AR064852A1 - PYRIMIDINES REPLACED IN POSITION 2 - Google Patents

PYRIMIDINES REPLACED IN POSITION 2

Info

Publication number
AR064852A1
AR064852A1 ARP080100115A ARP080100115A AR064852A1 AR 064852 A1 AR064852 A1 AR 064852A1 AR P080100115 A ARP080100115 A AR P080100115A AR P080100115 A ARP080100115 A AR P080100115A AR 064852 A1 AR064852 A1 AR 064852A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkynyl
cycloalkyl
alkenyl
radicals
Prior art date
Application number
ARP080100115A
Other languages
Spanish (es)
Original Assignee
Basf Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Basf Ag filed Critical Basf Ag
Publication of AR064852A1 publication Critical patent/AR064852A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Uso de pirimidinas de la formula 1 sustituidas en posicion 2 y de las sales farmacéuticamente aceptables de las pirimidinas de la formula 1 sustituidas en posicion 2 en terapia, en particular, en la terapia o en el tratamiento de enfermedades cancerosas. Reivindicacion 1: 5-fenilpirimidinas de la formula 1 sustituidas en posicion 2 y sus sales farmacéuticamente aceptables para su uso en terapia: caracterizadas porque los índices y los sustituyentes son tal como se los define infra: R1 representa alquilo C2-10, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-12, cicloalquenilo C3-10, fenilo o un heterociclo saturado, parcialmente insaturado o aromático de cinco a diez miembros, que está unido a través de un átomo carbono y que contiene uno, dos, tres o cuatro heteroátomos seleccionados de entre el grupo compuesto de O, N y S; en el que los grupos alifáticos, alicíclicos y/o aromáticos de las definiciones de radicales de R1 a su vez pueden estar parcial o totalmente halogenados o pueden portar uno, dos, tres o cuatro radicales Rv, que pueden ser iguales o diferentes unos de otros; Rv representa halogeno, ciano, alquilo C1-8, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-6, cicloalquenilo C4-6, hidroxilo, alcoxi C1-6, alqueniloxi C2-10, alquiniloxi C2-10, cicloalquiloxi C3-6, cicloalqueniloxi C4-6, -C(=O)-A1, -C(=O)-O-A1, -C(=O)-N(A2)A1, C(A2)(=N-OA1), N(A2)A1, N(A2)-C(=O)-A1, N(A3)-C(=O)-N(A2)A1, S(=O)m-A1, S(=O)m-O-A1 o S(=O)m-N(A2)A1, siendo también posible que dos radicales Rv vecinales juntos representen (=O), (=S) o (=N-OA1), o Rv representa fenilo, en el que la fraccion fenílica puede portar uno, dos o tres radicales que pueden ser iguales o diferentes unos de otros y que están seleccionados de entre el grupo compuesto de: halogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, haloalquilo C1-6, alcoxi C1-6, ciano, nitro, -C(=O)-A, -C(=O)-O-A, -C(=O)-N(A')A, C(A')(=N-OA) y N(A')A; en los que m representa 0. 1 o 2; A1, A2, A3, A y A', independientemente unos de otros, representan hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, cicloalquenilo C3-8 o fenilo, en los que los radicales orgánicos pueden estar parcial o totalmente halogenados o pueden estar sustituidos por halogeno, nitro, cianato, ciano y/o alcoxi C1-4; o A1 y A2, o A y A', respectivamente, junto con los átomos a los que están unidos representan un heterociclo saturado, parcialmente insaturado o aromático de cinco o seis miembros que comprende uno, dos, tres o cuatro heteroátomos seleccionados de entre el grupo compuesto de O, N y S; y en los que los grupos alifáticos, alicíclicos y/o aromáticos de las definiciones de radicales de Rv a su vez pueden estar parcial o totalmente halogenados; R2 representa halogeno, ciano, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, alcoxi C1-4, alqueniloxi C3-4, alquiniloxi C3-4, alquil C1-6-tio, di-(alquil C1-6)amino o alquil C1- 6-amino, en los que los grupos alifáticos y/o alicíclicos de las definiciones de radicales de R2 a sri vez pueden estar parcial o totalmente halogenados o pueden portar uno, dos, tres o cuatro radicales Ru, que pueden ser iguales o diferentes unos de otros; Ru representa halogeno, ciano, alquilo C1-8, alquenilo C2-10, alquinilo C2-10, hidroxilo, alcoxi C1-6, cicloalquilo C3-6, alqueniloxi C2-10, alquiniloxi C2-10, cicloalquenilo C4-6, cicloalquiloxi C3-6, cicloalqueniloxi C4-6, -C(=O)-A4, - C(=O)-O-A4, -C(=O)-N(A5)A4, C(A5)(=N-OA4), N(A5)A4, N(A5)-C(=O)-A4, N(A6)-C(=O)-N(A5)A4, S(=O)q-A4, S(=O)q-O-A4 o S(=O)q-N(A5)A4, siendo también posible que dos radicales Ru vecinales juntos representen (=O) o (=S), en los que q representa 0, 1 o 2; A4, A5 y A6, independientemente unos de otros, tienen los significados de A1, A2 y A3 tal como se los define supra; y en los que los grupos alifáticos, alicíclicos y/o aromáticos de las definiciones de radicales de Ru a su vez pueden estar parcial o totalmente halogenados o pueden portar uno, dos o tres radicales Rua, que pueden ser iguales o diferentes unos de otros y que tienen los significados de Ru tal como se los define supra; R3 está seleccionado de entre el grupo compuesto de ciano, C(=Z)ORa, C(=Z)NRzRb C(=Z)NRz-ORa, C(=Z)NRa-NRzRb, C(=Z)Ra, ON(=CRaRb), O-C(=Z)Ra, NRa(C(=Z)Rb), NRa(C(=Z)ORb), NRa(C(=Z)-NRzRb), NRa(N=CRcRb), Nra-NRzRb, NRz-ORa, y los radicales de formulas R3a y R3b en las que Z representa O, S, NRa1, NORa1 o N- NRz1Rc1, Ra, Ra1, Rb, Rc, Rc1, independientemente unos de otros, representan hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 o cicloalquenilo C4-6; Rb1 tiene los significados de Rb tal como se los define supra, excepto hidrogeno; y Rz, Rz1, independientemente el uno del otro, tienen los significados de Ra tal como se los define supra y adicionalmente pueden representar -CO-Ra2, en el que Ra2 tiene los significados de Ra tal corno se los define supra; en los que los grupos alifáticos y/o alicíclicos de las definiciones de radicales de Ra, Ra1, Rb, Rb1, Rc, Rc1, Rz y Rz1 a su vez pueden estar parcial o totalmente halogenados o pueden portar uno, dos, tres o cuatro grupos Rt, que pueden ser iguales o diferentes unos de otros, Rt representa halogeno, ciano, alquilo C1-8, alquenilo C2-10, alquinilo C2-10, alcoxi C1-6, alqueniloxi C2-10, alquiniloxi C2-10, cicloalquilo C3-6, cicloalquenilo C3-6, cicloalcoxi C3-6 o cicloalqueniloxi C3-6, y en los que dos de los radicales Ra, Ra1, Rb, Rb1, Rc, Rc1, Rz o Rz1 junto con los átomos a los que están unidos pueden formar un heterociclo saturado, parcialmente insaturado o aromático de cinco, seis o siete miembros que comprende uno, dos, tres o cuatro heteroátomos seleccionados de entre el grupo compuesto de O, N y S, y en los que en las formulas R3a y R3b indica el átomo que está enlazado a la posicion 2 del anillo pirimidínico, x representa 0 o 1; Re, Rf, Rg, Re , independientemente unos de otros, representan hidrogeno, alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-6, cicloalquenilo C4-6, Rf, Rg, junto con el átomo de nitrogeno al que están unidos, pueden tener el significado Re-Z-C(Rh)=N; Q representa oxígeno o N-Re , Q' representa C(H)-Rk, C-Rk, N-N(H)Re o N-Re ; à. puede ser un doble enlace o un simple enlace, Rh, Rk tienen los mismos significados que Re y adicionalmente pueden representar halogeno o ciano; o Rh junto con el átomo de carbono al que está unido puede representar un grupo carbonilo; en los que los grupos alifáticos, alicíclicos o aromáticos de las definiciones de radicales de Re, Re , Rf, Rg, Rh o Rk a su vez pueden estar parcial o totalmente halogenados o pueden portar de uno a cuatro grupos Rw, que pueden ser iguales o diferentes unos de otros, Rw representa halogeno, ciano, alquilo C1-8, alquenilo C2-10, alquinilo C2-10, alcoxi C1-6, alqueniloxi C2-10, alquiniloxi C2-10, cicloalquilo C3-6, cicloalquenilo C3-6, cicloalcoxi C3-6, cicloalqueniloxi C3-6, y en los que dos de los radicales Rf, Rg, Re o Re , junto con los átomos a los que están unidos pueden formar un heterociclo saturado, parcialmente insaturado o aromático de cinco o seis miembros que contiene de uno a cuatro heteroátomos del grupo compuesto de O, N y S; n representa 1, 2, 3, 4 o 5; L independientemente unos otros, están seleccionados de entre halogeno, ciano, cianato (OCN), alquilo C1-10, alquenilo C2-10, alquinilo C2-10, alcoxi C1-6, alqueniloxi C2-10, alquiniloxi C2-10, cicloalquilo C3-6, cicloalquenilo C4-6, cicloalquiloxi C3-6, cicloalqueniloxi C4-6, nitro, -C(=O)-A10, -C(=O)-O-A10, -C(=O)-N(A11)A10, -C(=S)-N(A11)A10, -C(=NA11)-SA10, C(A11)(=N-OA10), N(A11)A10, N(A11)-C(=O)-A10, N(A12)-C(=O)- N(A11 )A10, S(=O)p-A10, S(=O)p-O-A10 o S(=O)p-N(A11)A10, en los que p representa 0, 1 o 2; A10, A11, A12, independientemente unos de otros, tienen los significados de A1, A2 y A3 tal como se los define supra; en los que los grupos alifáticos, alicíclicos y/o aromáticos de las definiciones de radicales de L a su vez pueden estar parcial o totalmente halogenados o pueden portar uno, dos, tres o cuatro radicales RL, que pueden ser iguales o diferentes unos de otros, RL representa halogeno, ciano, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, hidroxilo, alcoxi C1-6, alqueniloxi C2-10, alquiniloxi C2-10, cicloalquilo C3-6, cicloalquenilo C4-6, cicloalquiloxi C3-6, cicloalqueniloxi C4-6, -C(=O)-A13, -C(=O)-O-A13, -C(=O)-N(A14)A13, - C(A14)(=N-OA13), -N(A14)A13, N(A14)-C(=O)-A13, N(A15)-C(=O)-N(A14 )A13, S(=O)s-A13, S(=O)s-O-A13 o S(=O)s-N(A14)A13, siendo también posible que dos radicales RL vecinales juntos representen (=O) o (=S), en los que s representa 0, 1 o 2; y A13, A14 y A15, independientemente unos de otros, tienen los significados de A1, A2 y A3 tal como se los define supra; y en los que los grupos alifáticos, alicíclicos y/o aromáticos de las definiciones de radicales de RL a su vez pueden estar parcial o totalmente halogenados o pueden portar uno, dos, tres o cuatro grupos RLA, que pueden ser iguales o diferentes unos de otros y que tienen los significados de RL tal como se los define supra.Use of pyrimidines of formula 1 substituted in position 2 and of the pharmaceutically acceptable salts of pyrimidines of formula 1 substituted in position 2 in therapy, in particular, in therapy or in the treatment of cancerous diseases. Claim 1: 5-phenylpyrimidines of formula 1 substituted in position 2 and their pharmaceutically acceptable salts for use in therapy: characterized in that the indices and substituents are as defined below: R1 represents C2-10 alkyl, C2 alkenyl 10, C2-10 alkynyl, C3-12 cycloalkyl, C3-10 cycloalkenyl, phenyl or a saturated, partially unsaturated or aromatic heterocycle of five to ten members, which is attached through a carbon atom and containing one, two, three or four heteroatoms selected from the group consisting of O, N and S; in which the aliphatic, alicyclic and / or aromatic groups of the radical definitions of R1 in turn can be partially or totally halogenated or can carry one, two, three or four radicals Rv, which may be the same or different from each other ; Rv represents halogen, cyano, C1-8 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, C4-6 cycloalkenyl, hydroxy, C1-6 alkoxy, C2-10 alkenyloxy, C2-10 alkynyloxy, C3 cycloalkyloxy -6, C4-6 cycloalkenyloxy, -C (= O) -A1, -C (= O) -O-A1, -C (= O) -N (A2) A1, C (A2) (= N-OA1 ), N (A2) A1, N (A2) -C (= O) -A1, N (A3) -C (= O) -N (A2) A1, S (= O) m-A1, S (= O) mO-A1 or S (= O) mN (A2) A1, it being also possible that two radical Rv radicals together represent (= O), (= S) or (= N-OA1), or Rv represents phenyl, in that the phenyl fraction may carry one, two or three radicals that may be the same or different from each other and that are selected from the group consisting of: halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxy, cyano, nitro, -C (= O) -A, -C (= O) -OA, -C (= O) -N (A ') A , C (A ') (= N-OA) and N (A') A; in which m represents 0. 1 or 2; A1, A2, A3, A and A ', independently of each other, represent hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 3-8 cycloalkenyl or phenyl, in which the organic radicals may be partially or totally halogenated or may be substituted by halogen, nitro, cyanate, cyano and / or C1-4 alkoxy; or A1 and A2, or A and A ', respectively, together with the atoms to which they are attached represent a saturated, partially unsaturated or aromatic heterocycle of five or six members comprising one, two, three or four heteroatoms selected from the group composed of O, N and S; and in which the aliphatic, alicyclic and / or aromatic groups of the radical definitions of Rv in turn may be partially or totally halogenated; R 2 represents halogen, cyano, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C 3-6 cycloalkyl, C 1-4 alkoxy, C 3-4 alkynyloxy, C 3-4 alkynyloxy, C 1-6 alkylthio, di- (C1-6 alkyl) amino or C1-6-amino alkyl, in which the aliphatic and / or alicyclic groups of the radical definitions of R2 may simultaneously be partially or totally halogenated or may carry one, two, three or four radicals Ru, which may be the same or different from each other; Ru represents halogen, cyano, C1-8 alkyl, C2-10 alkenyl, C2-10 alkynyl, hydroxy, C1-6 alkoxy, C3-6 cycloalkyl, C2-10 alkenyloxy, C2-10 alkynyloxy, C4-6 cycloalkenyl, C3 cycloalkyloxy -6, C4-6 cycloalkenyloxy, -C (= O) -A4, - C (= O) -O-A4, -C (= O) -N (A5) A4, C (A5) (= N-OA4 ), N (A5) A4, N (A5) -C (= O) -A4, N (A6) -C (= O) -N (A5) A4, S (= O) q-A4, S (= O) qO-A4 or S (= O) qN (A5) A4, it being also possible for two neighborhood Ru radicals together to represent (= O) or (= S), in which q represents 0, 1 or 2; A4, A5 and A6, independently of each other, have the meanings of A1, A2 and A3 as defined above; and in which the aliphatic, alicyclic and / or aromatic groups of the Ru radical definitions in turn may be partially or totally halogenated or may carry one, two or three Rua radicals, which may be the same or different from each other and that they have the meanings of Ru as defined above; R3 is selected from the group consisting of cyano, C (= Z) ORa, C (= Z) NRzRb C (= Z) NRz-ORa, C (= Z) NRa-NRzRb, C (= Z) Ra, ON (= CRaRb), OC (= Z) Ra, NRa (C (= Z) Rb), NRa (C (= Z) ORb), NRa (C (= Z) -NRzRb), NRa (N = CRcRb), Nra-NRzRb, NRz-ORa, and the radicals of formulas R3a and R3b in which Z represents O, S, NRa1, NORa1 or N- NRz1Rc1, Ra, Ra1, Rb, Rc, Rc1, independently of each other, represent hydrogen , C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl or C4-6 cycloalkenyl; Rb1 has the meanings of Rb as defined above, except hydrogen; and Rz, Rz1, independently of each other, have the meanings of Ra as defined above and can additionally represent -CO-Ra2, in which Ra2 has the meanings of Ra as defined above; in which the aliphatic and / or alicyclic groups of the radical definitions of Ra, Ra1, Rb, Rb1, Rc, Rc1, Rz and Rz1 in turn can be partially or totally halogenated or can carry one, two, three or four Rt groups, which may be the same or different from each other, Rt represents halogen, cyano, C1-8 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-6 alkoxy, C2-10 alkenyloxy, C2-10 alkynyloxy, cycloalkyl C3-6, C3-6 cycloalkenyl, C3-6 cycloalkoxy or C3-6 cycloalkenyloxy, and in which two of the radicals Ra, Ra1, Rb, Rb1, Rc, Rc1, Rz or Rz1 together with the atoms to which they are together they can form a saturated, partially unsaturated or aromatic heterocycle of five, six or seven members comprising one, two, three or four heteroatoms selected from the group consisting of O, N and S, and in which in formulas R3a and R3b indicates the atom that is linked to position 2 of the pyrimidine ring, x represents 0 or 1; Re, Rf, Rg, Re, independently of each other, represent hydrogen, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-6 cycloalkyl, C4-6 cycloalkenyl, Rf, Rg, together with the atom of Nitrogen to which they are attached, can have the meaning Re-ZC (Rh) = N; Q represents oxygen or N-Re, Q 'represents C (H) -Rk, C-Rk, N-N (H) Re or N-Re; to. it can be a double bond or a single bond, Rh, Rk have the same meanings as Re and can additionally represent halogen or cyano; or Rh together with the carbon atom to which it is attached may represent a carbonyl group; in which the aliphatic, alicyclic or aromatic groups of the radical definitions of Re, Re, Rf, Rg, Rh or Rk in turn can be partially or totally halogenated or can carry from one to four Rw groups, which can be the same or different from each other, Rw represents halogen, cyano, C1-8 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-6 alkoxy, C2-10 alkenyloxy, C2-10 alkynyloxy, C3-6 cycloalkyl, C3- cycloalkenyl 6, C3-6 cycloalkoxy, C3-6 cycloalkenyloxy, and in which two of the radicals Rf, Rg, Re or Re, together with the atoms to which they are attached can form a saturated, partially unsaturated or aromatic heterocycle of five or six members containing from one to four heteroatoms of the group consisting of O, N and S; n represents 1, 2, 3, 4 or 5; L independently of each other, are selected from halogen, cyano, cyanate (OCN), C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-6 alkoxy, C2-10 alkenyloxy, C2-10 alkynyloxy, C3 cycloalkyl -6, C4-6 cycloalkenyl, C3-6 cycloalkyloxy, C4-6 cycloalkenyloxy, nitro, -C (= O) -A10, -C (= O) -O-A10, -C (= O) -N (A11 ) A10, -C (= S) -N (A11) A10, -C (= NA11) -SA10, C (A11) (= N-OA10), N (A11) A10, N (A11) -C (= O) -A10, N (A12) -C (= O) - N (A11) A10, S (= O) p-A10, S (= O) pO-A10 or S (= O) pN (A11) A10 , in which p represents 0, 1 or 2; A10, A11, A12, independently of each other, have the meanings of A1, A2 and A3 as defined above; in which the aliphatic, alicyclic and / or aromatic groups of the radical definitions of L in turn may be partially or totally halogenated or may carry one, two, three or four RL radicals, which may be the same or different from each other , RL represents halogen, cyano, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, hydroxy, C1-6 alkoxy, C2-10 alkenyloxy, C2-10 alkynyloxy, C3-6 cycloalkyl, C4-6 cycloalkenyl, cycloalkyloxy C3-6, C4-6 cycloalkenyloxy, -C (= O) -A13, -C (= O) -O-A13, -C (= O) -N (A14) A13, - C (A14) (= N -OA13), -N (A14) A13, N (A14) -C (= O) -A13, N (A15) -C (= O) -N (A14) A13, S (= O) s-A13, S (= O) sO-A13 or S (= O) sN (A14) A13, it being also possible for two neighborhood RL radicals together to represent (= O) or (= S), where s represents 0, 1 or 2 ; and A13, A14 and A15, independently of each other, have the meanings of A1, A2 and A3 as defined above; and in which the aliphatic, alicyclic and / or aromatic groups of the radical definitions of RL in turn may be partially or totally halogenated or may carry one, two, three or four RLA groups, which may be the same or different from each other. others and that have the meanings of RL as defined above.

ARP080100115A 2007-01-11 2008-01-10 PYRIMIDINES REPLACED IN POSITION 2 AR064852A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07100426 2007-01-11

Publications (1)

Publication Number Publication Date
AR064852A1 true AR064852A1 (en) 2009-04-29

Family

ID=39103759

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080100115A AR064852A1 (en) 2007-01-11 2008-01-10 PYRIMIDINES REPLACED IN POSITION 2

Country Status (4)

Country Link
AR (1) AR064852A1 (en)
CL (1) CL2008000097A1 (en)
TW (1) TW200836741A (en)
WO (1) WO2008084081A2 (en)

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3919229A (en) * 1973-07-19 1975-11-11 Labaz Pyrimidine derivatives and process for preparing the same
EP1546115A4 (en) * 2002-09-27 2010-08-04 Merck Sharp & Dohme Substituted pyrimidines
CN100357297C (en) * 2003-02-06 2007-12-26 巴斯福股份公司 Pyrimidines, methods for the production thereof, and use thereof
WO2004087678A1 (en) * 2003-04-04 2004-10-14 Basf Aktiengesellschaft 2-substituted pyrimidines
US20040259887A1 (en) * 2003-06-18 2004-12-23 Pfizer Inc Cannabinoid receptor ligands and uses thereof
EP1663241B1 (en) * 2003-09-24 2009-05-27 Wyeth Holdings Corporation 5-arylpyrimidines as anticancer agents
US20050070712A1 (en) * 2003-09-26 2005-03-31 Christi Kosogof Pyrimidine derivatives as ghrelin receptor modulators
DE102004003493A1 (en) * 2004-01-23 2005-08-11 Bayer Cropscience Ag 5-Phenylpyrimidines
TW200637556A (en) * 2005-01-31 2006-11-01 Basf Ag Substituted 5-phenyl pyrimidines I in therapy
CL2007002231A1 (en) * 2006-08-02 2008-04-11 Basf Ag USE OF COMPOUNDS DERIVED FROM 5- (HET) ARILPIRIMIDINE TO COMBAT DANGINE FUNGES; COMPOUNDS DERIVED FROM 5- (HET) ARILPIRIMIDINA; FUNGICIDE AGENT; AND PHARMACEUTICAL AGENT.

Also Published As

Publication number Publication date
WO2008084081A3 (en) 2008-10-09
CL2008000097A1 (en) 2008-05-16
TW200836741A (en) 2008-09-16
WO2008084081A2 (en) 2008-07-17

Similar Documents

Publication Publication Date Title
AR053092A1 (en) COMPOUNDS DERIVED FROM PHENOXYACETIC ACID AND INTERMEDIATE SYNTHESIS COMPOUNDS
AR081315A1 (en) HETEROCICLIC DERIVATIVES OF PIPERIDIN AND PIRIMIDIN -4-IL-AZETIDINA, A CRYSTALLINE FORM OF THE SALT OF ACETONITRILADIPICO ACID OF A PYRIMIDINIC DERIVATIVE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME THINGS WITH THE TREATMENT OF INJECTION , T
UY32483A (en) NEW BENCIMIDAZOL COMPOUNDS FOR THE TREATMENT OF RESPIRATORY SINCICIAL VIRUS
AR076794A1 (en) DERIVATIVES OF N- (HETERO) ARIL-PIRROLIDINA DE PIRAZOL-4-IL-PIRROLO [2,3-D] PIRIMIDINES AND PIRROL-3-IL-PIRROLO [2,3-D] PYRIMIDINS AS INHIBITORS OF THE JANUS KINASE AND COMPOSITIONS PHARMACEUTICS THAT CONTAIN THEM
AR068045A1 (en) CATECOLAMINE DERIVATIVES AND DRUGS OF THE SAME
PE20130395A1 (en) PYRAZOLO [1,5-A] PYRIMIDINES FOR ANTIVIRAL TREATMENT
AR085960A1 (en) 1,3-OXAZINES AS INHIBITORS OF THE BACE1 AND / OR THE BACE2
SV2016005229A (en) SYK INHIBITORS
AR081628A1 (en) 5-FLUORO-1H-REPLACED PIRAZOLOPIRIDINES AND ITS USE
CO6290658A2 (en) DERIVATIVES OF AZETIDINE AND CYCLLOBUTANE AS JACK INHIBITORS
CR20120591A (en) AMINOPIRIMIDINE DERIVATIVES AS MODULATORS OF THE LRRK2
CR20130531A (en) DERIVATIVES OF NUCLEOSIDS 2'-SUBSTITUTES AND METHODS OF USE OF THE SAME FOR THE TREATMENT OF VIRAL DISEASES
AR078201A1 (en) COMPOUNDS OF 2-PIRIDONA AND ITS USE IN THE TREATMENT OF DISEASES MEDIATED BY THE ELASTASA OF NEUTROFILOS
AR086538A1 (en) COMPOUNDS TO REDUCE THE PRODUCTION OF B-AMYLOID
AR064010A1 (en) AKT ACTIVITY INHIBITORS
ECSP066947A (en) PHARMACOLOGICAL COMBINATIONS CONTAINING BENZOXAZINE FOR THE TREATMENT OF RESPIRATORY ROAD DISEASES
NI201200184A (en) MORPHOLINOPYRIMIDINES AND THEIR USE IN THERAPY
AR069524A1 (en) DERIVATIVES OF ISOXAZOLO - PIRAZINA, A PROCEDURE FOR THE PREPARATION OF THE COMPOUND, MEDICATION BASED ON THE COMPOUND AND USE OF THE COMPOUND TO PREPARE A MEDICINAL PRODUCT
AR058287A1 (en) ISOQUINOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION
AR086983A1 (en) DERIVATIVES OF AZETIDINIL FENIL, PIRIDIL OR PIRAZINIL CARBOXAMIDA AS JAK INHIBITORS
AR085471A1 (en) BIS COMPOUNDS (FLUOROALQUIL) -1,4-BENZODIAZEPINONA
AR078152A1 (en) HETEROCICLICAL COMPOUNDS, USEFUL FOR THE TREATMENT OF HCV AND PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM
AR072819A1 (en) DERIVATIVES OF TRIAZOLO [4,3-A] PIRIDINE, PREPARATION PROCEDURE, INTERMEDIARIES OF SUCH PROCESS, PHARMACEUTICAL COMPOSITIONS THAT UNDERSTAND AND USE THE SAME, AS INHIBITORS OF MET PROTEINQUINASE, FOR THE TREATMENT OF CANCERESIST, PSCESESIS, PSC CENTRAL NERVOUS AND OTHER
PE20150194A1 (en) NOVELTY N-PYRIDINYL AMIDES CYCLIC SUBSTITUTE AS KINASE INHIBITORS
AR075583A1 (en) ISOXAZOL / O-PYRIDINE DERIVATIVES WITH ETILO OR ETHYLENE LINK

Legal Events

Date Code Title Description
FA Abandonment or withdrawal