公开(公告)号：WO2006029075A2

公开(公告)日：2006-03-16

申请号：PCT/US2005031532

申请日：2005-09-06

Applicant: REDDYS LAB LTD DR ,  REDDYS LAB LTD DR ,  DAS SAIBAL KUMAR ,  SINGH SUNIL KUMAR ,  MADHAVAN GURRAM RANGA ,  BHUNIYA DEBNATH ,  IQBAL JAVED ,  SHARMA SUDHIR KUMAR ,  CHAKRABARTI RANJAN

Inventor： DAS SAIBAL KUMAR ,  SINGH SUNIL KUMAR ,  MADHAVAN GURRAM RANGA ,  BHUNIYA DEBNATH ,  IQBAL JAVED ,  SHARMA SUDHIR KUMAR ,  CHAKRABARTI RANJAN

IPC: A61K31/519 ,  C07D487/02

CPC classification number: C07D487/04 ,  C07D239/90

Abstract: There are provided derivatives having PPAR agonist activity. The derivatives include compounds and/or their pharmaceutically acceptable salts; the compounds having the formula (I) wherein A has the structure (II) or (III); X is chosen from -CH 2 -, -O-, -NH-, and -S-; Y is chosen from -O-, -NH-, and -S-; Z, which may be located in any position of substitution, is hydrogen or halogen; R 1 and R 2 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl, or R 1 and R 2 together form a carbocyclic ring having from 4 to 6 carbon atoms; R 3 is chosen from hydrogen and C 1 -C 8 alkyl; R 4 , R 5 , and R 6 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl; and n is 1 to 6. Various embodiments and variants are provided. In accordance with other aspects, the invention also provides methods of producing a PPARa agonist activity in a mammal, the methods including administering to the mammal an effective amount of certain derivative(s) of the first aspect of the invention, a method of producing a PPARa agonist activity and a PPARa agonist activity in a mammal, the method including administering to the mammal an effective amount of certain derivative(s); and a pharmaceutical composition that includes the derivative(s) of the first aspect of the invention and one or more pharmaceutically-acceptable excipients. Various embodiments and variants are provided.

Abstract translation: 提供具有PPAR激动剂活性的衍生物。 衍生物包括化合物和/或其药学上可接受的盐; 具有式（I）的化合物其中A具有结构（II）或（III）; X选自-CH 2 - ， - O - ， - N - 和-S-; Y选自-O - ， - NH-和-S-; 可以位于任何取代位置的Z是氢或卤素; R 1和R 2可以相同或不同，独立地选自氢和C 1 -C 8烷基， 或者R 1和R 2一起形成具有4至6个碳原子的碳环; R 3选自氢和C 1 -C 8烷基; R 4，R 5，R 5和R 6可以相同或不同，独立地选自氢和C 1 C 8 -C 14烷基; 并且n为1至6.提供了各种实施方案和变体。 根据其它方面，本发明还提供了在哺乳动物中产生PPARα激动剂活性的方法，所述方法包括向哺乳动物施用有效量的本发明第一方面的某些衍生物， PPARα激动剂活性和PPARα激动剂活性，所述方法包括向哺乳动物施用有效量的某些衍生物; 和包含本发明第一方面的衍生物和一种或多种药学上可接受的赋形剂的药物组合物。 提供了各种实施例和变型。

公开(公告)号：WO2006029075A8

公开(公告)日：2007-04-26

申请号：PCT/US2005031532

申请日：2005-09-06

Applicant: REDDYS LAB LTD DR ,  REDDYS LAB INC DR ,  DAS SAIBAL KUMAR ,  SINGH SUNIL KUMAR ,  MADHAVAN GURRAM RANGA ,  BHUNIYA DEBNATH ,  IQBAL JAVED ,  SHARMA SUDHIR KUMAR ,  CHAKRABARTI RANJAN

Inventor： DAS SAIBAL KUMAR ,  SINGH SUNIL KUMAR ,  MADHAVAN GURRAM RANGA ,  BHUNIYA DEBNATH ,  IQBAL JAVED ,  SHARMA SUDHIR KUMAR ,  CHAKRABARTI RANJAN

IPC: A61K31/519 ,  C07D487/02

CPC classification number: C07D487/04 ,  C07D239/90

Abstract: There are provided derivatives having PPAR agonist activity. The derivatives include compounds and/or their pharmaceutically acceptable salts; the compounds having the formula (I) wherein A has the structure (II) or (III); X is chosen from -CH 2 -, -O-, -NH-, and -S-; Y is chosen from -O-, -NH-, and -S-; Z, which may be located in any position of substitution, is hydrogen or halogen; R 1 and R 2 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl, or R 1 and R 2 together form a carbocyclic ring having from 4 to 6 carbon atoms; R 3 is chosen from hydrogen and C 1 -C 8 alkyl; R 4 , R 5 , and R 6 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl; and n is 1 to 6. Various embodiments and variants are provided. In accordance with other aspects, the invention also provides methods of producing a PPARa agonist activity in a mammal, the methods including administering to the mammal an effective amount of certain derivative(s) of the first aspect of the invention, a method of producing a PPARa agonist activity and a PPARa agonist activity in a mammal, the method including administering to the mammal an effective amount of certain derivative(s); and a pharmaceutical composition that includes the derivative(s) of the first aspect of the invention and one or more pharmaceutically-acceptable excipients. Various embodiments and variants are provided.

Abstract translation: 提供了具有PPAR激动剂活性的衍生物。 衍生物包括化合物和/或其药学上可接受的盐; 其中A具有结构（II）或（III）的具有式（I）的化合物; X选自-CH 2 - ， - O - ， - NH-和-S-; Y选自-O - ， - NH-和-S-; 可以位于任何取代位置的Z是氢或卤素; R 1和R 2可以相同或不同，独立地选自氢和C 1 -C 8烷基， 烷基或R 1和R 2一起形成具有4至6个碳原子的碳环; R 3选自氢和C 1 -C 8烷基; R 3选自氢和C 1 -C 8烷基; R 4，R 5和R 6可以相同或不同，独立地选自氢和C 1 -C 4烷基， -C 8烷基; 并且n是1至6.提供了各种实施例和变体。 根据其它方面，本发明还提供了在哺乳动物中产生PPARα激动剂活性的方法，所述方法包括向哺乳动物施用有效量的本发明第一方面的某些衍生物，产生 PPARα激动剂活性和PPARα激动剂活性，所述方法包括给哺乳动物施用有效量的某些衍生物; 以及包含本发明第一方面的衍生物和一种或多种药学上可接受的赋形剂的药物组合物。 提供了各种实施例和变体。

公开(公告)号：WO2009019598A3

公开(公告)日：2009-12-30

申请号：PCT/IB2008002133

申请日：2008-08-08

Applicant: REDDYS LAB LTD DR ,  ARGENTA DISCOVERY LTD ,  FOX JUSTIAN CRAIG ,  FINCH HARRY ,  FITZGERALD MARY FRANCES ,  CHAKRABARTI RANJAN ,  SINGH SUNIL KUMAR ,  SIHORKAR VAIBHAV ,  GUPTA PIYUSH

Inventor： FOX JUSTIAN CRAIG ,  FINCH HARRY ,  FITZGERALD MARY FRANCES ,  CHAKRABARTI RANJAN ,  SINGH SUNIL KUMAR ,  SIHORKAR VAIBHAV ,  GUPTA PIYUSH

IPC: A01N43/60 ,  A61K31/495

CPC classification number: A61K31/502

Abstract: The present invention relates to a novel method of preventing and treating respiratory disorders, such as asthma, COPD, cystic fibrosis and pulmonary fibrosis, in a subject by administering to the subject a compound (I) having the structure: or its pharmaceutically acceptable salt thereof and/or its polymorph thereof

Abstract translation: 本发明涉及一种通过给受试者施用具有如下结构的化合物（I）或其药学上可接受的盐来预防和治疗受试者中的呼吸病症，例如哮喘，COPD，囊性纤维化和肺纤维化的新方法： 和/或其多晶型物

公开(公告)号：EP1793828A4

公开(公告)日：2009-09-02

申请号：EP05794037

申请日：2005-09-06

Applicant: REDDYS LAB LTD DR ,  REDDYS LAB INC DR

Inventor： DAS SAIBAL KUMAR ,  SINGH SUNIL KUMAR ,  MADHAVAN GURRAM R ,  BHUNIYA DEBNATH ,  IQBAL JAVED ,  SHARMA SUDHIR K ,  CHAKRABARTI RANJAN

IPC: C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  C07C43/205 ,  C07C59/01 ,  C07C59/48 ,  C07C69/003 ,  C07D231/14 ,  C07D231/18 ,  C07D239/90

CPC classification number: C07D487/04 ,  C07D239/90

公开(公告)号：CA2579230A1

公开(公告)日：2006-03-16

申请号：CA2579230

申请日：2005-09-06

Applicant: REDDYS LAB LTD DR ,  REDDYS LAB INC DR

Inventor： IQBAL JAVED ,  BHUNIYA DEBNATH ,  MADHAVAN GURRAM RANGA ,  CHAKRABARTI RANJAN ,  SHARMA SUDHIR KUMAR ,  SINGH SUNIL KUMAR ,  DAS SAIBAL KUMAR

IPC: A61K31/519 ,  C07D487/02

Abstract: There are provided derivatives having PPAR agonist activity. The derivatives include compounds and/or their pharmaceutically acceptable salts; the compounds having the formula (I) wherein A has the structure (II) or (III); X is chosen from -CH 2 -, -O-, -NH-, and -S-; Y is chosen from -O-, -NH-, and -S-; Z, which may be located in any position of substitution, is hydrogen or halogen; R 1 and R 2 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl, or R 1 and R 2 together form a carbocyclic ring having from 4 to 6 carbon atoms; R 3 is chosen from hydrogen and C 1 -C 8 alkyl; R 4 , R 5 , and R 6 , which may be the same or different, are independently chosen from hydrogen and C 1 -C 8 alkyl; and n is 1 to 6. Various embodiments and variants are provided. In accordance with other aspects, the invention also provides methods of producing a PPARalpha agonist activity in a mammal, the methods including administering to the mammal an effective amount of certain derivative(s) of the first aspect of the invention, a method of producing a PPARalpha agonist activity and a PPARalpha agonist activity in a mammal, the method including administering to the mammal an effective amount of certain derivative(s); and a pharmaceutical composition that includes the derivative(s) of the first aspect of the invention and one or more pharmaceutically-acceptable excipients. Various embodiments and variants are provided.

公开(公告)号：MX2007002716A

公开(公告)日：2008-03-05

申请号：MX2007002716

申请日：2005-09-06

Applicant: REDDYS LAB LTD DR

Inventor： SHARMA SUDHIR KUMAR ,  IQBAL JAVED ,  BHUNIYA DEBNATH ,  DAS SAIBAL KUMAR ,  CHAKRABARTI RANJAN ,  GURRAM RANGA MADHAVAN ,  SINGH SUNIL KUMAR

IPC: A61K31/00 ,  C07D487/02

Abstract: Se proporcionan derivados que tienen actividad agonista de PPAR. Los derivados incluyen compuestos y/o sus sales farmaceuticamente aceptables; los compuestos que tienen la formula (I) en donde A tiene la estructura (II) o (III); X se elige de -CH2, -O-, -NH-, y -S; Y se elige de -O-, -NH, y -S-; Z que se puede localizar en cualquier posicion de sustitucion , es hidrogeno o halogeno; R1 y R2, que pueden ser los mismos o diferentes, se eligen independientemente de hidrogeno y C1-C8alquilo, o R1 y R2 forman conjuntamente un anillo carbociclico que tiene de 4 a 6 atomos de carbono; R3 se elige de hidrogeno C1-C8alquilo, o R4 y R5 y R6 que pueden ser los mismos o diferentes, se eligen independientemente de hidrogeno y C1-C8alquilo, y n es 1 a 6. Se proporcionan varias modalidades y variantes. De acuerdo con otros aspectos, La invencion tambien proporciona metodos para producir una actividad agonista de PPAR??en un mamifero, los metodos que incluyen administrar al mamifero una cantidad efectiva de ciertos derivados del primer aspecto de la invencion, un metodo para producir una actividad agonista de PPAR??y una actividad agonista de PPAR??en un mamifero, el metodo que incluye administrar al mamifero una actividad efectiva de ciertos derivados; y una composicion farmaceutica que incluye los derivados del primer aspecto de la invencion y uno o mas excipientes farmaceuticamente aceptables. Se proporcionan varias modalidades y variantes.