公开(公告)号：US06492348B1

公开(公告)日：2002-12-10

申请号：US09736018

申请日：2001-03-06

Applicant: David Edmund Bays ,  Richard Peter Charles Cousins ,  Hazel Joan Dyke ,  Colin David Eldred ,  Brian David Judkins ,  Martin Pass ,  Andrew Michael Kenneth Pennell

Inventor： David Edmund Bays ,  Richard Peter Charles Cousins ,  Hazel Joan Dyke ,  Colin David Eldred ,  Brian David Judkins ,  Martin Pass ,  Andrew Michael Kenneth Pennell

IPC: A61K3170

CPC classification number: C07D473/00 ,  C07H19/16

Abstract: A compound of formula (I) which is an agonist at the adenosine Al receptor, wherein Y, Z, and W represent heteroatoms, and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof for use in therapy.

Abstract translation: 作为腺苷A1受体的激动剂的式（I）化合物，其中Y，Z和W表示杂原子，以及其盐和溶剂化物，特别是用于治疗的生理学上可接受的溶剂合物及其盐。

公开(公告)号：US06740644B2

公开(公告)日：2004-05-25

申请号：US10373064

申请日：2003-02-26

Applicant: Colin David Eldred ,  Andrew Michael Kenneth Pennell

Inventor： Colin David Eldred ,  Andrew Michael Kenneth Pennell

IPC: A61K3170

CPC classification number: C07H19/16 ,  Y02P20/55

Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, —SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine A1 receptor.

Abstract translation: 式（I）的化合物，其中R 2表示C 1-3烷基，卤素或氢; R 3表示1-6个碳原子的直链或支链烷基; 条件是当R 3表示C 1-3烷基时，R 2表示C 1-3烷基，R 1不能表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基， 氰基，-CO 2 R c，-CONR c R d，-COR c，-SOR e，-SO 2 R e，-SO 3 H，-SO 2 NR c R d， OR c，-NHSO 2 R e，-NHCOR c和-NR c R d; 特别是其生理上可接受的溶剂合物及其盐。 这些化合物是腺苷A1受体的激动剂。

公开(公告)号：US06544960B1

公开(公告)日：2003-04-08

申请号：US09530575

申请日：2000-06-15

Applicant: Colin David Eldred ,  Andrew Michael Kenneth Pennell

Inventor： Colin David Eldred ,  Andrew Michael Kenneth Pennell

IPC: A61K3170

CPC classification number: C07H19/16 ,  Y02P20/55

Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine Al receptor.

Abstract translation: 式（I）的化合物，其中R 2表示C 1-3烷基，卤素或氢; R3表示1-6个碳原子的直链或支链烷基; 条件是当R 3表示C 1-3烷基时，R 2表示C 1-3烷基，R 1不能表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基，氰基，-CO 2 R c，-CONRc R d， CORc，-SORe，SO2Re，-SO3H，-SO2NRcRd，-ORc，-NHSO2Re，-NHCORc和-NRcRd; 特别是其生理上可接受的溶剂合物及其盐。 这些化合物是腺苷A1受体的激动剂。

公开(公告)号：US06455510B1

公开(公告)日：2002-09-24

申请号：US09530573

申请日：2000-06-15

Applicant: Richard Peter Charles ,  Brian Cox ,  Colin David Eldred ,  Andrew Michael Kenneth Pennell

Inventor： Richard Peter Charles ,  Brian Cox ,  Colin David Eldred ,  Andrew Michael Kenneth Pennell

IPC: A61K3170

CPC classification number: C07H19/16

Abstract: A compound of formula (I) which is an agonist at the adenosine A1 receptor wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the adenosine A1 receptor.

Abstract translation: 式（I）化合物，其为腺苷A1受体的激动剂，其中R2表示C1-3烷基，卤素或氢; R3表示1-6个碳原子的氟化直链或支链烷基及其盐和溶剂化物，特别是其生理上可接受的溶剂合物及其盐。 这些化合物是腺苷A1受体的激动剂。

公开(公告)号：US06677316B2

公开(公告)日：2004-01-13

申请号：US10217107

申请日：2002-08-13

Applicant: David Edmund Bays ,  Richard Peter Charles Cousins ,  Hazel Joan Dyke ,  Colin David Eldred ,  Brian David Judkins ,  Martin Pass ,  Andrew Michael Kenneth Pennell

Inventor： David Edmund Bays ,  Richard Peter Charles Cousins ,  Hazel Joan Dyke ,  Colin David Eldred ,  Brian David Judkins ,  Martin Pass ,  Andrew Michael Kenneth Pennell

IPC: A61K3170

CPC classification number: C07D473/00 ,  C07H19/16

Abstract: A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor. The adenosine derivative has a general formula (I) as follows:

Abstract translation: 治疗患有或易患缺血性心脏病，外周血管疾病或中风或受试者患有疼痛，CNS病症或睡眠呼吸暂停症的患者的方法，其包括给予治疗有效量的作为激动剂的腺苷衍生物 腺苷A1受体并且其表现出很少或没有A3受体的激动剂活性。 腺苷衍生物具有如下通式（I）：

公开(公告)号：US5998388A

公开(公告)日：1999-12-07

申请号：US180442

申请日：1998-11-06

Applicant: Frank Ellis ,  Stephen Swanson ,  Richard Peter Charles ,  Brian Cox ,  Andrew Michael Kenneth Pennell ,  Colin David Eldred

Inventor： Frank Ellis ,  Stephen Swanson ,  Richard Peter Charles ,  Brian Cox ,  Andrew Michael Kenneth Pennell ,  Colin David Eldred

IPC: C07H19/167 ,  A61K31/7076 ,  A61P9/00 ,  A61P25/00 ,  C07H15/04 ,  C07H19/16 ,  A61K31/70

CPC classification number: C07H15/04 ,  C07H19/16

Abstract: This invention relates to novel adenosine derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Thus the invention provides compounds of formula (I) which are agonists at the adenosine A1 receptor. ##STR1## wherein R.sup.1 represents phenyl optionally substituted by one or more substituents selected from halogen, C.sub.1-3 alkyl, trifluoromethyl, nitro, cyano, --CO.sub.2 R.sup.a.sub.1 --CONR.sup.a R.sup.b, --COR.sup.a, --SOR.sup.c, --SO.sub.2 R.sup.c, --SO.sub.3 H, --SO.sub.2 NR.sup.a R.sup.b, --OR.sup.a, --NHSO.sub.2 R.sup.c, --NHCOR.sup.a and --NR.sup.a R.sup.b,R.sup.2 represents a C.sub.1-6 alkyl or C.sub.3-6 alkenyl group; R.sup.3 represents C.sub.1-3 alkyl;R.sup.a and R.sup.b may each independently represent hydrogen or C.sub.1-3 alkyl or, when --NR.sup.a R.sup.b is directly attached to said phenyl, R.sup.a and R.sup.b together with the nitrogen atom may form a -5 or -6 or membered heterocyclic ring optionally containing a second heteroatom selected from oxygen or nitrogen, which second nitrogen heteroatom may optionally be further substituted by hydrogen or C.sub.1-3 alkyl;R.sup.c represents C.sub.1-3 alkyl;and salts and solvates thereof, in particular physiologically acceptable salts and solvates thereof.

Abstract translation: PCT No.PCT / EP97 / 02403 Sec。 371日期：1998年11月6日 102（e）日期1998年11月6日PCT提交1997年5月13日PCT公布。 WO97 / 43300 PCT出版物 日期1997年11月20日本发明涉及新型腺苷衍生物，其制备方法，含有它们的药物组合物及其在医药中的用途。 因此，本发明提供了作为腺苷A1受体的激动剂的式（I）化合物。 其中R 1表示任选被一个或多个选自卤素，C 1-3烷基，三氟甲基，硝基，氰基，-CO 2 R 1a -CONR a R b，-COR a，-SOR c，-SO 2 Rc，-SO 3 H，-SO 2 NR a R b，-OR a，-NHSO 2 R c ，-NHCOR a和-NR a R b，R 2表示C 1-6烷基或C 3-6烯基; R 3表示C 1-3烷基; R a和R b可各自独立地表示氢或C 1-3烷基，或当-NR a R b直接与所述苯基连接时，R a和R b与氮原子一起可以形成任选地含有选自第二杂原子的-5或-6元杂环 来自氧或氮，该第二氮杂原子可以任选地被氢或C 1-3烷基进一步取代; Rc表示C1-3烷基; 及其盐和溶剂合物，特别是其生理上可接受的盐和溶剂化物。

公开(公告)号：US20110039889A1

公开(公告)日：2011-02-17

申请号：US12989700

申请日：2009-04-29

Applicant: Colin David Eldred ,  Jag Paul Heer ,  Thomas Daniel Heightman ,  John Skidmore ,  Hailong Wang

Inventor： Colin David Eldred ,  Jag Paul Heer ,  Thomas Daniel Heightman ,  John Skidmore ,  Hailong Wang

IPC: A61K31/4709 ,  C07D413/10 ,  C07D413/14 ,  A61P19/02

CPC classification number: C07D413/04 ,  C07D413/14

Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

Abstract translation: 本发明涉及具有药理活性的新型恶二唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种病症中的用途。

公开(公告)号：US20090074675A1

公开(公告)日：2009-03-19

申请号：US11910935

申请日：2006-04-12

Applicant: Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

Inventor： Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

IPC: A61K9/12 ,  C07D401/04 ,  A61K31/4439

CPC classification number: C07D405/14 ,  C07D231/56 ,  C07D401/04 ,  C07D405/12

Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.

Abstract translation: 式（I）的化合物：其中A1表示2,3-二氢-1-苯并呋喃-7-基，5-氟-2-甲氧基 - 苯基或5-氟-2-羟基 - 苯基; X表示-C（R 3） - 或氮; 当X表示-C（R3） - 时，R2表示氢，R1表示氟，R3表示氢或氟，当X表示-C（R3） - 且R2和R1各自表示氢时，R3表示氢，羟基，甲氧基或氟 当X表示-C（R 3） - 且R 2表示羟基，甲氧基，-CO 2 CH 3或-CO 2 CH 2 CH 3时，R 1和R 3各自表示氢，当X表示氮时，R 1和R 2各自表示氢; Y表示H或甲基; 或其生理功能衍生物。

公开(公告)号：US08093281B2

公开(公告)日：2012-01-10

申请号：US11910935

申请日：2006-04-12

Applicant: Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

Inventor： Colin David Eldred ,  David House ,  Graham George Adam Inglis ,  Simon John Fawcett MacDonald ,  Philip Alan Skone

IPC: A61K31/416 ,  C07D231/56

CPC classification number: C07D405/14 ,  C07D231/56 ,  C07D401/04 ,  C07D405/12

Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.

Abstract translation: 式（I）的化合物：其中A1表示2,3-二氢-1-苯并呋喃-7-基，5-氟-2-甲氧基 - 苯基或5-氟-2-羟基 - 苯基; X表示-C（R 3） - 或氮; 当X表示-C（R3） - 时，R2表示氢，R1表示氟，R3表示氢或氟，当X表示-C（R3） - 且R2和R1各自表示氢时，R3表示氢，羟基，甲氧基或氟 当X表示-C（R 3） - 且R 2表示羟基，甲氧基，-CO 2 CH 3或-CO 2 CH 2 CH 3时，R 1和R 3各自表示氢，当X表示氮时，R 1和R 2各自表示氢; Y表示H或甲基; 或其生理功能衍生物。

公开(公告)号：US20090270444A1

公开(公告)日：2009-10-29

申请号：US11718892

申请日：2005-11-17

Applicant: Colin David Eldred ,  John Edward Robinson ,  Alison Judith Steel

Inventor： Colin David Eldred ,  John Edward Robinson ,  Alison Judith Steel

IPC: A61K31/4375 ,  C07D471/04 ,  A61P37/08

CPC classification number: C07D471/04

Abstract: There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein: R1 is phenyl which may be unsubstituted or substituted by one or two substituents selected from fluorine, chlorine, C1-2alkoxy-, —CN; phenyl fused to a 5-membered saturated ring containing one oxygen atom; pyridinyl which may be unsubstituted or substituted by one or two substituents selected from fluorine or chlorine; or C-linked pyrazolyl which may be unsubstituted or substituted by the substituent C1-2alkyl; R2 is C1-4alkyl; R3 is C1-2alkyl; and n is 0, 1 or 2.

Abstract translation: 根据本发明，提供新的式（I）化合物及其药学上可接受的盐和溶剂化物，其中：R1是可以是未取代的或被一个或两个选自氟，氯，C 1-2烷氧基 - ， - CN; 与含有一个氧原子的5元饱和环稠合的苯基; 吡啶基，其可以是未取代的或被一个或两个选自氟或氯的取代基取代; 或C连接的吡唑基，其可以是未取代的或被取代基C 1-2烷基取代; R2是C1-4烷基; R3是C1-2烷基; n为0,1或2。