号：PCT/US2007072891

申请日：2007-07-06

Applicant: SQUIBB BRISTOL MYERS CO , TINO JOSEPH A , CHENG PETER T W , SHI YAN , LI JUN , MUKHERJEE RANJAN

Inventor： TINO JOSEPH A , CHENG PETER T W , SHI YAN , LI JUN , MUKHERJEE RANJAN

IPC: C07D263/32 , A61K31/421 , A61P3/00

CPC classification number: C07D263/32

Abstract: Compounds are provided which have the structure of Formula (I): wherein R1 is halogen; and X is hydrogen or halogen, and salts thereof, which compounds are useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic, and anti-obesity agents.

Abstract translation: 提供具有式（I）结构的化合物：其中R1是卤素; X是氢或卤素，及其盐，该化合物可用作抗动脉粥样硬化，抗血脂异常，抗糖尿病和抗肥胖剂。

6.

发明申请
HETEROCYCLIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
Title translation: 杂环化合物可用作生长激素的秘密

公开(公告)号：WO2005070884A2

公开(公告)日：2005-08-04

申请号：PCT/US2005001013

申请日：2005-01-12

Applicant: SQUIBB BRISTOL MYERS CO , ZHAI WEIXU , GERRITZ SAMUEL , ANDRES CHARLES J JR , TINO JOSEPH A

Inventor： ZHAI WEIXU , GERRITZ SAMUEL , ANDRES CHARLES J JR , TINO JOSEPH A

IPC: A61K31/40 , C07D207/09 , C07D207/00

CPC classification number: C07D207/09

Abstract: The present invention relates to novel heterocyclic compounds, according to Formula I, that stimulate endogenous production and/or release of growth hormone, wherein R1, R2, R3, R4 and X are defined herein. Further, the present invention relates to methods for using such compounds and to pharmaceutical compositions containing such compounds.

Abstract translation: 本发明涉及根据式I的刺激内源性生产和/或释放生长激素的杂环化合物，其中R 1，R 2，R 3，R 4和X如本文所定义。此外，本发明涉及使用这些化合物的方法和含有这些化合物的药物组合物。

7.

发明申请
HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES 审中-公开
Title translation: 杂环芳族化合物可用作生长激素的秘密

公开(公告)号：WO0054729A8

公开(公告)日：2002-02-21

申请号：PCT/US0005704

申请日：2000-03-02

Applicant: SQUIBB BRISTOL MYERS CO

Inventor： ROBL JEFFREY , TINO JOSEPH A , HERNANDEZ ANDRES S , LI JAMES J , LI JUN , SWARTZ STEPHEN G

IPC: C07D249/08 , A61K31/41 , A61K31/4174 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/421 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/565 , A61K31/568 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P13/12 , A61P17/02 , A61P19/10 , A61P21/00 , A61P31/18 , C07D233/54 , C07D233/64 , C07D235/10 , C07D235/14 , C07D249/12 , C07D257/04 , C07D263/32 , C07D271/06 , C07D277/20 , C07D277/28 , C07D277/56 , C07D277/64 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , A61P5/08 , A61P5/48 , C07D403/14 , C07D413/14

CPC classification number: C07D233/54 , C07D235/14 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/64 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12

Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have structure (I) including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably (a), (b) or (c) and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.

Abstract translation: 提供了可用于刺激生长激素的内源性生产或释放以及治疗肥胖症，骨质疏松症（改善骨密度）和改善肌肉质量和肌肉力量的杂环芳族化合物。杂环芳族化合物具有包括其药学上可接受的盐及其所有立体异构体的结构（I），其中X a是杂芳基，优选（a），（b）或（c）和R 1，R 1a，R 6，Y，X b，A，B ，Z，R3，R4，R4a，R5和R5a如本文所定义。