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1. 发明专利

JP2004099618A Piperidine as ccr5 modulator 审中-公开
公开(公告)号：JP2004099618A
公开(公告)日：2004-04-02
申请号：JP2003358714
申请日：2003-10-20
申请人： Pfizer Inc , ファイザー・インク
发明人： ARMOUR DUNCAN ROBERT , PRICE DAVID ANTHONY , STAMMEN BLANDA LUZIA CHRISTA , WOOD ANTHONY , PERROS MANOUSSOS , EDWARDS MARTIN PAUL
IPC分类号： G01N33/50 , A61K20060101 , A61K31/4245 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/496 , A61K31/5377 , A61K45/00 , A61P11/00 , A61P11/06 , A61P27/00 , A61P29/00 , A61P31/00 , A61P31/14 , A61P31/18 , A61P43/00 , C07D20060101 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D451/02 , C07D451/04 , C07D498/08 , G01N33/15
CPC分类号： C07D451/02 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/14 , C07D451/04
摘要： PROBLEM TO BE SOLVED: To provide a therapeutic and preventive agent for antiinflammatory diseases, HIV-1 and genetic retrovirus infections. SOLUTION: The medicinal formulation comprising a piperidine derivative represented by chemical formula 1, chemical formula 2 or the like is useful as a modulator having chemokine activity. COPYRIGHT: (C)2004,JPO

2. 发明专利

JP2000212159A CCR5 MODULATOR 失效
公开(公告)号：JP2000212159A
公开(公告)日：2000-08-02
申请号：JP36357899
申请日：1999-12-22
申请人： PFIZER
发明人： ARMOUR DUNCAN ROBERT , PRICE DAVID ANTHONY , STAMMEN BLANDA LUZIA CHRISTA , ANTHONY WOOD , PERROS MANOUSSOS , EDWARDS MARTIN PAUL
IPC分类号： A61K31/40 , A61K31/4427 , A61K31/443 , A61K31/4468 , A61K31/4523 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K45/06 , A61P11/00 , A61P29/00 , A61P31/18 , A61P37/04 , A61P43/00 , C07D207/14 , C07D211/58 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D451/02 , C07D451/04 , C07D498/08
摘要： PROBLEM TO BE SOLVED: To obtain a new compound useful as a selective CCR5 receptor modulator, having a non-peptidyl structure, and useful for treating and preventing diseases or disorders mediated by or related to the modulation of the activity of CCR5 chemokine receptor. SOLUTION: A compound having [region α]-[region β]-[region γ]-[region δ] [region. α] is an arylheterocyclylsubstituent component comprising a heterophenylmethylene moiety of formula I (R5 is a direct bond or the like; R6 is H or the like); [region β] is an alkyl-cross-linking element of formula II (R40, R41 are each H or the like), [region γ] is an azamonocyclic moiety of formula III (→ is a covalent bond or the like); [region δ] is an aryl of formula IV (R73 is H or the like) and a heterocyclyl-(substituted)amide, carbamate or urea moiety}, preferably N-(1-phenyl-3- 4-[(2-phenylacetyl)amino]-1- piperidinyl}propyl)cyclobutane carboxamide. The compound is produced from a compound of formula V as a starting substance.

3. 发明申请

WO2005060963A8 BENZENESULFONYLAMINO-PYRIDIN-2-YL DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 (11-BETA-HSD-1) FOR THE TREATMENT OF DIABETES AND OBESITY 审中-公开
标题翻译：作为用于治疗糖尿病和肥胖症的11-β-羟基脱氢酶脱氢酶1型（11-BETA-HSD-1）的抑制剂的苯并呋喃亚胺基吡啶-2-基衍生物及其相关化合物
公开(公告)号：WO2005060963A8
公开(公告)日：2005-12-01
申请号：PCT/IB2004004056
申请日：2004-12-06
申请人： PFIZER , EDWARDS MARTIN PAUL , JOHNSON THEODORE OTTO JR , NAIR SAJIV KRISHNAN , SIU MICHAEL , TAYLOR WENDY DIANNE , CRIPPS STEPHAN JAMES , WANG YONG , CHENG HENGMIAO , SMITH CHRISTOPHER RONALD
发明人： EDWARDS MARTIN PAUL , JOHNSON THEODORE OTTO JR , NAIR SAJIV KRISHNAN , SIU MICHAEL , TAYLOR WENDY DIANNE , CRIPPS STEPHAN JAMES , WANG YONG , CHENG HENGMIAO , SMITH CHRISTOPHER RONALD
IPC分类号： A61K31/44 , A61K31/4436 , A61K31/4545 , C07C311/36 , C07C311/37 , C07D209/08 , C07D213/02 , C07D213/76 , C07D215/38 , C07D235/06 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04 , A61P3/04 , A61P3/10
CPC分类号： C07D209/08 , C07D213/76 , C07D215/38 , C07D235/06 , C07D239/42 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D513/04
摘要： The present invention relates to compounds with the formula (I), or a pharmaceutically acceptable salt thereof, wherein: R is selected from the group consisting of (C1-C6)alkyl, -(CR R )t(C3-C12)cycloalkyl, -(CR R )t(C6-C12)aryl, and -(CR R )t(4-10)-membered heterocyclyl; b and k are each independently selected from 1 and 2; j is selected from the group consisting of 0, 1, and 2; t, u, p, q, and v are each independently selected from the group consisting of 0, 1, 2, 3, 4, and 5; T is a (6-10)-membered heterocyclyl containing at least one nitrogen atom; R is selected from the group consisting of H, (C1-C6)alkyl, -(CR R )t(C3-C12)cycloalkyl, -(CR R )t(C6-C12)aryl, and -(CR R )t(4-10)-membered heterocyclyl; each R and R is independently selected from H and (C1-C6)alkyl, the carbon atoms of T, R , R , R and R may each be optionally, substituted by I to 5 R groups; R is defined in the claims; The compounds of the present invention are 11 ß-hsd-1 inhibitors, and are therefore believed to be useful in the treatment of diabetes, obesity, glaucoma, osteoporosis, cognitive disorders, immune disorders, depression, hypertension, and metabolic diseases.
摘要翻译：本发明涉及具有式（I）化合物或其药学上可接受的盐，其中：R 1选自（C 1 -C 6）烷基， - （CR 3 R 4））（C 3 -C 12）环烷基， - （CR 3 R 4）t（C 6 -C 12）芳基和 - （CR 3 R 4）t（4-10） - 杂环基; b和k各自独立地选自1和2; j选自0，1和2; t，u，p，q和v各自独立地选自0,1,2,3,4和5; T是含有至少一个氮原子的（6-10） - 杂环基; R 2选自H，（C 1 -C 6）烷基， - （CR 3 R 4）t（C 3 -C 12）环烷基， - （CR 3 R 4） t（C 6 -C 12）芳基和 - （CR 3 R 4）t（4-10） - 杂环基; 每个R 3和R 4独立地选自H和（C 1 -C 6）烷基，T，R 1，R 2，R 3和R 4的碳原子，可各自任选被I至5个R 5基团取代; R 5定义在权利要求中; 本发明的化合物是11β-hsd-1抑制剂，因此被认为可用于治疗糖尿病，肥胖，青光眼，骨质疏松症，认知障碍，免疫疾病，抑郁症，高血压和代谢疾病。

4. 发明专利

ME00513B AZABICIKLOALKANI KAO MODULATORI CCR5 未知
公开(公告)号：ME00513B
公开(公告)日：2011-10-10
申请号：MEP83708
申请日：1999-12-23
申请人： PFIZER LTD , PFIZER
发明人： ARMOUR DUNCAN ROBERT , PRICE DAVID ANTHONY , STAMMEN BLANDA LUZIA CHRISTA , WOOD ANTHONY , PERROS MANOUSSOS , EDWARDS MARTIN PAUL
IPC分类号： A61K45/06 , G01N33/50 , A61K20060101 , A61K31/4184 , A61K31/426 , A61K31/439 , A61K31/445 , A61K31/46 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/52 , A61K31/5386 , A61K31/547 , A61K31/551 , A61K31/7064 , A61K38/21 , A61K45/00 , A61P11/00 , A61P31/18 , A61P43/00 , C07D20060101 , C07D207/14 , C07D211/58 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D451/02 , C07D451/04 , C07D487/22 , C07D498/08 , C07D513/08 , G01N33/15 , G01N33/566
摘要： Jedinjenja formule (l) [Regionα] - [Regionβ] - [Regionγ] - [Regionδ], koja su korisna kao modulatori aktivnosti hemokina. Ovaj pronalazak takođe daje farmaceutske formulacije i postupke tretmana koji koriste ova jedinjenja.

5. 发明专利

ES2362711T3 AZABICICLOALCANOS COMO MODULADORES DE CCR5. 未知
公开(公告)号：ES2362711T3
公开(公告)日：2011-07-12
申请号：ES99959624
申请日：1999-12-23
申请人： PFIZER LTD , PFIZER , PHIVCO 1 LLC
发明人： ARMOUR DUNCAN ROBERT , PRICE DAVID ANTHONY , STAMMEN BLANDA LUZIA C , WOOD ANTHONY , PERROS MANOUSSOS , EDWARDS MARTIN PAUL
IPC分类号： A61K31/445 , A61K20060101 , A61K31/46 , C07D20060101 , C07D451/04
摘要： Un compuesto, de Fórmula (I) [Región α] - [Región β] - [Región γ] - [Región δ] (I) o una sal farmacéuticamente aceptable del mismo, en la que [Región α] es un resto de la fórmula en la que el símbolo "*" indica el punto de unión del resto de Fórmula (2.0.0) a la Región β; R4 es H o alquilo C1-C2; R6 es H; A es fenilo opcionalmente sustituido con uno o dos sustituyentes seleccionados de F y Cl; R5 a es un enlace directo; W1 es -CO-; R27 es (i) metilo, etilo, isopropilo, terc-butilo o alilo, cada uno sustituido opcionalmente con 0 a 3 sustituyentes R28, o (ii) ciclopropilo, ciclobutilo, ciclopentilo, ciclohexilo, ciclopropilmetilo, ciclobutiletilo, ciclopentilpropilmetilo, ciclopentilmetilo, cada uno sustituido opcionalmente con hasta 3 sustituyentes R28, o (iii) fenilo, tetrahidropiranilo, piridinilo, oxetanilo, pirrolidinilo, acetidinilo o tetrahidrofuranilo opcionalmente sustituido por 0 a 3 sustituyentes R28; R28 es fenilo; fluoro, cloro; oxo; -OH, alquilo C1-C2, alcoxi C1-C3, -COOR29; CO-alquilo C1-C4-SO2-alquilo C1-C4, CONR29R30-; -NR20R30; -NR20COR30; -NR20COR30; -NR29COOR30; -NR19S(O)pR30 y -SO2NR29R30; p es un número entero seleccionado de 0, 1 y 2; R29 y R30 son cada uno independientemente H o alquilo C1-C4 opcionalmente sustituido con hasta 3 sustituyentes seleccionados de flúor y cloro; la [Región β] es un elemento de unión de alquilo de la Fórmula parcial (3.0.0): en la que: "*" es un símbolo que representa el punto de unión del resto de Fórmula parcial (3.0.0) a la Región α; "→" es un símbolo que representa el punto de unión del resto de Fórmula parcial (3.0.0) a la Región γ; R40 y R41 son hidrógeno; la [Región γ] es un resto aza-bicíclico seleccionado del grupo que consisten en las Fórmulas parciales (4.2.17), (4.2.26) y (4.2.27) en las que las líneas discontinuas indican los puntos de unión; la [Región δ] es un miembro seleccionado del grupo que consiste en: en las que: el símbolo "*" indica el punto de unión de cada uno de los restos de las Fórmulas parciales (5.0.35) a (5.4.8) inclusive, a la Región δ, R90 b es metilo; R90 a es un miembro seleccionado independientemente del grupo que consiste en hidrógeno; -alquilcarbonil (C1-C2); -alquil (C1-C4); -(CH2)n-cicloalquil (C3-C7); -alquenil (C2-C3); -(CH2)n-(fenilo); y -(CH2)n-(HET2), en las que n es un número entero independientemente seleccionado de 0, 1 y 2; HET2 es un grupo heterociclilo seleccionado del grupo que consiste en tienilo; oxazolilo; isoxazolilo; tiazolilo; isotiazolilo; pirazolilo; oxadiazolilo; tiadiazolilo; triazolilo; piridilo; pirazinilo; piridazinilo; pirimidinilo; paratiazinilo; y morfolinilo.

6. 发明专利

ES2808987T9 Lactamas fusionadas con arilo y heteroarilo 未知
公开(公告)号：ES2808987T9
公开(公告)日：2021-11-29
申请号：ES17206218
申请日：2013-12-05
申请人： PFIZER
发明人： EDWARDS MARTIN PAUL , KUMPF ROBERT ARNOLD , KUNG PEI-PEI , MCALPINE INDRAWAN JAMES , NINKOVIC SACHA , RUI EUGENE YUANJIN , SUTTON SCOTT CHANNING , TATLOCK JOHN HOWARD , WYTHES MARTIN JAMES , ZEHNDER LUKE RAYMOND
IPC分类号： C07D401/06 , A61K31/4725 , A61P35/00 , C07D401/14 , C07D403/14 , C07D407/14 , C07D413/06 , C07D413/14 , C07D471/04

7. 发明专利

ME03793B LAKTAMI KONDEZIRANI S ARILOM I HETEROARILOM 未知
公开(公告)号：ME03793B
公开(公告)日：2021-04-20
申请号：MEP2020147
申请日：2013-12-05
申请人： PFIZER
发明人： EDWARDS MARTIN PAUL , KUMPF ROBERT ARNOLD , KUNG PEI-PEI , MCALPINE INDRAWAN JAMES , NINKOVIC SACHA , RUI EUGENE YUANJIN , SUTTON SCOTT CHANNING , TATLOCK JOHN HOWARD , WYTHES MARTIN JAMES , ZEHNDER LUKE RAYMOND
IPC分类号： A61K31/4725 , A61P35/00 , C07D401/06 , C07D401/14 , C07D403/14 , C07D407/14 , C07D413/06 , C07D413/14 , C07D471/04

8. 发明专利

HUE050009T2 Kondenzált aril- és heteroaril-laktámok 未知
公开(公告)号：HUE050009T2
公开(公告)日：2020-11-30
申请号：HUE17206218
申请日：2013-12-05
申请人： PFIZER
发明人： EDWARDS MARTIN PAUL , KUMPF ROBERT ARNOLD , KUNG PEI-PEI , MCALPINE INDRAWAN JAMES , NINKOVIC SACHA , RUI EUGENE YUANJIN , SUTTON SCOTT CHANNING , TATLOCK JOHN HOWARD , WYTHES MARTIN JAMES , ZEHNDER LUKE RAYMOND
IPC分类号： A61P35/00

9. 发明专利

EA028317B1 АРИЛ- И ГЕТЕРОАРИЛ-КОНДЕНСИРОВАННЫЕ ЛАКТАМЫ ДЛЯ ЛЕЧЕНИЯ ВИДОВ РАКА, АССОЦИИРОВАННЫХ С АКТИВНОСТЬЮ БЕЛКА EZH2 未知
公开(公告)号：EA028317B1
公开(公告)日：2017-11-30
申请号：EA201590879
申请日：2013-12-05
申请人： PFIZER
发明人： EDWARDS MARTIN PAUL , KUMPF ROBERT ARNOLD , KUNG PEI-PEI , MCALPINE INDRAWAN JAMES , NINKOVIC SACHA , RUI EUGENE YUANJIN , SUTTON SCOTT CHANNING , TATLOCK JOHN HOWARD , WYTHES MARTIN JAMES , ZEHNDER LUKE RAYMOND
IPC分类号： C07D401/06 , C07D401/14 , C07D403/14 , C07D407/14 , C07D413/06 , C07D413/14 , C07D471/04
摘要： Изобретениеотноситсяк соединениямформулы (II-А)где R, R, R, R, R, m, X, Y и Z являютсятакими, какопределенов описании, иихфармацевтическиприемлемымсолям, кфармацевтическимкомпозициям, содержащимтакиесоединенияи соли, ик применениютакихсоединений, солейи композицийдлялеченияаномальногоклеточногоростаи видоврака, ассоциированныхс активностью EZH2.

10. 发明专利

DOP2015000157A LACTAMAS FUSIONADAS DE ARILO Y HETEROARILO 未知
公开(公告)号：DOP2015000157A
公开(公告)日：2015-11-30
申请号：DO2015000157
申请日：2015-06-19
申请人： PFIZER
发明人： ZEHNDER LUKE RAYMOND , MCALPINE INDRAWAN JAMES , NINKOVIC SACHA , EDWARDS MARTIN PAUL , KUMPF ROBERT ARNOLD , KUNG PEL-PEL , RUI EUGENE YUANJIN , SUTTON SCOTT CHANNING , TATLOCK JOHN HOWARD , WYTHES MARTIN JAMES
IPC分类号： C07D401/06 , C07D401/14 , C07D403/14 , C07D407/14 , C07D413/06 , C07D413/14 , C07D471/04
摘要： ESTA INVENCIÓN SE REFIERE A COMPUESTOS DE LA FÓRMULA GENERAL (I), EN LA CUAL R1, R2, U, V, L, M, R5, M, X, Y Y Z SON COMO AQUÍ SE DEFINIERON, Y LAS SALES FARMACÉUTICAMENTE ACEPTABLES DEL MISMO, A COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN DICHOS COMPUESTOS Y SALES, Y A PROCEDIMIENTO PARA LA FABRICACIÓN DE MEDICAMENTOS MÉTODOS PARA UTILIZAR ESOS COMPUESTOS, SALES Y COMPOSICIONES PARA EL TRATAMIENTO DE CRECIMIENTO CELULAR ANORMAL, QUE INCLUYE CÁNCER.

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